Academic literature on the topic 'Biopharmaceutical Classification System – BCS'
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Journal articles on the topic "Biopharmaceutical Classification System – BCS"
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Biopharmaceutical, Classification System dissolution permeability Gastrointestinal track ., and J. Bhor1 Rashid Azeez2 Vinod A. Bairagi3 Kalyani. "Review: Biopharmaceutical Classification System." International Journal in Pharmaceutical Sciences 2, no. 3 (2024): 350–66. https://doi.org/10.5281/zenodo.10810211.
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Dr. Gordon Amidon developed the Biopharmaceutical Classification System (BCS) to classify pharmacological compounds based on their solubility in water and intestinal permeability. His work in this area earned him the Science Award from the International Pharmaceutical Federation (FIP) in August 2006. The BCS has since been used by the U.S. Food and Drug Administration to estimate the absorption of oral medications in the intestines. It has become an indispensable tool in regulatory decision-making for drug development, allowing for the evaluation of dissolution, solubility, and intestinal permeability, which are the three primary factors affecting the absorption of oral drugs from quick-release solid oral dosage forms. This study highlights the BCS's key objectives, benefits, and classification. The article illuminates the potential new standards and divisions suggested for additional biowaivers , which are based on the fundamental physiology of the gastrointestinal tract in necessary instances. It delves into the potential uses of BCS in the fields of drug discovery, drug delivery, and drug research, while also exploring its potential expansion.
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Dudhat, Kiran Rameshbhai. "Vital Medications in the World According to Preliminary BCS Classification: Prognostication of Solubility and Permeability." Journal of Clinical Trials and Regulations 4, no. 2 (2022): 1–19. http://dx.doi.org/10.46610/jctr.2022.v04i02.001.
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The Biopharmaceutical Classification System (BCS) has been used as a predictive method to evaluate potential formulation impacts on oral medication bioavailability in humans. The BCS can assist in the prediction of in vivo product performance and the construction of mechanistic models that enable formulation assessments through the generation of scenarios when used in conjunction with in vitro dissolution testing. The applicability of current human BCS standards has not yet been examined in dogs, which restricts its application in canine medication development. The BCS has had a significant impact on drug discovery, development, and regulation on a global scale and the BCS continues to receive much validation, discussion, and extension in the literature. Drug regulatory organizations from all across the world have fully deployed the BCS when establishing bioavailability/bio-equivalence requirements for the approval of oral drugs with instant release (IR). In this study, we examine the provisional BCS classification of the most popular medications sold worldwide and discuss the BCS scientific framework and its influence on regulatory exercise of oral medicinal products. Also mentioned is the Biopharmaceutical Drug Disposition Classification System and how it relates to the BCS.
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Miranda, Claudia, Alexis Aceituno, Mirna Fernández, et al. "ICH Guideline for Biopharmaceutics Classification System-Based Biowaiver (M9): Toward Harmonization in Latin American Countries." Pharmaceutics 13, no. 3 (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 (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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Srebro, Justyna, Witold Brniak, Renata Jachowicz, Klaudia Syty, and Katarzyna Tomaś. "Pediatric Biopharmaceutical Classification Systems (pBCS)." Farmacja Polska 79, no. 6 (2023): 319–28. http://dx.doi.org/10.32383/farmpol/174417.
