Journal articles: 'Biopharmaceutical Classification System – BCS'

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Miranda, Claudia, Alexis Aceituno, Mirna Fernández, Gustavo Mendes, Yanina Rodríguez, Verónica Llauró, and Miguel Ángel Cabrera-Pérez. "ICH Guideline for Biopharmaceutics Classification System-Based Biowaiver (M9): Toward Harmonization in Latin American Countries." Pharmaceutics 13, no. 3 (March 10, 2021): 363. http://dx.doi.org/10.3390/pharmaceutics13030363.

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The biopharmaceutical classification system (BCS) is a very important tool to replace the traditional in vivo bioequivalence studies with in vitro dissolution assays during multisource product development. This paper compares the most recent harmonized guideline for biowaivers based on the biopharmaceutics classification system and the BCS regulatory guidelines in Latin America and analyzes the current BCS regulatory requirements and the perspective of the harmonization in the region to develop safe and effective multisource products. Differences and similarities between the official and publicly available BCS guidelines of several Latin American regulatory authorities and the new ICH harmonization guideline were identified and compared. Only Chile, Brazil, Colombia, and Argentina have a more comprehensive BCS guideline, which includes solubility, permeability, and dissolution requirements. Although their regulatory documents have many similarities with the ICH guidelines, there are still major differences in their interpretation and application. This situation is an obstacle to the successful development of safe and effective multisource products in the Latin American region, not only to improve their access to patients at a reasonable cost, but also to develop BCS biowaiver studies that fulfill the quality standards of regulators in developed and emerging markets.

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Truzzi, Francesca, Camilla Tibaldi, Yanxin Zhang, Giovanni Dinelli, and Eros D′Amen. "An Overview on Dietary Polyphenols and Their Biopharmaceutical Classification System (BCS)." International Journal of Molecular Sciences 22, no. 11 (May 24, 2021): 5514. http://dx.doi.org/10.3390/ijms22115514.

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Polyphenols are natural organic compounds produced by plants, acting as antioxidants by reacting with ROS. These compounds are widely consumed in daily diet and many studies report several benefits to human health thanks to their bioavailability in humans. However, the digestion process of phenolic compounds is still not completely clear. Moreover, bioavailability is dependent on the metabolic phase of these compounds. The LogP value can be managed as a simplified measure of the lipophilicity of a substance ingested within the human body, which affects resultant absorption. The biopharmaceutical classification system (BCS), a method used to classify drugs intended for gastrointestinal absorption, correlates the solubility and permeability of the drug with both the rate and extent of oral absorption. BCS may be helpful to measure the bioactive constituents of foods, such as polyphenols, in order to understand their nutraceutical potential. There are many literature studies that focus on permeability, absorption, and bioavailability of polyphenols and their resultant metabolic byproducts, but there is still confusion about their respective LogP values and BCS classification. This review will provide an overview of the information regarding 10 dietarypolyphenols (ferulic acid, chlorogenic acid, rutin, quercetin, apigenin, cirsimaritin, daidzein, resveratrol, ellagic acid, and curcumin) and their association with the BCS classification.

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Arrunátegui, Lorena Barbosa, Neila Márcia Silva-Barcellos, Karime Rezende Bellavinha, Lisiane da Silveira Ev, and Jacqueline de Souza. "Biopharmaceutics classification system: importance and inclusion in biowaiver guidance." Brazilian Journal of Pharmaceutical Sciences 51, no. 1 (March 2015): 143–54. http://dx.doi.org/10.1590/s1984-82502015000100015.

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Pharmacological therapy is essential in many diseases treatment and it is important that the medicine policy is intended to offering safe and effective treatment with affordable price to the population. One way to achieve this is through biowaiver, defined as the replacement of in vivo bioequivalence studies by in vitro studies. For biowaiver of new immediate release solid oral dosage forms, data such as intestinal permeability and solubility of the drug are required, as well as the product dissolution. The Biopharmaceutics Classification System (BCS) is a scientific scheme that divides drugs according to their solubility and permeability and has been used by various guides as a criterion for biowaiver. This paper evaluates biowaiver application, addressing the general concepts and parameters used by BCS, making a historical account of its use, the requirements pertaining to the current legislation, the benefits and risks associated with this decision. The results revealed that the use of BCS as a biowaiver criterion greatly expands the therapeutics options, contributing to greater therapy access of the general population with drug efficacy and safety guaranteed associated to low cost.

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Charalabidis, Aggelos, Maria Sfouni, Christel Bergström, and Panos Macheras. "The Biopharmaceutics Classification System (BCS) and the Biopharmaceutics Drug Disposition Classification System (BDDCS): Beyond guidelines." International Journal of Pharmaceutics 566 (July 2019): 264–81. http://dx.doi.org/10.1016/j.ijpharm.2019.05.041.

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Darusman, Fitrianti, and Ulfa Siti M. "PENGARUH KONSENTRASI BETASIKLODEKSTRIN TERHADAP KELARUTAN GLIMEPIRID." Jurnal Ilmiah Farmasi Farmasyifa 1, no. 1 (August 20, 2017): 13–17. http://dx.doi.org/10.29313/jiff.v1i1.3061.

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Glimepirid (GMP) merupakan obat antidiabetika oral golongan sulfonilurea generasi ketiga yang mampu menurunkan kadar glukosa darah dengan efek samping hipoglikemia yang kecil. Namun GMP termasuk ke dalam Biopharmaceutical Classification System (BCS) kelas II yang memiliki kelarutan praktis tidak larut dalam air sehingga berpengaruh pada laju disolusi dan bioavailabilitasnya. Salah satu upaya untuk meningkatkan kelarutan GMP yaitu dengan pembentukan kompleks inklusi menggunakan betasiklodekstrin (BCD). Penentuan terbentuknya kompleks inklusi GMP-BCD menggunakan beberapa konsentrasi larutan BCD yang semakin meningkat dalam dapar asetat 0,01 M pH 6,2 dan dapar fosfat 0,01 M pH 7,4 yang diteliti dengan metode kelarutan dan ditentukan secara spektrofotometri ultraviolet pada panjang gelombang serapan maksimum 228 nm. Hasil penelitian menunjukkan bahwa kelarutan GMP meningkat dengan semakin meningkatnya konsentrasi BCD dengan harga tetapan stabilitas kompleks pada pH 7,4 lebih sebesar 0,650 lebih besar dari pada pH 6,2 yaitu sebesar 0,237 .

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Ono, Asami, Takumi Tomono, Takuo Ogihara, Katsuhide Terada, and Kiyohiko Sugano. "Investigation of biopharmaceutical drug properties suitable for orally disintegrating tablets." ADMET and DMPK 4, no. 4 (December 26, 2016): 335. http://dx.doi.org/10.5599/admet.4.4.338.

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<span style="color: black; font-family: 'Calibri','sans-serif'; font-size: 10pt; mso-fareast-font-family: 'Times New Roman'; mso-bidi-font-family: 'Times New Roman'; mso-ansi-language: EN-GB; mso-fareast-language: DE; mso-bidi-language: AR-SA;" lang="EN-GB">The purpose of this study was to evaluate the biopharmaceutical drug properties suitable for orally disintegrating tablets (ODTs). The net charge at pH 7.4, log D6.5, the highest dose strength, solubility in water, dose number, and elimination t1/2 of 57 ODT drugs and 113 drugs of immediate-release (IR) formulations were compared. These drugs were classified according to the Biopharmaceutical Classification System (BCS). A lower dose strength and a longer elimination t1/2 have been observed as characteristic properties of ODTs. The proportion of basic drugs was higher in the ODTs than in the IR. A significant difference was not observed between the ODT and the IR formulation for log D6.5, solubility in water, and dose number. The distributions of the ODT and IR formulations among each BCS class were similar, suggesting that an ODT can be developed regardless of the BCS class of a drug.

