Preparation And Evaluation Of Nitrendipine Inclusions Compound And Their Tablets

High blood pressure is the most dangerous disease so that it will threaten human being and has close relationship with other cardiovascular diseases. How effectively and low-costly cure the high blood pressure disease is the persistent goal of pharmacists. Nitrendipine is a usual medicine for this disease, but its solubility and stability are worried. Nitrendipine is the object in this work. Nitrendipine -β-cyclodextrin inclusion complex and its inclusion tablets have been prepared, the character of inclusion tablets and normal market tablets was also compared.Results are showed as follows:(1) Study on nitrendipine-β-cyclodextrin inclusion: Co-evaporated, kneaded, and ultrasonic systems were used in the preparation of nitrendipine-β-cyclodextrin inclusion complexes. The results indicated that the ultrasonic system was the best. The orthogonal experimental design was adopted in the determination of inclusion procedure, and prepared inclusion under the best parameters.(2)Analysis of nitrendipine-β-cyclodextrin inclusion complex: Microscopy, X-ray diffraction analysis and Differential Scanning Calorimetry were used to analysis the nitrendipine-β-cyclodextrin inclusion complex. Ultraviolet spectra were used to determine whether the nitrendipine was in nitrendipine-β-cyclodextrin inclusion complex and the stability of the complex. The results are as follows: nitrendipine-β-cyclodextrin was a new substance different from nitrendipine and cyclodextrin. The encapsulation of nitrendipine was about 74.68% and the load of nitrendipine in the inclusion complex was about 16.2%, which approximated to the theoretical values and the calculated values by XRD quantificational analysis. The stability and dissolution of nitrendipine-β-cyclodextrin were both better than the material drug of nitrendipine, and they meet the requirements of new drugs in pharmacopeias quite well.(3) Preparation of inclusion tablets: Based on the referenced prescription design, with 9.8mg disintegrant fillers, adaptive adhesive, 0.05g lubricant, inclusion tablets were prepared; comparing with the NTD tables which have been prepared using the same prescription, the solubility of inclusion tablets increased about 50% of initial. (4) Evaluation of inclusion tablets: In vitro pharmaceutical properties of inclusion tablets were determined and compared with market tablets. The results indicated that the dissolution property of the inclusion tablets were superior 1.5 times to the market tablets.