Relevant bibliographies by topics / Pharmaceutical crystal forms

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  1. Journal articles
  2. Dissertations / Theses
  3. Books
  4. Book chapters
  5. Conference papers

Academic literature on the topic 'Pharmaceutical crystal forms'

Author: Grafiati
Published: 4 June 2021
Last updated: 16 February 2022

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Journal articles on the topic "Pharmaceutical crystal forms"

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Sala, Andrea, Zakiena Hoossen, Alessia Bacchi та Mino R. Caira. "Two Crystal Forms of a Hydrated 2:1 β-Cyclodextrin Fluconazole Complex: Single Crystal X-ray Structures, Dehydration Profiles, and Conditions for Their Individual Isolation". Molecules 26, № 15 (2021): 4427. http://dx.doi.org/10.3390/molecules26154427.

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Inclusion complexes between cyclodextrins (CDs) and active pharmaceutical ingredients (APIs) have potential for pharmaceutical formulation. Since crystallization of a given complex may result in the isolation of multiple crystal forms, it is essential to characterize these forms with respect to their structures and physicochemical properties to optimize pharmaceutical candidate selection. Here, we report the preparation and characterization of two crystallographically distinct hydrated forms of an inclusion complex between β-cyclodextrin (β-CD) and the antifungal API fluconazole (FLU) as well as temperature–concentration conditions required for their individual isolation. Determination of crystal water contents was achieved using thermoanalytical methods. X-ray analyses revealed distinct structural differences between the triclinic (TBCDFLU, space group P1) and monoclinic (MBCDFLU, space group C2) crystal forms. Removal of the crystals from their mother liquors led to rapid dehydration of the MBCDFLU crystal, while the TBCDFLU crystal was stable, a result that could be reconciled with the distinct packing arrangements in the respective crystals. This study highlights (a) the importance of identifying possible multiple forms of a cyclodextrin API complex and controlling the crystallization conditions, and (b) the need to characterize such crystal forms to determine the extent to which their physicochemical properties may differ.
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Raheem Thayyil, Abdul, Thimmasetty Juturu, Shashank Nayak, and Shwetha Kamath. "Pharmaceutical Co-Crystallization: Regulatory Aspects, Design, Characterization, and Applications." Advanced Pharmaceutical Bulletin 10, no. 2 (2020): 203–12. http://dx.doi.org/10.34172/apb.2020.024.

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Pharmaceutical co-crystals are novel class of pharmaceutical substances, which possess an apparent probability of advancement of polished physical properties offering stable and patentable solid forms. These multi-component crystalline forms influence pertinent physicochemical parameters like solubility, dissolution rate, chemical stability, physical stability, etc. which in turn result in the materials with superior properties to those of the free drug. Co-crystallization is a process by which the molecular interactions can be altered to optimize the drug properties. Co-crystals comprise a multicomponent system of active pharmaceutical ingredient (API) with a stoichiometric amount of a pharmaceutically acceptable coformer incorporated in the crystal lattice. By manufacturing pharmaceutical co-crystals, the physicochemical properties of a drug can be improved thus multicomponent crystalline materials have received renewed interest in the current scenario due to the easy administration in the pharmaceutical industry. There is an immense amount of literature available on co-crystals. However, there is a lack of an exhaustive review on a selection of coformers and regulations on co-crystals. The review has made an attempt to bridge this gap. The review also describes the methods used to prepare co-crystals with their characterization. Brief description on the pharmaceutical applications of co-crystals has also been incorporated here. Efforts are made to include reported works on co-crystals, which further help to understand the concept of co-crystals in depth.
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Tian, Jian, Scott J. Dalgarno, and Jerry L. Atwood. "A New Strategy of Transforming Pharmaceutical Crystal Forms." Journal of the American Chemical Society 133, no. 5 (2011): 1399–404. http://dx.doi.org/10.1021/ja107617m.

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Wood, Peter A. "Towards knowledge-based design of pharmaceutical crystal forms." Acta Crystallographica Section A Foundations of Crystallography 65, a1 (2009): s104. http://dx.doi.org/10.1107/s0108767309097967.