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System klasyfikacji biofarmaceutycznej zaproponowany w 1995 roku przez Amidona w celu ułatwienia prowadzenia badań uwalniania i ich korelacji z dostępnością substancji leczniczej in vivo jest z powodzeniem stosowany od niemal 30 lat w naukach farmaceutycznych. Znajduje też odzwierciedlenie w wielu wytycznych dotyczących badań przedrejestracyjnych leków, zarówno opracowywanych przez Europejską Agencję Leków (EMA), Amerykańską Agencję Żywności i Leków (FDA), jak i Międzynarodową Radę Harmonizacji Wymagań Technicznych dla Rejestracji Produktów Leczniczych Stosowanych u Ludzi (ICH). System zakłada podział substancji leczniczych na 4 klasy różniące się rozpuszczalnością oraz przenikaniem przez błony biologiczne, co ma bezpośredni wpływ na losy leku po podaniu drogą doustną. Jednak jego założenia oparto na modelu podania leku pacjentowi dorosłemu, co powoduje, że stosowanie systemu BCS w przypadku preparatów pediatrycznych jest utrudnione. Pacjenci pediatryczni stanowią niejednorodną grupę. Wraz z wiekiem zmieniają się nie tylko wymiary i masa ciała. Zmiany dotyczą rozwoju narządów i układów fizjologicznych, co jest istotne w kontekście doboru leku dla dziecka w odpowiednim okresie rozwojowym. Wyróżnia się kilka grup wiekowych, takich jak wcześniaki, noworodki, niemowlęta, dzieci w wieku przed-przedszkolnym, przedszkolnym, szkolnym oraz nastolatki. Struktura grup jest heterogeniczna. Skutkuje to koniecznością indywidualizacji terapii i uważnego wyboru leku w zależności od wieku pacjenta. Na potrzebę opracowania systemu klasyfikacji biofarmaceutycznej odpowiedniego dla leków pediatrycznych zwrócono uwagę już ponad 10 lat temu. Do tej pory nie ma jednak jednolitego systemu zalecanego przez EMA, FDA, czy ICH. Różne propozycje uwzględniają przede wszystkim proporcjonalne zmniejszenie objętości medium służącego do określenia rozpuszczalności do bardziej zbliżonego do objętości soków żołądkowych u dzieci lub częściej objętości płynu, który dziecko jest w stanie przyjąć popijając lek. Do określenia przenikania substancji leczniczej przez błony biologiczne stosuje się modele analogiczne jak dla dorosłego, albo bazuje się na wartości współczynnika podziału n-oktanol/woda (logP). Stosowane są również bardziej zaawansowane modele oparte na analizie parametrów farmakokinetycznych podania drogą doustną i pozajelitową.
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Vohra, Payaam, Priya Patil, and Sudrshan Mirghal. "Liquisolid Compacts: A Paradigm in Drug Delivery System." International Journal of Pharmaceutical Sciences and Nanotechnology(IJPSN) 17, no. 5 (2024): 7646–47. https://doi.org/10.37285/ijpsn.2024.17.5.11.
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Liquisolid compacts (LSCs) are a fascinating drug delivery technology that offers numerous advantages, particularly for Biopharmaceutical Classification System (BCS) class 2 drugs. In essence, they convert liquid medications into free-flowing, compressible powder forms suitable for tablet production with improved drug release characteristics. Formulation of liquisolid compacts represents a valuable strategy for overcoming solubility challenges, ultimately contributing to the development of an effective and patient-friendly drug delivery system.
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*Aditya, R. Kirmirwar, Pankaj P. Fitwe Prof., Shivshankar D. Mhaske Dr., S. Masne Prathamesh, and R. Mehta Ganesh. "THE EFFECTS OF EXCIPIENTS ON DRUG SOLUBILITY & PERMEABILITY: A BIOPHARMACEUTICAL PERSPECTIVE." World Journal of Advance Pharmaceutical Sciences 2, no. 1 (2025): 104–16. https://doi.org/10.5281/zenodo.15519640.
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Despite being thought of as inert substances, excipients are essential forimproving drug permeability and solubility, which has a big impact onbioavailability and therapeutic results. Optimizing solubility and permeability iscrucial in biopharmaceutics, particularly for medications that fall into Classes IIand IV of the Biopharmaceutical Classification System (BCS) and are poorlysoluble in water and have low permeability. The mechanisms by whichexcipients affect drug permeability and solubility are examined in this review,with a focus on how they affect formulation development. To increase drugsolubility, excipients such lipid-based carriers, polymers, and surfactants havebeen used widely. By decreasing surface tension and improving drug particlewetting, surfactants, for instance, improve solubility and make it easier for drugsto dissolve in gastrointestinal (GI) fluids. Solid dispersions are produced byhydrophilic polymers such as polyethylene glycol (PEG) andpolyvinylpyrrolidone (PVP), which stabilize medications in an amorphous statethat is more soluble than crystalline forms. By increasing its dispersion in GIfluids, lipid-based formulations like liposomes and self-emulsifying drugdelivery systems (SEDDS) provide other ways to increase the solubility ofhydrophobic medications. Excipients are essential for boosting medicationpermeability in addition to improving solubility. Drug transport across intestinalbarriers is facilitated by penetration enhancers including bile salts, fatty acids,and surfactants, which alter the integrity of biological membranes. Theseexcipients function by promoting fluidity in membranes, facilitating tightjunctions, or blocking efflux transporters, such as P-glycoprotein, which activelyremove medications from cells. These excipients greatly enhance drugabsorption by removing permeability barriers, particularly for medications withlimited permeability in their native condition. Even while excipients havebenefits, using them might provide difficulties. Formulation development musttake into account safety issues, legal barriers, and the possibility of interactionsbetween excipients and active pharmaceutical ingredients (APIs). Furthermore,physiological variables including pH variations and GI tract enzyme activitymight cause excipient performance to vary, which could affect the uniformity ofmedication absorption. Excipients are essential to contemporary medicationformulation, especially when it comes to enhancing the permeability andsolubility of difficult drug candidates. New opportunities for improvingmedication absorption and bioavailability are constantly presented bydevelopments in excipient technology. Nonetheless, further investigation isrequired to tackle safety, stability, and regulatory issues, guaranteeing thatexcipients efficiently enhance drug delivery in biopharmaceutical applications.
