Prodn. of bio-adhesive medicament, e.g. oral or vaginal tablet - comprises mixing drug with swellable, bio-adhesive polymer, dispersant and opt. binder

摘要

Prodn. of bioadhesve medicaments comprises mixing conventional drug with bioadhesive polymer which is swellable in water and which contains hydrophilic functional groups. pref. hydroxy and/or carboxy groups and a dispersant and opt. binder. The medicaments pref. contain 1-98 wt. % esp. 40-90 wt. % polymer 1-90 wt. % esp. 1-50 wt. % dispersant and up to 30 wt. % esp. up to 5 wt. %, binder. The dispersant is substance which produces gas on contact with body fluids and the binder, which is present when the medicament is not mechanically stable is esp. copolymerisate of an acrylate with an acid or with di- or trimethylaminoethano. Further, carboxyl gps. on the polymer are wholly or partly neutralised with sodium, potassium, ammonium, or organic amine ions. USE/ADVANTAGE - The medicaments which can take the form of tablets, granulates or capsules, can be used for the admin. of e.g. antirheumatics, contraceptives, and cardiovascular drugs, esp. by the peroral or vaginal route. The medicaments have better release, stability, and/or bioavailability characteristics than known bioadhesive formulations such as those described in e.g. US4615697, US4795436, DE3800256 and DD-282551. In partic. they adhere to tissue, esp. mucous membranes, over a long period and swell rapidly to produce a non-toxic bioadhesive mucilage which covers a large surface and which promotes absorption of the drug.