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Formulation and Evaluation of Chondroitin Sulphate Tablets of Aceclofenac for Colon Targeted Drug Delivery

机译:醋氯芬酸软骨素硫酸盐片剂的结肠靶向给药研究与评价

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摘要

The aim of the present study was to develop a single unit, site-specific matrix tablets of aceclofenac allowing targeted drug release in the colon with a microbially degradable polymeric carrier, chondroitin suphate (CS) and to coat the optimized batches with a pH dependent polymeric. The tablets were prepared by wet granulation method using starch mucilage as a binding agent and HPMC K-100 as a swellable polymer. Chondroitin Sulphate and drug and physical mixture were characterized by Fourier transform infrared spectroscopy (FTIR) and differential scanning calorimetry (DSC). The tablets were tested for their in-vitro dissolution characteristics in various simulated gastric fluids for their suitability as a colon-specific drug delivery system and also the tablets were evaluated for physicochemical properties, drug content, water percentage swelling and erosion characteristics. The dissolution data demonstrates that the 10% w/w increase in coating level of the pH dependent polymer (Eudragit L-100 and Eudragit S-100 in a ratio of 1 : 4 prevented the drug release in the simulated gastric fluid (pH 1.2-SGF) and the simulated intestinal fluid (pH 7.4-SIF). The dissolution rate of the tablet is dependent upon the concentration of Chondroitin sulphate in the simulated colonic fluid (SCF). The rapid increase in release of aceclofenac in SCF was revealed as due to the degradation of the Chondroitin sulphate membrane by bacterial enzymes. The studies confirmed that, the designed system could be used potentially as a carrier for colon delivery of aceclofenac by regulating drug release in stomach and the small intestine.
机译:本研究的目的是开发醋氯芬酸的单一单位,位点特异性基质片剂,从而允许使用可微生物降解的聚合物载体软骨素硫酸盐(CS)在结肠中靶向释放药物,并用pH依赖的聚合物包被优化批次。 。通过湿法制粒法制备片剂,使用淀粉胶浆作为粘合剂和HPMC K-100作为可溶胀聚合物。通过傅立叶变换红外光谱(FTIR)和差示扫描量热法(DSC)对硫酸软骨素以及药物和物理混合物进行了表征。测试片剂在各种模拟胃液中的体外溶出特性,以适应其作为结肠特异性药物递送系统的适用性,还评估片剂的理化特性,药物含量,水百分比溶胀和侵蚀特性。溶出度数据表明,pH依赖性聚合物(Eudragit L-100和Eudragit S-100的比例为1:4)的涂层水平增加10%w / w阻止了药物在模拟胃液(pH 1.2- SGF)和模拟肠液(pH 7.4-SIF)。片剂的溶出度取决于模拟结肠液(SCF)中硫酸软骨素的浓度。醋氯芬酸在SCF中的释放迅速增加是由于研究证实,所设计的系统可以通过调节胃和小肠中的药物释放而潜在地用作醋氯芬酸结肠输送的载体。

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