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Tropical Journal of Pharmaceutical Research
Pharmacotherapy Group, Faculty of Pharmacy, University of Benin, Benin City, Nigeria
ISSN: 1596-5996
EISSN: 1596-9827
Vol. 15, No. 6, 2016, pp. 1123-1128
Bioline Code: pr16150
Full paper language: English
Document type: Research Article
Document available free of charge

Tropical Journal of Pharmaceutical Research, Vol. 15, No. 6, 2016, pp. 1123-1128

 en Dissolution rate enhancement of repaglinide by solid dispersion
Yang, Xiao-Dong; Li, Wan-Sen; Tian, Yan-Juan; Liu, Cheng-Gong; Gao, Da-Hong & Ma, Hai-Li

Abstract

Purpose: To enhance the solubility and dissolution rate of the antidiabetic drug repaglinide by solid dispersion (SD) technique
Method: The solid dispersion of repaglinide was prepared by solvent evaporation method using the hydrophilic carrier, polyethylene glycol 4000 (PEG 4000) in three drug:PEG 4000 ratios (1:1, 1:3, 1:5). For comparison, physical mixtures of repaglinide and PEG 4000 in the same ratios were also prepared. The formulations were characterized by Fourier transformed infrared spectroscopy (FTIR), x-ray diffractometry (XRD) and differential scanning colorimetry (DSC). Phase solubility study of pure repaglinide, physical mixture and solid dispersion was performed in distilled water. Dissolution studies were carried out in pH 7.4 phosphate buffer.
Results: DSC and XRD results indicate that repaglinide exists in amorphous form in solid dispersion. FT-IR analysis demonstrated the presence of intermolecular hydrogen bonding between repaglinide and PEG 4000 in the solid dispersion. The solubility of pure repaglinide was enhanced from 22.5± 5.0 to 235.5± 5.0 µg/mL in distilled water at 37 0C. Rapid burst release (80 - 86 %) from the solid dispersion formulations was observed within 15 min.
Conclusion: The solubility and dissolution rate of repaglinide are enhanced by formulating SDs of repaglinide with PEG 4000. This will likely lead to increase in bioavailability which would be beneficial for better glucose control in diabetic patients.

Keywords
Diabetes; Solid dispersion; Repaglinide; Solubility; Dissolution; Burst release

 
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