Prescription Optimization Of The Brucea Javanica Oil Emulsion And The Research Of Pharmacokinetics

Nowadays, cancer is still the main killer of mankind. Chemotherapy, for decades,has been clinically used as a main treatment for patients of cancer, but its severeside-effects also give people suffering. It is well known that traditional Chinesemedicine have advantages for few side-effects and prominent effects in treatingcancer in recent years. The Brucea javanica oil emulsion is one of the commonlyclinical Traditional Chinese medicine preparations for the treatment of cancer,including oral emulsion and injection. Emulsions are thermodynamically unstablesystems and will eventually undergo physical changes (e.g., aggregation, creaming,and droplet growth) over time. Because of its unstability, the droplet size of emulsionswill become bigger and then lead to demulsification and delamination if itsprescription and preservation are inappropriate, which greatly influence its curativeeffect. This article mainly studies the prescription optimization of the Brucea javanicaoil emulsion and the bioavailability of its prescription, including four parts as follows:1. Research of the prescription optimization of the Brucea javanica oil emulsionTo optimize the preparation process of the Brucea javanica oil emulsion andto study the appropriate amount of lecithin preparing the Brucea javanica oil emulsionalone by using the stability indices such as appearance, centrifugal stabilityparameters, average particle size and d90. The result shows thatthe appropriate amount of lecithin is1.4%, while the best ratio of mix emulsifier issoybean lecithin-poloxamer188（2.75:1）. With the same amount of emulsifier, thestability of the Brucea javanica oil emulsion prepared by mix emulsifier is better thanthe ones prepared by lecithin alone after placed alternately under the certainconditions of4℃and30℃for12hours respectively for4weeks. Additionally,as research continues, mix emulsifier containing lecithin-poloxamer188（2.75:1） has been found to be used more extensively to stabilize emulsions with lower dosage,compared to the Brucea javanica oil emulsion prepared by lecithin alone.2. Gas chromatography determination of oleic acid and linoleic acid in ratplasmaThe analyze method of determination of oleic acid and linoleic acid in rat plasmausing gas chromatography was built. Separations were carried out under the followingconditions: Chromatographic separation was achieved on a DB-FFAPcolumn(30m×0.25mm×0.25μm), maintained at205℃. The temperature of detectorand injection port were300℃and250℃, respectively. Samples (2.0μL) wereinjected with a microsyringe. Split (10:1) injection mode was used. The flowrate of carrier gas is1mL·min-1. The method is specific, stabilized, accurate, whichmeet the requirements for the dertermination of samples.3. The bioavailability research of the optimized prescription Brucea javanica oilemulsion and commercially available Brucea javanica oil emulsionThe SD rats were divided into two groups and each group of rats was given anoral gavage of commercially available Brucea javanica oil emulsion and theoptimized prescription Brucea javanica oil emulsion, respectively which contain equalamount of Oleic acid. The bioavailability of the prescription Optimized Bruceajavanica oil emulsion is evaluated by AUC0-t、Cmaxand Tmax.The result indicates thatthe prescription Optimized Brucea javanica oil emulsion is bioequivalent.4. The pharmacokinetics research of two different particle sizes of the Bruceajavanica oil emulsionTwo different particle sizes of the Brucea javanica oil emulsion were prepared bythe same prescription and different preparation processes and each group of rats weregiven an oral gavage of these two different emulsions, respectively. The resultindicates that the absorption of large particle size emulsion is slow and poor relativeto the small ones. The value of Cmax and AUC of large particle size emulsion isdistinctly below the small ones.