Solid peroral application form with regulated releasing

摘要

Solid peroral application form with regulated releasing, which consists of inert pharmaceutical balls coated with analgetic effective amount of opiate anaglesic or with the mixture of opiate analgesics, or salts thereof, whilst the inert pharmaceutical balls are coated with the cover regulating the releasing of the substance, whilst the dissolution speed of the application form, determined under the conditions in vitro USP by mixing method with 100 evolves per min. in 900 ml of aqueous buffer, pH 1.6 and 7.2 under 37 °C is from 12.5 wt. % to 42.5 wt. % of opiate released after 1 hour, from 25 wt. % to 65 wt. % of opiate released after 2 hours, from 45 wt. % to 85 wt. % of opiate released after 4 hours, and more than 60 wt. % of opiate released after 8 hours, whilst the releasing speed in vitro does not depend on pH, where the difference, in any time, between the amount of opiate released with one pH and the amount released with any other pH during the measurement in vitro, with using USP mixing method with 100 evolves per min. in 900 ml of aqueous buffer, is not more than 10 wt. %, and the said releasing speed in vitro is selected so that the maximal plasmatic level of the said opiate was under the conditions in vivo from 2 to 8 hours after administering the application form, whilst the said application form provides extended duration of therapeutical effect approximately 24 hours.