Department of Pharmaceutics, Faculty of Pharmacy, Universitas Airlangga, Surabaya, Indonesia.
J Basic Clin Physiol Pharmacol. 2021 Jun 25;32(4):669-673. doi: 10.1515/jbcpp-2020-0487.
In order to minimize gastrointestinal irritation and to extend the absorption of ketoprofen, microparticles prepared with chitosan have been developed. In this study, chitosan type and drug-chitosan ratio were investigated to prepare microparticles of ketoprofen and evaluated for physical characteristics and drug release profiles.
Microparticles were prepared by using ionic gelation methods with chitosan, which has two different viscosities i.e., 19 and 50 cPs, cross-linked with tripolyphosphate, and dried by spray drying method. The microparticles were made with a drug-chitosan ratio of 5:15 and 6:15.
The results showed that the microparticles had spherical shapes. Increasing the amount of ketoprofen improved the drug content and entrapment efficiency. Evaluation of drug release in simulated intestinal fluid (pH 6.8) showed that the microparticles prepared with chitosan 19 cPs had the slowest release rate than those of chitosan 50 cPs, while that of the microparticles prepared with chitosan 50 cPs with the ratio of drug/polymer 6:15 was the fastest, as shown by its slope value. The release rate of microparticles with chitosan 19 cPs was slower than those microparticles with chitosan 50 cPs.
It could be suggested that by increasing the amount of ketoprofen, it improved the entrapment efficiency and the release rate of microparticles.
为了最大限度地减少胃肠道刺激并延长酮洛芬的吸收，已经开发出了用壳聚糖制备的微粒。在这项研究中，考察了壳聚糖的类型和药物-壳聚糖的比例，以制备酮洛芬的微粒，并对其物理特性和药物释放曲线进行了评价。
采用离子凝胶法，用两种不同黏度（19 和 50 cPs）的壳聚糖与三聚磷酸交联，并通过喷雾干燥法干燥，制备了微粒。药物-壳聚糖的比例为 5:15 和 6:15。
结果表明，微粒呈球形。增加酮洛芬的用量可以提高药物含量和包封效率。在模拟肠液（pH 6.8）中的药物释放评价表明，用黏度为 19 cPs 的壳聚糖制备的微粒的释放速率比用黏度为 50 cPs 的壳聚糖制备的微粒慢，而用黏度为 50 cPs 的壳聚糖且药物/聚合物的比例为 6:15 的微粒的释放速率最快，这可以从斜率值看出。用黏度为 19 cPs 的壳聚糖制备的微粒的释放速率比用黏度为 50 cPs 的壳聚糖制备的微粒慢。
可以认为，增加酮洛芬的用量可以提高微粒的包封效率和释放速率。