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LAINE, E., P. KAHELA, R. RAJALA, T. HEIKKILA, K. SAARNIVAARA, and I. PIIPPO. "Crystal forms and bioavailability of erythromycin." International Journal of Pharmaceutics 38, no. 1-3 (1987): 33–38. http://dx.doi.org/10.1016/0378-5173(87)90094-9.

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Martins Santos, Olimpia Maria, Jennifer Tavares Jacon Freitas, Monalisa Bitencourt, Felipe Terra Martins, and Antonio Carlos Doriguetto. "Three new orbifloxacin multicomponent crystal forms towards pharmaceutical improvement†." Journal of Molecular Structure 1217 (October 2020): 128371. http://dx.doi.org/10.1016/j.molstruc.2020.128371.

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Lyn, Lim, Huan Sze, Adhiyaman Rajendran, Gorajana Adinarayana, Kamal Dua, and Sanjay Garg. "Crystal modifications and dissolution rate of piroxicam." Acta Pharmaceutica 61, no. 4 (2011): 391–402. http://dx.doi.org/10.2478/v10007-011-0037-z.

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Crystal modifications and dissolution rate of piroxicam Piroxicam is a nonsteroidal anti-inflammatory drug with low aqueous solubility which exhibits polymorphism. The present study was carried out to develop polymorphs of piroxicam with enhanced solubility and dissolution rate by the crystal modification technique using different solvent mixtures prepared with PEG 4000 and PVP K30. Physicochemical characteristics of the modified crystal forms of piroxicam were investigated by X-ray powder diffractometry, FT-IR spectrophotometry and differential scanning calorimetry. Dissolution and solubility profiles of each modified crystal form were studied and compared with pure piroxicam. Solvent evaporation method (method I) produced both needle and cubic shaped crystals. Slow crystallization from ethanol with addition of PEG 4000 or PVP K30 at room temperature (method II) produced cubic crystal forms. Needle forms produced by method I improved dissolution but not solubility. Cubic crystals produced by method I had a dissolution profile similar to that of untreated piroxicam but showed better solubility than untreated piroxicam. Cubic shaped crystals produced by method II showed improved dissolution, without a significant change in solubility. Based on the XRPD results, modified piroxicam crystals obtained by method I from acetone/benzene were cube shaped, which correlates well with the FTIR spectrum; modified needle forms obtained from ethanol/methanol and ethanol/acetone showed a slight shift of FTIR peak that may be attributed to differences in the internal structure or conformation.
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Banerjee, Manali, and Blair Brettmann. "Combining Surface Templating and Confinement for Controlling Pharmaceutical Crystallization." Pharmaceutics 12, no. 10 (2020): 995. http://dx.doi.org/10.3390/pharmaceutics12100995.

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Poor water solubility is one of the major challenges to the development of oral dosage forms containing active pharmaceutical ingredients (APIs). Polymorphism in APIs leads to crystals with different surface wettabilities and free energies, which can lead to different dissolution properties. Crystal size and habit further contribute to this variability. An important focus in pharmaceutical research has been on controlling the drug form to improve the solubility and thus bioavailability of APIs. In this regard, heterogeneous crystallization on surfaces and crystallization under confinement have become prominent forms of controlling polymorphism and drug crystal size and habits; however there has not been a thorough review into the emerging field of combining these approaches to control crystallization. This tutorial-style review addresses the major advances that have been made in controlling API forms using combined crystallization methods. By designing templates that not only control the surface functionality but also enable confinement of particles within a porous structure, these combined systems have the potential to provide better control over drug polymorph formation and crystal size and habit. This review further provides a perspective on the future of using a combined crystallization approach and suggests that combining surface templating with confinement provides the advantage of both techniques to rationally design systems for API nucleation.
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Viscomi, G. C., M. Campana, M. Barbanti, et al. "Crystal forms of rifaximin and their effect on pharmaceutical properties." CrystEngComm 10, no. 8 (2008): 1074. http://dx.doi.org/10.1039/b717887e.

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Ellena, Javier. "Crystal Engineering in the design of New Solid Pharmaceutical Forms with enhanced pharmaceutical properties." Journal of Experimental Techniques and Instrumentation 4, no. 03 (2021): 72–80. http://dx.doi.org/10.30609/jeti.v4i03.12950.

