药物固体制剂的接触角与湿润性

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固体药物的湿润性对于粉末的吸湿性、化学稳定性和片剂包衣的粘着力以及粉末在液体中的分散性等有着重要的影响,尤其是固体粉末的湿润性作为溶出初始阶段的首要条件,对片剂的溶出速度影响很大。如片剂压制过程添加的润滑剂大多为疏水性,由此引起颗粒湿润性的改变常常影响片剂的崩解时限与溶出速率,而难溶性药物片剂的水透入速度及崩解后粒子的絮凝或分散等均与粉末的湿润性有关,进而影响片剂的溶出和疗效。无论是直接以接触角衡量药物固体制剂的湿润性,还是以固体表面自由能所求的极性指数作为湿润性的定量指标,都基于测定固体的接触角。固体接触角的测定方法众多,而原理不一,在药物制剂中的应用日趋见多,文献报道值也各有出入。本文将着重讨论接触角的测定方法及应用。 The wettability of the solid drug has an important influence on the hygroscopicity of the powder, the chemical stability and the adhesion of the tablet coating, and the dispersibility of the powder in the liquid, and especially the wettability of the solid powder as the primary condition for the initial stage of dissolution , The dissolution rate of the tablet has a great impact. Lubricants, such as those added during tablet compression, are mostly hydrophobic, thereby causing changes in the wettability of the particles often affecting the tablet’s disintegration time and dissolution rate, while the rate of water penetration into the poorly soluble drug tablet and the rate of disintegration of the particles Flocculation or dispersion are related to the wettability of the powder, thereby affecting the tablet dissolution and efficacy. Whether directly measuring the wettability of pharmaceutical solid formulations with a contact angle or the polar index based on the free surface energy of the solid as a quantitative indicator of wettability are all based on determining the solid contact angle. There are many methods to determine the solid contact angle, but the principles are different. The application of the drug in the pharmaceutical preparations is becoming more and more frequent, and the reported values ​​in the literature also vary. This article will focus on the determination of contact angle and its application.
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