Abstract: The 1-deoxynojirimycin(DNJ) bi-layer osmotic pump tablets were prepared, and the prescription was optimized by dissolution. The in vitro release of DNJ bi-layer osmotic pump tablets was investigated. And the pharmacokinetics of bi-layer osmotic pump tablets and immediate release tablets were studied in Beagle dogs. The optimal prescription for DNJ bi-layer osmotic pump tablets was the dosage of containing drug layer hydroxypropylmethyl cellulose(HPMC) E50 10 mg, the boost layer polyoxyethylene(PEO, M_r6×10⁶) 80 mg, the coating layer cellulose acetate(CA) 15 mg and polyethylene glycol(PEG) 4000 5 mg. Under these conditions, the dissolution rate of DNJ was the most suitable, and it was not affected by the change of pH value. The drug was completely dissolved in 12 h and slowly released at a constant rate. Comparing the bi-dose two-cycle crossover test of DNJ bi-layer osmotic pump tablets and immediate release tablets in Beagle dogs, the results showed that the time to peak(t_max) (9.3±3.8) h of the release of bi-layer osmotic pump tablets was longer than that of the immediate release tablets (4.4±2.2) h, achieving the purpose of controlled release. The relative bioavailability of osmotic pump tablets was (96.1±9.8)%, and the 90% confidence interval was 84.8%-103.7%. And the absorption degrees of osmotic pump tablets and immediate release tablets were organisms equivalent.

Key words: 1-deoxynojirimycin, bi-layer osmotic pump tablets, cumulative release, pharmacokinetics