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L. Prasanna Tarivitla and M. Sunitha Reddy. "An Overview of the Biopharmaceutics Classification System (BCS)." GSC Biological and Pharmaceutical Sciences 14, no. 2 (2021): 217–21. http://dx.doi.org/10.30574/gscbps.2021.14.2.0012.
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The Biopharmaceutics Classification System (BCS) is an essential tool in pharmaceutical sciences, providing a scientific framework for classifying drugs based on their solubility and permeability characteristics. This system, developed in 1995, helps streamline drug development and regulatory approval processes by predicting in vivo drug performance from in vitro data. This paper reviews the four BCS classes, their solubility and permeability criteria, detailed procedures for determining these characteristics, and suitable formulation strategies for each class. Additionally, it explores the concept of biowaivers, which allows for the waiver of in vivo bioavailability and bioequivalence studies under certain conditions, primarily for BCS Class I drugs. The advantages, challenges, and limitations of biowaivers are discussed, emphasizing the need for global harmonization to fully realize the BCS's potential.
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Jung, Ha Neul, and Jin-Seok Choi. "Development and Evaluation of Febuxostat Solid Dispersion through Ternary System." Yakhak Hoeji 68, no. 2 (2024): 105–11. http://dx.doi.org/10.17480/psk.2024.68.2.105.
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Febuxostat is classified as a biopharmaceutical with low solubility in aqueous solution and high intestinal permeability (Biopharmaceutics Classification System [BCS] Class II drug). The solubility of a drug has the characteristic of increasing as pH increases. This study aims to improve the dissolution of febuxostat with Neusilin® US2 and Gelucire®50/13 by a solvent evaporation method. The optimal formulation (solid dispersion, SD1) is developed as a solid dispersion of febuxostat : Gelucire®50/13 : US2®= 1:2:4 (w/w), with a final weight of 280 mg. The dissolution of SD1 in distilled water is 72.0±2.8%, which is 1.67-fold higher than that of the commercial product, Feburic Tab® (43.2±1.8%). The SD1 formulation is believed to have improved dissolution due to changes in physicochemical properties (thermal, interaction, and crystallinity). In conclusion, through the solid dispersion manufacturing method, febuxostat is changed from a crystalline form to an amorphous form in SD1 formulation, and the improved dissolution of febuxostat formulation is developed.
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Anjali, Motwani* Pooja Hatwar Dr. Ravindra Bakal. "Advances in Solubility Enhancement of Poorly Soluble Drugs in Pharmaceutical Development: A Review of Current Techniques and Strategies." International Journal of Pharmaceutical Sciences 2, no. 11 (2024): 138–48. https://doi.org/10.5281/zenodo.14029216.
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Solubility is a key determinant in the bioavailability of drugs, particularly those categorized under Class II and IV of the Biopharmaceutical Classification System (BCS), which exhibit poor aqueous solubility. This review provides an introduction to the concept of solubility, alongside a brief discussion on the BCS classification. Key definitions of solubility are presented, followed by a mention of several factors affecting solubility, such as temperature, pH, and particle size. The article then outlines various techniques employed to enhance solubility, including physical methods like particle size reduction and solid dispersions, as well as chemical strategies such as salt formation and co-crystallization. These approaches are crucial for improving drug absorption and formulation development. This review offers an overview of current solubility enhancement techniques, contributing to the advancement of pharmaceutical science and drug delivery systems.
Dissertations / Theses on the topic "Biopharmaceutical Classification System – BCS"
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Felisberto, Ana Paula Barbosa. "Estudos de caracterização e estabilidade de dispersões sólidas contendo ibuprofeno." Universidade Estadual da Paraíba, 2015. http://tede.bc.uepb.edu.br/tede/jspui/handle/tede/2481.