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Mariappan, T. T., and Saranjit Singh. "Positioning of Rifampicin in the Biopharmaceutics Classification System (BCS)." Clinical Research and Regulatory Affairs 23, no. 1 (January 2006): 1–10. http://dx.doi.org/10.1080/10601330500533990.

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Smetanová, Libuše, Věra Štětinová, Zbyněk Svoboda, and Jaroslav Květina. "Caco-2 Cells, Biopharmaceutics Classification System (BCS) and Biowaiter." Acta Medica (Hradec Kralove, Czech Republic) 54, no. 1 (2011): 3–8. http://dx.doi.org/10.14712/18059694.2016.9.

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Almost all orally administered drugs are absorbed across the intestinal mucosa. The Caco-2 monolayers are used as an in vitro model to predict drug absorption in humans and to explore mechanism of drug absorption. The Caco-2 cells are derived from a human colon adenocarcinoma and spontaneously differentiate to form confluent monolayer of polarized cells structurally and functionally resembling the small intestinal epithelium. For studying drug permeability, Caco-2 cells are seeded onto the Transwell inserts with semipermeable membrane and grown to late confluence (21 days). After determination of cell viability, the integrity of monolayer is checked by phenol red permeability and by 14C-mannitol permeability. The transport from apical to basolateral (AP-BL) and basolateral to apical (BL-AP) is studied by adding the diluted drug on the apical or basolateral side and withdrawing the samples from the opposite compartment, respectively, for HPLC analysis or liquid scintillation spectrometry. Ca2+- free transport medium is used to determine paracellular component of the drug transport. On the basis of permeability and solubility, drugs can be categorized into four classes of Biopharmaceutics Classification System (BCS). For certain drugs, the BCS-based biowaiver approach can be used which enables to reduce in vivo bioequivalence studies.

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Sagar, Nidhi, Iva Dhulia, Himani Patel, Umesh Dobariya, and Sandip Sarvaiya. "Overview on Biopharmaceutics Classification System (BCS) based biowaiver requirements in African countries." International Journal of Drug Regulatory Affairs 9, no. 2 (June 15, 2021): 26–29. http://dx.doi.org/10.22270/ijdra.v9i2.465.

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Biopharmaceutics Classification System (BCS)-based biowaiver are meant to reduce the need for establishing in vivo bioequivalence in situations where in vitro data may be considered to provide a reasonable estimate of the relative in vivo performance of two products. The BCS is a scientific approach designed to predict medicinal absorption based on the aqueous solubility and intestinal absorptive characteristics of the Pharmaceutical product. To ensure interchangeability, the multisource product must be therapeutically equivalent to the comparator product. Types of in vivo equivalence studies include comparative pharmacokinetic studies, comparative pharmacodynamic studies and comparative clinical studies. This article briefly explains the BCS based biowaiver requirements in six major African countries i.e. Zimbabwe, South Africa, Uganda, Kenya, Botswana and Tanzania which facilitates regulatory medicine approval process when the dossier (application) is approved based on evidence of equivalence other than In vivo studies.

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Zakeri-Milani, Parvin, Zohreh Fasihi, Jafar Akbari, Ensieh Jannatabadi, Mohammad Barzegar-Jalali, Raimar Loebenberg, and Hadi Valizadeh. "Crystal-liquid Fugacity Ratio as a Surrogate Parameter for Intestinal Permeability." Journal of Pharmacy & Pharmaceutical Sciences 19, no. 3 (August 18, 2016): 312. http://dx.doi.org/10.18433/j3ks4p.

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Background: We assessed the feasibility of using crystal-liquid fugacity ratio (CLFR) as an alternative parameter for intestinal permeability in the biopharmaceutical classification (BCS) of passively absorbed drugs. Methods: Dose number, fraction of dose absorbed, intestinal permeability, and intrinsic dissolution rate were used as the input parameters. CLFR was determined using thermodynamic parameters i.e., melting point, molar fusion enthalpy, and entropy of drug molecules obtained using differential scanning calorimetry. Results: The CLFR values were in the range of 0.06-41.76 mole percent. There was a close relationship between CLFR and in vivo intestinal permeability (r > 0.8). CLFR values of greater than 2 mole percent corresponded to complete intestinal absorption. Applying CLFR versus dose number or intrinsic dissolution rate, more than 92% of tested drugs were correctly classified with respect to the reported classification system on the basis of human intestinal permeability and solubility. Conclusion: This investigation revealed that the CLFR might be an appropriate parameter for quantitative biopharmaceutical classification. This could be attributed to the fact that CLFR could be a measure of solubility of compounds in lipid bilayer which was found in this study to be directly proportional to the intestinal permeability of compounds. This classification enables researchers to define characteristics for intestinal absorption of all four BCS drug classes using suitable cutoff points for both intrinsic dissolution rate and crystal-liquid fugacity ratio. Therefore, it may be used as a surrogate for permeability studies. This article is open to POST-PUBLICATION REVIEW. Registered readers (see “For Readers”) may comment by clicking on ABSTRACT on the issue’s contents page.

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Benet, Leslie Z. "The Role of BCS (Biopharmaceutics Classification System) and BDDCS (Biopharmaceutics Drug Disposition Classification System) in Drug Development." Journal of Pharmaceutical Sciences 102, no. 1 (January 2013): 34–42. http://dx.doi.org/10.1002/jps.23359.

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Berginc, Katja, Nadica Sibinovska, Simon Žakelj, Jurij Trontelj, and Igor Legen. "Biopharmaceutical classification of desloratadine – not all drugs are classified the easy way." Acta Pharmaceutica 70, no. 2 (June 1, 2020): 131–44. http://dx.doi.org/10.2478/acph-2020-0006.

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AbstractThe biopharmaceutical classification of drugs was designed as a basis for bio-waivers – a mechanism with the double ethical benefit of delivering new drug formulations to the market with less human testing and lower cost. However, many drugs defy simple classification because in vitro permeability and stability assessment can be challenging as shown in this study for desloratadine. Literature shows that desloratadine is highly soluble, while data on luminal stability and permeability are circumstantial. Combined with borderline bioavailability and not really known fraction of absorbed dose, desloratadine was found to be a good example for showing the innovative in vitro approaches necessary to unambiguously classify desloratadine according to Biopharmaceutical Classification System (BCS) guideline. Presented study undoubtedly confirmed that desloratadine solubility is high and dissolution is very rapid for immediate release reference tablets. We have demonstrated deslorata-dine stability under legally required conditions and also in more physiologically relevant media. High in vitro desloratadine permeability was confirmed using Caco-2 and Parallel Artificial Membrane Permeability Assay (PAMPA). Well-established in vitro model with rat intestinal tissue could not be used due to reasons elaborated in this paper.

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Fagerholm, Urban. "Evaluation and suggested improvements of the Biopharmaceutics Classification System (BCS)." Journal of Pharmacy and Pharmacology 59, no. 6 (June 2007): 751–57. http://dx.doi.org/10.1211/jpp.59.6.0001.

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de Castro, Lara Maria Lopes, Jacqueline de Souza, Tamires Guedes Caldeira, Bruna de Carvalho Mapa, Anna Flávia Matos Soares, Bruna Gomes Pegorelli, Carolina Carvalho Della Croce, and Neila Márcia Silva Barcellos. "The Evaluation of Valsartan Biopharmaceutics Properties." Current Drug Research Reviews 12, no. 1 (June 19, 2020): 52–62. http://dx.doi.org/10.2174/2589977511666191210151120.

