| Objective:To establish a scientific and reasonable method for determination of content and dissolution,and the optimal preparation technology and process parameters were selected to improve the solubility of anhydroicaritin to improve bioavailabilityMethods:(1)In the pre study,the physical and chemical properties and the properties of the powder were examinedaccording to the 2015 Chinese Pharmacopoeia.(2)In the Study on solubilization of icariin,Firstly,inclusion technique and solid dispersion technology of two kinds of input means solubilization screening,results showed that solid dispersion solubilizing effect is more significant.The single factor investigation was used for studying the effect of carrier material,preparation method,preparation temperature,proportion of drug carrier,stirring time,dosage of solvent,dissolving speed to the dissolution.Single factor test had been done and the orthogonal design was adopted to obtain the optimized prescription.(3)Then combine the solubility curve and thermodynamic parameters to analysis of dispersion reaction types and solid dispersion reaction mechanism,which corroborate the stability and accuracy of the optimal process.Finally,using IR,DSC and PXRD on solid dispersion were characterized.(4)After the solid dispersion was prepared,the capsule was selected as the final dosage form Firstly,the properties of the solid dispersions were investigated.(5)In this paper,the quality and stability of the solid dispersion capsules were studied.When the quality research results were as follows.Then,in order to check the influence factors test and accelerated testResult:(1)The results show that Anhydroicaritin's melting point is 254.0~254.7 ?,Anhydroicaritin's equilibrium in water and phosphate buffer with different p H were all below the detection limit,Even if the addition of the surfactant has little effect on the improvement.But,SD can significantly improve the solubility it can basically satisfy the condition of leakage in the 0.2% Twain p H6.8 PBS.According to the study of the physical and chemical properties of icariin,the analytical method for the determination of the content and dissolution was established.(2)Finally,the best solution of solid dispersion was prepared by melt-solvent method,using P188 as the carrier material,the proportion of the drug carrier was 1:4,the preparation temperature was 55,the stirring time was min,the solvent dosage was 40 m L.(3)The ?rH??rS and ?rG were less than 0,indicating the formation process of icariin solid dispersions was an exothermic process.The results of DSC mapping cannot distinguish that soliddispersion,But,IR and PXRD spectra of solid dispersions showed a physical mixture of icariin and P188 and their difference was significant.(4)The results showed that the solid dispersion had the effect of solubilization,but also increased the hygroscopicity and reduced the fluidity,It needs to be added to the appropriate accessories to improve.Finally,it was determined that the flux was silica gel with a dosage of 2%.(5)results showed that icariin in high temperature,high humidity and light conditions related substances increased,but still within the allowable range,and within six months of preparation of aluminum bag in abnormal test condition indicators can meet the requirements.Conclusion:Research shows that Anhydroicaritin has a good application prospect.But the study found that anhydroicaritin has poor water solubility,the water solubility is less than 1?g/m L.Due to the poor oral absorption,the apparent permeability coefficient in each intestinal segment is small,and the bioavailability is low,which restricts the efficacy of the drug.So there is no listing of its related preparations.Consequently,In this study,the preparation of icariin /P188 solid dispersion capsule was successfully prepared,and the best prescription was optimized by single factor and orthogonal test.and It provides a reference for clinical and clinical research. |
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