Open AccessPreparation and characterization of rilpivirine solid dispersions with the application of enhanced solubility and dissolution rate
Author(s) -
Pavan Kommavarapu,
Arthanareeswari Maruthapillai,
P. Kamaraj,
Manasvi Sunkara
Publication year - 2015
Publication title -
beni-seuf university journal of basic and applied sciences /beni-suef university journal of basic and applied sciences
Language(s) - English
Resource type - Journals
eISSN - 2314-8543
pISSN - 2314-8535
DOI - 10.1016/j.bjbas.2015.02.010
Subject(s) - solubility , dissolution , bioavailability , differential scanning calorimetry , rilpivirine , chemistry , nuclear chemistry , fourier transform infrared spectroscopy , dissolution testing , chromatography , materials science , chemical engineering , organic chemistry , biopharmaceutics classification system , pharmacology , medicine , family medicine , human immunodeficiency virus (hiv) , antiretroviral therapy , viral load , engineering , physics , thermodynamics
Rilpivirine (RPV) is a pharmaceutical drug used for the treatment of HIV infection. The drug is characterized with poor aqueous solubility and dissolution rate leading to low bioavailability of the drug. Hence, there is a need for the improvement of the solubility and dissolution of such drugs. In this exertion, enhancement of the solubility and dissolution of the practically water insoluble drug rilpivirine was achieved by solid dispersion (SD) preparation using solvent evaporation method which eventually leads to bioavailability enhancement. SD's were formed using Kollidon VA 64 which is a water-soluble copolymer and varying copolymer ratio to Avicel PH-101, Gelucire 50/13 and lecithin soya. Solubility studies were carried out to establish the solubility-enhancing property of the SD's. To support solubility analysis results, powder dissolution studies were carried out. The SD's were characterized by Fourier transform infrared spectroscopy, differential scanning calorimetry, X-ray powder diffraction studies, scanning electron microscopy. It was found that the SD's formed showed the absence of crystalline nature of the drug and its conversion to amorphous state. The solubility and dissolution of the rilpivirine SD's were enhanced. There is a 14.9 fold increase in solubility for Drug: Kollidan VA 64: Gelucire 50/13 (1:4:1). For Drug: Kollidan VA 64 (1:5), Drug: Kollidan VA 64: Lecithin soya (1:4:1) and Drug: Kollidan VA 64: Avicel PH-101 (1:4:1) it was 5.9, 5.4 and 4.2 respectively. In-vitro drug release kinetics was investigated. This study demonstrates the use of solvent evaporation method for the preparation of SD’S in solubility and dissolution enhancement