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Background: Solubility, intestinal permeability and dissolution are the main factors that govern the rate and extent of drugs absorption and are directly related to bioavailability. Biopharmaceutics Classification System (BCS) is an important tool which uses in vitro results for comparison with bioavailability in vivo (biowaiver). Valsartan is widely used in the treatment of hypertension and shows different BCS classification in the literature (BCS class II or III). Objective: This work proposes the study of valsartan biopharmaceutics properties and its BCS classification. Methods: High Performance Liquid Chromatography (HPLC) method was developed and validated to quantify the drug in buffers pH 1.2, 4.5 and 6.8 respectively. Valsartan solubility was determined in these three different media using shake flask method and intrinsic dissolution rate. Evaluation of dissolution profile from coated tablets was conducted. Results: The low solubility (pH 1.2 and 4.5) and high solubility (pH 6.8) were observed for both solubility methods. Permeability data reported from the literature showed that valsartan is a low permeability drug. Valsartan presented the rapid release profile only in pH 6.8. Conclusion: We defined that valsartan is a class IV drug, in disagreement with what has been published so far. It is important to emphasize that the conditions considered here are indicated to define the biopharmaceutics classification by regulatory agencies.

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Papich, Mark G., and Marilyn N. Martinez. "Applying Biopharmaceutical Classification System (BCS) Criteria to Predict Oral Absorption of Drugs in Dogs: Challenges and Pitfalls." AAPS Journal 17, no. 4 (April 29, 2015): 948–64. http://dx.doi.org/10.1208/s12248-015-9743-7.

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Cysewski, Piotr, and Maciej Przybyłek. "Predicting Value of Binding Constants of Organic Ligands to Beta-Cyclodextrin: Application of MARSplines and Descriptors Encoded in SMILES String." Symmetry 11, no. 7 (July 15, 2019): 922. http://dx.doi.org/10.3390/sym11070922.

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The quantitative structure–activity relationship (QSPR) model was formulated to quantify values of the binding constant (lnK) of a series of ligands to beta–cyclodextrin (β-CD). For this purpose, the multivariate adaptive regression splines (MARSplines) methodology was adopted with molecular descriptors derived from the simplified molecular input line entry specification (SMILES) strings. This approach allows discovery of regression equations consisting of new non-linear components (basis functions) being combinations of molecular descriptors. The model was subjected to the standard internal and external validation procedures, which indicated its high predictive power. The appearance of polarity-related descriptors, such as XlogP, confirms the hydrophobic nature of the cyclodextrin cavity. The model can be used for predicting the affinity of new ligands to β-CD. However, a non-standard application was also proposed for classification into Biopharmaceutical Classification System (BCS) drug types. It was found that a single parameter, which is the estimated value of lnK, is sufficient to distinguish highly permeable drugs (BCS class I and II) from low permeable ones (BCS class II and IV). In general, it was found that drugs of the former group exhibit higher affinity to β-CD then the latter group (class III and IV).

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Sarangi, Babita, Utpal Jana, Narahari N. Palei, Guru P. Mohanta, and Prabal K. Manna. "Solid Lipid Nanoparticles: A Potential Approach for Drug Delivery System." Nanoscience &Nanotechnology-Asia 9, no. 2 (June 25, 2019): 142–56. http://dx.doi.org/10.2174/2210681208666180321144536.

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The therapeutic efficacy of perorally administered drug is often concealed by their poor oral bioavailability (BA) and low metabolic stability in the gastrointestinal tract (GIT). Most of the newly discovered drug molecules are of high molecular weight and belong to biopharmaceutical classification system (BCS) – II. Poor aqueous solubility and high membrane permeability characteristics of BCS – II drugs limit BA after oral administration. Recently, lipid-based drug delivery (LBDD) systems have gained much importance due to their ability to improve the solubility and BA of poorly soluble drugs. Oral delivery of drugs incorporated in solid lipid nanoparticles (SLNs) has gained considerable interest since the last two decades. SLNs have advantages above the others, as compared to polymer toxicity which is low, as inexpensive excipients and organic solvents are not used. SLNs offer the possibility to develop new therapeutics due to their unique size-dependent properties. An attempt to incorporate drugs into SLNs offers a new prototype in drug delivery system which can be utilized for drug targeting to specific tissue. This review presents elaborate information of SLNs with their aim, advantages, challenges and limitations, the principle of formulation, routes of administration and their biodistribution. It also describes the gastrointestinal absorption and the factors affecting absorption of SLNs from GIT along with its application.

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delMoral-Sanchez, Jose-Manuel, Isabel Gonzalez-Alvarez, Marta Gonzalez-Alvarez, Andres Navarro, and Marival Bermejo. "Classification of WHO Essential Oral Medicines for Children Applying a Provisional Pediatric Biopharmaceutics Classification System." Pharmaceutics 11, no. 11 (October 31, 2019): 567. http://dx.doi.org/10.3390/pharmaceutics11110567.

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The objective was using the Essential Medicines List for children by the World Health Organization (WHO) to create a pediatric biopharmaceutics classification system (pBCS) of the oral drugs included in the Essential Medicines List by the World Health Organization and to compare our results with the BCS for adults (aBCS). Several methods to estimate the oral drug dose in different pediatric groups were used to calculate dose number (Do) and solubility (high/low). The estimation of the gastrointestinal water volume was adapted to each pediatric group. Provisional permeability classification was done by comparison of each drug lipophilicity versus metoprolol as the model drug of high permeability. As a result, 24.5% of the included drugs moved from the favorable to unfavorable class (i.e., from high to low solubility). Observed changes point out potential differences in product performance in pediatrics compared to adults, due to changes in the limiting factors for absorption. BCS Class Changes 1 to 2 or 3 to 4 are indicative of drugs that could be more sensitive to the choice of appropriate excipient in the development process. Validating a pBCS for each age group would provide a valuable tool to apply in specific pediatric formulation design by reducing time and costs and avoiding unnecessary pediatric experiments restricted due to ethical reasons. Additionally, pBCS could minimize the associated risks to the use of adult medicines or pharmaceutical compound formulations.

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del Moral Sanchez, Jose Manuel, Isabel Gonzalez-Alvarez, Aaron Cerda-Revert, Marta Gonzalez-Alvarez, Andres Navarro-Ruiz, Gordon L. Amidon, and Marival Bermejo. "Biopharmaceutical optimization in neglected diseases for paediatric patients by applying the provisional paediatric biopharmaceutical classification system." British Journal of Clinical Pharmacology 84, no. 10 (July 17, 2018): 2231–41. http://dx.doi.org/10.1111/bcp.13650.

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Albetawi, Saba, Amer Abdalhafez, Ala Abu-Zaid, Aseel Matrouk, and Noor Alhourani. "Recent solubility and dissolution enhancement techniques for repaglinide a BCS class II drug: a review." Pharmacia 68, no. 3 (August 4, 2021): 573–83. http://dx.doi.org/10.3897/pharmacia.68.e66586.

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Repaglinide is an oral blood-glucose-lowering drug used to manage type-2 diabetes mellitus by lowering post-prandial glucose by stimulating insulin secretion from pancreatic beta cells. According to the biopharmaceutical classification system, repaglinide falls under the class II category. For such drugs, limited solubility and poor dissolution rate are the major hurdles to overcome by formulation scientists, as they hinder drug absorption and lead to inadequate therapeutic effects. Therefore, this review aims to discuss in depth the various approaches investigated in the past five years to improve the solubility and dissolution of orally administered repaglinide: namely, solid dispersion, co-amorphous technology, cyclodextrin complexation, phospholipid complexes and polymeric micelles, nanocrystals, nanosuspensions and nanofibers.

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Kus-Slowinska, Marta, Monika Wrzaskowska, Izabela Ibragimow, Piotr Igor Czaklosz, Anna Olejnik, and Hanna Piotrowska-Kempisty. "Solubility, Permeability, and Dissolution Rate of Naftidrofuryl Oxalate Based on BCS Criteria." Pharmaceutics 12, no. 12 (December 19, 2020): 1238. http://dx.doi.org/10.3390/pharmaceutics12121238.