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High-efficiency drugs and pharmaceutical formulations, produced in a sustainable way, and that present a favorable performance are widely required in Public Health. Among the pharmacokinetic properties of active pharmaceutical ingredients (APIs), the solubility is main variable since it regulate the availability in the biological target. Numerous formulations on the market and in the National Health System (SUS) present serious drawbacks related to quality, manufacture and performance. In general, APIs are delivered in solid formulations and this characteristic represents a challenge for industry and academia since the therapeutic efficiency of and APIs is related to their crystalline structure, i.d structural multiplicity, polymorphism and composition. APIs may exist in different forms presenting different pharmacokinetic profiles. In addition, the characterization of the diversities of solid forms of an IFA, constitutes an innovative strategy to optimize pharmaceutical properties, providing opportunities for the creation of intellectual property and innovation for the country. In this work we will discuss several strategies related to the problem aiming to show the importance in the pharmaceutical area of solid state techniques like crystal engineering.
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Dissertations / Theses on the topic "Pharmaceutical crystal forms"

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McMahon, Jennifer Anne. "Crystal engineering of novel pharmaceutical forms." [Tampa, Fla] : University of South Florida, 2006. http://purl.fcla.edu/usf/dc/et/SFE0001792.

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Shattock, Tanise R. "Crystal engineering of co-crystals and their relevance to pharmaceutical forms." [Tampa, Fla.] : University of South Florida, 2007. http://purl.fcla.edu/usf/dc/et/SFE0002101.

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Weyna, David Rudy. "Crystal Engineering of Multiple Component Crystal Forms of Active Pharmaceutical Ingredients." Scholar Commons, 2011. http://scholarcommons.usf.edu/etd/3406.

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Enhancing the physicochemical properties of solid-state materials through crystal engineering enables optimization of these materials without covalent modification. Cocrystals have become a reliable means to generate novel crystalline forms with multiple components and they exhibit different physicochemical properties compared to the individual components. This dissertation exemplifies methodologies to generate cocrystals of active pharmaceutical ingredients (API's) based upon knowledge of supramolecular interactions (supramolecular synthons), while focusing on enhanced delivery through in vitro and in vivo processes with both salts and cocrystals respectively. The utility of mechanochemistry involving small amounts of an appropriate solvent, or solvent drop grinding (SDG), has been shown to reliably reproduce cocrystals with the anti-convulsant carbamazepine that were originally obtained by solution crystallization. This technique has been confirmed as a reliable screening method using solvents in which both components exhibit some solubility. The benefits of this technique lie in the time and cost efficiency associated with it as well as its inherently small environmental impact making it a "Green" method. SDG was also used as an efficient way to discover cocrystals of the anti-inflammatory meloxicam with carboxylic acids after analysis of existing reports and the analysis of structural data from the Cambridge Structural Database (CSD) to guide the choice of coformer. It has been shown that SDG can be used to screen for cocrystalline forms that are also obtainable by solution crystallization which is important in later stage development and manufacturing including but not limited to large scale up processes. Single crystals suitable for single crystal X-ray diffraction were obtained with meloxicam and two of the coformers, fumaric and succinic acid. Some of the meloxicam cocrystals exhibited enhanced pharmacokinetic (PK) profiles in rats exemplifying significantly higher serum concentrations after only fifteen minutes and consistently higher exposure over the time studied while others maintained lower exposure. This reveals that cocrystals can fine tune the PK profile of meloxicam in order to reduce or enhance exposure. Two different sulfonate salts, 4-hydroxybenzenesulfonate (p-phenolsulfonate) and 4-chlorobenzenesulfonate, of the anti-spastic agent (R,S) baclofen were developed by strategically interrupting the intramolecularly stabilized zwitterionic structure of baclofen. This zwitterionic structure results in low solubility associated with physiological pH required for intrathecal administration. Structural data for both salts in the form of single crystal X-ray diffraction data was successfully obtained. Solubility based on baclofen was assessed and shown to increase in pure water and at pH's 1 and 7. Only the 4-chlorobenzenesulonate salt maintained an increased solubility over two days at pH 7 making it a viable candidate for further study in terms of intrathecal administration. During crystallization experiments with (R,S) baclofen two polymorphic forms of the baclofen lactam were generated, Forms II and III. Both forms are conformational polymorphs confirmed by single crystal X-ray diffraction and Form II has a Z' of 4 with an unusual arrangement of enantiomers.
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Clarke, Heather Dawn Marie. "Crystal Engineering of Multi-Component Crystal Forms: The Opportunities and Challenges in Design." Scholar Commons, 2012. http://scholarcommons.usf.edu/etd/4013.

