Paclitaxel alhumin submicron for injection and preparation method thereof

Abstract

The invention discloses a paclitaxel alhumin submicron for injection. The paclitaxel alhumin submicron comprises 1-10% (W / W) of paclitaxel, 10-80%(W / W) of alhumin and 10-85% (W / W) of freeze-drying protective agent. The invention also discloses a preparation method of the paclitaxel alhumin submicron. The method comprises the following steps of 1) adding paclitaxel into tert-butyl alcohol, stirring and dissolving to be used as an organic phase; 2) adding the alhumin and the freeze-drying protective agent to water or a buffer with a pH within 6.0-8.5, stirring and dissolving to be used as a water phase; 3) adding the organic phase into water with stirring, stirring and dissolving, filtering and degerming through a millipore filtration method, and placing in a clean container; 4) freezing at-30- -50 DEG C, removing tert-butyl alcohol and water through freeze-drying by a lyophilizer to obtain freeze-drying powder with good profile and loosening quality. During usage, the freeze-drying powder is added to a solvent for injection and redissolved, so that paclitaxel alhumin submicrons with an average particle size of 100-600nm are formed. The paclitaxel alhumin submicron for injection ofthe invention has advantages of a simple preparation technology, no high toxic organic solvent and long-term storage, etc.

Description

technical field

[0001] The invention belongs to the field of pharmaceutical preparations, in particular to a paclitaxel albumin subparticle for injection and a preparation method thereof. Background technique

[0002] Paclitaxel (Taxol) is a natural active ingredient extracted and developed from the trunk and bark of Taxus yew. Treatment of breast cancer, ovarian cancer, non-small cell lung cancer and prostate cancer, etc. Although the antitumor effect of paclitaxel was recognized by people in the 1960s, it was not until 1992 that Bristol-Myers Squibb successfully developed paclitaxel injection (Taxol) and applied it clinically. One of the reasons is that its Water solubility is very low. The solvent system used in commercially available paclitaxel injections is polyoxyethylene castor oil (Cremophor EL, CrEL): ethanol (≈1:1, V / V). In the case of clinically given therapeutic doses, CrEL can cause severe respiratory symptoms. Distress, hypotension, angioedema and generalize...

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