首页> 美国卫生研究院文献>Saudi Pharmaceutical Journal : SPJ >Enhancement of dissolution rate of class II drugs (Hydrochlorothiazide); a comparative study of the two novel approaches; solid dispersion and liqui-solid techniques
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Enhancement of dissolution rate of class II drugs (Hydrochlorothiazide); a comparative study of the two novel approaches; solid dispersion and liqui-solid techniques

机译:提高II类药物(氢氯噻嗪)的溶出度;对两种新颖方法的比较研究;固体分散和液固技术

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摘要

Liqui-solid technique and solid dispersion formation are two novel approaches for enhancement of dissolution rate of BCS class II drugs. Liqui-solid compact converts a liquid drug or drug solution into a free flowing powder with enhanced dissolution rate. In case of solid dispersion drug is molecularly dispersed in a hydrophilic polymer in solid state. In the present study, Liqui-solid and solid dispersion techniques were applied to enhance the dissolution of the Hydrochlorothiazide. Three formulations of Hydrochlorothiazide were prepared by liqui-solid technique using micro crystalline cellulose as carrier material and colloidal silicon dioxide as coating material. Water, poly ethylene glycol-400 and Tween-60 were used as solvent system. Solid dispersions of Hydrochlorothiazide were prepared by solvent fusion method using PEG-4000 as carrier polymer. Tablets were subjected to evaluation of various physical and chemical characteristics. Dissolution profiles of tablets prepared by the novel techniques were compared with marketed conventional tablets. Model independent techniques including similarity factor, dissimilarity factor and dissolution efficiency were applied for comparison of dissolution profiles. The results obtained indicated that liqui-solid compact formulations were more effective in enhancing the dissolution rate compared with solid dispersion technique. The liqui-solid compacts improved the dissolution rate up to 95% while the solid dispersion increased it to 88%.
机译:液固技术和固体分散体形成是提高BCS II类药物溶出度的两种新方法。液体固体压块将液体药物或药物溶液转变成具有增加的溶解速率的自由流动的粉末。在固体分散的情况下,药物以固态分散在亲水聚合物中。在本研究中,采用液体-固体和固体分散技术来增强氢氯噻嗪的溶解。以微晶纤维素为载体材料,胶体二氧化硅为包衣材料,采用液固法制备了氢氯噻嗪三种配方。水,聚乙二醇-400和吐温60用作溶剂体系。以PEG-4000为载体,通过溶剂熔融法制备氢氯噻嗪固体分散体。对片剂进行各种物理和化学特性的评估。将通过新技术制备的片剂的溶出曲线与市售的常规片剂进行比较。采用模型独立技术,包括相似因子,不相似因子和溶出效率,比较溶出曲线。所得结果表明,与固体分散技术相比,液体-固体致密制剂在提高溶解速率方面更有效。液体固体压块将溶出率提高到95%,而固体分散体将溶出率提高到88%。

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