Studies on bi-layer osmotic pump tablets of water-insoluble allopurinol with large dose: in vitro and in vivo.
Controlled release bi-layer osmotic pump tablets (BOPT) of water-insoluble allopurinol with large dose (150 mg/BOPT) were successfully prepared merely with sodium chloride as osmotic promoting agent and polyethylene oxide (PEO) as suspending agent. Formulations of the two kinds of agents were investigated in order to discuss their effects on the release behavior of BOPT, and then the optimal formulation was evaluated. The pharmacokinetics studies of allopurinol and its active metabolite oxypurinol in two-preparation and two-period crossover design relative to the equivalent dose of commercially common allopurinol tablets were evaluated in six Beagle dogs. And the pharmacokinetics results showed that allopurinol BOPT were able to provide a slow release of allopurinol, and oxypurinol were bioequivalent between allopurinol BOPT and common allopurinol tablets. A good in vitro-in vivo correlation of allopurinol was also proved. In conclusion, water-insoluble drugs with large dose can be designed to BOPT for efficacy and safety use.
Wang
Xun
X
School of Pharmacy, Shenyang Pharmaceutical University, Shenyang, PR China.
Nie
Shu-fang
SF
Li
Wei
W
Luan
Lin
L
Pan
Weisan
W
D000493:Allopurinol / Q000737:chemistry / Q000493:pharmacokinetics*; D000818:Animals; D001682:Biological Availability; D018592:Cross-Over Studies; D003692:Delayed-Action Preparations; D004285:Dogs; D005079:Excipients / Q000737:chemistry*; D006074:Gout Suppressants / Q000737:chemistry / Q000493:pharmacokinetics*; D009995:Osmosis; D009997:Osmotic Pressure; D010117:Oxypurinol / Q000493:pharmacokinetics*; D011092:Polyethylene Glycols / Q000737:chemistry; D012965:Sodium Chloride / Q000737:chemistry; D012995:Solubility; D013607:Tablets; D013810:Therapeutic Equivalency
D003692:Delayed-Action Preparations; D005079:Excipients; D006074:Gout Suppressants; D013607:Tablets; D011092:Polyethylene Glycols; D012965:Sodium Chloride; D000493:Allopurinol; D010117:Oxypurinol