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难溶于水的药物,由于服后在胃肠液中溶解度小,溶出速度慢,吸收缓慢且不完全而影响疗效的发挥。药物溶出速度与其表面积是直接成比例的,故减小药物粒子就可增加溶出速度,从而在体内就有较快的吸收和较高的生物利用度。近代,基于药物粒子大小与溶出速度及吸收速度关系而发展起来的固态分散法,是解决难溶性药物体内吸收问题的一项新技术。它是将难溶性药物和一种生理上惰性、易溶于水的固体载体以熔融、溶剂或溶剂-熔融相结合的方法制成的药物在固体载体中的高度分散体系。服用后,载体溶解并使药物以分子状态释出,从而具有比原来快得多的溶出速度和生物利用度。近年来,国内已用此法改善一些药物的吸收,取得成效。
Difficult to dissolve in water drugs, due to the service in the gastrointestinal fluid solubility, dissolution rate is slow, slow and incomplete absorption and affect the efficacy of play. Drug dissolution rate and its surface area is directly proportional to, so reduce the drug particles can increase the dissolution rate, which has faster absorption and higher bioavailability in the body. In recent years, the solid dispersion method based on the relationship between drug particle size and dissolution rate and absorption rate is a new technology to solve the problem of absorption in insoluble drugs. It is a highly dispersed drug in a solid carrier made by a combination of a poorly soluble drug and a physiologically inert, water-soluble solid carrier in a melt, solvent or solvent-melt combination. After administration, the carrier dissolves and releases the drug in a molecular state, thereby having a much faster dissolution rate and bioavailability than the original. In recent years, this method has been used in China to improve the absorption of some drugs and achieve results.