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首页> 外文期刊>Drug delivery. >Improved solubility and in vitro dissolution of Ibuprofen from poloxamer gel using eutectic mixture with menthol.
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Improved solubility and in vitro dissolution of Ibuprofen from poloxamer gel using eutectic mixture with menthol.

机译：使用与薄荷醇的共晶混合物，提高了布洛芬从泊洛沙姆凝胶中的溶解度和体外溶出度。

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摘要

To improve the solubility and in vitro dissolution of poorly water-soluble ibuprofen with poloxamer and menthol, the effects of menthol and poloxamer 188 on the aqueous solubility of ibuprofen were investigated. The dissolution study of ibuprofen delivered by poloxamer gels composed of poloxamer 188 and menthol were performed. In the absence of poloxamer, the solubility of ibuprofen increased until the ratio of menthol to ibuprofen increased from 0:10 to 4:6, followed by an abrupt decrease in solubility above the ratio of 4:6, indicating that 4 parts of ibuprofen formed eutectic mixture with 6 parts of menthol. In the presence of poloxamer 188, the solutions with the same ratio of menthol to ibuprofen showed abrupt increase in the solubility of ibuprofen. Furthermore, the solution with ratio of 4:6 showed more than 2.5- and 6-fold increase in the solubility of ibuprofen compared with that without poloxamer and that without menthol, respectively. The poloxamer gel with menthol/ibuprofen ratio of 1:9 andhigher than 15% poloxamer 188 showed the maximum solubility of ibuprofen, 1.2 mg/ml. Menthol improved the dissolution rates of ibuprofen from poloxamer gels. Dissolution mechanism showed that the dissolution rate of ibuprofen from the poloxamer gels without menthol was independent of the time, but the drug might be dissolved from the poloxamer gels with menthol by Fickian diffusion. Thus, the poloxamer gels developed using eutectic mixture with menthol, which gave the improved solubility and dissolution of drug, are potential candidates for ibuprofen-loaded transdermal and rectal delivery system.
机译：为了提高水溶性差的布洛芬与泊洛沙姆和薄荷醇的溶解度和体外溶出度，研究了薄荷醇和泊洛沙姆188对布洛芬的水溶性的影响。进行了由泊洛沙姆188和薄荷醇组成的泊洛沙姆凝胶递送的布洛芬的溶出研究。在没有泊洛沙姆的情况下，布洛芬的溶解度增加，直到薄荷醇与布洛芬的比例从0:10增加到4：6，然后溶解度突然下降，超过4：6的比例，表明形成了4份布洛芬与6份薄荷醇的低共熔混合物。在泊洛沙姆188的存在下，薄荷醇与布洛芬比例相同的溶液显示布洛芬的溶解度突然增加。此外，与没有泊洛沙姆和没有薄荷醇的溶液相比，比率为4：6的溶液的布洛芬溶解度分别增加了2.5倍和6倍以上。薄荷醇/布洛芬比例为1：9且高于15％的泊洛沙姆188的泊洛沙姆凝胶显示布洛芬的最大溶解度为1.2 mg / ml。薄荷醇提高了布洛芬从泊洛沙姆凝胶中的溶解速率。溶出机理表明，布洛芬在无薄荷醇的泊洛沙姆凝胶中的溶出速率与时间无关，但药物可能通过Fickian扩散从有薄荷醇的泊洛沙姆凝胶中溶出。因此，使用具有薄荷醇的共晶混合物开发的泊洛沙姆凝胶具有改善的药物溶解性和溶解性，是布洛芬负载的透皮和直肠输送系统的潜在候选者。

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