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The Biopharmaceutics Classification System (BCS) was conceived to classify drug substances by their in vitro aqueous solubility and permeability properties. The essential activity of naftidrofuryl oxalate (NF) has been described as the inhibition of the serotonin receptors (5-HT2), resulting in vasodilation and decreasing blood pressure. Since the early 1980s, NF has been used to treat several venous and cerebral diseases. There is no data available on the BCS classification of NF. However, based on its physical-chemical properties, NF might be considered to belong to the 1st or the 3rd BCS class. The present study aimed to provide data concerning the solubility and permeability of NF through Caco-2 monolayers and propose its preliminary classification into BCS. We showed that NF is a highly soluble and permeable drug substance; thus, it might be suggested to belong to BCS class I. Additionally, a high dissolution rate of the encapsulated NF based on Praxilene® 100 mg formulation was revealed. Hence, it might be considered as an immediate-release (IR).

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Gandhi, Shivani V., William Rodriguez, Mansoor Khan, and James E. Polli. "Considerations for a Pediatric Biopharmaceutics Classification System (BCS): Application to Five Drugs." AAPS PharmSciTech 15, no. 3 (February 21, 2014): 601–11. http://dx.doi.org/10.1208/s12249-014-0084-0.

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Islami, Ayudyah, Iyan Sopyan, Dolih Gozali, and Hairunnisa Hairunnisa. "REVIEW MODIFIKASI KELARUTAN PIROKSIKAM." Jurnal Ilmiah Farmako Bahari 11, no. 1 (February 7, 2020): 89. http://dx.doi.org/10.52434/jfb.v11i1.697.

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Piroksikam, merupakan golongan NSAID, digunakan pada rheumatoid arthritis dan osteoarthritis untuk mengurangi rasa sakit. Waktu paruh piroksikam adalah 24 hingga 48 jam. Berdasarkan Biopharmaceutical Classification System (BCS), piroksikam termasuk dalam kelas II yang memiliki kelarutan air rendah, titik lelehnya 190-200oC, nilai log P 3,06, nilai pKa 6,3, dan Vd 0,14 L / kg. Kelarutan piroksikam ditentukan oleh tingkat ionisasi. Ketika pH diperoleh melalui pKa, terjadi peningkatan kelarutan dan disolusi. Oleh karena itu, modifikasi piroksikam dengan dispersi padat dan teknik kristristalisasi diharapkan dapat meningkatkan kelarutan piroksikam dan memfasilitasi formulasi piroksikam menjadi bentuk sediaan yang efektif. Namun, setiap modifikasi memiliki kelebihan dan kekurangan masing-masing yang dapat dipertimbangkan ketika merancang piroksikam menjadi bentuk sediaan. Kata kunci: kokristal, dispersi padat, piroksikam, kelarutan, disolusi

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Patel, Jimi, Priti Mehta, and Vaishali Kothari. "COMPARISON OF GLOBAL REGULATORY GUIDELINES FOR AVAILABILITY OF DIFFERENT BIOWAIVER PROVISIONS AND APPLICATION REQUIREMENTS OF BIOPHARMACEUTICS CLASSIFICATION SYSTEM (BCS) BASED BIOWAIVER." International Journal of Drug Regulatory Affairs 3, no. 3 (February 13, 2018): 8–20. http://dx.doi.org/10.22270/ijdra.v3i3.167.

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To waive a complete and systemic Bioequivalence (BE) study, Biowaiver or Request for a Biowaiver is a fast track approach to boost the drug development process. Over the past three-four years the Biowaiver market shows greater number of Biowaiver submissions and the wider use of In-vitro permeability study. Biowaiver is a beneficial approach for getting approval of Abbreviated New Drug Application (ANDA) while, BCS based Biowaiver is the novel approach to gain approval for New Drug Application (NDA) as well as ANDA. A Biopharmaceutics Classification System (BCS) based Biowaiver is an exemption from conducting human bioequivalence studies when active ingredient and dosage form meet criteria of solubility, permeability and dissolution. The Paper covers different kind of Biowaiver approaches and the criteria for the applicability of BCS based Biowaivers in the different geographic scopes with regard to global development strategy. There is a comparison of global guidelines on provisions availability for different types of Biowaiver approaches as well as for requirements of Biowaiver based on BCS. From comparison of different global guidelines it is reviewed that most of the guidance resembles to the USFDA, EU and WHO guidelines because most of the regulatory authorities are following the BCS based Biowaiver concept as one of the three main guidance documents (USFDA, EMA, WHO) or a combination of specific requirements.

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El Harti, J., Y. Cherrah, and A. Bouklouze. "Improvement of Water Solubility of Josamycin by Inclusion Complex with -Cyclodextrin." ISRN Analytical Chemistry 2012 (March 4, 2012): 1–6. http://dx.doi.org/10.5402/2012/673564.

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Josamycin propionate (JMP) is an antibiotic belonging to the family of macrolide. According to the Biopharmaceutical Classification System (BCS), this compound can be classed in class II, low solubility and high permeability. In order to increase its apparent water solubility, inclusion complexation between Josamycin propionate and γ-cyclodextrin (γ-CD) was studied. UV spectrophotometric method was employed to investigate the phase-solubility profile and the stability constant of the complexation in aqueous medium. Solid state of the binary system prepared by coevaporation (in 50%-50% ethanol/water) has been characterized using powder X-ray diffraction (XRD) and Fourier transformation-infrared spectrometry (FTIR). These techniques indicate that JMP forms an association complex with γ-CD. The shift in the nuclear magnetic resonance spectroscopy (1H NMR) confirms the existence of the inclusion complex. Also the results obtained showed an enhancement of the solubility in water of Josamycin propionate.

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Lassoued, Mohamed Ali, Fathia Khemiss, and Souad Sfar. "Comparative study of Two In Vitro Methods for Assessing Drug Absorption: Sartorius SM 16750 Apparatus Versus Everted Gut Sac." Journal of Pharmacy & Pharmaceutical Sciences 14, no. 1 (April 8, 2011): 117. http://dx.doi.org/10.18433/j3gc7r.

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– Purpose. Oral drug administration remains the most common and most convenient way used in clinical therapy. The availability of a simple, rapid, economic and reproducible in vitro method to assess drug absorption is a very helpful tool. The purpose of this study is to compare the performance of Sartorius SM 16750 Absorption Simulator apparatus to Everted Gut Sac (EGS) technique in terms of predicting drug absorption. Methods. Permeation studies across these two in vitro models were performed with six drugs selected across the Biopharmaceutics Classification System (BCS) categories: Tramadol (class I of BCS), doxcycycline (class I of BCS), diclofenac (class II of BCS), clopidogrel (class II of BCS), metformin (class III of BCS) and chlorothiazide (class IV of BCS). Results. Apparent permeability coefficient (Papp) and diffusion profiles obtained with EGS and Sartorius SM 16750 apparatus were similar for diclofenac and metformine. But there were differences in results, for the other molecules. Conclusion. It could be concluded that the Sartorius SM 16750 apparatus, easier to carry out, could be an alternative to EGS when drug passage across intestinal barrier occurs by passive diffusion and when no efflux system is implicated in limiting the transepithelial passage.

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Uzunović, Alija, Edina Vranić, and Šeherzada Hadžidedić. "Impairment of the in vitro Release of Carbamazepine from Tablets." Bosnian Journal of Basic Medical Sciences 10, no. 3 (August 20, 2010): 234–38. http://dx.doi.org/10.17305/bjbms.2010.2693.

