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生物黏附型酮洛芬液体栓剂的性质:制备、胶凝温度测定、黏度研究以及使用 4×4 析因设计的质构仪评估机械性能。

Properties of bioadhesive ketoprofen liquid suppositories: preparation, determination of gelation temperature, viscosity studies and evaluation of mechanical properties using texture analyzer by 4 × 4 factorial design.

机构信息

Faculty of Pharmacy, Department of Pharmaceutical Technology, Ege University, Bornova, İzmir , Turkey.

出版信息

Pharm Dev Technol. 2014 Dec;19(8):968-75. doi: 10.3109/10837450.2013.846373. Epub 2013 Oct 24.

DOI:10.3109/10837450.2013.846373
PMID:24156540
Abstract

CONTEXT

Development and evaluation of thermosensitive and bioadhesive liquid suppositories containing ketoprofen (KP).

OBJECTIVE

This study was conducted to develope thermosensitive and bioadhesive liquid suppositories containing KP using poloxamer and different bioadhesive polymers and to investigate their gelation temperature, viscosity and mechanical properties.

MATERIALS AND METHODS

Bioadhesive liquid suppositories were prepared by the cold method using poloxamer 407 (P 407), Poloxamer 188 (P 188) and various amounts of different bioadhesive polymers. Their gelation temperatures, viscosity values and mechanical properties were determined using texture analyzer by 4 × 4 factorial design.

RESULTS

It was seen that in presence of KP, gelation temperature of formulation P 407/P 188 (4/20%) significantly decreased from 64 to 37.1 °C. It is to be noted that addition of increasing concentrations of bioadhesive polymers lowered gelation temperature and its decrease was highest with addition of Carbopol 934 P (C). Results of texture profile analysis (TPA) showed that formulations containing C have significantly higher hardness and adhesiveness values than other bioadhesive formulations. According to TPA, gel structure of liquid suppository formulation F5, containing P 407/P 188/KP/C (4/20/2.5/0.8%), exhibited the greatest hardness, compressibilty, adhesiveness and besides greatest viscosity.

DISCUSSION AND CONCLUSION

According to mechanical properties and viscosity values, it was concluded that F5 could be a promising formulation.

摘要

背景

开发并评价含有酮洛芬的温敏型生物黏附性液体栓剂。

目的

本研究旨在采用泊洛沙姆和不同的生物黏附性聚合物开发含有酮洛芬的温敏型生物黏附性液体栓剂,并考察其胶凝温度、黏度和力学性能。

材料和方法

采用冷法制备生物黏附性液体栓剂,使用泊洛沙姆 407(P407)、泊洛沙姆 188(P188)和不同用量的多种生物黏附性聚合物。采用质构仪通过 4×4 析因设计考察其胶凝温度、黏度值和力学性能。

结果

结果显示,在含有酮洛芬的情况下,处方 P407/P188(4/20%)的胶凝温度从 64℃显著降低至 37.1℃。值得注意的是,随着生物黏附性聚合物浓度的增加,胶凝温度降低,其中添加 Carbopol 934 P(C)时降低幅度最大。质构分析(TPA)结果表明,含有 C 的制剂的硬度和黏附性显著高于其他生物黏附性制剂。根据 TPA,含有 P407/P188/KP/C(4/20/2.5/0.8%)的液体栓剂制剂 F5 的凝胶结构具有最大的硬度、可压缩性、黏附性和最大的黏度。

讨论与结论

根据力学性能和黏度值,认为 F5 可能是一种有前途的制剂。

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