Preparation And In Vitro Evaluation Of Berberine Hydrochloride Loaded Intestines Difftuence Microcapsules

Berberine hydrochloride was used to cure intestinal diseases. Bitterness and side effect of gastrointestinal tract may affect clinic application of Berberine hydrochloride. In this paper, Berberine hydrochloride loaded intestines difftuence microcapsules were prepared. It was expected to releasing drug in small intestine and large intestine and decreasing the side effect of gastrointestinal tract. In addition, it can cover bitterness and improve patient compliance. The main results are as follows:(1)Berberine hydrochloride loaded intestines difftuence microcapsules were prepared by solvent evaporation method. Single factor and L 9(34) orthogonal experiments were designed. The optimum prescription and preparation technics was selected.The optimum prescription is as follows: Eudragit L100 0.30 g, antiseize compound 0.03 g, mixing solvent 6.0 mL (methanol/acetone=1:5), liquid paraffin 75.0 mL, span80 0.40 g. berberine hydrochloride 0.05 g. The optimum preparation technics is as follows: Stirring speed 300 rpm. The temperature 35℃. The emulsification time 20 min.(2)Quality research work of microcapsules has been initially done. The amount of drug in Berberine hydrochloride loaded intestines difftuence microcapsules by UV method was determined. The method of determining the amount of drug was studied. The drug loading and encapsulation efficiency of Berberine hydrochloride loaded intestines difftuence microcapsules were determined. The drug loading of microcapsules is 11.18%. The encapsulation efficiency of microcapsules is 85.00%. And the factors of affecting their property were reviewed. The shape of microcapsules was observed by optical microscope. The particle size distribution of microcapsules is between 150-450μm. The bulk density of microcapsules is 387.57 mg/mL. The truce corner of microcapsules is 18.43°.(3)In vitro drug release behavior of microcapsules was determined conforming to the method in Chinese pharmacopoeia in artificial gastric juice(pH=1.0)and artificial intestinal juice (pH=6.4,6.8,7.4). The release of drug was initially investigated. The release degree of microcapsules was more than 70% in 120 min at pH 6.8 and 7.4. The release degree of microcapsules was less than 10% in 120 min at pH 1.0. It accords with the standard of pharmacopoeia.In addition, the microcapsules can cover the bitterness of drug and improve patient compliance. The research provide experimental base for new intestines difftuence drug delivery system.