APPLICATION OF SOLID DISPERSION TECHNIQUE IN SOLUBILITY AND DISSOLUTION RATE ENHANCEMENT OF NATEGLINIDE

Prasanthi Boddu; Venkata Lakshmi Cherakapu; Uma Devi Ponukumati

doi:10.22159/ajpcr.2017.v10i11.14489

Authors

Prasanthi Boddu Department of Pharmaceutical Technology, Vignan Institute of Pharmaceutical Technology, Visakhapatnam - 530 049, Andhra Pradesh, India.
Venkata Lakshmi Cherakapu Department of Pharmaceutical Technology, Viswanadha institute of Pharmaceutical Sciences, Visakhapatnam - 530 017, Andhra Pradesh, India.
Uma Devi Ponukumati Department of Pharmaceutical Technology, Viswanadha institute of Pharmaceutical Sciences, Visakhapatnam - 530 017, Andhra Pradesh, India.

DOI:

https://doi.org/10.22159/ajpcr.2017.v10i11.14489

Keywords:

Controlled release, Diabetes mellitus, Dissolution, Meglitinides, Solid dispersion, Solubility

Abstract

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Â Objective: Nateglinide (NTG) is a potent short-acting biopharmaceutical classification system class II antidiabetic medication. The primary objective of the present investigation was to prepare and evaluate solid dispersions of NTG to enhance the component solubility and immediate release (IR) profile. The secondary objective was to formulate sustained release (SR) matrix layer of NTG for prolonging its effect in the body and to decrease oscillations in plasma concentration level.

Methods: NTG (270 mg) SR layer was formulated using release retardant polymers such as Carbopol, ethyl cellulose (EC), hydroxy EC, hydroxypropyl methylcellulose (HPMC), Kollidon, and locust bean gum at concentrations of 15% and 30%. IR layer of NTG (60 mg) was formulated using drug: Polymer inclusion complexes (1:1 and 1:2) of Î²-cyclodextrin (CD), HP Î²-CD, polyvinylpyrrolidone (PVP) K-15, and PVP K-30 by physical mixing and kneading methods (KMs).

Results: Among the all the carriers tested HP Î²-CD at 1:2 ratio prepared by KM (I3) gave highest enhancement of dissolution rate and dissolution efficiency with acceptable f1 (10.5) and f2 (51.0) values in comparison to marketed IR tablets (Starlix-60Â®). The SR formulation S12 was able to show a minimum amount of drug release (15%) within 1 hr comparatively, with a complete and sustained effect on drug release.

Conclusion: Thus, HPMC K-100M at a concentration of 30% in the SR layer in combination with HP Î²-CD (1:2) solid dispersions in the IR layer may be used in the design of oral controlled drug delivery system for NTG.

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Author Biographies

Prasanthi Boddu, Department of Pharmaceutical Technology, Vignan Institute of Pharmaceutical Technology, Visakhapatnam - 530 049, Andhra Pradesh, India.

Assistant Professor, Department of Pharmaceutics

Venkata Lakshmi Cherakapu, Department of Pharmaceutical Technology, Viswanadha institute of Pharmaceutical Sciences, Visakhapatnam - 530 017, Andhra Pradesh, India.

Department of Pharmaceutics

Uma Devi Ponukumati, Department of Pharmaceutical Technology, Viswanadha institute of Pharmaceutical Sciences, Visakhapatnam - 530 017, Andhra Pradesh, India.

principal, professor in pharmaceutics,

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