Preparation and Quality Evaluation of Berberine Hydrochloride Resin Complex Lyophilized Oral Disinte-gration Tablets
OBJECTIVE To prepare berberinehydrochloride resincomplex for good taste-masking effectof lyophilized oraldisintegra-tion tablets using berberine hydrochloride as a model drug and using Kyron-T114 as the drug-loaded resin.METHODS The drug-resin composites were prepared by using the static method.Then drawn the adsorption isotherm and adsorption kinetic curves to study the adsorption mechanism of the resin.Afterwards,the characteristic of the berberine hydrochloride resin complex was studied by using the SEM,DSC,XRD and FTIR.Finally,prepared the oral disintegration tablets of berberine hydrochloride and its resin complex by using the lyophilized extrusion technology.Next,studied the in vitro release experiments and evaluated the effect of masking taste.RESULTS According to the research,a berberine hydrochloride-resin complex with the drug loaded of 43.04％was prepared.And the analysis showed that the adsorption of the drug on the resin was the multilayered chemical adsorption.The dissolution of berberine hydro-chloride's powder is mainly affected by the solubility of berberine hydrochloride.Moreover,the dissolution mechanism is mainly based on Fick diffusion.The dissolution of berberine hydrochloride's powder is mainly affected by the pH of the solution,along with the concentra-tion and the type of the ion in the solution.In artificial gastric juice,the drug dissociates rapidly from the resin.So the film diffusion was the rate-limiting step for dissolution.On the contrary,the drug dissociated slowly in the water,artificial saliva,artificial intestinal fluids including pH 4.5 and pH 6.8.So the particle diffusion was the rate-limiting step for dissolution.Besides,the dissolution of lyophilized oral disintegration tablets of drug-resin complexes in artificial saliva was significantly lower than that of berberine hydrochloride oral disin-tegration tablets.Lastly,the results from sensory evaluation and electronic tongue detection proved that the lyophilized oral disintegration tablets of berberine hydrochloride-resin compound has good taste masking effect.CONCLUSION Berberine hydrochloride resin com-plex lyophilized mouth collapse has good taste masking effect.Moreover,the drug-resin complex prepared by Kyron-T114,a weak cation exchange resin,is beneficial to improve the dissolution of poorly soluble drugs in artificial gastric juice,thereby improving their oral bio-availability.Thus,it can provide a new idea for the taste masking of traditional Chinese medicine.
berberine hydrochlorideion exchange resinKyron-T114effect of masking tastedrug-resin complex
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