4.2 Article

Pharmacokinetics and hypoglycemic effect of gliclazide loaded in Isabgol husk mucilage microparticles

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JOURNAL OF PHARMACEUTICAL INVESTIGATION
卷 51, 期 2, 页码 159-171

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SPRINGERNATURE
DOI: 10.1007/s40005-020-00494-9

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Method validation; Diabetes; Microparticles

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The study found that the hypoglycemic effect and bioavailability of gliclazide loaded in Isabgol husk microparticles were better than pure gliclazide, suggesting the potential of microparticulate formulation as a novel anti-diabetic drug delivery system.
Purpose Among the several therapeutic agents available for the management of diabetes mellitus, sulfonylureas such as gliclazide have several advantages. The hypoglycemic effect and bioavailability of gliclazide loaded in Isabgol husk mucilage microparticles were assessed. The hypoglycemic effect of drug-loaded microparticles was compared with that of pure gliclazide. Methods Gliclazide was incorporated into Isabgol husk mucilage microparticles using an emulsification-crosslinking technique. Gliclazide characterization was performed using a chromatographic method. Results Gliclazide loading in the microparticles was up to 91.23 +/- 0.981% w/w. The pharmacokinetic parameters for pure gliclazide (control) were different from those of gliclazide loaded in microparticles (test). After oral administration, the AUC(0-24 h) of gliclazide in blood samples of the control and test groups was 10.840 +/- 0.018 and 17.608 +/- 0.035 mu g/(mL h), respectively. In 24 h after oral administration, the percentage reduction from the baseline glucose level in diabetic rabbits was 36.66 +/- 4.509% and 98.11 +/- 1.018% for the test and control groups, respectively. Conclusion The prolonged hypoglycemic effect and increased bioavailability of gliclazide loaded in Isabgol husk microparticles compared with those of pure drug indicate the applicability of the microparticulate formulation as a novel anti-diabetic drug delivery system.

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