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首页> 外文期刊>Pharmaceutical research >Novel gastroretentive dosage forms: evaluation of gastroretentivity and its effect on riboflavin absorption in dogs.
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Novel gastroretentive dosage forms: evaluation of gastroretentivity and its effect on riboflavin absorption in dogs.

机译：新型胃滞留剂型：胃滞留性及其对犬核黄素吸收的影响的评估。

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PUPOSE: The purpose of this study was to design novel gastroretentive dosage forms (GRDFs) based on unfolding multilayer polymeric films, to investigate the mechanism of their gastroretentivity in dogs, and to assess the effect of compounding a narrow absorption window drug in a GRDF on the drug's absorption properties. METHODS: Dosage forms (DFs) with different dimensions and mechanical properties were administered to beagle dogs with acidic buffer (pH = 1.5), whose gastric retention time (GRT) was then determined by X-ray pictures. Concurrent administration of radiopaque markers was used to assess the effect of the GRDF and/or acidic buffer on GRT. The absorption of riboflavin from a prototype GRDF was compared with a nongastroretentive controlled-release DF and to an oral solution of the drug. RESULTS: Large DFs (> or = 2.5 x 2.5 cm) containing rigid frame had prolonged GRT (>4 h). Administration of 400 mL of acidic buffer (or water) prolonged GRT whereas the GRDF did not cause additional prolongation. The extended absorption phase (>48 h) of riboflavin administered in a GRDF led to 4-fold increased bioavailability. CONCLUSION: The combination of large dimensions with rigidity produce gastroretentivity that can be used to improve absorption properties of a model of narrow absorption window drugs in the gastrointestinal tract.
机译：目的：本研究的目的是设计基于展开的多层聚合物薄膜的新型胃滞留剂型（GRDF），研究其在犬中的胃滞留性机制，并评估在GRDF中将窄吸收窗药物配混于动物体内的作用。药物的吸收特性。方法：给具有酸性缓冲液（pH = 1.5）的比格犬施用不同尺寸和机械性能的剂型（DFs），然后通过X射线照片确定其胃retention留时间（GRT）。同时使用不透射线的标记物来评估GRDF和/或酸性缓冲液对GRT的影响。将原型GRDF中的核黄素吸收与非胃滞性控释DF以及该药物的口服溶液进行了比较。结果：包含刚性框架的大型DF（>或= 2.5 x 2.5 cm）具有较长的GRT（> 4 h）。施用400 mL酸性缓冲液（或水）可延长GRT的时间，而GRDF不会引起额外的时间延长。在GRDF中施用的核黄素的吸收期延长（> 48小时），生物利用度提高了4倍。结论：大尺寸与刚度的结合产生了胃滞留性，可用于改善胃肠道中窄吸收窗药物模型的吸收性能。

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