Controlled release delivery system for nasal applications
View Patent ↗This invention relates to a pernasally administrable preparation for the controlled release of sexual hormones to the systemic circulation, in particular to a formulation which enables its active ingredient to be absorbed in a sustained manner providing a better bioavailability at very low doses and longer duration of action.
1. A testosterone gel formulation for nasal administration to a patient for controlled release of testosterone into systemic circulation of the patient following the nasal administration for treating the patient with testosterone therapy, the testosterone gel formulation comprising:
(a) testosterone, wherein said testosterone is present within the testosterone gel formulation in an amount of from about 0.5% to about 10% by weight of the testosterone gel formulation:
(b) at least one lipophilic or partly lipophilic carrier present in an amount of from about 60% to about 98% by weight of the testosterone gel formulation;
(c) a compound or a mixture of compounds having surface tension decreasing activity present in an amount of from about 1% to about 20% by weight of the testosterone gel formulation; and
(d) a viscosity regulating agent present in an amount of from about 0.5% to about 10% by weight of the testosterone gel formulation.
2. The testosterone gel formulation according to claim 1 , wherein said lipophilic carrier comprises an oil.
3. The testosterone gel formulation according to claim 2 , wherein said oil is a vegetable oil.
4. The testosterone gel formulation according to claim 3 , wherein said vegetable oil is castor oil.
5. The testosterone gel formulation according to claim 1 , wherein said compound or said mixture of compounds having surface tension decreasing activity comprise an oleoyl macrogolglyceride or a mixture of oleoyl macrogolglycerides.
6. The testosterone gel formulation according to claim 1 , wherein said viscosity regulating agent is colloidal silicon dioxide.
7. A testosterone gel formulation for nasal administration for controlled release of testosterone into systemic circulation of a patient following nasal administration to the patient, the testosterone gel formulation comprising:
(a) testosterone, wherein said testosterone is present within the testosterone gel formulation in an amount of from about 0.5% to about 6% by weight of the testosterone gel formulation;
(b) castor oil in an amount of from about 75% to about 95% by weight of the testosterone gel formulation;
(c) oleoyl macrogolglycerides in an amount of from about 1% to about 5% by weight of the testosterone gel formulation; and
(d) colloidal silicon dioxide in an amount of from about 0.5% to about 5% by weight of the testosterone gel formulation;
wherein the testosterone serum level achieved following the nasal administration of the testosterone gel formulation to the patient is sustained above the patient's testosterone baseline for at least 6 hours.