Preparation And Evaluation Of Rhynchophylla Total Alkaloids Sustained-release Dropping Pills

ObjectiveStudy on the extraction process of uncaria, preparation technology , quality standard and acute toxicity of Rhynchophylla total alkaloids sustained-release dropping pills.And it is a good basis for register of new antihypertensive drug.MethodAdopting orthogonal experimental design,and with ratio of dry extraction and Rhynchophylla total alkaloids for indicatrix,the extraction process and technical condition of preparation was optimized.Orthogonal design was applied to optimize the preparation technology of Rhynchophylla total alkaloids sustained-release dropping pills with the hardness, the tailed degree, the spherical degree, the coefficient of heavy variation and the release rate of the dropping pills , and others as the index.The identification of uncaria and the measurement of Rhynchophylline in the preparation were be made with theTLC and HPLC respectively.Study preliminary stability investigation of 3 batches of Rhynchophylla total alkaloids sustained-release dropping pills for 6 months under room temperature storage. In order to get the furher information about the safety of this preparation, mice were employed to investigate the toxicology of Rhynchophylla total alkaloids sustained-release dropping pills by stomach perfusion according to Acute Toxicity Guiding Principle Of Chinese Medicine.ResultsThe most proper extraction condition for RTA was as follows:the uncaria material was refluxed with80% alcohol for two times and each time was 2 hours, concentration temperature was 65℃and drying temperature was 75℃.The best condition was as follows: the proportion of drug- matrix 1:2, the proportion of stearic acid -PEG6000 1:4,temperature:70℃, dripping speed:45d/min.The method of TLC could identify angelica,chuanxiong rhizome and safflower in preparation.In HPLC,the linear range for rhynchophylline was0.48-1.12μg(r=0.9998),the recoveries for it was 99.5%the RSD was 1.38%(n=6). The cumulative release amount of rhynchophylla total alkaloids sustained-release dropping pills at10h was above 80%,and the drug release in vitro followed the Higuchi equation Q=0.2548t1/2+0.0453 r=0.9923.The characters, identification, content and the release rate of rhynchophylla total alkaloids sustained-release dropping pills was similar to 0 month after 6 months of study.The LD50 value of Rhynchophylla total alkaloids is 649.85mg/kg. The LD50 value of Rhynchophylla total alkaloids sustained-release dropping pills is 1900.7 mg/kg. The LD50 of RTA is 970 times than the clinical daily dose.ConculusionThe techniques and methodical control of quality of RTA sustained-release dropping pills are convenient,feasible,stable and credible.The dropping pills is an ideal sustained-release agent. The RTA sustained-release dropping pills are stable during six months and safe in clinical therapeutical dose.