Cocrystal engineering of pharmaceutical solids: therapeutic potential and challenges

Abstract

Cocrystals are an emerging class of crystalline materials composed of two or more different molecules in the same crystal lattice that are physically connected by non-ionic and non-covalent bonds. Formulating...

Crystal Structure, Solubility, and Pharmacokinetic Study on a Hesperetin Cocrystal with Piperine as Coformer

“…The increase in solubility of the above HES cocrystals is due to the water-soluble coforms. Currently, many other water-soluble components were selected for drugs' cocrystals, such as nicotinamide, isonicotinamide, theobromine, theophylline, caffeine, betaine, and urea [25][26][27][28][29].…”

“…The increase in solubility of the above HES cocrystals is due to the water-soluble coforms. Currently, many other water-soluble components were selected for drugs' cocrystals, such as nicotinamide, isonicotinamide, theobromine, theophylline, caffeine, betaine, and urea [25][26][27][28][29]. Although solubility is a major limiting factor in hydrophobic drugs' bioavailability, the efflux of intestinal P-glycoprotein (P-gp), the metabolism of cytochrome P450, and the degradation of drugs by intestinal bacterial enzymes also significantly contribute to reduce drugs' oral bioavailability [30,31].…”

Rational Development of a Carrier-Free Dry Powder Inhalation Formulation for Respiratory Viral Infections via Quality by Design: A Drug-Drug Cocrystal of Favipiravir and Theophylline

“…In the future in vivo study, smaller doses will be used to ensure the safety of animals. It should be noted that the utility of drug-drug cocrystal in medicine is generally restricted by the inflexible dosage regimen, considered as one of the major challenges in the formulation development [54]. Excessive amount of either cocrystal formers appears inevitable, which has been seen in many reported systems and may pose toxicity concern.…”

“…The assumption lies in the fact that a cocrystal can modulate a series of pharmaceutical properties, such as dissolution, stability, hygroscopicity, mechanical properties, and bioavailability, etc. [49][50][51][52][53][54][55], and thereby potentially replacing the function of conventional excipients. It is worth mentioning that the majority of cocrystal research has been focusing on the oral dosage forms over the past two decades.…”

“…It is worth mentioning that the majority of cocrystal research has been focusing on the oral dosage forms over the past two decades. In contrast, effort devoted to the development of inhalable drug-drug cocrystal for combination therapy is scarce [54]. This unique niche deserves more attention since significant clinical demand in handling the growing global prevalence of respiratory diseases is foreseeable due to population aging and increased exposure to high air pollutants.…”