Gastric retention properties of superporous hydrogel composites.
In many applications, usefulness of conventional hydrogels is limited by their slow swelling. To improve the swelling property of the conventional hydrogels, we have synthesized superporous hydrogels (SPHs) which swell fast to equilibrium size in minutes due to water uptake by capillary wetting through numerous interconnected open pores. The swelling ratio was also large in the range of hundreds. The mechanical strength of the highly swollen SPHs was increased by adding a composite material during the synthesis. The composite material used in the synthesis of SPH composites was Ac-Di-Sol((R)) (croscarmellose sodium). The gastric retention property of the prepared SPH composites was tested in dogs both in fasted and fed conditions. The SPH composites were placed in a hard gelatin capsule (size 000) for oral administration. All dogs tested were fasted for 36 h before experiments. Under the fasted condition, the SPH composite remained in the stomach for 2-3 h after before breaking into two pieces and being emptied. When food was given before the experiment just once following 36 h of fasting, the SPH composite remained in the stomach for more than 24 h, even though the fed condition was maintained only for the first few hours. Our study indicated that SPH composites possessed three properties necessary for gastric retention: fast swelling; superswelling; and high mechanical strength. While more improvements need to be made, the SPH composites provide the basis for the development of effective long-term gastric retention devices.
Chen
J
J
Merial Limited, Pharm. R&D, West Point, PA 19486, USA.
Blevins
W E
WE
Park
H
H
Park
K
K
D000818:Animals; D003692:Delayed-Action Preparations; D004285:Dogs; D005215:Fasting; D018565:Food-Drug Interactions; D020100:Hydrogels / Q000737:chemistry / Q000493:pharmacokinetics*; D008855:Microscopy, Electron, Scanning; D016062:Porosity; D013270:Stomach / Q000502:physiology*; D013997:Time Factors
D003692:Delayed-Action Preparations; D020100:Hydrogels