Sustained delivery of propranolol by using multiparticulate gastroretentive drug delivery system

R. Fursul, C. Patr, S. Kosalg, D. Pati, Prashant K. Deshmukh
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引用次数: 9

Abstract

PURPOSE: Gastroretentive systems can significantly prolong the gastric residence time of drugs. If a drug is stable in gastric acid, prolonged gastric retention improves bioavailability. The objective of the present investigation was to develop an extended and controlled release composition and formulation of propranolol using expandable, gelling, swellable hydrocolloid polymer along with mineral oil. METHODS: A formulation was prepared without using mineral oil by conventional ionotropic gelation method. All other formulations of oil entrapped floating gel beads of propranolol hydrochloride were prepared by using emulsion gelation method in which sodium alginate was used as a gelling agent and mineral oil was used to impart buoyancy to the formulation Spherical gel beads were formed instantaneously. The prepared beads were evaluated for diameter, surface morphology, encapsulation efficiency and drug release. RESULTS: Low concentration of oil containing formulation exhibited greater release of drug. As the concentration of oil increases, drug release decreases to certain extent. Percentage buoyancy of floating propranolol hydrochloride gel beads was found satisfactory. The highest mean diameter was observed in the formulation with 30% of mineral oil. The formulation with 35% of mineral oil had the highest drug loading and scanning electron microscopy revealed that the beads were spherical in shape with rough surfaces. CONCLUSION: Oil entrapped gel beads can be used as floating drug delivery system for extended drug release for both local and systemic drug delivery. Keywords: Floating drug delivery system; Emulsion gelation; Sodium alginate; Mineral oil; Propranolol hydrochloride.
多颗粒胃保留给药系统持续给药心得安
目的:胃保留系统能显著延长药物在胃中的停留时间。如果药物在胃酸中是稳定的,延长胃潴留时间可以提高生物利用度。本研究的目的是利用可膨胀、凝胶化、可膨胀的水胶体聚合物和矿物油开发一种缓释组合物和心得安的配方。方法:采用常规的离子化凝胶法制备不含矿物油的配方。以海藻酸钠为胶凝剂,矿物油为浮力,采用乳液凝胶法制备了盐酸心得洛尔的油包浮凝胶珠,可瞬间形成球形凝胶珠。对制备的微球直径、表面形貌、包封率和药物释放度进行了评价。结果:低浓度含油制剂释药效果明显。随着油浓度的增加,药物释放量有一定程度的降低。盐酸心得安漂浮凝胶珠浮力满意。在矿物油含量为30%的配方中,平均直径最大。矿物油含量为35%的配方载药量最高,扫描电镜显示微珠呈球形,表面粗糙。结论:油包膜凝胶珠可作为缓释药物的漂浮给药系统,既可用于局部给药,又可用于全身给药。关键词:漂浮给药系统;乳液凝胶;海藻酸钠;矿物油;盐酸普萘洛尔。
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