新型聚合物在浮式原位胶凝体系开发中的评价

Ghare Jl, Mundada As
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引用次数: 2

摘要

本研究的目的是评价从天然来源向日葵(Helianthus annuus)中获得的新聚合物在盐酸雷尼替丁漂浮原位凝胶形成中的作用。利用低甲氧基果胶(LMP)、碳酸钙、柠檬酸钠、d -甘露醇、对羟基苯甲酸甲酯和对羟基苯甲酸丙酯制备漂浮原位胶凝配方。对所开发的配方进行了各种物理化学性质的评估,如粘度、漂浮滞后时间、漂浮持续时间、体外凝胶和体外药物释放。采用32全因子设计,以LMP浓度和碳酸钙浓度为自变量,以漂浮滞后时间和8 h后药物释放量(Q8)为因变量。所有配方(F1-F9)均在60秒内出现漂浮,并保持漂浮约24小时。所有配方在与胃液接触前均可浇注。结果表明,LMP和碳酸钙的浓度对药物的漂浮滞后时间和累积释药百分比有影响。配方F5在制备的原位凝胶中具有最佳的漂浮滞后时间(37 s)和8 h释药率(98.09%)。因此,盐酸雷尼替丁可以用LMP作为胶凝聚合物制成漂浮原位凝胶,使药物释放持续8小时。
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Evaluation of Novel Polymer in the Development of Floating In situ GellingSystem
The objective of this work was to assess the new polymer obtained from natural source (Helianthus annuus) in the formation of floating in situ gel of Ranitidine HCl. Low Methoxy Pectin (LMP), calcium carbonate, sodium citrate, D-mannitol, methylparaben and propylparaben were utilized in developing floating in situ gelling formulations. The developed formulations were evaluated for various physicochemical properties like viscosity, floating lag time, and duration of floating, in vitro gelation and in vitro drug release. The 32 full factorial design was applied wherein concentration of LMP and calcium carbonate were considered as independent variables whereas floating lag time and drug release after 8 h (Q8 ) were taken as dependent variables. All formulations (F1–F9) exhibited floating within 60 s and remained floated for around 24 h. All the formulations were pourable before coming in contact with gastric fluid. It was seen that floating lag time and cumulative percentage drug release was influenced by concentration of LMP and calcium carbonate. Formulation F5 showed optimum floating lag time (37 s) and drug release after 8 h (98.09%) amongst developed in situ gels. Thus it can be concluded that Ranitidine HCl can be formulated as floating in situ gel using LMP as a gelling polymer to sustain the drug release for 8 h.
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