Irinotecan hydrochloride pharmaceutical composition and preparation method thereof

Abstract

The invention discloses irinotecan hydrochloride pharmaceutical composition and a preparation method thereof. The composition contains irinotecan hydrochloride and mannitol. The preparation method comprises the following steps: 1), preparation is performed: ambroxol hydrochloride and mannitol are placed into a preparation tank in a weight ratio of 1:(1-20), water for injection is added, and the mixture is stirred until complete dissolution and uniform mixing are achieved; 2), sterile filtration, subpackaging and half stoppering are performed; and 3), vacuum freeze drying is performed to obtain a product. The composition and the preparation method have the advantages that the formula is simple, the technology is advanced, the quality is uniform and stable, moisture drying is thorough, and the redissolution performance is better.

Description

technical field [0001] The invention belongs to the field of medical technology preparation, and in particular relates to an irinotecan hydrochloride composition for injection and a preparation method thereof. Background technique [0002] Irinotecan hydrochloride Irinotecan is a semi-synthetic derivative of camptothecin. Camptothecin can specifically bind totoisomerase I, which induces reversible single-strand breaks, thereby unwinding the DNA double-strand structure; irinotecan and its active metabolite SN-38 can bind totoisomerase The I-DNA complex binds, thereby preventing the rejoining of the broken single strands. Existing studies suggest that the cytotoxic effect of irinotecan is due to the interaction between replicase and topoisomerase I-DNA-irinotecan (or SN-38) triple complex during DNA synthesis, thereby causing DNA double Chain break. Mammalian cells cannot efficiently repair such DNA double-strand breaks. It is suitable for the treatment of metastatic color...

AI Technical Summary

Problems solved by technology

Using the traditional freeze-drying process, because part of the HCl in irinotecan hydrochloride is pumped away under high vacuum conditions, the salt formation of irinotecan hydrochloride is not complete, and part of irinotecan hydrochloride exists in the form of bases, which cannot be completely dissolved in clinical use. Visible foreign matter, insoluble particles and unqualified clarity appear, all of which indicate that there may be more tiny particles in irinotecan hydrochloride for injection prepared by traditional freeze-drying process

Among these particles, particles with a diameter of 5-20 microns and above can block blood flow when passing through pulmonary capillaries, thereby causing complications such as pulmonary embolism and even death. Exogenous particles can also form phlebitis at the injection site, At the same time, it may also cause venous vascular obstruction and patient injury, and there is a large clinical safety hazard.

Images