Bibliographic Details
Title: |
Gastroretentive Floating Microsponges of Mitiglinide: Design, Preparation, and Pharmacokinetic Evaluation. |
Authors: |
Patel, Meenakshi, Shelke, Santosh, Shaikh, Farhatjahan, Surti, Naazneen, Panzade, Prabhakar, Panjwani, Deepak |
Source: |
Journal of Pharmaceutical Innovation; Sep2023, Vol. 18 Issue 3, p1500-1514, 15p |
Abstract: |
Purpose: Gastroretentive floating microsponges are interesting because they remain buoyant for a long time and release the drug gradually to avoid fluctuations in plasma concentration. The present study involves the design, preparation, and pharmacokinetic evaluation of gastroretentive floating mitiglinide microsponges. Methods: The microsponges were prepared by a quasi-emulsion solvent diffusion method using ethyl cellulose and polyvinyl alcohol polymers and evaluated for morphology, product yield, bulk density, entrapment efficiency, in vitro buoyancy, and drug release. Besides, the optimised formulation was subjected to a stability study and pharmacodynamic and pharmacokinetic evaluation in rabbits. Results: Results displayed that microsponges possessed high production yield, entrapment efficiency, and particle size of 250.42–361.53 μm, and they remained buoyant over 0.1 N HCl for 12 h. The optimised formulation exhibited 94.75 ± 0.09% drug release after 12 h. The developed microsponges were spherical, porous, and spongy. Moreover, no significant change was observed in the drug content or drug release pattern after storage for 6 months. In vivo X-ray imaging study in rabbits indicated microsponges can remain floating for 12 h in the stomach. The pharmacodynamic study revealed that optimized microsponge formulation was very efficient in controlling the body glucose level as compared to pure drug. The residence time of microsponges was greater (8.847 ± 1.62 h) than that of pure mitiglinide (4.29 ± 1.03 h). The AUC0—∞ of the optimised formulation was significantly greater (13.824 ± 1.48 μg/mL h) than pure drug (8.167 ± 1.73 μg/mL h). Conclusion: The developed mitiglinide microsponges can prolong the drug's action and circumvent frequent dosing in diabetic patients to enhance patient compliance. [ABSTRACT FROM AUTHOR] |
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Database: |
Complementary Index |