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http://dx.doi.org/10.5762/KAIS.2017.18.1.506

Immediate Drug Release Enhancement of Nateglinide Using Fumaric Acid  

Lee, Sung-Hoon (Department of pharmaceutical Engineering, Cheongju University)
Publication Information
Journal of the Korea Academia-Industrial cooperation Society / v.18, no.1, 2017 , pp. 506-512 More about this Journal
Abstract
The purpose of this study was to improve release rate and bioavailability of nateglinide formulation. Polymorphism selection and particle size control were performed to enhance formulation dissolution rate, and a pH modifier was included in the formulation to overcome pH-dependent solubility of nateglinide. The enhanced dissolution rate was characterized by using a dissolution test. The results showed that H-type raw material had a higher dissolution rate than that of B-type raw material. There was 6.2% difference in dissolution between the two materials at 60 min. With regard to particle size, raw material with a $1.13{\mu}m$ particle size showed a 20% faster release rate than that of raw material with a $2.28{\mu}m$ particle size. Furthermore, fumaric acid was included in formulation as a pH modifier. That addition produced a greater than 50% improvement in dissolution rate. In conclusion, dissolution rate of nateglinide can be enhanced by optimizing its polymorphism and particle size; moreover, a synergistic effect on the enhancement of dissolution rate is obtained by including fumaric acid, a pH modifier, in the formulation.
Keywords
Nateglinide; Immediate release formulation; Fumaric acid; Organic acid;
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