Study On Triamcinolone Acetonide Microemulsion For Injection

Triamcinolone acetonide is a kind of adrenocortical hormones with manypharmacological effects,such as anti-inflammatory,anti-allergic and immunosuppressive.It is difficult to be liquid preparation due to the insolublility in water. Microemulsionwas chosen as carrier to develop and research the triamcinolone acetonide drug deliverysystem, which is able to reduce drug toxicity, increase its solubility in water andimprove the bioavailability of the drug. In this paper，the formula and process of theTriamcinolone acetonide microemulsion for injection were studied, and its quality,pharmacokinetics and safety were also imvestigated.HPLC method for triamcinolone acetonide was established as the basis for thefollowing experiments. The formula for triamcinolone acetonide self-emulsify systemwas screened by studying excipients’ nature and solubility of triamcinolone acetonide inoil phase, drawing ternary phase diagram, doing stability experiment and so on. theoptimal formula for triamcinolone acetonide self-emulsify system was as follows:aethylis oleas: Solutol HS15: absolute alcohol=0.2:0.6:0.2(in the weight basis), withdrug loading of8mg/g.Study for the quality of self-emulsify system and microemulsion for injectionshowed that self-emulsify system was transparent and stable, as the O/Wmicroemulsion. After dilution of different level, the pH of the microemulsion wasstable,the viscosity small and average particle size of11.48nm. Accelerated testsshowed that the self-emusify system was sensitive for light, heat and humidity. Thelong-time testing showed that the microemulsion was stable at4℃in nine months.Preliminary evaluation of the safety of the triamcinolone acetonide selfemulsifysystem were investigated through the hemolysis test. Results showed that there was nohemolysis in all tested groups.Pharmacokinetics of triamcinolone acetonide microemulsion for injection wasstudied. The main pharmacokinetic parameters as follows:4.554μg/mL for peakconcentration of drug (Cmax),35min for peak time of drug (tmax),12.020mL for apparentvolume of distribution (Vd),4.871h for half life time (t1/2),573.5for area under thecurve (AUC) and2.819mL/h for clearance(CL).