Preparation And Evaluation Of Hongjingtian Injection

Hongjingtian which was ever listed in《Pharmacopoeia of the People's Republic of China》(Edition 1977,VolumnⅠ)has curative effects on removing heat and toxic, depriving the evil wetness and it was originally used in the treatment of lung heat, pulse heat, seasonal febrile disease and four limbs swelling. Modern pharmacology indicates that Hong Jingtian activates blood flow and removes blood stasis, anti-myocardium ischemia. At present, the compound tablets of Hongjingtian and the capsules of Hongjingtian are applied to treat coronary heart disease and angina pectoris with definite therapeutic effectiveness and neglectable side effects. If Hongjingtian is prepared into injection with modern technology, its curative effect must be enhanced and adapt to treating acute and heavy disease for Traditional Chinese Medicine. This research included: (1) the establishment of analytical methods of typical principles (2) the optimization on purification process of the active constituents (3) the pharmacodynamic study and special safety tests of Hongjingtian (4) the design of Hongjingtian injection and the study of its quality control (5) the study of fingerprints of Hongjingtian injection.Salidroside and p-Tyrosol, as typical principles were qualitalively analyzed with TLC methods and the corresponding R_f values were 0.358 and 0.584. HPLC methods were developed to determine their concentration in the medicinal materials and preparations. Using colored-reaction methods, the amylose in the preparations were determined. All of these methods were accurate and sensitive.The extraction and purification process of the active constituents were studied by the criterion of transference rate of Salidroside, p-Tyrosol and the extraction rate of the solid. The extracting solvents, the size that the medicinal materials were comminuted and the soaking time were studied to investigate the influence of single factor. Orthogonal tests were used to optimize the decoction time, decoction times and solvent volume. Alcohol precipitation method, basic alcohol precipitation, heat-treatment and cold-storage and gel flocculating method were used to optimize purification process. The impurities such as protein, resin, oxalate and Potassium were removed by 70% alcohol precipitation method. Tannin could be removed by basic alcohol precipitation and gel flocculating method, while gel flocculating method was better than the others.The special safety tests indicated the intermediate of Hongjingtian injection was safe, without vassal stimulus, hemolysis and allergy. The curative effects on acute experimental Ischemia rats, the effects on thrombocyte aggregation, the thrombus formation and the blood viscosity indicated that the action intense of Hongjingtian byⅣwas similar to compound Danshen injection. All of these indicated that Hongjingtian had definite effect on anti-ischemia, activating blood flow and removing blood stasis.The dose of Hongjingtian injection was confirmed according to the results of the pharmacodynamic study, and the preparation of Hongjingtian injection accorded with injection demand. The inspection of the preparations was eligible. Three months tests under room temperature or under accelerated circumstance indicated that the preparations are stable.Fingerprints of ten batches of medicinal materials, the intermediate and preparations were developed respectively, so quality control from "microscopic" and "macroscopic" was formulated in order to more effectively judge and evaluate the injection. According to the test results, the standard fingerprints were established by average vector. The similarity with the cosine value of vectorial angle was calculated: the similarity of medicinal materials, the intermediate and preparations were 0.976～0.999, 0.973～0.998 and 0.976～0.999 respectively, indicating that the produced process of Hongjingtian injection were steady and repeatable.