Lactate-Based Fulvestrant or Fulvestrant Derivative Oily Preparation and Preparation Method Thereof

摘要

An oily formulation of fulvestrant or derivatives thereof and a method for producing the same. The oily formulation comprises: fulvestrant or derivatives thereof in an amount of 10 mg/ml to 170 mg/ml; a lactate compound in an amount of 5 to 80% of the total weight of the formulation; a vegetable oil or synthetic oil (ester); an analgesic; and an optional antioxidant.

主权项

1. An oily formulation of fulvestrant or derivatives thereof, characterized in that, the formulation comprises per ml:
(a) fulvestrant or derivatives thereof, 10 to 170 mg; (b) a lactate compound, 0.05 to 0.80 ml; (c) an analgesic, 3 to 5 mg/30 to 50 μl; and (d) a dispersant, balanced to 1 ml, wherein said fulvestrant or derivatives thereof has the following structure: wherein 1) both of R1 and R2 are —OH; or 2) one of R1 and R2 is —H, —O—CO—R, —CO—R or —O—R, and the other one is —OH; and one, or a mixture of two or more of fulvestrant or derivatives thereof may be used in the formulation.