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Previous issue date: 2015-08-24<br>Coordenação de Aperfeiçoamento de Pessoal de Nível Superior - CAPES<br>Most active pharmaceutical ingredients are made largely for being administered orally. A major challenge for medicinal products development containing Active Pharmaceutical Ingredients (APIs) with low solubility, especially Class II according to Biopharmaceutical Classification System - BCS, is to add technology to the development process in order to increase the bioavailability of these APIs and at the same time ensure their stability. Thus, the objective was to develop analytical methods to characterize lyophilized solid dispersions of ibuprofen obtained by using carboxymethylcellulose (CMC), hydroxymethylpropylcellulose (HPMC) and polyethylene glycol (PEG) 6000, comparing them in terms of thermal stability. The dispersions were characterized correlating the data obtained by the following techniques: Differential Scanning Calorimetry (DSC), Differential Scanning Calorimetry Coupled to a Photovisual System (DSC-photovisual), Thermogravimetry Analysis (TG) and Vibrational Absorption using Fourier Transform Infrared Spectroscopy (FTIR) to investigate possible physical and/or chemical interaction between the ibuprofen and its excipients. For thermal stability evaluation, the products were subjected to dynamic thermogravimetric analysis, by applying Osawa kinetic model, and to isothermal analysis by Arrhenius model at temperatures of 125, 130, 135, 140 and 145 °C, showing zero order kinetics reaction for the drug in the two models applied. According to the data obtained from the thermal analysis for the characterization and stability, the lyophilized solid dispersions containing PEG as a dispersing agent were more stable. The DSC and FTIR data showed the absence of physical and chemical interaction between the formulation components.<br>A maioria dos insumos farmacêuticos ativos é viabilizada em grande parte para serem administrados por via oral. Um dos grandes desafios para o desenvolvimento de medicamentos contendo Insumos Farmacêuticos Ativos (IFAs) com baixa solubilidade, em especial os de Classe II relacionados no Sistema de Classificação Biofarmacêutica – SCB, é agregar tecnologias ao processo de desenvolvimento no sentido de aumentar a biodisponibilidade destes IFAs ao mesmo tempo que possa garantir a estabilidade dos mesmos. Assim, objetivou-se desenvolver metodologias analíticas para caracterizar dispersões sólidas liofilizadas de ibuprofeno obtidas com carboximetilcelulose (CMC), hidroximetilpropilcelulose (HPMC) e polietilenoglicol (PEG) 6000, comparando-as em termos de estabilidade térmica. As dispersões foram caracterizadas correlacionando-se os dados obtidos pelas técnicas de calorimetria exploratória diferencial (DSC), calorimetria exploratória diferencial acoplada ao sistema fotovisual (DSC-fotovisual), termogravimetria (TG) e espectroscopia vibracional de absorção na região do infravermelho com transformada de Fourier (FTIR), a fim de investigar possíveis interações físicas e/ou químicas entre o ibuprofeno e seus excipientes. Para avaliação da estabilidade térmica, os produtos foram submetidos à análise termogravimétrica dinâmica, aplicando-se o modelo cinético de Osawa, e isotérmica pelo modelo de Arrhenius nas temperaturas de 125, 130, 135, 140 e 145 °C, apresentando cinética de reação de ordem zero para o fármaco nos dois modelos aplicados. De acordo com os dados obtidos a partir da análise térmica para caracterização e estabilidade, as dispersões sólidas liofilizadas contendo PEG como agente dispersante mostraram-se mais estáveis. Nos dados de DSC e FTIR mostraram a ausência de interação física e química entre os componentes da formulação.
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Cintron, Roberto. "Human Factors Analysis and Classification System Interrater Reliability for Biopharmaceutical Manufacturing Investigations." ScholarWorks, 2015. https://scholarworks.waldenu.edu/dissertations/194.
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Human errors are an expected result of operations performed by individuals and frequently lead to accidents and other catastrophic events. The problem is that the current process used to investigate and mitigate human errors in the biopharmaceutical manufacturing industries is not effective, as it does not include the effects of human factors found to be effective in aviation and nuclear power organizations. The human factors and classification system (HFACS) was created for the investigations of accidents using the Swiss cheese model of accident causation as a theoretical framework. The purpose of this quantitative, inter-rater reliability study was to demonstrate the utility of the HFACS for human error investigations in the biopharmaceutical industry. The research questions focused on the level of agreement between independent raters using HFACS, as well as the difference in the level of agreement across different areas of biopharmaceutical manufacturing processes. In a fully crossed design, raters evaluated a stratified sample of 161 incident records further analyzed using Cohen's kappa, percentage agreement, and a 1-way analysis of variance test with Scheffe post hoc tests. Study results indicated the reliability of the modified HFACS taxonomy, which included no statistical difference (p < .05) with substantial Cohen's kappa values of .66. The social benefit of this study may stem from biopharmaceutical manufacturers using these findings to decrease human errors, improve the safety and reliability of their processes, decrease manufacturing costs, and support the development of drugs to address the unmet medical needs of society.
