采用凝胶44/14和labrasol提高吡罗西康的溶解度和溶出率

Ayşegül Karataş, Nilüfer Yüksel, Tamer Baykara
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引用次数: 126

摘要

吡罗昔康是一种非甾体抗炎药,其特点是低溶解度-高渗透性。本研究旨在通过利用凝胶和拉布拉西醇制备药物半固体分散体,提高吡罗西康在生理pH值下的溶解度,提高其溶出率。这些赋形剂的主要特征是它们的熔点和HLB(亲水-亲脂平衡)值。在不同pH的培养基中进行了溶出试验。采用差示扫描量热法(DSC)研究吡罗西康与辅料之间的相互作用。Gelucire 44/14和Labrasol在水中浓度为15% w/v时,吡罗西康的溶解度分别提高了20倍和50倍。半固体分散体含有1/20的药物/辅料混合物(20%格鲁西尔44/14和80% Labrasol (w/w)),在每种溶解介质(模拟胃液(SGF), pH 1.2;磷酸盐缓冲液,pH为4.5和6.8;和水)。对该半固态分散体的DSC分析表明,药物与辅料之间没有发生化学反应,形成了吡罗昔康与辅料的固态溶液。
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Improved solubility and dissolution rate of piroxicam using gelucire 44/14 and labrasol

Piroxicam is a nonsteroidal anti-inflammatory drug that is characterized by low solubility-high permeability. The present study was designed to improve the dissolution rate of piroxicam at the physiological pH's through its increased solubility by preparing semi-solid dispersions of drug using Gelucires and Labrasol. These excipients are essentially characterized by their melting points and HLB (hydrophilic–lipophilic balance) values. The dissolution tests of the preparations were performed in the media with different pH's. Differential scanning calorimetry (DSC), were used to examine the interaction between piroxicam and excipients. Gelucire 44/14 and Labrasol at the concentration of 15% w/v in water provided 20- and 50-fold increase in the solubility of piroxicam, respectively. The semi-solid dispersion containing 1/20 of drug/excipient mixture (20% Gelucire 44/14 and 80% Labrasol in w/w) produced the dissolution not less than 85% of piroxicam within 30 min in each dissolution media (simulated gastric fluid (SGF), pH 1.2; phosphate buffers, pH 4.5 and 6.8; and water). DSC analysis of this semi-solid dispersion indicated that there was no chemical reaction between the drug and excipients, and that a solid-state solution of piroxicam with excipient formed.

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