The Research Of Producing Modified-release Dosage Of Microsphere Of Berenil

Diminazene aceturas (berenil) is a drug for anti-protozoan , which is used for therapy Babesiidaesis , Therleriidaesis , Trypanosomiasis equiperdum , Trypanosomiasis evansi , and Eperthrozoonosis. This experiment is base on the defects of berenil which are the single type of dosage, too few researching dosage , the high drug toxicity , and the narrow scope ,in order to develop new dosage of berenil and microphere of poly-lactic acid(PLA) of berenil .The chosing modified material which is biodegradative high polymer PLA and gelatin . The ways which are used to produce microsphere of PLA microsphere are volatilizing solvent way , melt way, and mist-spraying-dehydration way. The principle of this experiment is volatilizing the solvent in order to produce the microsphere of PLA of berenil .Single factor design was used in this experiment , which is precedence level in the carrying dosage of microsphere , and which integrate the inside diameter of microsphere of PLA of berenil , which are the rate of berenil and PLA is 1:2(w/w), which are the concentration of PLA is 6.67%, which are the time of ultrasonic treating is 30 s , which are non-solvent system is PBS which contains 1.0% gelatin , which are the velocity of evaporating methylene chloride is 0.05 ml/min , which are the room temperature to dehydrate(15℃-20℃),and which the velocity of the suspension of berenil and PLA inpouring into the non-solvent is 0.3ml/min .The carrying dosage of berenil in microsphere of PLA of berenil was determined by diffusion -extration , and the mean carrying dosage , mean recovery rate , mean utility rate of microsphere of PLA of berenil are 20.61(0.6840%, 71.47(3.077%, 42.20(2.8647, respectively. The mean inside diameter of microsphere of PLA of berenil are X1=73.17(2.0844μm, X2=65.41(0.7562μm, X3=72.053(2.0117μm, respectively. The mean recovery rate outcome of berenil and microsphere of PLA of berenil are 99.44%(RSD=1.77%, n=6), 99.02%(RSD=2.90%, n=7) , respectively, and the releasing the microsphere ofPLA of in vitro is conform to the diffusion mechanism model , which was adapted by Huguchi , whose equation is Y=-0.8586+15.1892X(r=0.9982), and which is extremely significance correlation. The outcome releasing drug in vitro which was drafted by zero level velocity , is Y=-8.1799+0.4170X(r=0.9198).The outcomes of berenil and microsphere of PLA of berenil and physical conjugation of vacuo microsphere are the time of accumulating releasing rate the peak of berenil , the physical conjugation of berenil and vacuo microsphere , and the microsphere of PLA of berenil are 5h, 16h, and 48h, respectively, which suggested that the microsphere of PLA of berenil , has very evidence releasing function .The outcome of releasing microsphere of PLA of berenil which were produced by PLA , and whose molecular weight of PLA lower, the fast releasing drug in microspere.