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There is heightened interest to diversify the range of crystal forms exhibited by active pharmaceutical ingredients (APIs) in the pharmaceutical industry. The crystal form can be regarded as the Achilles' heel in the development of an API as it directly impacts the physicochemical properties, performance and safety of the API. This is of critical importance since the crystal form is the preferred method of oral drug delivery by industry and regulatory bodies. The ability to rationally design materials is a lucrative avenue towards the synthesis of functional molecular solids with customized physicochemical properties such as solubility, bioavailability and stability. Pharmaceutical cocrystals have emerged as a new paradigm in pharmaceutical solid form development because they afford the discovery of novel, diverse crystal forms of APIs, generate new intellectual property and modify physicochemical properties of the API. In addition, pharmaceutical cocrystals are amenable to design from first principles of crystal engineering. This dissertation focuses on the crystal engineering of multi-component crystal forms, in particular pharmaceutical cocrystals and crystalline hydrates. It addresses: (i) the factors involved in the selection of cocrystal formers (ii) design strategies for APIs that exhibit complexity, (iii) the role of water molecules in the design of multi-component crystal forms and (iv) the relationship between the crystal structure and thermal stability of crystalline hydrates. In general, cocrystal former libraries have been limited to pharmaceutically acceptable substances. It was investigated to expand this library to include substances with an acceptable toxicity profile such as nutraceuticals. In other words, can nutraceuticals serve as general purpose cocrystals formers? The model compounds, gallic acid and ferulic acid, were selected since they possess the functional moieties carboxylic acids and phenols, that are known to form persistent supramolecular synthons with complementary functional groups such as basic nitrogen and amides. The result yielded pairs of cocrystals and revealed the hierarchical nature of hydrogen bonding between complementary functional groups. In general, pharmaceutical cocrystals have been designed by determining the empirical guidelines regarding the hierarchy of supramolecular synthons. However, this approach may be inadequate when considering molecules that are complex in nature, such as those having a multiplicity of functional groups and/or numerous degrees of conformational flexibility. A crystal engineering study was done to design multi-component crystal forms of the atypical anti-psychotic drug olanzapine. The approach involved a comprehensive analysis and data mining of existing crystal structures of olanzapine, grouped into categories according to the crystal packing exhibited. The approach yielded isostructural, quaternary multi-component crystal forms of olanzapine. The crystal forms consist of olanzapine, the cocrystal former, a water molecule and a solvate. The role of water molecules in crystal engineering was addressed by investigating the crystal structures of several cocrystals hydrates and their related thermal stability. The cocrystal hydrates were grouped into four categories based upon the thermal stability they exhibit and it was concluded that no structure/stability correlations exist in any of the other categories of hydrate. A Cambridge Structural Database (CSD) analysis was conducted to examine the supramolecular heterosynthons that water molecules exhibit with two of the most relevant functional groups in the context of active pharmaceutical ingredients, carboxylic acids, and alcohols. The analysis suggested that there is a great diversity in the supramolecular heterosynthons exhibited by water molecules when they form hydrogen bonds with carboxylic acids or alcohols. This finding was emphasized by the discovery of two polymorphs of gallic acid monohydrate to it the first tetramorphic hydrate for which fractional coordinates have been determined. Analysis of the crystal structures of gallic acid monohydrate polymorphs revealed that forms I and III exhibit the same supramolecular synthons but different crystal packing and forms II and IV exhibit different supramolecular synthons. Therefore, the promiscuity of water molecules in terms of their supramolecular synthons and their unpredictable thermal stability makes them a special challenge in the context of crystal engineering.
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Cheney, Miranda L. "The Role of Cocrystals in Solid-State Synthesis of Imides and the Development of Novel Crystalline Forms of Active Pharmaceutical Ingredients." Scholar Commons, 2009. http://scholarcommons.usf.edu/etd/3693.

