Experimental design approach for development of cocrystals and immediate release cocrystal tablet of atorvastatin calcium for enhancement of solubility and dissolution

Trivedi, Hemangi R.; Borkar, Dhananajay S.; Puranik, P. K.

doi:10.35333/jrp.2020.226

Cited by 2 publications

(1 citation statement)

References 23 publications

(36 reference statements)

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“…HSP is used as an indicator of the miscibility between the component molecules to predict the likelihood of cocrystal formation. ,, In this model, the total force of various interactions can be divided into several partial solubility parameters, namely, dispersion (δ d ), polarity (δ p ), and hydrogen bonding (δ h ). , Each partial solubility parameter corresponds to the possibility of intermolecular interactions between molecules. Total solubility parameter (δ t ) is defined as The miscibility of compound molecules is estimated by various criterions, and all of them are based on the principle of “like dissolves like”.…”

Section: Methodsmentioning

confidence: 99%

Evaluation on Cocrystal Screening Methods and Synthesis of Multicomponent Crystals: A Case Study

Zhang

Yao

et al. 2021

Crystal Growth & Design

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Screening of suitable coformers is a major challenge during the development of cocrystals. To guide and simplify the cocrystal synthesis process, we evaluated three different predictive methods as well as their combinations during the cocrystallization of 2-amino-4,6-dimethoxypyrimidine (MOP) with 63 components. The conductor-like screening model for the real solvents (COSMO-RS) approach offered the best predictive results among three methods with an overall success rate of 84.1%. When combined with molecular complementarity (MC) analysis, the success rate was up to 85.7%. The Hansen solubility parameters (HSP) method did not deliver a satisfying outcome no matter if used individually or in combination for the MOP system. In addition, based on the screened results, 21 new solid phases of MOP were experimentally observed. Among them, the crystal structures of 10 multicomponent crystals (cocrystals and salts) were revealed by single crystal X-ray diffraction analysis (SCXRD), and their thermodynamic and spectroscopy properties were also characterized. The Hirshfeld surface analysis and the molecular electrostatic potential (MEP) surface analysis were conducted to explore the interactions in multicomponent crystals and the origin for salts and cocrystals. The cases in this study not only enriched the solid forms of MOP, evidenced the feasibility of the combined screening method, but also set an effective example for choosing potential coformers to prepare multicomponent crystals.

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Section: Methodsmentioning

confidence: 99%

Evaluation on Cocrystal Screening Methods and Synthesis of Multicomponent Crystals: A Case Study

Zhang

Yao

et al. 2021

Crystal Growth & Design

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Cocrystals and Drug–Drug Cocrystals of Anticancer Drugs: A Perception towards Screening Techniques, Preparation, and Enhancement of Drug Properties

Kara

Rathnanand

2022

Crystals

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The most favored approach for drug administration is the oral route. Several anticancer drugs come under this category and mostly lack solubility and oral bioavailability, which are the most common causes of inadequate clinical efficiency. Enhancing oral absorption of anticancer drugs with low aqueous solubility and drug impermeability is currently an effective area of research. Many scientists have looked into pharmaceutical cocrystals as a way to improve the physicochemical properties of several anticancer drugs. Benefits of pharmaceutical cocrystals over other solid forms may include improved solubility, bioavailability, and a reduced susceptibility for phase transition. Cocrystal strategy also stands as a green synthesis tool by using very limited organic solvents during its formulation. Having so many advantages, to date, the reported cocrystals and drug–drug cocrystals of anticancer drugs are limited. Here we review the pharmaceutical cocrystals and drug–drug cocrystals of the anticancer drugs reported in the last decade and their future in imaging, and also shed light on the opportunities and challenges for the development of anticancer drug cocrystals.

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Experimental design approach for development of cocrystals and immediate release cocrystal tablet of atorvastatin calcium for enhancement of solubility and dissolution

Cited by 2 publications

References 23 publications

Evaluation on Cocrystal Screening Methods and Synthesis of Multicomponent Crystals: A Case Study

Evaluation on Cocrystal Screening Methods and Synthesis of Multicomponent Crystals: A Case Study

Cocrystals and Drug–Drug Cocrystals of Anticancer Drugs: A Perception towards Screening Techniques, Preparation, and Enhancement of Drug Properties

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