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Paraiso, Rafael Leal Monteiro. "Determinação da solubilidade e permeabilidade de fármacos conforme o Sistema de Classificação Biofarmacêutica (SCB)." Universidade de São Paulo, 2012. http://www.teses.usp.br/teses/disponiveis/9/9139/tde-15072013-160559/.
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A avaliação da classe biofarmacêutica dos fármacos assume importância na política de medicamentos genéricos, já que as características de solubilidade e permeabilidade de um fármaco, conforme definidas pelo Sistema de Classificação Biofarmacêutica (SCB), constituem critério essencial para bioisenção na obtenção de registro de genéricos. O propósito do trabalho foi o de determinar a classe biofarmacêutica dos fármacos benzilato de anlodipino, fluconazol e cloridrato de fluoxetina, por meio da determinação de seus parâmetros de solubilidade e permeabilidade. Para o teste de solubilidade, foram desenvolvidos e validados métodos para a quantificação do benzilato de anlodipino, fluconazol e cloridrato de fluoxetina em água e nos tampões farmacopéicos pH 1,2; pH 4,5;pH 6,8 e 7,5. O estudo de solubilidade foi realizado pelo método shake flask num período de 72 horas de agitação a 37°C. A maior dose comercializada no mercado é de 10 mg, 200 mg e 20 mg respectivamente para o besilato de anlodipino, fluconazol e cloridrato de fluoxetina. Os valores de solubilidade para o besilato de anlodipino nos meios avaliados foram de 0,88 a 2,35 mg/mL enquanto intervalo da razão dose: solubilidade (D: S) foi de 4,24 mL a 11,36 mL. Para o fluconazol os valores de solubilidade foram: 8,22 a 14,4 mg/mL, e o intervalo da razão D: S foram de 13,38 mL a 24,33 mL. Já para o cloridrato de fluoxetina a solubilidade foi de 5,12 a 44,36 mg/mL, e o intervalo razão D: S foram de 0,45 a 3,91 mL. De acordo com o SCB, para classifacar um fármaco como de alta solubilidade a dose mais alta cormecializada do fármaco deve ser solúvel em 250 mL de meio aquoso na faixa de pH de 1 a 7,5 a 37º C e um fármaco é considerado como de alta permeabilidade quando a sua fração absorvida seja ≥ 90%. De acordo com esse critério, ambos os fármacos apresentam alta solubilidade. A avaliação da permeabilidade dos fármacos foi realizada por meio da determinação do fluxo de fármaco através de segmentos intestinais de ratos, isolados e contidos em câmaras de difusão vertical da plataforma manual para testes de permeabilidade. Os valores de permeabilidade aparente (Papp) obtidos nos experimentos indicam que o besilato de anlodipino e o fluconazol são fármacos de baixa permeabilidade, portanto, classe III e o cloridrato de fluoxetina alta permeabilidade, classe I.<br>The Biopharmaceutical Classification System (BCS) concept was established by Amidon and co-workers (1995) and BCS allows expectations regarding correlation between in vitro dissolution data and in vivo bioavailability data. According to the BCS, three major factors govern drug bioavailability: the drug aqueous solubility, the ability of the drug molecules to permeate biologic membranes and drug dissolution from the dosage form. Solubility criteria defined by the FDA to classify a drug as highly soluble requires the highest dose strength to be soluble in 250 mL of aqueous media over the pH range of 1-7.5 at 37°C and a drug is considered with high permeability when its fraction absorbed is ≥ 90%. The purpose of this study was to evaluate the solubility and permeability of amlodipine benzylate, fluconazole and fluoxetine hidrochoride in order to determine them BCS class. The solubility study was performed using the drug over a 72 hours period of agitation as the shake flask method at 37 °C. The results from solubility values are given in mg/mL and dose: solubility ratio is given in mL. The highest dose marketed is 10 mg, 200 mg and 20 mg, respectively for the amlodipine besylate, fluconazole and fluoxetine hydrochloride. The solubility values for the amlodipine besylate in the tested aqueous media range from 0.88 to 2.35 mg/mL, while dose solubility ratio (D: S) values range from 4.24 to 11.36 mL. The values for fluconazole solubility were 8.22 to 14.4 mg/mL, and the D: S was 13.38 to 24.33 mL. The fluoxetine hydrochloride solubility is range from 5.12 to 44.36 mg/mL, and the ratio D: S from 0.45 to 3.91 mL. According to BCS all the drugs have high solubility. The evaluation of the drugs permeability was performed by determining the drug flow through the rat intestinal segments, isolated and contained in vertical diffusion chambers platform for manual testing permeability. The apparent permeability values (Papp) obtained in the experiments indicate that the amlodipine besylate and fluconazole are low permeability drugs and fluoxetine hydrochloride high permeability. Considering Solubility and permeability assay, amlodipine besylate and fluconazole are Class III and fluoxetine hydrochloride is Class I.