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With a greater understanding of the fundamentals of crystal engineering lays the potential for the development of a vast array of novel materials for a plethora of applications. Addressed herein is the latent potential of the current knowledge base with an emphasis upon cocrystallization and the desire for scientific exploration that will lead to the development of a future generation of novel cocrystals. The focus of this dissertation is to expand the cocrystallization knowledge base in two directions with the utilization of cocrystals in the novel synthetic technique of cocrystal controlled solid-state synthesis and in the development of active pharmaceutical ingredients. Cocrystal controlled solid-state synthesis uses a cocrystal to align the reactive moieties in such a way that the reaction occurs more quickly and in higher yield than the typical solution methodology. The focus herein is upon cocrystal controlled solid-state synthesis of imides where an anhydride and primary amine were the reactive moieties. Forty-nine reactions were attempted and thirty-two resulted in successful imide formation. In addition, the cocrystal was isolated as part of the reaction pathway in three cases and is described in detail. The impact of cocrystals upon active pharmaceutical ingredients is also addressed with a focus upon generating novel crystal forms of lamotrigine and meloxicam. Cocrystallization attempts of lamotrigine resulted in ten novel crystal forms including three cocrystals, one cocrystal solvate, three salts, one solvated salt, a methanol solvate, and an ethanol hydrate. Additionally, cocrystallization attempts of meloxicam afforded seven novel cocrystals. Solubility and pharmacokinetic studies were conducted for a selected set of lamotrigine and meloxicam crystal forms to determine the crystal form with the most desirable properties. Properties between crystal form and cocrystal former were also examined.
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Kesani, Sheshanka. "Crystallization studies of epigallocatechin gallate." [Tampa, Fla.] : University of South Florida, 2007. http://purl.fcla.edu/usf/dc/et/SFE0002100.

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Eddleston, Mark David. "Crystal form and defect analysis of pharmaceutical materials." Thesis, University of Cambridge, 2012. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.610090.

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Ibrahim, Mohamed Asim Y. "Co-processing of drugs and co-crystal formers and its effect on pharmaceutical dosage-form performance. Co-crystallization of urea/ 2-methoxybenzamide, caffeine/ malonic acid, caffeine/ oxalic acid and theophylline/ malonic acid systems: Solid-state characterization including imaging, thermal, X-ray and Raman spectroscopic techniques with subsequent evaluation of tableting behaviour." Thesis, University of Bradford, 2008. http://hdl.handle.net/10454/12760.

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This dissertation has focused on the solid-state characterization of different co-crystal system as well as the effect of co-crystallization of these systems on pharmaceutical dosage form performance. Urea/ 2-MB, caffeine/ malonic acid, caffeine/ oxalic acid and theophylline/ malonic acid co-crystals were prepared using co-grinding- and co-precipitation techniques. In addition, the synthesis of co-crystals through two novel methods has been demonstrated. This includes compaction and convection mixing. The solid-state characterization of the co-crystals has been carried out using XRPD, Raman spectroscopy, DSC, TGA, hot-stage microscopy and SEM. After preparation of co-crystals, tablets have been produced from co-ground-, co-precipitated-, and physical mixtures using Compaction Studies Press (Kaleva), and the data were recorded to compare between the different mixtures, regarding compactibilty, compressibility and deformational properties. The DSC results showed that the physical mixtures of all systems, formed co-crystals during heating process. For systems of urea/ 2-MB, caffeine/ malonic acid and theophylline/ malonic acid, the co-ground mixture produced tablets with higher tensile strength compared with either co-precipitated or physical mixture. However, for caffeine/ oxalic acid system, the tensile strengths of compacts produced from the physical mixture were greater than those obtained from either co-ground or co-precipitated mixtures. The Heckel data suggested that urea/ 2-MB, caffeine/ malonic acid and theophylline/ malonic acid systems are Type 1 materials, as an extensive linearity during compression was indicative of a plastic deformation mechanism, while the caffeine/ oxalic acid system was Type 2 materials. However, the co-precipitated mixture of urea/ 2-MB system was the least compressible, as it possessed the greatest value of yield pressure (85 MPa) and the highest elastic recovery (7.42%). The co-precipitated mixture of both of caffeine/ malonic acid and theophylline/ malonic acid systems was the most compressible with small yield pressure values of (44 & 80 MPa) and elastic recovery of (7.2% & 6.56%), respectively. The co-ground mixture of caffeine/ oxalic acid possessed the highest value of yield pressure (166 MPa) and thus the lowest compressibility among other mixtures. Furthermore, the addition of microcrystalline cellulose and α-lactose monohydrate has affected the crystallinity as well as the tableting properties of the co-crystals. After the addition of excipients, the tensile strength of compacts was about 2 times higher than any other mixture. Finally, urea/ 2-MB and caffeine/ malonic acid co-crystals were successfully synthesized through convection mixing and compaction.<br>Islamic University of Omdurman and the Ministry of Higher Education in Sudan
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Ibrahim, Mohamed Asim Yousif. "Co-processing of drugs and co-crystal formers and its effect on pharmaceutical dosage-form performance : co-crystallization of urea/2-methoxybenzamide, caffeine/malonic acid, caffeine/oxalic acid and theophylline/malonic acid systems : solid-state characterization including imaging, thermal, X-ray and Raman spectroscopic techniques with subsequent evaluation of tableting behaviour." Thesis, University of Bradford, 2008. http://hdl.handle.net/10454/12760.

