Pharmaceutical cocrystals of Efavirenz: Towards the improvement of solubility, dissolution rate and stability

Gowda, B.H. Jaswanth; Nechipadappu, Sunil Kumar; Shankar, S. J.; Chavali, Murthy; Paul, Karthika; Ahmed, Mohammed Gulzar; Sanjana, A; Shanthala, H K

doi:10.1016/j.matpr.2021.05.535

Cited by 9 publications

(1 citation statement)

References 23 publications

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“…A typical example is the carbamazepine-nicotinamide co-crystal that spontaneously converts to carbamazepine dehydrate during dissolution, which has a lower solubility, and the theoretical solubility/dissolution improvement of the co-crystal cannot be obtained [59]. Similarly, co-crystals of efavirenz were developed using several coformers [60]. When compared to pure efavirenz, efavirenz-DL-alanine and efavirenz-oxalic acid co-crystals had higher solubility and enhanced dissolution profiles, while efavirenz-maleic acid and efavirenz-nicotinamide co-crystals had decreased dissolution.…”

Section: Solid Form Impact On Physicochemical and Biopharmaceutical P...mentioning

confidence: 99%

Pharmaceutical Crystals: Development, Optimization, Characterization and Biopharmaceutical Aspects

Bongioanni¹,

Bueno²,

Mezzano³

et al. 2023

Crystal Growth and Chirality - Technologies and Applications

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In the solid state, the active pharmaceutical ingredients tend to exhibit crystalline order. In this regard, the interest in the crystalline solid state has expanded to include single-component compounds as well as multicomponent systems such as salts, hydrates, solvates, and co-crystals. The study of crystalline behavior is recognized as an essential component of preformulation research in pharmaceutical sciences and industries. The crystalline form can impact the drug properties such as solubility, dissolution rate, stability, hygroscopicity, and toxicity profile. Therefore, each solid form must be appropriately identified and characterized because it will affect the drug formulation, including the pharmacokinetic, pharmacodynamic, and safety properties of the formulation. In this context, this chapter will cover topics such as synthesis approaches (including nucleation and crystallization procedures), crystal polymorphism, solid state characterization techniques and the impact of crystals on physicochemical and biopharmaceutical properties.

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Section: Solid Form Impact On Physicochemical and Biopharmaceutical P...mentioning

confidence: 99%

Pharmaceutical Crystals: Development, Optimization, Characterization and Biopharmaceutical Aspects

Bongioanni¹,

Bueno²,

Mezzano³

et al. 2023

Crystal Growth and Chirality - Technologies and Applications

View full text Add to dashboard Cite

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Preparation and characterization of efavirenz cocrystals: An endeavor to improve the physicochemical parameters

Gowda

Ahmed

Shankar

et al. 2022

Materials Today: Proceedings

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Taming the dynamics in a pharmaceutical by cocrystallization: investigating the impact of the coformer by solid-state NMR

et al. 2021

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Pharmaceutical cocrystals of Efavirenz: Towards the improvement of solubility, dissolution rate and stability

Cited by 9 publications

References 23 publications

Pharmaceutical Crystals: Development, Optimization, Characterization and Biopharmaceutical Aspects

Pharmaceutical Crystals: Development, Optimization, Characterization and Biopharmaceutical Aspects

Preparation and characterization of efavirenz cocrystals: An endeavor to improve the physicochemical parameters

Taming the dynamics in a pharmaceutical by cocrystallization: investigating the impact of the coformer by solid-state NMR

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