通过使用聚乙烯酒精(PVA)形成固体分散物(PVA)来解决酮含量的增加

Asriana Sultan, N. Ida, I. Ismail
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引用次数: 1

摘要

酮洛芬由于溶解度低,被列入生物制药分类系统(BCS) II类。溶解度低会影响溶出速率和溶出浓度,因此吸收度和生物利用度也低。为了提高这类药物的溶解度和溶出度,人们进行了一些研究,如采用固体分散体系。本研究旨在测定聚乙烯醇(PVA)对酮洛芬在固体分散体和物理混合物中溶解浓度的影响,并确定最佳配方。分别以1:1、1:2和1:4的比例配制酮洛芬- PVA的固体分散体和物理混合物,并与标准酮洛芬进行比较。采用紫外可见分光光度计以PVA为基质对标准酮洛芬最大波长的干预试验,在不含胃蛋白酶的人工胃液介质中采用篮式搅拌器在pH±1,2、温度37±0.5℃、设备转速50 rpm条件下进行溶出试验,评价固体分散度。在10、20、30、45和60分钟采集样本。采用紫外可见分光光度计在260 nm波长下测定酮洛芬的溶出量。结果表明,在固体分散体和物理混合体中,最大波长点没有移位。固体分散体中溶解的酮洛芬浓度高于物理混合物和标准酮洛芬。固体分散配方中酮洛芬的最高溶解浓度为1:1。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Peningkatan Kadar Ketoprofen Terdisolusi melalui Pembentukan Dispersi Padat menggunakan Polivinil Alkohol (PVA)
Ketoprofen is included in the Class II of Biopharmaceutical Classification System (BCS) which has low solubility. Low solubility will affect the dissolution rate and the dissolved concentration, so the absorption and bioavailability are low as well. Several studies have been conducted to improve the solubility and the dissolution of drugs from these group, such as by solid dispersion system. This study aims to determine the effect of polyvinyl alcohol (PVA) on the dissolved concentration of ketoprofen in solid dispersion and in physical mixture, and to decidethe optimum formula.Solid dispersion and physical mixture of ketoprofen - PVA were formulated with the ratio of 1:1, 1:2 and 1:4, and then compared with the standard ketoprofen. Evaluation of solid dispersion was performed by the intervention test of PVA as a matrix on the maximum wavelength of standard ketoprofen using a UV-Vis spectrophotometer and the dissolution test in artificial gastric fluid media without pepsin using a basket stirrer at pH ± 1,2, the temperature of 37 ± 0.5ºC, and device speed of 50 rpm. The sample was collected at 10, 20, 30, 45, and 60 minutes. The amount of dissolved ketoprofen was determined by a UV-Vis spectrophotometer at a wavelength of 260 nm. The results showed that there was no shifting on maximum wavelength point in both solid dispersions and physical mixtures. The dissolved ketoprofen concentration that was represented in solid dispersion was greater than in physical mixture and standard ketoprofen. The highest dissolved ketoprofen concentration was indicated in solid dispersion formula with the ratio of 1:1.
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