Properties controlling the diffusion and release of water-soluble solutes from poly(ethylene oxide) hydrogels. 2....

The mechanisms which control the release of dispersed water-soluble drugs from an initially dry hydrogel are complex. The release profile derives from a combination of several contributing factors which may change with time at different rates. It has been possible to isolate controlling factors and investigate their individual contributions to the release kinetics. The hydrogels presented in this paper owe their hydrophilicity to their poly(ethylene oxide) content. They swell and can absorb up to three times their dry weight in water. Having a glass transition temperature (Tg) below body temperature they are essentially different to those studied theoretically or experimentally, by other groups, which have Tg values above body temperature and are initially glassy. A range of diffusates was studied ranging from low water-soluble prostaglandin E2 to highly water-soluble lithium chloride. Device geometry was restricted to approximations to infinite slabs with more than 85% total surface area over the top and bottom surfaces so that release was predominantly one-dimensional and the controlling variable was thickness. The increase in surface area with time, drug-solubility in the water-swelling matrix and the presence of crystallinity were shown to be important factors governing the profile and level of release rate with time. It was observed that the release profile could be separated into three parts, the most important being the middle section from early in the release until at least the half-life time. This period could be characterized by the exponential time function, tn. The diffusional exponent, n, is an important indicator of the release mechanism and ranged from 0.79 to 1, i.e. good anomalous to zero order. This is a highly desirable range of values for controlled release devices. The value of n decreases at late-time. The very early-time release can also show a burst or lag effect depending on the diffusate solubility and its loading in the xerogel.