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Pharmaceutical cocrystals: A review of preparations, physicochemical properties and applications.

ABSTRACT: Pharmaceutical cocrystals are multicomponent systems in which at least one component is an active pharmaceutical ingredient and the others are pharmaceutically acceptable ingredients. Cocrystallization of a drug substance with a coformer is a promising and emerging approach to improve the performance of pharmaceuticals, such as solubility, dissolution profile, pharmacokinetics and stability. This review article presents a comprehensive overview of pharmaceutical cocrystals, including preparation methods, physicochemical properties, and applications. Furthermore, some examples of drug cocrystals are highlighted to illustrate the effect of crystal structures on the various aspects of active pharmaceutical ingredients, such as physical stability, chemical stability, mechanical properties, optical properties, bioavailability, sustained release and therapeutic effect. This review will provide guidance for more efficient design and manufacture of pharmaceutical cocrystals with desired physicochemical properties and applications.

SUBMITTER: Guo M

PROVIDER: S-EPMC8424375 | biostudies-literature | 2021 Aug

REPOSITORIES: biostudies-literature

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Pharmaceutical cocrystals: A review of preparations, physicochemical properties and applications.

Guo Minshan M Sun Xiaojie X Chen Jiahui J Cai Ting T

Acta pharmaceutica Sinica. B 20210323 8

Pharmaceutical cocrystals are multicomponent systems in which at least one component is an active pharmaceutical ingredient and the others are pharmaceutically acceptable ingredients. Cocrystallization of a drug substance with a coformer is a promising and emerging approach to improve the performance of pharmaceuticals, such as solubility, dissolution profile, pharmacokinetics and stability. This review article presents a comprehensive overview of pharmaceutical cocrystals, including preparation ...[more]

PMID: 34522597

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Project description:ObjectivesThe last systematic review of physicochemical research performed on homeopathic preparations was published in 2003. The aim of the study is to update and expand the current state of knowledge in the area of physicochemical properties of homeopathic preparations. In part 1 of the study, we aim to present an overview of the literature with respect to publication quality and methods used. In part 2, we aim to identify the most interesting experimental techniques. With this, we aim to be in a position to generate meaningful hypotheses regarding a possible mode of action of homeopathic preparations.MethodsA two-step procedure was adopted: (1) an extensive literature search, followed by a bibliometric and quality analysis on the level of publications and (2) a thorough qualitative analysis of the individual physicochemical investigations found. In this publication, we report on step (1). We searched major scientific databases to find publications reporting physicochemical investigations of homeopathy from its origin to the end of 2015. Publications were assessed using a scoring scheme, the Manuscript Information Score (MIS). Information regarding country of origin of the research and experimental techniques used was extracted.ResultsWe identified 183 publications (compared to 44 in the last review), 122 of which had an MIS ≥5. The rate of publication in the field was ∼2 per year from the 1970s until 2000. Afterward, it increased to over 5.5 publications per year. The quality of publications was seen to increase sharply from 2000 onward, whereas before 2000, only 12 (13%) publications were rated as "high quality" (MIS ≥7.5); 44 (48%) publications were rated as "high quality" from 2000 onward. Countries with most publications were Germany (n = 42, 23%), France (n = 29, 16%), India (n = 27, 15%), and Italy (n = 26, 14%). Techniques most frequently used were electrical impedance (26%), analytical methods (20%), spectroscopy (20%), and nuclear magnetic resonance (19%).ConclusionsPhysicochemical research into homeopathic preparations is increasing both in terms of quantity and quality of the publications.

Project description:Objectives: In Part 1 of the review of physicochemical research performed on homeopathic preparations the authors identified relevant publications of sufficient reporting quality for further in-depth analysis. In this article, the authors analyze these publications to identify any empirical evidence for specific physicochemical properties of homeopathic preparations and to identify most promising experimental techniques for future studies. Methods: After an update of the literature search up to 2018, the authors analyzed all publications in terms of individual experiments. They extracted information regarding methodological criteria such as blinding, randomization, statistics, controls, sample preparation, and replications, as well as regarding experimental design and measurement methods applied. Scores were developed to identify experimental techniques with most reliable outcomes. Results: The publications analyzed described 203 experiments. Less than 25% used blinding and/or randomization, and about one third used adequate controls to identify specific effects of homeopathic preparations. The most promising techniques used so far are nuclear magnetic resonance (NMR) relaxation, optical spectroscopy, and electrical impedance measurements. In these three areas, several sets of replicated high-quality experiments provide evidence for specific physicochemical properties of homeopathic preparations. Conclusions: The authors uncovered a number of promising experimental techniques that warrant replication to assess the reported physicochemical properties of homeopathic preparations compared with controls. They further discuss a range of experimental aspects that highlight the many factors that need to be taken into consideration when performing basic research into homeopathic potentization. For future experiments, the authors generally recommend using succussed (vigorously shaken) controls, or comparing different homeopathic preparations with each other to reliably identify any specific physicochemical properties.

Dataset Information

Pharmaceutical cocrystals: A review of preparations, physicochemical properties and applications.

Publications

Pharmaceutical cocrystals: A review of preparations, physicochemical properties and applications.

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