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氢化植物油与聚羧乙烯(carbopol)曾分别作为口服缓释制剂的不溶性骨架与浸润性基质使用。近有用扩散与浸润的机制阐述释放过程。本文以亲水-疏水组分形成的基质(氢化植物油和聚羧乙烯)研究了溶解度和可湿性各异的非甾体激素类抗炎药吲哚美辛、布洛芬和双氯芬酸钠的释放率及其影响因素。溶质的溶解度试验,是取过量的药品粉末约1.5g 混悬于 pH6.5磷酸缓冲液中,于25℃振摇72h,上清液经适当稀释后,用分光光度法测定,求出溶解度的平均值。药物的可湿润性试验,采用两种方法,其一为Kossen 法,另一为 Wilhelmy plate 法,均以接触角(θ°)表示。试验表明,双氯芬酸钠的溶解度和可湿性最强,吲哚美辛和布洛芬的可湿性相似,但其溶解度相差10倍。吲哚美辛在药物/基质比为2时,释放最慢,布洛芬在药物/基质比为0.5时释放最快,药物释放率主要受药物可湿性的影响,可湿性强的的双氯芬酸钠释放率随药物/基质比增加而增加,而吲哚美辛和布洛芬恰恰相反。
Hydrogenated vegetable oil and carbopol were used as insoluble matrix and infiltrative matrix for oral sustained release formulations, respectively. Nearly diffusion and infiltration mechanism elaborates the release process. In this paper, the release rate of indometacin, ibuprofen and diclofenac sodium, a nonsteroidal antiinflammatory drug with different solubility and wettability, was studied on the basis of hydrophilic-hydrophobic components (hydrogenated vegetable oil and carbopol) And its influencing factors. The solute solubility test is that about 1.5g of excess drug powder is suspended in pH6.5 phosphate buffer and shaken at 25 ° C for 72h. The supernatant is diluted appropriately and determined by spectrophotometry to determine the solubility average value. Drug wettability test, the use of two methods, one Kossen method and the other is Wilhelmy plate method, all in contact angle (θ °) said. Tests show that diclofenac sodium strongest solubility and wettability, indomethacin and ibuprofen wettability similar, but its solubility difference of 10 times. Indomethacin showed the slowest release at the drug / matrix ratio of 2, the fastest release of ibuprofen at the drug / matrix ratio of 0.5, the drug release rate was mainly affected by the drug wettability, and the wettable diclofenac sodium The rate of release increased with the drug / matrix ratio, whereas indomethacin and ibuprofen were exactly the opposite.