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Carbamazepine belongs to the class II biopharmaceutical classification system (BCS) which is characterized by a high per-oral dose, a low aqueous solubility and a high membrane permeability. The bioavailability of such a drug is limited by the dissolution rate. The present study deals with the formulations of immediate release tablets of poorly soluble carbamazepine. As model tablets for this investigation, two formulations (named “A” and “B” formulations) of carbamazepine tablets labeled to contain 200 mg were evaluated. The aim of this study was to establish possible differences in dissolution profile of these two formulations purchased from the local market.The increased crystallinity together with enlarged particle size, enhanced aggregation and decreased wettability of the drug, resulted in insufficient dissolution rate for formulation “B’.’ From the dissolution point of view, this formulation was inferior to the formulation “A, due to the solubilization effect.

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Nainwal, Nidhi, Ranjit Singh, Sunil Jawla, and Vikas Anand Saharan. "The Solubility-Permeability Interplay for Solubility-Enabling Oral Formulations." Current Drug Targets 20, no. 14 (October 14, 2019): 1434–46. http://dx.doi.org/10.2174/1389450120666190717114521.

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The Biopharmaceutical classification system (BCS) classifies the drugs based on their intrinsic solubility and intestinal permeability. The drugs with good solubility and intestinal permeability have good bioavailability. The drugs with poor solubility and poor permeability have solubility dependent and permeability dependent bioavailability, respectively. In the current pharmaceutical field, most of the drugs have poor solubility. To solve the problem of poor solubility, various solubility enhancement approaches have been successfully used. The effects of these solubility enhancing approaches on the intestinal permeability of the drugs are a matter of concern, and must not be overlooked. The current review article focuses on the effect of various solubility enhancing approaches viz. cyclodextrin, surfactant, cosolvent, hydrotropes, and amorphous solid dispersion, on the intestinal permeability of drugs. This article will help in the designing of the optimized formulations having balanced solubility enhancement without affecting the permeability of drugs.

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Kolluru, Lakshmi, Prachi Atre, and Syed Rizvi. "Characterization and Applications of Colloidal Systems as Versatile Drug Delivery Carriers for Parenteral Formulations." Pharmaceuticals 14, no. 2 (January 29, 2021): 108. http://dx.doi.org/10.3390/ph14020108.

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Preparing a suitable formulation for parenteral administration is already a difficult task; this, coupled with poor water-soluble new chemical entity (NCE), complicates this situation even further. There are several methodologies available to enhance water solubility, but this alone does not entail successful formulation. Making a micro/nano emulsion with a suitable surfactant not only increases the drug solubility but also the cell membrane permeability. Thus, not only biopharmaceutic classification system (BCS)-II (low solubility compounds) but also BCS-III (low permeability) and BCS-IV drugs (low solubility and low permeability) can be further exploited. Those drug candidates otherwise will not move further in NCE evaluation or clinical trials. This succinct review article delves into various aspects of biphasic micro/nano emulsion systems for parenteral drug delivery including the structure of the biphasic colloidal systems, characterization parameters, stability issues, regulatory considerations, and applications in life sciences.

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Kumar, Sachin, Ramneek Kaur, Rashi Rajput, and Manisha Singh. "Bio Pharmaceutics Classification System (BCS) Class IV Drug Nanoparticles: Quantum Leap to Improve Their Therapeutic Index." Advanced Pharmaceutical Bulletin 8, no. 4 (November 29, 2018): 617–25. http://dx.doi.org/10.15171/apb.2018.070.

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Purpose: Biopharmaceutics classification system (BCS) class IV compounds, exhibits least oral bioavailability, low solubility and intestinal permeability among all pharmaceutical classes of drugs. Thus, these drugs need more compatible and efficient delivery system. Since, their solubility in various medium, remains a limitation so, polymeric nano coacervates based drug loading with modified approach for them may prove to be a solution ahead. Therefore, in present study Chitosan is opted for encapsulating the BCS class IV drug (Hydrochlorothiazide) to attain better stability, enhanced permeability and lower toxicity. Methods: For this study, Hydrochlorothiazide (HCTZ) was opted for formulating chitosan based nano-coacervate system. Results: Optimized HCTZ nanocoacervates exhibited the average particle size of 91.39 ± 0.75 nm with Poly-dispersity index score of 0.159 ± 0.01, indicating homogeneity of colloidal solution. Zeta potential and encapsulation efficiency of HCTZ nanocoacervates were recorded as -18.9 ± 0.8 mV and 76.69 ± 0.82 % respectively. Further, from TEM and SEM evaluation the average particle size for the same were found in conformity (35-50 nm), with almost spherical morphology. Also, the EDX (Electron Dispersive X-ray) spectrometry and FT – IR analysis of optimized formulation indicated the balanced chemical composition and interaction between the polymeric molecules. The HCTZ nano coacervates showed the linear diffusion profile through the dialysis membrane. Conclusion: We can conclude from the present study that the optimized HCTZ nano coacervates may prove to be a suitable potential option for effective delivery of BCS class IV drugs.

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Kshirsagar, Ajay D., Omkar N. Shikare, and Haidarali M. Shaikh. "BIOAVAILABILITY AND BIOEQUIVALENCE STUDY IN CORRELATION OF BIOPHARMACEUTICS CLASSIFICATION SYSTEM (BCS) AND POSSIBLE MODIFICATION." Journal of Pharmaceutical and Scientific Innovation 2, no. 6 (December 15, 2013): 10–16. http://dx.doi.org/10.7897/2277-4572.02681.

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Blume, Henning H., and Barbara S. Schug. "The biopharmaceutics classification system (BCS): Class III drugs — better candidates for BA/BE waiver?" European Journal of Pharmaceutical Sciences 9, no. 2 (December 1999): 117–21. http://dx.doi.org/10.1016/s0928-0987(99)00076-7.

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Mehta, Mehul U., Ramana S. Uppoor, Dale P. Conner, Paul Seo, Jayabharathi Vaidyanathan, Donna A. Volpe, Ethan Stier, et al. "Impact of the US FDA “Biopharmaceutics Classification System” (BCS) Guidance on Global Drug Development." Molecular Pharmaceutics 14, no. 12 (November 7, 2017): 4334–38. http://dx.doi.org/10.1021/acs.molpharmaceut.7b00687.

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Kharb, Manju, Pawan Jalwal, Shikha Rathi, and Suresh Kumar. "Preparation and Characterization of Novel Anti-cancer drug (s) loaded Co-crystals." Journal of University of Shanghai for Science and Technology 23, no. 09 (September 21, 2021): 1006–19. http://dx.doi.org/10.51201/jusst/21/09647.

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Background: Taxanes constitute an important class of anti-cancer agents, which are widely prescribed for the management of cancers like breast, lung and ovaries. These agents belong to Biopharmaceutical Classification System (BCS) class IV, which are neither soluble in the aqueous systems nor permeable across the biological membranes. Objectve: Due to these concerns only, the oral bioavailabilities of these drugs are too low. Looking into these concerns, it was envisaged to develop co-crystals of docetaxel with syringic acid. Methods: For the preparation of co-crystals no single method is used. The methods range from spray drying, crystallization, ultrasonication and freeze drying to supercritical fluid methodologies. Results: The novel co-crystal not only improved the solubility and dissolution rates of the drug, but also resulted in improved pharmacokinetic profile. Conclusion: The present findings provide an economic and viable approach to improve the solubility and absorption profile of a drug, which is a vital component of the anticancer chemotherapy. Such studies provide a hope for the development of approaches to improve the solubility and permeability of drugs with challenges.

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Varshosaz, Jaleh, Erfaneh Ghassami, and Saeedeh Ahmadipour. "Crystal Engineering for Enhanced Solubility and Bioavailability of Poorly Soluble Drugs." Current Pharmaceutical Design 24, no. 21 (October 15, 2018): 2473–96. http://dx.doi.org/10.2174/1381612824666180712104447.

