Study On Breviscapine Proliposome Capsule And Quality Control

Breviscapine was one of the flavonoids abstracted from Herba Erigerontis（vant.）.Scutellarin is the major active constituent.Breviscapine shows wide pharmacological effects,such as dilating blood vessels,increasing cerebral blood flow,improving microcirculation,inhibiting platelet aggregation,lowering blood viscosity.It also plays important roles in ameliorating hemorrheology,decreasing the activity of fibrinogen,preventing thrombus and anti-peroxidation of lipid,scavenging free radicals,reducing cerebral edema,inhibiting PKC,delaying ischemia apoptosis,and ameliorating hyperglycemia and dyslipidemia at some levels.It has been widely used in the therapy of cardiovascular and cerebrovascular diseases.There is only a tablet dosage for the oral preparation of breviscapine by now.But the absolute bioavailability is less than 10%.The powder of breviscapine proliposome was prepared by spray drying method according to the preliminary study of breviscapine’s physico-chemical properties Influences of purities of stock drug and phosphatidylcholine on the formulation was studied.And the best prescription was settled down with the Encapsulation efficiency（EE%）,the content of drug and burst release being evaluation standards.Powder of this prescription showed not very good flowability.The angle of repose determined by funnel method was 45 degree.And the mean diameter observed by Motic microscope was 32μm.After hydration of this proliposome, bilayer of liposome was observed by Transmission Electronic Microscope（TEM）.And EE%of the liposome was above 80%.Mean diameter of the liposome were 516.3±7.6 nm,and the distribution showed a double peak phenomenon.The quality standards of breviscapine proliposome capsule were studied.The identification of breviscapine was recognized by the color reaction of flavonoids and HPLC,while liposome was recognized by TEM.A series of tests had been done to evaluate the quality of the product, including weight variation test,disintegration limit test,burst release test,determining the value of peroxide,EE%.Three batches of samples were tested and all of them were consistent with the standards.The assaying of this product was carried out by HPLC-UV.And all of the tested samples were qualified. The influencing factors experiment of breviscapine proliposome powder was carded out,The results showed that the product was affected predominantly by temperature and humidity.So commercially available package was sealed up by aluminum foil after capsulation,and then packaged in cardboard boxes.Acceleration test and long-term test showed that the product in this package was with good stability.The vitro release of breviscapine liposome was studied.And the result showed that breviscapine liposome was integrity in the pH 1.2 HCl solution and 10 mmol·L^-1bile salt solution.The safety of breviscapine proliposome was studied.The result of gastric infusion of breviscapine liposome showed that this formulation of the drug was very safe.The breviscapine liposomal systems were also studied for PK in rat using oral administration.The test samples were evaluated by compared to reference preparation.