Tramadol 24h, a new prolonged release once-daily pharmaceutical preparation with the active substance Tramadol HCl in the indication moderate to severe pain

Description: Tramadol-HCl is a well-known generic compound available in various formulations for the treatment of moderate to severe pain. So far in the EU there are Tramadol tablets, capsules and drops, sustained release tablets or capsules as well as a limited number of once-daily Tramadol tablets available in various dosage strengths ranging from 100 to 400mg Tramadol-HCl. In Germany, there are no 300mg once-daily Tramadol tablets available.

We have developed a modified-release 300mg Tramadol-HCl formulation with the aims (1) fast onset of action at sufficient plasma concentrations and (2) sustained 24 h effect. Reduced dosage strengths (100mg and 200mg) are also being developed. A genuine technological approach was applied - incorporation of the active substance in hydrophilic matrix structure based on high molecular weight polymer. The in vitro dissolution tests showed a dissolution rate profile close to the ideal profile. Using an established in vivo-in vitro correlation model a calculated plasma concentration profile was calculated and indicated that the desired plasma concentration profile would be achieved. This was confirmed in an orientating pilot phase I clinical trial with the 300mg dosage strength which demonstrated sufficient in vivo plasma kinetic profile over 24 h and kinetic equivalence to 2 single doses of a 150 mg s.r. formulation given at an interval of 12 h. A Clinical Development Program has been agreed on after consultations with the German Authorities for national registration of the 300mg dosage strength in Germany, which will be completed in the second half of 2005. Additional Clinical Studies which may be required for registration in other countries or other dosage strengths (100mg and 200mg).

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