The Studies On Stavudine Osmotic Pump Tablet

In this paper, Stavudine (STVD) was selected as the model drug to prepare osmotic pump tablet and the drug release character and mechanism were studied. At last, the pharmacokinetic study of STVD tablet was performed.In the formulation and the technique study of STVD tablet, sodium chloride, MCC, and PVP K-30 were used to make the tablet core, cellulose acetate(CA) and polyethylene glycol 4000(PEG4000) were selected as the coating materials , acetone solvent was employed as the coating medium. The effects of many factors including the formulation of tablet core and the coating membrane, the arts of preparing tablet and the condition of drug release on the release behavior of STVD tablet were investigated.Based on the single-factor and factor-screening experiments, the amount of sodium chloride, PEG4000 and the ratio of coating weight were selected as the causal factors. The formulation optimized according to orthogonal experiment design was proved to have the similar in vitro release behavior as the imported tablets. The investigation of the mechanism of STVD tablet release showed that the main power of the drug release was the difference of osmotic pressure between the tablet core and the dissolution medium during drug release.With the commercial common capsule as the reference, the pharmacokinetic study of self-prepared STVD elementary osmotic pump tablet was performed in six Beagle dogs. With the crossover design, HPLC method was employed to detect the drug concentration in plasma of dogs administered with single dose. The pharmacokinetic parameters of the test and reference tablets were as follows: AUC were 14289.08±1704.15 and 13254.33±1754.47(ng·mL^-1), C_maxwere 1408.21 ±438.35 and 4524.55±81 6.00 ( ng·mL(-1)) , T_max were 6.17±0.75 and 1.58±0.34(h) ,the relative bioavailability was 108.06%. The two one-sided test results showed...