The Pharmaceutical Study On The Extractum Folium Ginkgo Siccus Sustained Release Capsules

The Pharmaceutical Study on the Extractum Folium Ginkgo Siccus Sustained Releases CapsulesSince 19th century,Ginkgo leaves have been studied a lot all over the world.It has been found the flavonol glycosides and terpene trilactones are considered the two pharmacologically most important groups present.Ginkgo biloba is an ancient Chinese phytomedicine used to treat various ailments including circulatory and demential disorders.The positive effects of Ginkgo extracts are thought to result from the synergistic action of two distinct groups of compounds,the flavonoids and triterpene lactones.The flavonoids are responsible for the free radical scavenging effects of Ginkgo,while the ginkgolides are potent anti-platelet factor (PAF) antagonists.With global research and development of new chemistry entity have becoming difficult,people have averted their eyes to research the target areas and monomer of plant extracts.Ginkgo biloba preparations are extracted from Ginkgo biloba effective substances. The appearance and successfully clinical application of Ginkgo biloba preparations have become a milestone in the history of the development of plant drug.Under the impulse of modern drug delivery technology and a variety of dosage forms,Ginkgo biloba preparations will become one of the most popular varieties in the plant market.In order to develop The Extractum Ginkgo Siccus sustained-release capsules preparations,several studies have been conducted.The results showed as the follows:Part 1 Studies on the Extraction Technology & Separation and Purification TechnologyPreparation of the extraction,choose to return the ethanol extraction and orthogonal experiment was applied to optimize factors effecting extraction efficiency.Concentration of ethanol, alcohol consumption,extraction time and from the number four factors by L9(3)⁴ orthogonal experiment,the optimization of the effective parts of Ginkgo biloba flavonol glycosides and terpenelactones constituents to the best of alcohol:80%Alcohol from returning three times and eight times the volume of Alcohol, from two hour.The extracts of Ginkgo biloba were purified with five kinds of macroporous adsorbing resins.The adsorption rate,desorption rate and adsorption kinetics of each resin were studied,and same technical conditionswere optimized via static and dynamic experiments The results showed that hydrogen bonding HPD417 was good sorbents of flavonoids and terpenelactones in static experiments.The optimum adsorption conditions of the resins: extracts pH5.0,resin:extracts was 1:8,and eluant was 75%ethanol. The dynamic experiments suggested that flavonoids and terpenelactones from Ginkgo biloba could be eluted from HPD417 with seven tines of 75%ethanol.The content of flavonoids and terpenelactones in the purified extracts reached 28.54%,8.83% with HPD417 in the optimized conditionsPart 2 Study on the Preparation TechnologyThe present study prepared the GBE(Ginkgo Biloba Extract ) sustained-release capsules by utilizing hydroxypropyl methylcellulose(HPMC) and 10%polyvinylpyrrolidone(PVP) alcoholic solution as the excipient.HPLC method was used to evaluate the release characteristics of GBE sustained-release capsules in vitro during screening of the prescription.The paper also studied the factors which influenced the release of GBE sustained-release capsules.The results indicated that HPMC and 10% PVP alcoholic solution block the relese of GBE from the capsules. And the release velocity could be adjusted by altering the ratio of HPMC and PVP in the prescription.To evaluate the dissolution of GBE sustained-release capsules, HPLC method by measuring of effective components flavonoids and terpenelactones release rate.The release results of the optimized prescription showed that the GBE sustained-release capsules fitted the estimation,the cumulative percents releaseed of the sustained release capsules at 6h and 12h were 50%and 90%, respectively.The dissolution of GBE sustained release capsules in pure water was in agreement with Higuchi equation. Part 3 Study on Content Determination of the PreparationTo determine the total flavonol glycosides and terpenelactones in the Extractum Folium Ginkgo Siccus sustained release capsules.The HPLC methods was adopted.The Aglient C₁₈(250mm×4.6mm,5μzm) column was carried out with methanol-0.4%phosphate(52:48) and methanol-waters(35:65) as a mobile phase respectively,solution flow rate of 1.0ml ? min^-1.The ginkgetins and the jingko terpene lactones could be completely separated from each other,and had good linear relationship.The method is accurate,reliable,sensitive and repeated,which can be used for quality control on the Extractum Folium Ginkgo Siccus sustained release capsules.