FORMULATION AND EVALUATION OF FLOATING-MUCOADHESIVE MICROSPHERES OF NOVEL NATURAL POLYSACCHARIDE FOR SITE SPECIFIC DELIVERY OF RANITIDINE HYDROCHLORIDE
FORMULATION AND EVALUATION OF FLOATING-MUCOADHESIVE MICROSPHERES OF NOVEL NATURAL POLYSACCHARIDE FOR SITE SPECIFIC DELIVERY OF RANITIDINE HYDROCHLORIDE
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用于盐酸雷尼替丁定点递送的新型天然多糖浮动粘膜粘附微球的配制和评价
DOI：
10.22159/ijap.2017v9i3.16137
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发表时间：
2017
期刊：
影响因子：
--
通讯作者：
S. Saraf
中科院分区：
文献类型：
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作者：
V. K. Sahu;N. Sharma;P. Sahu;S. Saraf
目的：盐酸雷尼替丁（RH）的肠道定位有利于提高药物的生物利用度。本工作描述了一种新型植物多糖漂浮微球的制备方法，用于药物胃内给药。方法：从植物罗望子种子中提取多糖。提取的多糖进行了评价的一些理化参数。以提取多糖为粘膜粘附赋形剂，丙烯酸树脂为控释聚合物，采用乳液交联法制备漂浮-粘膜粘附微球。用环氧氯丙烷进行化学交联。采用傅立叶变换红外光谱（FT-IR）对制备的微球进行了药物-聚合物相容性研究。进行了进一步表征，例如尺寸、表面性质、溶胀指数、包封百分比、体外浮力和药物释放。结果：FT-IR研究证实了提取多糖的化学交联，以及微球加工过程中药物的稳定性。微球的尺寸在5.38至7.84 μm的范围内。SEM图像显示所有批次的尺寸均为球形，表面光滑。溶胀指数在158- 257%范围内显示出更好的溶胀。降低多糖的浓度会降低包封率。体外浮力研究表明，配方F1显示出比其他配方更好的漂浮能力。体外释药实验表明，所制备的微球在8-12 h内释药100%，具有缓释特性。结论：TI多糖可作为制备漂浮粘附微球的辅料。
Objective: Localization of ranitidine hydrochloride (RH) into the upper part of the intestinal tract is beneficial for better drug bioavailability. Present work described the method of preparation of novel plant polysaccharide based floating microspheres for delivery of the drug into the stomach. Methods: Polysaccharide was extracted from the seeds of plant Tamarindus indica (TI). Extracted polysaccharide was evaluated for some physicochemical parameters. Floating-mucoadhesive microspheres were prepared by using extracted polysaccharide as mucoadhesive excipients while eudragit as a release controlling polymers by using emulsion crosslinking method. Chemical crosslinking was done by using epichlorohydrin. Prepared microspheres were evaluated for their drug-polymer compatibility study by using fourier transform infrared spectroscopy ( FT-IR) . Further characterization such as size, surface properties, swelling index, percentage encapsulation, in vitro buoyancy and drug release was performed. Results: FT-IR study confirms the chemical crosslinking of extracted polysaccharide and also drug stability during processing of microspheres. The size of microspheres was in the range of 5.38 to 7.84 µm. SEM images revealed that all batches were of spherical in size and smooth surface. The swelling index showed better swelling in the range of 158-257 percentages. Encapsulation efficiency was found to be decreased by decreasing the concentration of polysaccharide. In vitro buoyancy study possesses that formulation F1 showed better floating ability as compared to the others. Finally, in vitro drug release study revealed that prepared microspheres were able to release the 100% drug within 8-12 h, indicating sustain release behavior. Conclusion: Present study concludes that polysaccharide of TI may be used as excipients for the preparation of floating-mucoadhesive microspheres.