Concentrated solution for temsirolimus injection and preparation method thereof

Abstract

The invention provides a preparation method of a concentrated solution for temsirolimus injection. The concentrated solution is mainly prepared from active component, benzyl alcohol, butyl hydroxybenzoate, organic acid or inorganic acid, pH regulator and absolute ethyl alcohol. The prepared preparation has few related substances, is stable in long-term storage process, and meanwhile solves the problem that due to the introduction of water, temsirolimus isomers and related substances are increased.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a concentrated solution of temsirolimus for injection and a preparation method thereof. Background technique [0002] Tesirolimus, also known as Temsirolimus, trade name: Torisel (temsirolimus, CCI-779) is a derivative of rapamycin C42 propionate, developed by Wyeth, and approved by the US FDA in May 2007. , temsirolimus injection for the treatment of advanced renal cell carcinoma, and designated as an orphan drug, is the first anti-tumor mTOR inhibitor. [0003] Temsirolimus is the 42-bis-hydroxymethyl propionate of rapamycin, which exhibits cell growth and proliferation inhibition in vivo, and can delay the time of tumor cell development or tumor recurrence. Temsirolimus binds to the cellular protein FKBP and forms a complex that inhibits the enzyme mTOR (mammalian target of rapamycin). Inhibition of mTOR's kinase activity inhibits various signal transduction path...

AI Technical Summary

Problems solved by technology

[0006] Chinese patent CN103989676A discloses an injectable temsirolimus composition, which consists of a concentrated solution and a diluent, wherein the concentrated solution contains the main drug temsirolimus, absolute ethanol, organic acid and propylene glycol, and the diluent Contains polysorbate 80, ethanol, polyethylene glycol 400, which effectively reduces the problem that the isomers of temsirolimus become larger in the injection due to the introduction of water during long-term storage, but it still cannot reduce the increase of related substances. big trend

[0007] Temsirolimus injection needs to reduce the water content in its preparation as much as possible, avoiding the degradation of temsirolimus due to the participation of water, resulting in the increase of its isomers and related substances. The growth of the conformation and related substances has been greatly improved, but it is still not enough to solve the safety of temsirolimus injection

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