Articles
Controlled Release Formulation Of Tamsulosin HCl Using EUDRAMODE® Technology
January 16, 2009
•Poster: Controlled Release Formulation Of Tamsulosin HCl Using EUDRAMODE® Technology
By Evonik Röhm GmbH
Tamsulosin HCl is used for the treatment of obstructive urinary tract disorders3 and benign prostrate enlargement. It is an alpha adrenoceptor blocking agent and exhibits selectivity for alpha receptors in the human prostrate2. Following intravenous or oral administration of an immediate-release formulation, the elimination half-life of the drug in plasma, is in the of range 5 to 7 hours. The daily recommended dose is in the range of 0.2 to 0.8 mg, which indicates the high potency of the drug. Owing to its high potency there is an associated risk of excessive increase of the initial level of Tamsulosin HCl in the blood, due to its fast absorption in the stomach which may cause side effects such as orthostatic hypotension. In order to prevent such a rapid initial absorption from the stomach, the release of the drug needs to be controlled during its transit from the upper gastrointestinal tract. Latter as the formulation leaves the stomach, a slow release of the drug over a period of 12 hours is desired, to maintain an optimum level of the drug in the blood steam for a longer period of time.
The technology is based on the ionic interaction of an organic acid/salt and the quaternary ammonium groups of the EUDRAGIT® RS/RL. It is designed as a multi unit dosage form, with a central salt core coated with the EUDRAGIT® NE, drug layered & further coated with EUDRAGIT® RS/RL. The following is a diagrammatic representation of a single unit resulting out of the application:
The process involves the following sequential steps to achieve the final multi units having a controlled release profile:
- An appropriate size fraction of the organic acid/salt crystals used as the initiating cores.
- The cores are coated with the modulating layer of EUDRAGIT® NE polymer.
- The EUDRAGIT® NE coated cores are loaded with the drug.
- The drug loaded cores are coated with the functional EUDRAGIT® RS/RL polymer.
•Poster: Controlled Release Formulation Of Tamsulosin HCl Using EUDRAMODE® Technology
