Dissolution Characteristics Of Berberine Hydrochloride Tablets Based On Drug Crystal Forms And Excipients

1 ObjectiveBerberine hydrochloride tablets are antibacterial drugs,effective for intestinal infections caused by Escherichia coli and dysentery bacillus,and are mainly used to treat intestinal infections and diarrhea.Berberine hydrochloride is soluble in hot water,slightly soluble in water or ethanol,extremely soluble in chloroform,and insoluble in ether.At present,there are very few reports on the crystal form of berberine hydrochloride at home and abroad.This study focuses on crystallography and excipients,pre-prescribing research,and multi-media dissolution of the formulation.Establish the sufficient research foundation for the key quality factors of the original drug development agent and the consistency evaluation of its generic drugs.2 MethodsFirstly,the high-performance liquid chromatography was used to investigate the dissolution differences of commercially available berberine hydrochloride tablets of the same specifications(0.1 g / tablet)in different dissolution media.Then polymorphic berberine hydrochloride powder was prepared by a single solvent recrystallization method,and qualitative analysis was performed on the polymorphic berberine hydrochloride powder by microscopy,thermal analysis,spectroscopy,X-ray diffraction,and the like.After that,the prescriptions of berberine hydrochloride tablets were analyzed,and the effects of the types and contents of the binders and disintegrants on the dissolution of berberine hydrochloride tablets were investigated,so as to screen out the optimal berberine hydrochloride tablets.Finally,polymorphic berberine hydrochloride powder was prepared with the optimal prescription,and the effect of the crystalline form on the dissolution behavior of berberine hydrochloride tablets in different dissolution media was investigated.3 ResultsIn the in vitro dissolution experiments of 11 different manufacturers of berberine hydrochloride tablets on the market.The results of berberine hydrochloride APIs fromdifferent manufacturers on the market showed that there were two crystal forms,berberine hydrochloride crystal form A and berberine hydrochloride crystal form B.By recrystallization,berberine hydrochloride crystal form I(needle crystal form),berberine hydrochloride crystal form II(column crystal form),berberine hydrochloride crystal form III(flaky crystal form),berberine hydrochloride were prepared There are 5berberine hydrochloride crystal forms: alkali crystal form IV(irregular bulk crystal form)and berberine hydrochloride crystal form V(narrow and long needle crystal form).In the screening and investigation of binders and disintegrants of berberine hydrochloride tablets,the results show that the types of binders and disintegrants have a significant effect on the dissolution of tablets.The binders dissolve with the increase of the prescription content.The more difficult,the effect of disintegrant content on dissolution is not obvious.Finally,the dissolution of polymorphic berberine hydrochloride tablets shows that the crystal form will affect the dissolution of the tablets in vitro.4 ConclusionThe main drug crystal form of berberine hydrochloride tablets,the types of excipients and the content of prescriptions all affect its dissolution behavior in vitro.In the production process of tablets,the selection and testing of raw materials,solvents,excipients and production processes should be formulated with corresponding standards,which will directly affect the clinical efficacy and application of drugs.