Research On Masking The Bitterness Of Berberine Hydrochloride And Sanhuang Tablets By The Powder Modification Technology

The taste of drugs is an important factor affecting patient medication compliance,so it,s a significant issue for pharmaceutical researchers to study masking bitter taste of Chinese materia medica.In this paper,by taking two typical Chinese medicine,Berb-berine hydrochloride and Sanhuang Tablets as the research objects,powder modification technology used as the technology,the masking bitterness of them are studied.The composite particles are prepared by mechanical crushing methods and characterized by pharmaceutical and micromeritic properties using for materials science methods,which the composite particles would be characterized and evaluated;At the same time,we would illustrate the process principles of powder modification technology in masking the bitterness of solid preparations.The dissertation is summari zed as follows:To study the properties of the powder and feeding status of drugs and modifiers,the crushing rule and characterization of Berberine hydrochloride and modifiers are researched.Their micromeritic properties are evaluated systematialiy from crushing rule,DSC to flowability,density.Their individual characteristics are acquired.The effect of masking bitterness is selected to be the evaluation index,composite for time,modifiers species and dosages are studied.The results suggest that when the proportion of drug and modifier is 6:4 and composite for 2 min,the bitterness of Berberine hydrochloride can be improved preferably.By the complex process validation test,some microetric properties such as contact angle,DSC,IR and SEM,are compared for the extracts and modified powder.The results reveal that the powder properties and particle surface functional groups of composite particles have good similarity with those of modifier.The test results of SEM,IR,DSC etc.demonstrate that the intermolecular forces and mechanical bite force maybe the important factor in the powder modification technology structure forming.The original drug and artificial mixing powers used as control group,the taste masking and chemical evaluation are used by evaluating the effect of bitter taste masking.The results show that the composite’s effect of bitter taste masking is superior to the powder of physical mixing and original powder obviously.Based on the masking bitterness of Berberine hydrochloride,compound preparation the prescription of Sanhuang Tablets is selected as the second research object.The size distribution,powder properties are selected to be the evaluation index,the grinding regularity of Rhubarb,Rhubarb extract and Scutellaria extract are studied.The study demonstrates that the property of smash of Rhubarb extract and Scutellaria extract are favorable.The result reveals during the modified powder process,the two kinds of extracts can be considered as shell particles.According to the purpose of research,we analyze the bitterness of drugs in the prescription of Sanhuang Tablets,selecting Mannitol as the modifier of bitterness masking.To verify the rationality of Sanhuang-Tablets composite particles coated process by the evaluation of powder and pharmacy science,the result showes that it is more feasible to make the composite particles,which is the Mannitol with the drugs of Sanhuang-Tablets added in one time.The optimization tests for recombination technology demonstrates that the optium conditions are as follows:the proportion of drug and excipient being 6.5:3.5 and composite for 2 min.The complex processvalidation test showes that the coating time of Mannitol-Sanhuang Tablets intermediate powder is screened,the bitterness of 2-min composite particles is the lightest;Drugs,Mannitol,corresponding particle composite intermediate and mixture are characterized from contact angle,microstructure,IR spectra,and elemental compositon.The test results of the powder properties,particle surface functional groups,elemental compositon,SEM and crystalline structure of composite particles have good similarity with Mannitol.The study infers that the surface of Sanhuang Tablets is covered by Mannitol,therefore it presents some properties of mannitol.Choosing the dissolution of Berberine hydrochloride in Sanhuang Tablets as the index,compared the composite powder with the powders of simple physical mixing,the study showes that the composite powder prepared by powder modification technology are superior to the mixing obviously.The study shows that the Powder modification technology can be used to mask the bitter formulation and improve the compliance.Therefore,this paper select Berberine hydrochloride and Sanhuang Tablets as modeles,the feasibility of powder modification technology used to relieve drug bitterness is explor-ed.The full text provides new research ideas and technical direction for masking bitterness of solid preparations.