The purpose of this research was to prepare and evaluate sustained release mucoadhesive tablets of Itraconazole. It is practically insoluble in aqueous fluids hence its solid dispersion with Eudragit E100 was prepared by spray drying. This was formulated in matrix of hydrophilic mucoadhesive polymers Carbopol 934P (CP) and Methocel K4M (HPMC). The formulation was optimized using a 32 factorial design. Amounts of CP and HPMC were taken as formulation variables for optimizing response variables i.e. mucoadhesion and dissolution parameters. The optimized mucoadhesive formulation was orally administered to albino rabbits, and blood samples collected were used to determine pharmacokinetic parameters. The solid dispersion markedly enhanced the dissolution rate of itraconazole. The bioadhesive strength of formulation was found to vary linearly with increasing amount of both polymers. Formulations exhibited drug release fitting Peppas model with value of n ranging from 0.61 to 1.18. Optimum combination of polymers was arrived at which provided adequate bioadhesive strength and fairly regulated release profile. The experimental and predicted results for optimum formulations were found to be in close agreement. The formulation showed Cmax 1898 ± 75.23 ng/ml, tmax of the formulation was 2 h and AUC was observed to be 28604.9 ng h/ml
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机译：这项研究的目的是制备和评估伊曲康唑的缓释粘膜粘附片剂。它实际上不溶于水性流体，因此可通过喷雾干燥制备与Eudragit E100的固体分散体。将其配制在亲水性粘膜粘附聚合物Carbopol 934P（CP）和Methocel K4M（HPMC）的基质中。使用32因子设计优化了配方。将CP和HPMC的量作为用于优化响应变量即粘膜粘附和溶解参数的制剂变量。将优化的粘膜粘附制剂口服给予白化病兔子，并使用收集的血样确定药代动力学参数。固体分散体显着提高了伊曲康唑的溶解速率。发现制剂的生物粘附强度随两种聚合物的量的增加线性变化。制剂显示出适合药物释放的Peppas模型，n值介于0.61至1.18之间。达到了最佳的聚合物组合，从而提供了足够的生物粘附强度和合理调节的释放特性。发现最佳配方的实验结果和预测结果非常吻合。制剂的Cmax为1898±75.23 ng / ml，制剂的tmax为2小时，AUC为28604.9 ng /毫升
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