包合物对布洛芬栓剂溶出释放特性的改善

F. Darusman, M. I. Septian, E. Kartadarma
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引用次数: 0

摘要

布洛芬因其低溶解度和高渗透性而被归类为BCS II类。利用β-环糊精形成包合物是提高药物溶解度的一种方法。除了增加溶解度的方法外,剂型和给药途径的选择对治疗的成功起着很大的作用,因为它可以增加药物的起效,同时避免副作用。直肠栓剂可以提供比口服制剂更快的解热效果。研究β-环糊精包合物对布洛芬栓剂溶出度和释放特性的影响。栓剂配方使用不同浓度的十六烷基醇来增加可可脂基础的稠度。通过将β-环糊精布洛芬包合栓剂与纯布洛芬栓剂的摩尔比分别为1:1、1:2和2:1,评价布洛芬在栓剂中的释放特性,包括感官、融化时间、重量多样性、溶出率和溶出效率。布洛芬与β-环糊精摩尔比为2:1的包合物提高了布洛芬在栓剂中的溶解度和溶出率,具有良好的物理特性和释放特性。关键词:布洛芬;包合物;栓剂
本文章由计算机程序翻译,如有差异,请以英文原文为准。
The Improvement of the Dissolution and Release Characteristics of Ibuprofen Suppository Through Inclusion Complexes with
Ibuprofen is classified as a BCS class II because of its low solubility and high permeability. Inclusion complex formation using β-cyclodextrin is one method to increase a drug’s solubility. In addition to the method of increasing the solubility, the choice of dosage form and route of administration has a big role in the success of therapy because it can increase the onset of action of drugs while avoiding side effects. Rectal suppositories can provide a faster antipyretic effect than oral preparations. The purpose of this study was to determine the effect of inclusion complexes formation with β-cyclodextrin in increasing the dissolution rate and release characteristics of ibuprofen suppositories. The suppository formulation used various concentrations of cetylalcohol to increase the consistency of the cocoa butter base. The release characteristics of ibuprofen in suppositories were evaluated, including, organoleptic, melting time, weight diversity, dissolution rate and dissolution efficiency, by comparing ibuprofen inclusion complex suppositories with β-cyclodextrin all three mole ratios, namely 1:1, 1:2 and 2:1, to pure ibuprofen suppositories. The inclusion complex of ibuprofen with β-cyclodextrin at a mole ratio of 2:1 showed to increase the solubility and dissolution rate of ibuprofen in suppositories with good physical and release characteristics. Keywords: ibuprofen, inclusion complexes, suppository
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