Methods and pharmaceutical compositions for reliable achievement of acceptable serum testosterone levels
View Patent ↗The present invention relates to pharmaceutical compositions, formulated for injectable administration, which comprises a testosterone ester, in particularly testosterone undecanoate, in a vehicle comprising castor oil and a co-solvent. Upon injecting the compositions according to a particular administration scheme, reliable levels of testosterone in serum in the normal physiological range is achieved for a long period. This allows for the use of the compositions in hormone replacement therapy and male contraception without concomitant monitoring of testosterone levels in serum by a physician.
1. A composition formulated for intramuscular injection in a form for single injection which contains 250 mg/ml testosterone undecanoate in a vehicle containing a mixture of castor oil and benzyl benzoate wherein the vehicle contains castor oil in a concentration of 40 to 42 vol %.
2. A composition formulated for intramuscular injection in a form for single injection according to claim 1 , which contains 750 mg testosterone undecanoate.
3. The composition according to claim 1 , which contains 1000 mg of testosterone undecanoate.
4. The composition according to claim 2 , wherein the vehicle comprises the castor oil in a concentration of 25 to 30 vol %.
5. The composition according to claim 1 , wherein the benzyl benzoate is in an amount of 55 to 65 vol % in the composition.
6. The composition of claim 1 , wherein the vehicle consists of castor oil and benzyl benzoate.
7. The composition of claim 2 , wherein the vehicle consists of castor oil and benzyl benzoate.
8. A composition formulated for intramuscular injection in a form for single injection which contains 250 mg/ml testosterone undecanoate in a vehicle containing a mixture of castor oil and benzyl benzoate, wherein the vehicle contains the castor oil in a concentration of about 40 vol %.
9. A composition according to claim 8 , which contains 750 mg testosterone undecanoate.
10. The composition according to claim 8 , which contains 1000 mg of testosterone undecanoate.
11. The composition of claim 8 , wherein the composition contains no plant oil other than castor oil.
12. The composition of claim 9 , wherein the composition contains no plant oil other than castor oil.
13. The composition of claim 8 , wherein the vehicle consists of castor oil and benzyl benzoate.
14. The composition of claim 9 , wherein the vehicle consists of castor oil and benzyl benzoate.