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Background: Crystal engineering is dealing with the creation of new structures and new properties in drug molecules through inter-molecular interactions. Researchers of pharmaceutical sciences have used this knowledge to alter the structure of crystalline medications in order to remedy the problems of more than 40% of the new designed drugs which suffer from low solubility and consequently, low bioavailability which have limited their clinical application. Methods: This review covers a broad spectrum of aspects of the application of crystal engineering in pharmaceutics and includes a comprehensive wide range of different techniques used in crystal engineering of active pharmaceutical ingredients (API) to compensate the low water solubility and bioavailability of drugs related specially to class II of biopharmaceutical classification system (BCS). Results: These techniques include; crystalline habit modification, polymorphism, solvates and hydrates, cocrystals, surface modification, crystallization, spherical agglomeration, liquisolid crystals and solid dispersions which are introduced and discussed in this review article. Conclusion: Each of these techniques has advantages and limitations which are emphasized on them.

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Mantas, Athanasios, Valentine Labbe, Irena Loryan, and Albert Mihranyan. "Amorphisation of Free Acid Ibuprofen and Other Profens in Mixtures with Nanocellulose: Dry Powder Formulation Strategy for Enhanced Solubility." Pharmaceutics 11, no. 2 (February 6, 2019): 68. http://dx.doi.org/10.3390/pharmaceutics11020068.

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The formulation of arylpropionic acid derivatives (profens), which are poorly soluble Biopharmaceutical Classification System (BCS) Type II drugs, has a strong impact on their therapeutic action. This article shows that heat-treated powder mixtures of free acid profens with high surface area Cladophora cellulose induces drug amorphization and results in enhanced solubility and bioavailability. Similar mixtures produced using conventional low surface area cellulose, i.e., microcrystalline cellulose, does not produce the same effect. The concept is thoroughly described and links the solid-state characterization data, such as differential scanning calorimetry, X-ray powder diffraction, and Fourier-transform infra-red spectroscopy, with in vitro dissolution in biorelevant media and in vivo pharmacokinetic analysis in rats. The concept is demonstrated for several substances from the profens group, including ibuprofen (main model drug), ketoprofen, flurbiprofen, and naproxen. The presented approach opens new ways to produce solid dosage forms of profen drugs in their free acidic form as alternatives to existing analogues, e.g., drug-salt conjugates or soft gel liquid capsules.

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Darusman, Fitrianti, and Endah Rahayu. "Penentuan Parameter Termodinamika Pembentukan Kompleks Inklusi Glimepirid-Betasiklodekstrin." Indonesian Journal of Pharmaceutical Science and Technology 4, no. 3 (October 24, 2017): 112. http://dx.doi.org/10.15416/ijpst.v4i3.13858.

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Glimepirid merupakan obat antidiabetika oral golongan sulfonilurea generasi ketiga yang termasuk dalam Biopharmaceutical Classification System (BCS) kelas II dengan sifat kelarutan praktis tidak larut dalam air sehingga dapat ditingkatkan kelarutannya dengan pembentukan kompleks inklusi menggunakan senyawa turunan siklodekstrin yaitu betasiklodekstrin yang memiliki rongga toroidal dengan bagian dalam bersifat hidrofobik dan bagian luar bersifat hidrofilik. Penelitian ini dilakukan untuk menentukan harga tetapan stabilitas kompleks berdasarkan parameter termodinamika (ΔH, ΔG, dan ΔS) pada proses pembentukan kompleks inklusi glimepirid-betasiklodekstrin. Penelitian dilakukan dalam dapar asetat pH 6,2 dan dapar fosfat pH 7,4 pada suhu 32°, 37° dan 42°C. Hasil penelitian menunjukkan bahwa glimepirid dapat berinteraksi membentuk kompleks inklusi dengan betasiklodekstrin. Interaksi antara glimepirid dengan betasiklodekstrin pada pH 6,2 berlangsung secara eksotermik (ΔH<0), proses terjadi secara spontan (ΔG<0) dan terjadi peningkatan ketidakteraturan sistem (ΔS positif). Pada pH 7,4 interaksi berlangsung secara eksotermik, proses terjadi secara spontan (ΔG<0) dan terjadi penurunan ketidakteraturan sistem (ΔS negatif).Kata kunci : glimepirid, betasiklodesktrin, kompleks inklusi, termodinamika.

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Gunda, Raghavendra Kumar. "Design, formulation and characterization of oral disintegrating tablets for lamotrigine." Journal of Analytical & Pharmaceutical Research 9, no. 2 (March 20, 2020): 60–66. http://dx.doi.org/10.15406/japlr.2020.09.00353.

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Objective: The purpose of present investigation to formulate, characterize the oral dissolving tablets (ODT) for Lamotrigine. Lamotrigine, an antiepileptic agent, belongs to type –II as per Biopharmaceutical Classification System (BCS). Methods: ODT formulations of Lamotrigine were prepared using different quantities of Sodium Starch Glycolate & Crospovidone employed as Super disintegrants by Direct Compression technique. Nine trials were formulated and evaluated for Pharmaceutical Product Performance. Results: Results shows that all the formulations were lie within the acceptance criterion and the In-vitro dissolution profiles were subjected to kinetic modeling. Conclusion: Formulation (F4) containing 35 mg of Sodium Starch Glycolate & 40 mg of Crospovidone was found to be best one among all and also similar to the Marketed product (LAMICTAL-25) (f2=73.17, f1=3.65 & No significant difference, t=0.0218) to marketed product. Formulation (F4) follows First order, Higuchi’s kinetics, mechanism of drug release was found to be Non-Fickian Diffusion (n= 0.554).

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Maestrelli, Francesca, Marzia Cirri, Fátima García-Villén, Ana Borrego-Sánchez, César Viseras Iborra, and Paola Mura. "Tablets of “Hydrochlorothiazide in Cyclodextrin in Nanoclay”: A New Nanohybrid System with Enhanced Dissolution Properties." Pharmaceutics 12, no. 2 (January 28, 2020): 104. http://dx.doi.org/10.3390/pharmaceutics12020104.

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Hydrochlorothiazide (HCT), a Biopharmaceutical Classification System (BCS) class IV drug, is characterized by low solubility and permeability, that negatively affect its oral bioavailability, reducing its therapeutic efficacy. The combined use of cyclodextrins (CDs) and nanoclays (NCs) recently proved to be a successful strategy in developing delivery systems able to merge the potential benefits of both carriers. In this work, several binary systems of CDs or NCs with the drug were obtained, using different drug:carrier ratios and preparation techniques, and characterized in solution and in solid state, to properly select the most effective system and preparation method. Then, the best CD (RAMEB) and NC (sepiolite), at the best drug:carrier ratio, was selected for preparation of the ternary system by co-evaporation and emerged as the most effective preparation method. The combined presence of RAMEB and sepiolite gave rise to a synergistic improvement of drug dissolution properties, with a two-fold increase in the amount of drug dissolved as compared with the corresponding HCT-RAMEB system, resulting in an approximately 12-fold increase in drug solubility as compared with the drug alone. The ternary system that was co-evaporated was then selected for a tablet formulation. The obtained tablets were fully characterized for technological properties and clearly revealed a better drug dissolution performance than the commercial reference tablet (Esidrex®).

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Hibatullah Rahadatul Aisy, Zalfa, Oktavia Eka Puspita, and Alvan Febrian Shalas. "Optimasi Formula Nanoemulsi Nifedipin Dengan Metode Self-Nanoemulsifying Drug Delivery System (SNEDDS)." Pharmaceutical Journal of Indonesia 6, no. 2 (June 30, 2021): 85–95. http://dx.doi.org/10.21776/ub.pji.2021.006.02.3.