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Gonçalves, José Eduardo. "Padronização das condições para cultura de células Caco-2 visando à obtenção de membranas viáveis ao estudo da permeabilidade in vitro da rifampicina." Universidade de São Paulo, 2010. http://www.teses.usp.br/teses/disponiveis/9/9139/tde-31012011-162346/.
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A permeabilidade através do epitélio intestinal tem se tornado um importante aspecto a ser determinado nas avaliações biofarmacotécnicas envolvendo fármacos e medicamentos. A técnica mais empregada para essa determinação in vitro é aquela que utiliza a cultura de células Caco-2. Entretanto, ainda são discutíveis as condições para a realização desses experimentos, uma vez que a padronização das mesmas é fator fundamental para a confiabilidade dos resultados. Nesta tese, foram avaliadas as condições para realização dos estudos de permeabilidade através de membranas de células Caco-2 para a rifampicina, principal fármaco utilizado no tratamento da tuberculose. Para tanto, foram investigados fatores tais como a citotoxicidade da rifampicina em diferentes concentrações, a influência da concentração do fármaco sobre a permeabilidade, do pH de realização dos experimentos e da presença de proteínas do muco intestinal, além da influência de proteínas plasmáticas. Foi também investigado o potencial indutor da rifampicina sobre a expressão da glicoproteína-P (Pgp) e seu impacto na permeabilidade da própria rifampicina. Os estudos foram desenvolvidos utilizando membranas de células Caco-2 provenientes da American Type Culture Collection (ATCC) cultivadas em placas Transwel®, a quantificação da fração permeada foi por cromatografia líquida de alta eficiência com métodos validados. A análise da indução da expressão da Pgp foi realizada por PCR-RT. Demonstrou-se que as concentrações da rifampicina (10,0; 25,0 e 50,0 µg/mL) não ocasionaram danos às células Caco-2 no estudo de citotoxicidade pela técnica que emprega o sal do brometo de 3-(4,5-dimetil-2-tiazoli)-2,5-difenil-2H-tetrazólio (MTT). As concentrações de rifampicina (5,0; 10,0 e 25,0 µg/mL) não resultaram em valores estatisticamente diferentes de permeabilidade aparente (Papp) em células Caco-2 nas condições do estudo. A rifampicina apresentou valor de Papp significativamente maior em pH 6,8 dentre os valores de pH avaliados (5,8 ; 6,8; 7,4). A presença de muco simulado e de soro fetal bovino não resultou em valores de permeabilidade significativamente distintos do resultado obtido sem a sua adição ao experimento. A expressão da Pgp em células Caco-2 é induzida pela adição da rifampicina (10µg/mL), ocasionando diminuição da sua permeabilidade por mecanismo de efluxo. Pelos resultados de permeabilidade obtidos em todas as condições avaliadas, a rifampicina pode ser considerada um fármaco de alta permeabilidade de acordo com o Sistema de Classificação Biofarmacêutica.<br>The permeability through the intestinal epithelium has become an important aspect to be determined in evaluations involving drugs and pharmaceutical products. The most common technique for this determination in vitro is one that uses the culture of Caco-2 cells. Nevertheless, the conditions for carrying out such experiments are still questionable, since the standardization of them is essential to the reliability of the results. In this thesis, we evaluate the conditions for the studies of permeability of rifampicin through membranes of Caco-2 cells, the main drug used in the treatment of tuberculosis. To this end, we examined factors such as cytotoxicity of rifampicin at different concentrations, the influence of drug concentration on the permeability, as well as the pH of the experiments, the presence of proteins of intestinal mucus, and the influence of plasma proteins. It was also investigated the potential of rifampicin on the expression of P-glycoprotein (Pgp) and its impact on the permeability of rifampicin itself. The studies were developed using membranes of Caco-2 cells from American Type Culture Collection (ATCC) grown on plates Transwel®, and the quantification of the fraction of drug permeated was obtained by high performance liquid chromatography with validated methods. The analysis of induction of expression of Pgp was performed by RT-PCR. It was demonstrated that the concentrations of rifampicin (10,0; 25,0 and 50,0 µg/mL) did not cause damage to Caco-2 cells in the study of the cytotoxicity technique that uses a bromide salt of 3 - (4,5-dimethyl-2 - thiazol) -2,5-diphenyl-2H-tetrazolium (MTT). The concentrations of rifampicin (5,0; 10,0 and 25,0 µg/mL) did not result in statistically different values of apparent permeability (Papp) in Caco-2 cells under the conditions of the study. Rifampicin showed a value of Papp significantly higher at pH 6.8 in comparison with other measured pH values (5,8 and 7,4). The presence of mucus simulated and fetal calf serum did not result in permeability values significantly different from the result obtained without its addition to the experiment. The expression of P-gp in Caco-2 cells is induced by the addition of rifampicin (10 µg/ml), decreasing its permeability by efflux mechanism. Taking into account the results of permeability obtained in all conditions, the rifampicin can be considered a high permeability drug according to the biopharmaceutical classification system.
