The study on the development of self-emulsifying compositions with simvastatin

Abstract

Self-emulsifying compositions are the basis of oral drug delivery systems used to improve the solubility and increase the bioavailability of active pharmaceutical ingredients that are poorly soluble in the aqueous medium of gastric juice. Aim. To develop self-emulsifying compositions using simvastatin as an active pharmaceutical ingredient. Materials and methods. During the development of the composition of the self-emulsifying mixture, excipients, such as solvents, co-solvents, surfactants and co-surfactants, allowed in pharmaceutical production were used. The studies of solubility, the formation rate of emulsions of the self-emulsifying composition and stability were carried out by generally accepted methods according to the methods of the SPhU and other valid normative documents. Results and discussion. The studies of the solubility of simvastatin allowed choosing a mixture of castor oil and PEG-40 GRO as a solvent, which improved the solubility of the substance in oil. It was determined that it was efficient to use Tween-80 as the main surfactant. Glycerol monostearate, distilled monoglycerides, polyethylene oxide-400, polyethylene oxide-1500 and polyethylene glycol-100 stearate were introduced into the composition as co-surfactants. It was found that the compositions, which included polyethylene oxide-400 and polyethylene oxide-1500, had significantly worse indicators of the formation rate of emulsions than the rest of the samples. The sample containing distilled monoglycerides did not withstand a decrease in the pH value of the medium. Conclusions. According to the results obtained, samples containing castor oil, PEG-40 hydrogenated castor oil, Tween-80, glycerol monostearate or PEG-100 stearate were selected for further research.