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首页> 外文期刊>Asian Journal of Pharmaceutical Sciences >A time-released osmotic pump fabricated by compression-coated method: Formulation screen, mechanism research and pharmacokinetic study
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A time-released osmotic pump fabricated by compression-coated method: Formulation screen, mechanism research and pharmacokinetic study

机译：压缩包衣法制造的延时渗透泵：制剂筛选，机理研究和药代动力学研究

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Abstract In this investigation, time-released monolithic osmotic pump (TMOP) tablets containing diltiazem hydrochloride (DIL) were prepared on the basis of osmotic pumping mechanism. The developed dosage forms were coated by Kollidon?SR-Polyethylene Glycol (PEG) mixtures via compression-coated technology instead of spray-coating method to form the outer membrane. For more efficient formulation screening, a three-factor five-level central composite design (CCD) was introduced to explore the optimal {TMOP} formulation during the experiments. The in?vitro tests showed that the optimized formulation of DIL-loaded {TMOP} had a lag time of 4?h and a following 20-h?drug release at an approximate zero-order rate. Moreover, the release mechanism was proven based on osmotic pressure and its profile could be well simulated by a dynamic equation. After oral administration by beagle dogs, the comparison of parameters with the {TMOP} tablets and reference preparations show no significant differences for Cmax (111.56?±?20.42, 128.38?±?29.46?ng/ml) and AUC0-48?h (1654.97?±?283.77, 1625.10?±?313.58?ng?h/ml) but show significant differences for Tmax (13.00?±?1.16, 4.00?±?0.82?h). These pharmacokinetic parameters were consistent with the dissolution tests that the {TMOP} tablets had turned out to prolong the lag time of {DIL} release.
机译：摘要在本研究中，根据渗透泵的作用原理，制备了含盐酸地尔硫卓（DIL）的缓释单片渗透泵（TMOP）片剂。研制的剂型通过Kollidon？SR-聚乙二醇（PEG）混合物通过压缩包衣技术而不是喷雾包衣方法进行包衣以形成外膜。为了更有效地进行配方筛选，引入了三因素五级中央复合设计（CCD），以探索实验过程中的最佳 {TMOP }配方。体外试验表明，装载DIL的 {TMOP }的优化配方具有约4？h的滞后时间和随后以约零级速率释放20小时的药物。此外，基于渗透压证明了释放机理，并且其分布可以通过动力学方程很好地模拟。比格犬口服给药后，与 {TMOP }片剂和参考制剂的参数比较显示，Cmax（111.56±±20.42，128.38±±29.46μng/ ml）和AUC0-48±Cmax无显着差异。 h（1654.97±±283.77，1625.10±±313.58±ng / h），但显示出Tmax的显着差异（13.00±±1.16，4.00±±0.82±h）。这些药代动力学参数与溶出度测试相符，溶出度测试证明 {TMOP }片剂可延长 {DIL }释放的滞后时间。

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