A novel gastro-retentive osmotic pump capsule using asymmetric membrane technology: in vitro and in vivo evaluation.
OBJECTIVE
The purpose of this paper is to develop a novel gastro-retentive osmotic pump capsule using asymmetric membrane technology.


METHODS
The physical characteristics of capsule walls and drug delivery behaviors of the system were compared through different coating solutions. The formulation with the glycerin and diethyl phthalate ratio of 5:4 appears to be the best. The thickness of asymmetric membranes was evaluated by withdrawing speed. The relation between the two can be fitted to a linear model. The floating abilities were investigated through filling polyethylene oxide of different molecular weight into the capsules. WSR N-80 (molecular weight 200000) is chosen for the longest floating time. Central composite design-response surface methodology was used to investigate the influence of factors on the responses. The in vivo pharmacokinetics were studied in beagle dogs.


CONCLUSIONS
A second-order polynomial equation was fitted to the data, and the actual response values are in good accordance with the predicted ones. The optimized formulation displays a complete drug delivery, zero-order release rate and 12 h floating time. The in vivo study results clearly indicate the controlled and sustained release of Famotidine from the system, and the relative bioavailability of this preparation is about 1.605 in comparison to that of the marketed preparation.
Guan
Jin
J
Department of Pharmaceutics, School of Pharmacy, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenyang, 110016, China.
Zhou
Liying
L
Pan
Yusheng
Y
Han
Haitao
H
Xu
Hongtao
H
Pan
Weisan
W
D000818:Animals; D002214:Capsules / Q000138:chemical synthesis* / Q000493:pharmacokinetics; D003692:Delayed-Action Preparations / Q000138:chemical synthesis / Q000493:pharmacokinetics; D004285:Dogs; D004337:Drug Carriers / Q000138:chemical synthesis* / Q000737:chemistry / Q000493:pharmacokinetics; D004339:Drug Compounding / Q000379:methods; D015738:Famotidine / Q000493:pharmacokinetics; D005746:Gastric Emptying; D066298:In Vitro Techniques; D008297:Male; D008567:Membranes, Artificial; D009997:Osmotic Pressure; D012995:Solubility
D002214:Capsules; D003692:Delayed-Action Preparations; D004337:Drug Carriers; D008567:Membranes, Artificial; D015738:Famotidine