Process for the preparation of pharmaceutical compositions for the sustained release of somatostatin analogs

摘要

The invention relates to a process for the preparation of injectable pharmaceutical compositions for the sustained release of somatostatin analogues and to pharmaceutical compositions prepared according to the process. In a preferred aspect the process comprises the steps of combining lanreotide acetate and acetic acid, lyophilizing the resulting mixture only once, and hydrating the lyophilizate. Acetic acid may be added to a desired pH during the final step of the process.

主权项

1. A method for preparing an injectable sustained release pharmaceutical composition, comprising the steps of:
lyophilizing a mixture of a lanreotide salt and an aqueous acid solution in a stepwise temperature pattern, wherein the stepwise temperature pattern is:
initially reduced from room temperature to 2° C.±1° C. and then held constant;further reduced from 2±1° C. to −40±5° C. and then held constant;increased from −40±5° C. to 25±5° C. and then held constant; andfurther increased to 35±5° C. and then held constant; the resulting mixture to form a lyophilizate; and hydrating the lyophilizate; wherein the composition has a final pH ranging between pH 5.8 to 6.4; and the method comprising only one lyophilization.