Preclinical Pharmacy Study On Preparations Of Iridoid Glycosides From Lamiophlomis Rotata

Objective:The plant Lamiophlomis rotata (Benth.)Kudo (LR) is of the Labiatae family.The aerial parts and the root of L. rotata have been used as a traditional drug in Tibet. The large number of research shows that the total iridoid glycosides are the effective parts of hemostasis and analgesic. Using the effective parts of Lamiophlomis rotata to produce new preparation could achieve the secondary development of traditional Tibetan medicine. This thesis studies on the pre-clinical pharmaceutical documents of the powder and capsule of L. rotata iridoid glycosides, which would be the fifth class new drug according to the Registration of new traditional Chinese medicine.Methods:1.In order to control the quality of the water extract of Lamiophlomis rotata (Benth.),iridoid glycosides were identified with TLC and the contents of total iridoid glycosides and total flavonoid were determined by UV. The contents of shanzhiside methyl ester and 8-O-acetylshanzhiside methyl ester were determined by HPLC.2.According to the former series of technology experiments, completed by our group, the better parameter of semi-industry production was studied. The total iridoid glycosides extract from water extract was produced magnificently by more than 10 times of the amount of prescription and the production condition was consistent with industrialization. The yield and transfer rate of the total iridoid glycosides were examined.3.The preclinical pharmaceutical documents of iridoid glycosides powder was studied, which including the parameters of manufacturing process, quality standards, relevant examination and stability.4.Iridoid glycoside capsule was prepared.The prescription compose, manufacturing process parameters, quality standards, relevant examination and stability of this capsule were investigated.Results:1.The water extract of Lamiophlomis rotata (Benth.)was identified with TLC and the spots was clear. The contents of total iridoid glycosides the total flavonoid was 119,161 mg/g respectively by UV, and contents of shanzhiside methyl ester and 8-O-acetylshanzhiside methyl ester in the capsule were 8.11 mg/g,11.74 mg/g respectively by HPLC. 2.The iridoid glycoside was separated and enriched by macroporous adsorptive resins chromatographic column combining with polyamide chromatographic column.70% alcohol was used as dissolvent to elute the iridoid glycoside, which was adsorbed by macroporous adsorptive resins chromatographic column. The extract of iridoid glycoside was dried and the yield and the transfer rate was 20%,70%respectively.3.The critical relative humidity of iridoid glycoside powder was 74.38%±5.92%, the angle of repose was 39.90±0.40°, and the bulk density was 0.68±0.60 g/mL. The iridoid glycoside powder was brown and bitter. The uniformity appearance, particle size, moisture and load difference were eligible for the request of Pharmacopeia. The iridoid glycoside powder was identified by TLC. The contents of total iridoid glycosides was 565.4 mg/g approximately by the first derivation UV-spectra, and the contents of shanzhiside methyl ester and 8-O-acetylshanzhiside methyl ester in the powder were 74.45 mg/g,70.26 mg/g respectively by HPLC. The bacteriology test, heavy metals, arsenic salt, and total ash were qualified and the iridoid glycoside powder was stable.4.The iridoid glycosides capsule was prepared with adding 0.3% Gum Acacia of prescription. The load difference, moisture, disintegration time were eligible for the request of Pharmacopeia. The iridoid glycoside capsule was identified by TLC. The content of total iridoid glycosides was 543.5 mg/g approximately by the first derivation UV-spectra, and the contents of shanzhiside methyl ester and 8-O-acetylshanzhiside methyl ester in the capsule were 73.96 mg/g,72.43 mg/g respectively by HPLC. The iridoid glycoside powder was stable.Conclusion:The result indicated that:the quality standards of Lamiophlomis rotata (Benth.)Kudo is simple, reproducible, specific, and could control water extract quality comprehensively; the industrialized method of iridoid glycosides of Lamiophlomis rotata (Benth.) Kudo is simple, workable, and stability. The large-scale industrial production has been achieved;This thesis has completed most of the preclinical pharmacy study of the powder and capsule of the iridoid glycosides from L. rotata.