Opiod analgesic
AssigneeEuro-Celtique S.A.
InventorsWalter Wimmer, Bianca Brogmann, Udo Hahn, Christof Spitzley
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Abstract
The invention is relative to a pharmaceutical preparation, especially for oral administration, with at least one active substance and with formulation components influencing the release of active substance, which preparation comprises at least one opiod analgesic as active substance that is formulated proportionally on the one hand for rapid release and on the other hand for delayed release in such a manner that the in vitro release rate from the preparation according to the Ph. Eur. paddle test shows a mean value of above 40% by weight after one hour and that the in vitro release rate shows a mean value that is still below 80% by weight after four hours.
Claims15
A pharmaceutical preparation, especially for oral administration, with at least one active substance and with formulation components influencing the release of active substance, which preparation comprises at least one opiod analgesic as active substance that is formulated proportionally on the one hand for rapid release and on the other hand for delayed release in such a manner that the in vitro release rate from the preparation according to the Ph. Eur. paddle test shows a mean [average] value of above 40% by weight after one hour, characterized in that the in vitro release rate shows a mean value that is still below 80% by weight after four hours.
A pharmaceutical preparation, especially for oral administration, with at least one active substance and with formulation components influencing the release of active substance, which preparation comprises at least one opiod analgesic as active substance that is formulated proportionally on the one hand for rapid release and on the other hand for delayed release, characterized in that the active-substance plasma level displays the following development in time in the agent:
- 4 Es pe- cial ly Pre- pre- fer- fer- ably ably At at at least 2 ng/ml least 3 ng/ml least 4 ng/ml after 0.15 h ″ 10 ng/ml ″ 13 ng/ml ″ 15 ng/ml after 0.30 h ″ 35 ng/ml ″ 40 ng/ml ″ 45 ng/ml after 0.50 h ″ 55 ng/ml ″ 60 ng/ml ″ 65 ng/ml after 0.75 h ″ 75 ng/ml ″ 80 ng/ml ″ 85 ng/ml after 1.0 h ″ 85 ng/ml ″ 90 ng/ml ″ 95 ng/ml after 1.25 h ″ 100 ng/ml ″ 105 ng/ml ″ 110 ng/ml after 1.5 h
- based on a one-time administration of 100 mg of the analgesic, or displays a corresponding development in time based on an other [different] one-time dose of the analgesic.
The preparation according to one of the preceding claims, characterized in that the active substance is an opiod analgesic, preferably bupivacaine, buprenorphine, clofenadol, codeine, dextromoramide, diamorphine, dihydrocodeine, dihydromorphine, ethylmorphine, fentanyl, hydrocodone, hydromorphone, levomethadone, meperidine, methadone, morphine, nalbuphine, nefopam, normethadone, oxycodone, oxymorphone, pentazocine, pethidine, phenpyramide, piritramide, propoxyphene, tebacone, tilidine, tramadol and/or their physiologically compatible salts as well as derivatives of the previously cited active substances.
The preparation according to one of the preceding claims, characterized in that the preparation is formed as a tablet and is provided with a coating that is neutral in taste.
Dependencies are inferred from the claim text.