Book chapters on the topic "Biopharmaceutical Classification System – BCS"
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Quiroga, Pablo A. M. "Biopharmaceutical Classification System Subclasses." In The ADME Encyclopedia. Springer International Publishing, 2022. http://dx.doi.org/10.1007/978-3-030-84860-6_139.
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Quiroga, Pablo A. M. "Biopharmaceutical Classification System Subclasses." In The ADME Encyclopedia. Springer International Publishing, 2021. http://dx.doi.org/10.1007/978-3-030-51519-5_139-1.
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Bowen, William E., Qingxi Wang, W. Peter Wuelfing, et al. "A Biopharmaceutical Classification System Approach to Dissolution: Mechanisms and Strategies." In Biopharmaceutics Applications in Drug Development. Springer US, 2008. http://dx.doi.org/10.1007/978-0-387-72379-2_9.
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Singh, Sudarshan, and Warangkana Chunglok. "Pharmacokinetics and Toxicology of Pharmaceutical Excipients." In Biopolymers Towards Green and Sustainable Development. BENTHAM SCIENCE PUBLISHERS, 2022. http://dx.doi.org/10.2174/9789815079302122010011.
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Progress, innovation, and development of new chemical entities fetched new defies in the drug delivery arena, and also put forward several issues including bioavailability with intestinal metabolism or efflux mechanism. However, some excipients such as surfactants have demonstrated improvement in drug bioavailability. Thus, these excipients can no longer be considered inert and require attention from a pharmaceutical regulatory perception. Biopolymers and their derivatives are gaining attention in pharmaceutical manufacturing due to their biodegradability and compatibility. However, based on the Food and Drug and Administration (FDA) guidelines, the manufacturers are required to evaluate their pharmacokinetic and toxicological properties. Several methods including Rule-of-Five and Biopharmaceutical Classification System (BCS) are used for early pharmacokinetic prediction of active and inactive pharmaceutical ingredients. Although polymers differ from therapeutic agents, similar methods can be smeared for the understanding of the absorption, distribution, metabolism, and excretion profile of bio-based pharmaceutical excipients. This chapter explores pharmacokinetic and pharmacodynamics information of biopolymers used in the design, and development of several pharmaceutical formulations.
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Gineetadevi, Mrs. "ADVANCED TOPICAL DRUG DELIVERY SYSTEM CONTAINING FENOPROFEN OINTMENT FOR RHEUMATOID ARTHRITIS." In Futuristic Trends in Pharmacy & Nursing Volume 3 Book 20. Iterative International Publisher, Selfypage Developers Pvt Ltd, 2024. http://dx.doi.org/10.58532/v3bgpn20p3ch1.