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Nifedipin adalah obat golongan calcium channel blocker yang digunakan untuk terapi angina pektoris dan hipertensi. Nifedipin memiliki kelarutan yang rendah dalam air dan bioavailabilitas yang rendah. Berdasarkan penggolongan Biopharmaceutical Classification System (BCS), nifedipin termasuk dalam kelas II. Salah satu cara untuk meningkatkan kelarutan nifedipin adalah membuat formulasi nanoemulsi nifedipin. Penelitian ini bertujuan untuk memperoleh nanoemulsi nifedipin yang optimal menggunakan metode Self-Nanoemulsifying Drug Delivery System (SNEDDS). SNEDDS merupakan campuran isotropik dari fase minyak, surfaktan, dan kosurfaktan yang akan membentuk nanoemulsi minyak dalam air saat ditambahkan media aqueous dengan sedikit pengadukan. Nanoemulsi nifedipin diperoleh melalui formula SNEDDS yang terdiri dari castor oil sebagai fase minyak, Croduret 50SS dan Span 80 sebagai surfaktan, dan PEG 400 sebagai sebagai kosurfaktan dengan rasio fase minyak:surfaktan:kosurfaktan sebesar 1:6:3. Hasil karakterisasi SNEDDS nifedipin yang optimal menunjukkan karakteristik organoleptik homogen, berwarna kuning, jernih, kental, memiliki aroma khas SNEDDS, persen transmitansi sebesar 98,37 ± 0,49%, waktu emulsifikasi dalam akuades dan dalam HCl 0,1 N berturut-turut sebesar 14,09 ± 1,05 detik dan 11,38 ± 0,66 detik, ukuran globul sebesar 24,05 ± 0,02 nm, indeks polidispersitas sebesar 0,277 ± 0,0038, pH sebesar 6,95, loading dose capacity sebesar 50 mg nifedipin dalam 1 g SNEDDS dan kadar nifedipin dalam formula SNEDDS sebesar 9,857 ± 0,345 mg/g. Uji stabilitas termodinamika dan uji stabilitas on going menunjukkan bahwa sediaan stabil

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Gupta, Shweta, Rajesh Kesarla, and Abdelwahab Omri. "Formulation Strategies to Improve the Bioavailability of Poorly Absorbed Drugs with Special Emphasis on Self-Emulsifying Systems." ISRN Pharmaceutics 2013 (December 26, 2013): 1–16. http://dx.doi.org/10.1155/2013/848043.

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Poorly water-soluble drug candidates are becoming more prevalent. It has been estimated that approximately 60–70% of the drug molecules are insufficiently soluble in aqueous media and/or have very low permeability to allow for their adequate and reproducible absorption from the gastrointestinal tract (GIT) following oral administration. Formulation scientists have to adopt various strategies to enhance their absorption. Lipidic formulations are found to be a promising approach to combat the challenges. In this review article, potential advantages and drawbacks of various conventional techniques and the newer approaches specifically the self-emulsifying systems are discussed. Various components of the self-emulsifying systems and their selection criteria are critically reviewed. The attempts of various scientists to transform the liquid self-emulsifying drug delivery systems (SEDDS) to solid-SEDDS by adsorption, spray drying, lyophilization, melt granulation, extrusion, and so forth to formulate various dosage forms like self emulsifying capsules, tablets, controlled release pellets, beads, microspheres, nanoparticles, suppositories, implants, and so forth have also been included. Formulation of SEDDS is a potential strategy to deliver new drug molecules with enhanced bioavailability mostly exhibiting poor aqueous solubility. The self-emulsifying system offers various advantages over other drug delivery systems having potential to solve various problems associated with drugs of all the classes of biopharmaceutical classification system (BCS).

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Cristofoletti, Rodrigo, Vinod P. Shah, Peter Langguth, James E. Polli, Mehul Mehta, Bertil Abrahamsson, Jennifer B. Dressman, and Pablo Quiroga. "Meeting Report: International Workshop on Implementation of Biowaivers Based on the Biopharmaceutics Classification System (BCS)." Dissolution Technologies 22, no. 2 (2015): 77–81. http://dx.doi.org/10.14227/dt220215p77.

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Van Oudtshoorn, Joy Elizabeth, Alfredo García-Arieta, Gustavo Mendes Lima Santos, Christopher Crane, Clare Rodrigues, Craig Simon, Ji Myoung Kim, et al. "A Survey of the Regulatory Requirements for BCS-Based Biowaivers for Solid Oral Dosage Forms by Participating Regulators and Organisations of the International Generic Drug Regulators Programme." Journal of Pharmacy & Pharmaceutical Sciences 21, no. 1 (January 31, 2018): 27. http://dx.doi.org/10.18433/j3x93k.

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Purpose: The Biopharmaceutics Classification System (BCS) based biowaiver is a scientific model which enables the substitution of in vivo bioequivalence studies with in vitro data as evidence of therapeutic equivalence subject to certain conditions. Despite being based on the same principles, BCS-based biowaivers are interpreted and regulated differently among international regulatory agencies. In this survey, the Bioequivalence Working Group (BEWG) of the International Generic Drug Regulators Programme (IGDRP) compared the criteria for BCS-based biowaivers applied by the participating regulators and organisations. Methods: Differences and similarities regarding solubility, permeability, dissolution, excipients and fixed-dose combination products, were identified and compared in a detailed survey of each participant’s criteria for BCS-based biowaivers. These criteria were determined based upon the participants’ respective regulatory guidance documents, policies and practices. Results: This review has, with the exception of two participants who do not accept BCS-based biowaivers, revealed that most IGDRP participants interpret the BCS principles and conditions similarly but notable differences exist in the application of these principles. Conclusion: Although many similarities exist, this review identifies several opportunities for greater convergence of regulatory requirements amongst the surveyed jurisdictions. This article is open to POST-PUBLICATION REVIEW. Registered readers (see “For Readers”) may comment by clicking on ABSTRACT on the issue’s contents page

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Khames, Ahmed. "Formulation and Characterization of Eplerenone Nanoemulsion Liquisolids, An Oral Delivery System with Higher Release Rate and Improved Bioavailability." Pharmaceutics 11, no. 1 (January 18, 2019): 40. http://dx.doi.org/10.3390/pharmaceutics11010040.

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Because Eplerenone (EPL) is a Biopharmaceutical Classification System (BCS) class-II drug and is prone to extensive liver degradation, it suffers from poor bioavailability after oral administration. This work aimed to prepare liquisolids loaded with EPL-nanoemulsions (EPL-NEs) that have a higher drug release rate and improved bioavailability by the oral route. Based on solubility studies, mixtures of Triacetin (oil) and Kolliphor EL/PEG 400 surfactant/co-surfactant (Smix) in different ratios were used to prepare EPL-NE systems, which were characterized and optimized for droplet size, zeta potential, polydispersity index (PDI), and drug content. Systems were then loaded onto liquisolid formulations and fully evaluated. A liquisolid formulation with better drug release and tableting properties was selected and compared to EPL-NEs and conventional EPL oral tablets in solid-state characterization studies and bioavailability studies in rabbits. Only five NEs prepared at 1:3, 1:2, and 3:1 Smix met the specified optimization criteria. The drug release rate from liquisolids was significantly increased (90% within 45 minutes). EPL-NE also showed significantly improved drug release but with a sustained pattern for four hours. Liquisolid bioavailability reached 2.1 and 1.2 relative to conventional tablets and EPL-NE. This suggests that the EPL-NE liquisolid is a promising oral delivery system with a higher drug release rate, enhanced absorption, decreased liver degradation, and improved bioavailability.

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Nurismi, Eldya, Henni Rosaini, and dan Maria Dona Octavia. "Review: Effect of Different Methods on the Multicomponents Crystal Formation from Medicinal Natural Ingredient Compounds." International Journal of Pharmaceutical Sciences and Medicine 6, no. 5 (May 30, 2021): 32–39. http://dx.doi.org/10.47760/ijpsm.2021.v06i05.004.

