The Preparation Of Zedoary Turmeric Oil And Drug Release In Vitro Studies

Objective:Oil of zedoary turmeric For traditional Chinese medicine shows oil shows naphtha, according to the pharmacological studies show that shows the oil has antivirus, antitumor, of antithrombotic, anti-inflammation, infection and so on many kinds of pharmacological effects, but shows oil has not soluble in water, bitter in taste, not easy to oral, the living creature exploitation degree shortcomings etc. At present, the main clinical use is shows oil injection and shows oil glucose injection, but because of its poor stability, which is of great stimulating and adverse reaction shortcomings and be eliminated. Liposomes (Liposomes) is a kind of similar to the biological membrane structure bilayer millirod, is a directional drug carrier, belongs to the targeted drug delivery system (Targeting drug delivery system, TDDS) a new dosage form. Entering the human body passively targeting is mainly meshy endodermis system to gobble up (RES) and activate the body’s own immune function, and change the body sealing wrapped up drug distribution drugs mainly in the liver, spleen, lung tissue organ of savings, and first gathered in infection, inflammation, cancer and other parts, so as to improve the drug treatment index, reduce drug treatment dose and lower drug toxicity. The experimental results liposome as drug carrier, will be prepared to shows oil shows oil plasmids, which aims to enhance the therapeutic efficacy of drugs and reduce the dose of drug, and reduce the side effects of oil shows and irritant, improve its drug safety.Methods:The experiments of steam distillation process of extracting oil shows orthogonal design, to determine the optimal process shows that oil extraction, and shows the extraction of oil for qualitative and quantitative research. And established in liposome shows the oil analysis method, the choice Mange bull ketene as indexes composition, using high performance liquid chromatography (HPLC) method to grease content determination of geological body to shows and the methodology investigation.In the basis of experiments shows that determined initially oil stratum method of preparation and prescription, and then through the single factor investigation determined primarily influence the preparation of liposome factors. The preparation of geologic shows oil, grease on the preparation method of the geological body shows, the film ultrasound dispersing method, ethanol injection method, reverse evaporation method the three methods of liposome preparation, using gleans gel column on the liposome with the free drugs for the separation and determination of oil in geologic shows the oil sealed rate, final film ultrasound dispersing method shows for the preparation method of the geological body fat.In packets seal rate for index, through the single factor investigation shows that grease the preparation of geologic optimization process, investigation and cholesterol than, the quality of lecithin phospholipids drugs and quality than, buffer pH, the influence of hydrated time. On this basis, the four factors of the three level orthogonal experiment design to the level of the various factors screening, the analysis of all prescription poor rating, the final determination of the best prescription shows oil geological body.Are charted in vitro release of oil shows geological body curve and in vitro penetration curve, compare the in vitro release process, USES the level, level1, with zero Waybill and Higuchi equation, by fitting investigation correlation coefficient. With particle size, appearance, color as the index, the stability of the geological investigation shows that oil.Results:The experimental results show that Mange bull ketene of chromatographic peak linear relationship is good, the regression equation is Y=44110C+12100, r=0.9996, test precision and add kind recovery are in line with demand, can be used for the quality of the geological analysis shows that the oil. The proposed oil Mange shows the content of10.40%to the cow ketone, comply with the requirements.Film ultrasound dispersing method of preparation of oil that shows the encapsulation geologic rate is higher, through the orthogonal design to confirm the best prescription conditions for:phospholipids40mg, cholesterol10mg, shows oil10mg, phosphate buffer pH6.5, hydrated15min. The preparation of the geological body bag sealing grease shows rate is85.17%, the drug for5.84%, pH value of6.06+/-0.01, in light and transmission electron microscopy of a circular and oval, average particle size of138.9nm, Zeta potential value is41.3.Stability results show that the geological conditions in heating oil shows not stability; In the25℃conditions storage a month, the encapsulation efficiency has a larger drop, down20.6%, liposomes precipitation stratification is obvious; At4℃conditions storage a month, the encapsulation rate by6.8%, Zeta potential value is26.1, the average size of238.7, still in the nano distribution range, and more uniform particle size distribution, the preparation of oil that shows good geological stability, suggest that oil needs to be in geologic showsIn simulated gastric fluid, the ZTO release behavior from ZTO Injection in vitro was in accord with Weibull equation and the equation was as follows:ln[-ln(1Q)]=-1.30121nt+2.0785, r2=0.9941; The ZTO release behavior from ZTO lipidosomes in vitro was in accord with zero-order equation and the equation was as follows:Q=0.1015t+0.0025, r2=0.9932. In simulated intestinal fluid, the ZTO release behavior from ZTO Injection in vitro was in accord with Weibull equation and the equation was as follows:ln[-ln(l-Q)]=-1.1200Int+1.8463, r2=0.9934; The ZTO release behavior from ZTO lipidosomes in vitro was in accord with zero-order equation and the equation was as follows: Q=0.0880t+0.0952, r2=0.9912.So, ZTO lipidosomes has better slow-release than ZTO Injection. The ZTO release cumulant from ZTO lipidosomes in vitro was in accord with Higuchi equation, and it is considering to join penetration enhancers in order to achieve better permeation effect.Conclusion:With cancer fightting drug-ZTO as drugs model, phospholipid and cholesterol as main materials, Film ultrasound dispersing method for ZTO lipidosomes preparation is simple and efficient. The quality of ZTO lipidosomes is controllable and it can remarkably enhances the medicine curative effect and reduces the side effects.