Drug–Drug Multicomponent Crystals as an Effective Technique to Overcome Weaknesses in Parent Drugs

Putra, Okky Dwichandra; Furuishi, Takayuki; Yonemochi, Etsuo; Terada, Katshuhide; Uekusa, Hidehiro

doi:10.1021/acs.cgd.6b00639

Cited by 58 publications

(48 citation statements)

References 45 publications

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“…As described earlier, in the piperine-succinic acid cocrystal, succinic acid molecules formed a channel structure. Solubility enhancements arising from a channel structure have been reported previously, and this piperine-succinic acid cocrystal structure strongly indicated the occurrence of this improvement mechanism [56,57]. Putra et al explained the mechanism as follows [58]: First, the more highly soluble coformer molecules dissolve from a cocrystal, leaving void channel structure in the crystal.…”

Section: Resultssupporting

confidence: 51%

Improved Solubility and Dissolution Rates in Novel Multicomponent Crystals of Piperine with Succinic Acid

et al. 2020

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The objectives of this study were to prepare and characterize a novel piperine–succinic acid multicomponent crystal phase and to evaluate the improvement in the solubility and dissolution rate of piperine when prepared in the multicomponent crystal formation. The solid-state characterization of the novel multicomponent crystal was performed by powder X-ray diffraction (XRD), differential scanning calorimetry (DSC), and Fourier transform-infrared (FT-IR) spectroscopy. Solubility and dissolution rate profiles were evaluated in distilled water. The physical stability was evaluated under high relative humidity (75% and 100% RH). The determination of the single crystal X-ray diffraction structure revealed that this novel multicomponent crystal was a cocrystalline phase of piperine–succinic acid (2:1 molar ratio). The differential scanning calorimetry thermogram of the cocrystal showed a single and sharp endothermic peak at 110.49 °C. The cocrystal resulted in greater solubility and a faster dissolution rate of piperine than intact piperine. This improvement was a result of the formation of a channel structure in the cocrystal. In addition, the cocrystal was stable under a humid condition.

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Section: Resultssupporting

confidence: 51%

Improved Solubility and Dissolution Rates in Novel Multicomponent Crystals of Piperine with Succinic Acid

et al. 2020

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“…Putra et al reported [92] a multidrug crystal of antidiabetic drug gliclazide (GLI) and metformin (MET). Combining these two non-insulin-dependent diabetes mellitus (NIDDM) drug, they have prepared a salt that is more soluble and have higher dissolution rate compared to GLI; and less hygroscopic compared to MET.…”

Section: Gliclazide-metformin Saltmentioning

confidence: 99%

Drug‑Drug and Drug‑Nutraceutical Cocrystal/Salt as Alternative Medicine for Combination Therapy: A Crystal Engineering Approach

2018

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The pre-formulation of pharmaceutical cocrystals and salts is a concept of crystal engineering that has emerged as a promising technique for drug development in pharmaceutical industry. Recent introduction of pharmaceutical cocrystals in regulatory guidelines of US Food and Drug Administration (FDA) made them one of the potential alternatives when salt preparation is not feasible. Apart from generally regarded as safe (GRAS) coformers, drug-drug and drug-nutraceutical cocrystals are recent additions to pharmaceutical cocrystal family that have additional health benefits. Indeed, preparation of salt forms is a routine practice to deal with inadequacies associated with the active pharmaceutical ingredient (API) and happens to be a potentially reliable method. Amongst them, drug-drug and drug-nutraceutical cocrystals have drawn significant importance in the recent past as they reduce drug load and cost effects during multiple disease diagnosis. However, one has to be prudent in the selection of drug molecules, the presence of complementary hydrogen bond synthon, disease management during multiple disease therapy, etc. that play important roles in their preparation. That is the reason why drug-drug cocrystals are scarce in the literature compared to pharmaceutical cocrystals containing GRAS coformers and salt forms. Herein, we discuss case studies preferably the reported drug-drug, drug-nutraceutical cocrystals, and a few salts with an emphasis on their role in physicochemical property modulation.

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“…200 Formation of drug-drug pharmaceutical co-crystals results to overcome the problems related with a traditional combination of drugs by modifying the properties of both drugs. 59,198,203 Telmisartan: Atenolol co-crystals 204 proved that multidrug co-crystals could be a great replacement for standard therapy with more than one API. Almansa prepared tramadol hydrochloride: celecoxib co-crystals which showed favourable physicochemical and dissolution profiles.…”

Section: Applicationsmentioning

confidence: 99%

Insight into Concept and Progress on Pharmaceutical Co-Crystals: An overview

Vemuri¹,

Srinivas²

2019

IJPER

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Pharmaceutical co-crystals have conferred significant recognition in recent past as a new solid form by virtue their capability to modulate physicochemical properties of Active Pharmaceutical Ingredient (API). Nevertheless, pharmaceutical progress of cocrystals could be provocation, the requirement for high-throughput screening methods and the techniques capable of co-crystal production in industrial scale still hamper the co-crystal used by industries. In this review, well ordered overview of pharmaceutical co-crystal is provided, with focus on role of supramolecular chemistry, co-crystal design strategies, preparation methods, physicochemical property studies, mechanism of solubility enhancement, evaluation techniques. In the present commentary, the impact of choosing appropriate process design and formulation on translational challenges has been discussed. Eventually, a short outline of applications and marketed drug products of pharmaceutical co-crystal drug substance is also described.

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Drug–Drug Multicomponent Crystals as an Effective Technique to Overcome Weaknesses in Parent Drugs

Cited by 58 publications

References 45 publications

Improved Solubility and Dissolution Rates in Novel Multicomponent Crystals of Piperine with Succinic Acid

Improved Solubility and Dissolution Rates in Novel Multicomponent Crystals of Piperine with Succinic Acid

Drug‑Drug and Drug‑Nutraceutical Cocrystal/Salt as Alternative Medicine for Combination Therapy: A Crystal Engineering Approach

Insight into Concept and Progress on Pharmaceutical Co-Crystals: An overview

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