Enhancement of Solubility and Dissolution Rate of Lopinavir by Solid Dispersion Technique.

Roop, Ravi Chand Digavalli (2012) Enhancement of Solubility and Dissolution Rate of Lopinavir by Solid Dispersion Technique. Masters thesis, Nandha College of Pharmacy, Erode.

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Abstract

This study is to improve the dissolution rate of Lopinavir by improving its solubility in dissolution medium by Solid Dispersion Technique. Poorly water soluble drugs require high doses in-order to reach therapeutic plasma levels after oral administration. Improvement in-extent and rate of dissolution is highly desirable for such compound as this can lead to an increased and more re-producible oral bioavailability and sub-sequent to clinical relevant dose reduction to more reliable therapy. Now-a-days, pharmaceutical techniques provide many approaches to enhance the dissolution rate of poorly water soluble drugs. Solid dispersion technique can be used to enhance the solubility dissolution rate and absorption of several insoluble drugs. Various hydrophilic carries like, PEG, PVP, HPMC, SLS, Gums have been investigated for improvement of dissolution characteristics, bio-availability for poorly aqueous soluble drugs. Lopinavir is an anti-retroviral drug of protease inhibitor. According to biopharmaceutical classification system (B.C.S)-II. It is a poorly water soluble drug, having bio-availability of less than 5% and high permeability so it was chosen as a model for this research work. In the present research work an attempt was made to develop solid dispersion Lopinavir by solvent evaporation method for improving the solubility and bioavailability of drug. From the experimental findings,Polyvinyl pyrrolidone is the better polymer than urea, SLS and Mannitol and is not producing any interaction with drug when compared with other formulations. The percentage drug content in all formulations was found in the range of 73.99 to 97.17 %. All the solid dispersion showing better saturation cumulative drug release compared to pure Lopinavir. The in-vitro drug release studies shows that all the formulation releasing maximum amount of drug within 60 min and formulation F5 showing maximum drug release. The optimum drug to polymer ratio was found to be in F5 (1:4), depending on in-vitro drug release studies. There is a significant increase in drug release with increase in drug to polymer ratio. The stability studies showed that the remaining drug content is within the limits at different temperature and humidity levels.

Item Type: Thesis (Masters)
Uncontrolled Keywords: Lopinavir; Solid Dispersion Technique; In-vitro drug release studies
Subjects: PHARMACY > Pharmaceutics
Depositing User: Ravindran C
Date Deposited: 18 Aug 2017 10:10
Last Modified: 18 Aug 2017 10:10
URI: http://repository-tnmgrmu.ac.in/id/eprint/2689

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