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Solubility is an important parameter for the bioavailability of drugs that are difficult to dissolve. Natural compounds that are included in class II in the Biopharmaceutics Classification System (BCS) are Apigenin, Quercetin, Genistein, Curcumin, and Piperin. These drugs have low solubility in water and high permeability so that they affect the dissolution rate and as well as their bioavailability, to increase the solubility they are made with multicomponent crystals. This review aims to provide information on the method of making crystal multicomponent to increase the solubility and dissolution rate of BCS II drugs. Several methods that can be used in multicomponent are solvent drop grinding, solvent evaporation, assisted grinding, and slurry. The results showed that multicomponent crystals using several methods could increase the solubility and dissolution rates.

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Bhadale, Rupali, and Vaishali Londhe. "Inclusion Complex of Iloperidone with Sulfobutyl Ether Beta-Cyclodextrin: Characterization and Dissolution Studies." Proceedings 78, no. 1 (December 1, 2020): 22. http://dx.doi.org/10.3390/iecp2020-08715.

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Iloperidone (ILO) is a second-generation antipsychotic drug and a first-line treatment approved by USFDA in May 2009. Iloperidone belongs to Biopharmaceutical Classification Systems (BCS) class II; thus, it is poorly water-soluble, highly permeable, and has pH-dependent solubility. Cyclodextrins and their derivatives have a wide range of applications in different formulations due to their complexation ability, which improves the solubility, stability, safety, and bioavailability of a drug. We have tried the complexation of iloperidone with sulfobutyl ether-β-cyclodextrin (SEβCD) to improve its solubility and dissolution. Complexation was done by the kneading method. The characterization of the SEβCD complexes with Iloperidone was done by FTIR, differential scanning calorimetry (DSC), saturation solubility, etc. A multimedia dissolution of the complex was carried out and compared with the plain drug. A significant improvement in drug release was found from SEβCD complexes in all media when compared with the drug alone.

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Chaturvedi, Shashank, and Raghav Mishra. "Insight into Delivery Approaches for Biopharmaceutics Classification System Class II and IV Drugs." Drug Delivery Letters 10, no. 4 (November 20, 2020): 255–77. http://dx.doi.org/10.2174/2210303110999200712185109.

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: Formulation development of BCS Class II and IV drugs is a challenging task due to their poor solubility and permeability issue. : An extensive literature survey was conducted to explore the relevant pharmaceutical approaches that have been used for solving the issue of poor solubility and permeability in the recent past. : It has been found that a plethora of approaches have been investigated for addressing the issue of poor solubility and or permeability. These include physical modifications (modification of crystal habit, particle size reduction, complexation, polymorphism and drug dispersion in carriers), chemical modifications (salt formation), and formulation modifications (Nanotechnology-based approaches and hydrotropy). : The physical and chemical modification approaches can be effectively used to enhance the solubility and dissolution rate of poorly soluble drugs, but the additional problem of poor permeability has been better addressed by lipid-based drug delivery systems. As the latter presents the drug in the solubilized state, bypass first-pass effects, circumvent the effect of Para-glycoprotein mediated efflux of drugs, hence contributing to overall bioavailability enhancement.

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Agiba, Ahmed M. "Liquisolid Technology: A State-of-the-Art Review on the Current State, Challenges, New and Emerging Technologies for Next Generation." Current Drug Delivery 17, no. 9 (October 27, 2020): 736–54. http://dx.doi.org/10.2174/1567201817999200729121914.

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Nowadays, the focus has been shifted to new technologies for improving drug solubility, permeability, and bioavailability, amid unprecedentedly increasing the number of newly discovered Active Pharmaceutical Ingredients (APIs), which are mostly categorized under Biopharmaceutical Classification System (BCS) as class-II and class IV. Traditional technologies and classical formulation strategies often fail to address most of the formulation problems associated with new APIs, particularly solubility and bioavailability. Therefore, exploring new and innovative technologies on an industrial scale is a prerequisite and requires modernization of manufacturing processes, as well as more advanced research and development. Liquisolid technology is a new, innovative industrial technology, particularly designed for either improving the release rates of poorly absorbed drugs or controlling their release pattern by achieving sustained-release profiles with zero-order release kinetics. Besides, it is a promising photoprotective system for photosensitive drugs and can further be used for modulating the drug microenvironmental pH. The next generation of liquisolid systems stems from a set of emerging technologies, such as liqui-pellet technology, which originates from combining liquisolid technology with pelletization technique, particularly extrusion-spheronization technique. This review article highlights the current state of liquisolid technology, ongoing challenges, characterization and applications, possible future prospects, the advent of new and emerging technologies, and the revolution of the next generation of liquisolid technology.

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Asati Amit V, Salunkhe Kishor S, Chavan Machindra J, Chintamani Ravindra B, and Rajput Singh Rudra Pratap. "Solubility enhancement of BCS classified IV drug - Apixaban by preparation and evaluation of Mesoporous Nanomatrix." International Journal of Research in Pharmaceutical Sciences 11, no. 1 (January 28, 2020): 880–90. http://dx.doi.org/10.26452/ijrps.v11i1.1910.

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Biopharmaceutics classification system (BCS) class IV compounds, exhibits low solubility, intestinal permeability and oral bioavailability among all the pharmaceutical class of drugs. Therefore, these drugs need a more compatible and efficient delivery system. Since, their solubility in various mediums will remains a limitation. Hence, the mesoporous Nanomatrix approach may prove to be a suitable solution ahead. Therefore, in the present study, the polymer-coated mesoporous material like Sylysia 350, Carbon, Tin Oxide are opted for the BCS class IV drug like Apixaban to attain higher solubility and dissolution. The prepared Nanomatrix was evaluated for its particle size, DSC, Solubility and dissolution studies. For this study, Apixaban was opted for formulating Sylysia 350, Carbon, Tin Oxide based Mesoporous Nanomatrix system. Nanomatrix was prepared by the Amorphous solid dispersion method using probe sonication. The mesoporous Nanomatrix of Apixaban showed improvement in the solubility in water by approx.7 folds when Apixaban used in combination with Sylysia 350 and Polymer HPMC K15M. From the present study, we can conclude that the optimized Apixaban mesoporous Nanomatrix may prove to be a suitable potential option for solubility enhancement, increase in-vitro drug release and effective delivery of BCS class IV drugs.

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Tian, Yiwei, Kaijie Qian, Esther Jacobs, Esther Amstad, David S. Jones, Lorenzo Stella, and Gavin P. Andrews. "The Investigation of Flory–Huggins Interaction Parameters for Amorphous Solid Dispersion Across the Entire Temperature and Composition Range." Pharmaceutics 11, no. 8 (August 19, 2019): 420. http://dx.doi.org/10.3390/pharmaceutics11080420.

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Abstract:

Amorphous solid dispersion (ASD) is one of the most promising enabling formulations featuring significant water solubility and bioavailability enhancements for biopharmaceutical classification system (BCS) class II and IV drugs. An accurate thermodynamic understanding of the ASD should be established for the ease of development of stable formulation with desired product performances. In this study, we report a first experimental approach combined with classic Flory–Huggins (F–H) modelling to understand the performances of ASD across the entire temperature and drug composition range. At low temperature and drug loading, water (moisture) was induced into the system to increase the mobility and accelerate the amorphous drug-amorphous polymer phase separation (AAPS). The binodal line indicating the boundary between one phase and AAPS of felodipine, PVPK15 and water ternary system was successfully measured, and the corresponding F–H interaction parameters (χ) for FD-PVPK15 binary system were derived. By combining dissolution/melting depression with AAPS approach, the relationship between temperature and drug loading with χ (Φ, T) for FD-PVPK15 system was modelled across the entire range as χ = 1.72 − 852/T + 5.17·Φ − 7.85·Φ2. This empirical equation can provide better understanding and prediction for the miscibility and stability of drug-polymer ASD at all conditions.

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Journal articles on the topic 'Biopharmaceutical Classification System – BCS'

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