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Rheumatoid Arthritis (RA) is a chronic, Inflammatory autoimmune disease. That initially affect the small joints of patients, and progression occurs in large joints and ultimately to the eye, skin, heart, kidney, lungs. frequently when the bone and cartilage get destroyed then ligaments and tendons got weaken. The risk factors are age, gender, genetic and the environmental exposure (air pollutants, smocking cigarette smoking). In this disease mostly NSAID’s drugs are used for reducing the pain and inflammation. The fenoprofen is propionic acid derivative NSAID’s class of COX-1 selective and non-selective inhibitor and it come into II class of biopharmaceutical classification (BCS) which are poorly water soluble. The main purpose of this study to prepare a fenoprofen ointment for topical application to treat Rheumatoid Arthritis (RA). Ointment is prepared by fusion method the preparation contains different excipients like gelling agent, surfactants, ointment bases. Ointment base is prepared by the melting of some ingredients are wool fat, cetostearyl alcohol, hard paraffin, white soft paraffin, or yellow soft paraffin sun flower wax. Nature of ointment base selection is very important because it control the performance of formulation. The formulation was prepared and evaluated for its Physicochemical properties, stability study, spreadability, drug content, PH studies, viscosity of the ointment. The ointment base act as carrier or vehicle for the medication. All the prepared formulation were evaluated for its physicochemical parameter and all the results obtained were within the limits. As compared to the standard preparation as per IP, USP, the formulation.
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"Bioequivalence and Biopharmaceutical Classification System." In Biopharmaceutics Modeling and Simulations. John Wiley & Sons, Inc., 2012. http://dx.doi.org/10.1002/9781118354339.ch9.
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Agnihotri, Tejas Girish, Pankaj Kumar Paradia, and Aakanchha Jain. "Biopharmaceutical Classification System: a strategic tool in pharmaceutical formulation." In Dosage Forms, Formulation Developments and Regulations. Elsevier, 2024. http://dx.doi.org/10.1016/b978-0-323-91817-6.00016-4.
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Golovenko, M. Ya, V. B. Larionov, and I. P. Valivodz`. "BIOPHARMACEUTICAL CLASSIFICATION SYSTEM - SCIENTIFIC BASIS OF CREATING OF EFFICIENT AND SAFE MEDICIAL PRODUCTS." In SUSTAINABLE HEALTHCARE DEVELOPMENT: NATIONAL AND GLOBAL DIMENSIONS. Baltija Publishing, 2024. http://dx.doi.org/10.30525/978-9934-26-466-5-12.
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Mohanto, Sourav, Mohammed Gulzar Ahmed, Adrija Bhunia, and Mithun Bhowmick. "Development of RP-HPLC-PDA Method Validation for the Simultaneous Estimation of Zidovudine, Lamivudine, and Nevirapine in Bulk and Dosage Forms and in Dissolution Samples." In Current Trends in Drug Discovery, Development and Delivery (CTD4-2022). Royal Society of Chemistry, 2023. http://dx.doi.org/10.1039/9781837671090-00493.
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Cinnarizine belongs to the Class II of Biopharmaceutical classification system, and its absorption from the gastrointestinal tract can be limited by various factors, with the most significant contributors being poor aqueous solubility and membrane permeability of the drug molecule, which further affects the oral bioavaibility. Bio nanocomposite is the process of complex formation between drug and polymers/excipients where microwave energy plays a significant role in reducing the particle size of materials. It breaks intermolecular bonding, which further reduces the particle size, enhanced the effective surface area, solubility, and bioavailability. In the present study, an attempt has been made to formulate and characterize the Cinnarizine loaded Bio-nanocomposites consisting of Xanthan and Guar gum for enhanced solubility of Cinnarizine and percentage drug release from nanocomposite that is satisfactory and bioavailability also comparable to better than other marketed formulations of Cinnarizine. The microwave assisted Cinnarizine loaded Xanthan gum-based nanocomposite formulation was shown a higher percentage of yield (80.80±0.8%), higher solubility (0.830±0.008), nano ranged hydrodynamic diameter (169.36 nm with Polydispersity Index 23.6%), zeta potential (34.4 mv). The transmission electron microscopy study of nanocomposite formulation showed crystal shape of Cinnarizine was completely changed in nanocomposite, showing embedded Cinnarizine crystals in the matrix. This In vitro study concluded that the preparation method of bio-nano composite was simple, reproducible, and provides good solubility in alkaline medium and drug content. Thus, Xanthan gum can be considered as an effective carrier for the crystallization of the drug, possessing suitable microstructural properties to prevent recrystallization of the drug.
Conference papers on the topic "Biopharmaceutical Classification System – BCS"
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Rolletschke, Tony, Rico Thomanek, Christian Roschke, and Marc Ritter. "Development of a Holistic System for Activity Classification Based on Multimodal Sensor Data." In Proceedings of the 32nd International BCS Human Computer Interaction Conference. BCS Learning & Development, 2018. http://dx.doi.org/10.14236/ewic/hci2018.167.
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