难溶性药物共晶的溶出与吸收研究进展

Recent advance on the dissolution and absorption of the cocrystals of poorly soluble drugs

药物共晶是改善难溶性药物溶出与生物利用度有效的策略之一,但其在溶出过程中容易发生相转变导致原料药重结晶,失去增溶优势,该问题已成为难溶性药物共晶应用的主要瓶颈之一。选择合适的添加剂能够有效抑制药物共晶溶出过程中的相转变,提高难溶性药物共晶溶出与吸收程度;此外,复杂的胃肠道给药环境与药物共晶体内吸收行为,均会对药物共晶的生物利用度产生明显影响。因此,本文总结了关于难溶性药物共晶溶出与吸收的研究进展,期望为药物共晶制剂处方的开发提供指导。

Pharmaceutical cocrystals are one of the effective strategies to improve the solubility and bioavailability of poorly water-soluble drugs.However,the phase transformation of cocrystals during dissolution can lead to the recrystallization of the parent drugs,and thus negating the solubility advantage of cocrystals.The introduction of suitable excipients into the cocrystal formulation may inhibit the phase transformation during dissolution,resulting in the enhanced dissolution and bioavailability of poorly soluble drugs.In addition,the complex gastrointestinal environment and absorption behavior of drugs can have significant impacts on the oral bioavailability of cocrystals.This review summarizes the recent studies of the dissolution and absorption of pharmaceutical cocrystals,and aims to provide guidance for the rational design of pharmaceutical cocrystal formulations.