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This dissertation has focused on the solid-state characterization of different co-crystal system as well as the effect of co-crystallization of these systems on pharmaceutical dosage form performance. Urea/ 2-MB, caffeine/ malonic acid, caffeine/ oxalic acid and theophylline/ malonic acid co-crystals were prepared using co-grinding- and co-precipitation techniques. In addition, the synthesis of co-crystals through two novel methods has been demonstrated. This includes compaction and convection mixing. The solid-state characterization of the co-crystals has been carried out using XRPD, Raman spectroscopy, DSC, TGA, hot-stage microscopy and SEM. After preparation of co-crystals, tablets have been produced from co-ground-, co-precipitated-, and physical mixtures using Compaction Studies Press (Kaleva), and the data were recorded to compare between the different mixtures, regarding compactibilty, compressibility and deformational properties. The DSC results showed that the physical mixtures of all systems, formed co-crystals during heating process. For systems of urea/ 2-MB, caffeine/ malonic acid and theophylline/ malonic acid, the co-ground mixture produced tablets with higher tensile strength compared with either co-precipitated or physical mixture. However, for caffeine/ oxalic acid system, the tensile strengths of compacts produced from the physical mixture were greater than those obtained from either co-ground or co-precipitated mixtures. The Heckel data suggested that urea/ 2-MB, caffeine/ malonic acid and theophylline/ malonic acid systems are Type 1 materials, as an extensive linearity during compression was indicative of a plastic deformation mechanism, while the caffeine/ oxalic acid system was Type 2 materials. However, the co-precipitated mixture of urea/ 2-MB system was the least compressible, as it possessed the greatest value of yield pressure (85 MPa) and the highest elastic recovery (7.42%). The co-precipitated mixture of both of caffeine/ malonic acid and theophylline/ malonic acid systems was the most compressible with small yield pressure values of (44 & 80 MPa) and elastic recovery of (7.2% & 6.56%), respectively. The co-ground mixture of caffeine/ oxalic acid possessed the highest value of yield pressure (166 MPa) and thus the lowest compressibility among other mixtures. Furthermore, the addition of microcrystalline cellulose and α-lactose monohydrate has affected the crystallinity as well as the tableting properties of the co-crystals. After the addition of excipients, the tensile strength of compacts was about 2 times higher than any other mixture. Finally, urea/ 2-MB and caffeine/ malonic acid co-crystals were successfully synthesized through convection mixing and compaction.
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Lee, Hung-Lin, and 李弘霖. "Novel Crystallization Processes for Preparing Various Crystal Forms of Active Pharmaceutical Ingredients." Thesis, 2018. http://ndltd.ncl.edu.tw/handle/pf7w79.

