克拉霉素漂浮片的体外、体内评价。

Manojkumar Patil, A. Mali, S. Mali
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摘要

本研究的主要目的是利用亲水性聚合物羟丙基甲基纤维素和气体发生剂碳酸氢钠和柠檬酸,设计克拉霉素漂浮片口服漂浮给药系统并进行工艺优化。采用32随机全因子设计进行研究。本设计评估了2个因素,每个因素在3个水平上进行评估,并对所有9种可能的组合进行了实验试验。选取自变量和因变量进行优化研究。在优化的配方中加入硫酸钡制备放射性标记浮片,用于体内放射学研究。多元回归分析结果表明,因子X1和X2对相关参数均有显著影响。以浮力和体外释药为指标对该制剂进行优化。由此可见,随着服药时间的延长,肿胀指数也随之增加,这是由于服药后体重的增加与补水速率成正比。采用x射线成像技术对优化后的配方进行了白化兔体内x线成像研究。体内x线成像和x线片研究清楚地表明,制备的优化浮片在家兔胃中保留时间较长,具有良好的体内性能。放射学证据表明,配制的抗生素漂浮片在家兔胃中漂浮良好,漂浮时间超过6 h。
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In-Vitro, In-Vivo Evaluation of Floating Tablets of Clarithromycin.
The main purpose of this research work was to design and process optimization of oral floating drug delivery system of Clarithromycin floating tablets by using the hydrophilic polymer Hydroxylpropyl methyl cellulose and gas generating agent sodium bicarbonate and citric acid. A 32 randomized full factorial design was used to study. In this design 2 factors were evaluated, each at 3 levels and experimental trials were performed at all 9 possible combinations. The independent and dependent variables are selected for optimization study. The radio-labelled floating tablets were prepared by adding barium sulphate in the optimized formulations for in- vivo radiographic study. The Results of multiple regression analysis indicated that both factors X1 and X2 significantly affected on the dependent parameters. The formulation was optimized on the basis of floating ability and in-vitro drug release. It should be concluded that as the time increases, the swelling index was increased, because weight gain by tablet was increased proportionally with rate of hydration. In-vivo radiographic studies of the optimized formulations were performed using New Zeal Albino rabbits by X-ray imaging technique. The in-vivo X-ray imaging and radiographic studies clearly indicated that the prepared optimized floating tablets were retained in the rabbit stomach over a prolonged period of time and had good in-vivo performance. Radiological evidences suggest that the formulated floating tablets of antibiotics were well floated more than 6 h in rabbit stomach.
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