新型聚合物共混法制备克拉霉素保胃片的配方及评价

Sharwaree Hardikar , Ashok Bhosale
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引用次数: 9

摘要

克拉霉素是一种半合成的大环内酯类抗生素,被证明是治疗幽门螺杆菌感染非常有效的单一疗法。据报道,部分根除幽门螺杆菌感染的各种原因之一是抗菌药物在胃中的停留时间短。因此,本研究的主要目的是设计和研制克拉霉素浮胀胃留置片,使克拉霉素在胃中缓释。本研究将HPMC k100lv与从罗勒种子中分离的凝胶混合,以克服前者随时间侵蚀的缺点。研究了这种新型聚合物共混物,并将其作为制备克拉霉素胃留置片的基质材料。设想了凝胶组分葡甘露聚糖与HPMC K100LV之间的氢键,并通过ATR-FTIR进一步证实。凝胶与HPMC K100LV聚合物共混制备的克拉霉素片剂表现出快速肿胀,几乎瞬间浮力,随后药物从肿胀的浮动剂型中释放时间延长。通过γ闪烁图证实了优化后的克拉霉素片剂在胃中的保留率。
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Formulation and evaluation of gastro retentive tablets of clarithromycin prepared by using novel polymer blend

Clarithromycin is a semi synthetic macrolide antibiotic that is proved to be extremely effective mono therapy in treating H. pylori infection. One of the various reasons reported for partial eradication of H. pylori infection is that the short dwelling time of antimicrobial agents in the stomach. Hence the principal object of the present work was to design and develop floating and swellable gastro retentive tablet of clarithromycin to obtain its prolonged release in the stomach. HPMC K 100LV was blended in the present study with the Gel isolated from the seeds of Ocimum basilicum to overcome the drawback of time dependent erosion of former. This novel polymer blend was investigated and exploited as a matrix material for the development of gastro retentive tablets of clarithromycin as drug delivery system. Hydrogen bonding between the Glucomannan – a component of the Gel and HPMC K100LV was envisaged and further confirmed by ATR-FTIR. Tablets of clarithromycin prepared by using the polymer blend of Gel and HPMC K100LV exhibited fast swelling with almost instantaneous buoyancy followed by prolonged release of drug from the swollen, floating dosage form. The retention of the optimized tablet formulation of clarithromycin in the stomach was confirmed by γ scintigraphy.

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