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博士<br>國立中央大學<br>化學工程與材料工程學系<br>106<br>An overview on (Taiwan’s) pharmaceutical industry was presented. Making tablets of drug has become the most commonly used dosage form due to the ease of manufacturing and administration, accurate dosing, and stability (long shelf life). Crystallization is one of the oldest unit operations in a chemical engineering sense, which is an important separation and purification process employed for producing highly crystalline products, isolating from intermediates and byproducts in the synthesis, achieving a high degree of purity, and determining crystal quality and handling characteristics. In the pharmaceutical industry, crystallization operation often serves as the crucial final step of active pharmaceutical ingredient (API) manufacturing, and enables the control of crystal habit, polymorph and size distribution, which have profound effects on the downstream behaviors. In this dissertation, the novel crystallization processes for preparing various crystal forms of APIs including polymorph (Chapter 3), co-crystal (Chapter 4), and salt (Chapter 5) from solvent-based to solvent-free processes and from batch to continuous processes. More than 40 g of Form II acetaminophen crystals were made successfully in a 500 mL batch reactor by coupling the acetylation of p-aminophenol with neutralization of acetic acid before the crystallization of Form II crystals in an aqueous solution. The novel working principle involves a sudden drop in the solubility curves of acetaminophen from the acetic acid-water environment to the acetate-water system in addition to temperature cooling but without agitation. Four pharmaceutical co-crystals were assembled directly via chemical synthesis by cooling under three new strategies. The screening method for direct co-crystal assembly by a chemical reaction was developed based on liquid-assisted grinding. The ternary phase diagram involving a chemical reaction and co-crystallization was established for 2:1 co-crystal of benzoic acid-sodium benzoate. The potential for preparing pharmaceutical salt between haloperidol and maleic acid by a novel solvent-free method using twin-screw melt extruder was investigated. The pH-solubility relationship between haloperidol and maleic acid in aqueous medium was first determined, which demonstrated that 1:1 salt formation was feasible. The effects of operating temperature and screw configuration on salt formation were also investigated, and identified as key processing parameters. Salts were also prepared by solution crystallization, liquid-assisted grinding and heat-assisted grinding, and compared with those obtained by melt extrusion. This solvent-free twin-screw melt extrusion method for the preparation of pharmaceutical salt is amenable to continuous manufacturing and easy to scale up.
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Books on the topic "Pharmaceutical crystal forms"

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Bernstein, Joel. Polymorphism in Molecular Crystals. Oxford University Press, 2020. http://dx.doi.org/10.1093/oso/9780199655441.001.0001.

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First recognized in 1822, polymorphism of crystals is now a widely recognized and observed phenomenon, with both fundamental and commercial ramifications in disciplines and industries that study and utilize solid forms of matter. The purpose of this edition is to summarize and to bring up to date the current knowledge and understanding of polymorphism in molecular crystals, and to concentrate it in one source. The information has been gleaned from a wide variety (~2500) of sources in the open literature; however, because of the increasing commercial importance of the phenomenon, a significant portion of the information is less accessible, we have attempted to include both the information from those sources as well with full details of their citations. An introductory chapter on fundamental concepts, definitions, and historical development is followed by a presentation of the physical and structural bases for crystallization and polymorphism. The exploration of the crystal form landscape is described in detail, including polymorph screens, concomitant polymorphs, and disappearing polymorphs. A survey of analytical methods for studying and characterizing polymorphs is followed by a discussion of rapidly developing computational methods for studying and attempting to predict polymorphic behavior. A chapter with many examples of the utilization of polymorphic systems to investigate structure–property relationships in solids precedes three individual chapters on the role and importance of polymorphism in pharmaceuticals, high energy materials, and pigments. The book closes with a chapter on the role of polymorphism in establishing and protecting intellectual property connected with polymorphs through the patent system.
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Book chapters on the topic "Pharmaceutical crystal forms"

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Bernstein, Joel, and Jill MacAlpine. "Pharmaceutical Crystal Forms and Crystal-Form Patents: Novelty and Obviousness1." In Polymorphism in the Pharmaceutical Industry. Wiley-VCH Verlag GmbH & Co. KGaA, 2018. http://dx.doi.org/10.1002/9783527697847.ch16.

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Kawakami, Kohsaku. "Isothermal Crystallization of Pharmaceutical Glasses: Toward Prediction of Physical Stability of Amorphous Dosage Forms." In Advances in Organic Crystal Chemistry. Springer Japan, 2015. http://dx.doi.org/10.1007/978-4-431-55555-1_18.

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Price, Sarah L. "Crystal Energy Landscapes for Aiding Crystal Form Selection." In Computational Pharmaceutics. John Wiley & Sons, Ltd, 2015. http://dx.doi.org/10.1002/9781118573983.ch2.

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Wouters, Johan, Dario Braga, Fabrizia Grepioni, Luc Aerts, and Luc Quéré. "Alternative Solid Forms: Co-crystals." In Polymorphism in the Pharmaceutical Industry. Wiley-VCH Verlag GmbH & Co. KGaA, 2018. http://dx.doi.org/10.1002/9783527697847.ch3.

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Price, Christopher J. "Continuous Pharmaceutical Crystallization from Solution." In Engineering Crystallography: From Molecule to Crystal to Functional Form. Springer Netherlands, 2017. http://dx.doi.org/10.1007/978-94-024-1117-1_19.

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Turner, Thomas D., Peter J. Halfpenny, and Kevin J. Roberts. "Pharmaceutical Solid-State Characterisation Techniques." In Engineering Crystallography: From Molecule to Crystal to Functional Form. Springer Netherlands, 2017. http://dx.doi.org/10.1007/978-94-024-1117-1_23.

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Bernstein, Joel. "Polymorphism of pharmaceuticals." In Polymorphism in Molecular Crystals. Oxford University Press, 2020. http://dx.doi.org/10.1093/oso/9780199655441.003.0007.

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Chapter 7 deals with polymorphism in pharmaceuticals. Following a discussion of the problem of determining the statistics of the occurrence of polymorphism in pharmaceuticals, I present a discussion and examples of the connection between polymorphism and the rate of dissolution and solubility, bioavailability, and the importance of phase changes and mixtures of forms in pharmaceutical preparations. I survey some of the considerations and techniques involved in screening for crystal forms: solvent selection, specific screening for solvates and hydrates, gel crystallization, crystallization in ionic liquids, the challenge of difficult to obtain stable forms and unstable new forms, and the outlook on new techniques and conditions for crystallization. The chapter also deals with polymorphism in pharmaceutical co-crystals, excipients, and amorphous forms and the importance and utility of chemical microscopy in the study of polymorphism of pharmaceuticals.
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8

Chaudhary, Kamal Kumar, Pooja Kannojia, and Nidhi Mishra. "Liquid Crystal Systems in Drug Delivery." In Advances in Medical Technologies and Clinical Practice. IGI Global, 2017. http://dx.doi.org/10.4018/978-1-5225-0751-2.ch009.

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Liquid crystals have been recently studied as novel drug delivery system. The reason behind this is their similarity to colloidal systems in living organisms. They have proven to be advantageous over Traditional, Dermal, Parentral and Oral Dosage forms. Liquid crystals are thermodynamically stable and possess long shelf life. Liquid crystals show bio adhesive properties and sustained release effects. Objective of this book chapter is to provide in-depth information of Pharmaceutical crystal technology. It shall deal with cubic and hexagonal liquid crystal and their applications in Drug delivery system.
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9

Andre, Vania, and M. Teresa. "Novel Challenges in Crystal Engineering: Polymorphs and New Crystal Forms of Active Pharmaceutical Ingredients." In Current Trends in X-Ray Crystallography. InTech, 2011. http://dx.doi.org/10.5772/28954.

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10

Bernstein, Joel. "Polymorphism and patents." In Polymorphism in Molecular Crystals. Oxford University Press, 2020. http://dx.doi.org/10.1093/oso/9780199655441.003.0010.

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A brief introduction to patents is followed by a discussion of the two main issues of patents on (pharmaceutical) polymorphs from the scientific perspective: novelty and obviousness, with an emphasis on the latter. The issues, decisions, and ramifications of six landmark patent litigations involving solid forms are described. These involved the following drugs: cefadroxil, terazosin hydrochloride, ranitidine hydrochloride, paroxetine hydrochloride, armodafinil, and tapentadol hydrochloride. The chapter closes with a description of the litigation on the synthetic sweetener aspartame which involved an issue of habit (shape) rather than the form (crystal structure).
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Conference papers on the topic "Pharmaceutical crystal forms"

1

van de Streek, Jacco. "Theoretical Calculations to Assist Experimental Crystal Form Screening." In The 2nd Electronic Conference on Pharmaceutical Sciences. MDPI, 2012. http://dx.doi.org/10.3390/ecps2012-00820.

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