Preparation method of human serum albumin nano granules coated with oxaliplatin

Abstract

The invention relates to human serum albumin nano granules coated with oxaliplatin and a preparation method thereof. The human serum albumin nano granules comprise oxaliplatin bulk pharmaceutical chemicals and human serum albumin HSA; in a preparation process, water for injection, anhydrous alcohol, glutaric dialdehyde and sodium hydroxide are used; the mass ratio of the oxaliplatin bulk pharmaceutical chemicals to the albumin is 10-25%, the concentration of an albumin water solution is 1-2.5% (g / ml), and the volume ratio of a precipitator of the anhydrous alcohol to the albumin water solution is 2:1-3:1; and the amino mole ratio of a cross-linking agent of the glutaric dialdehyde to the albumin is 75-200%, and the quantity of the sodium hydroxide is proper. The preparation method of the human serum albumin nano granules comprises the following five steps of directly carrying a medicine and removing a solvent, adsorbing the carried medicine and crosslinking, evaporating in a rotary way, precipitating in a centrifugal way and freeze-drying. The invention has the following advantages: (1) the anti-tumour efficacy of the oxaliplatin is retained, the limitation of quick metabolism of the oxaliplatin is changed, and the slow-release property of the medicine is enhanced; (2) the human serum albumin is used as a framework material, the compatibility of a human body is good, the human serum albumin nano granules are safe and innoxious and can be biodegradable, and the concentration of a lymph circulation medicine can be increased.

Description

Technical field: [0001] The invention relates to a preparation of medicines, in particular to a preparation method of human albumin nanoparticles loaded with oxaliplatin. Background technique: [0002] Oxaliplatin (L-OHP) is the main core drug used in the chemotherapy of colorectal cancer, ovarian cancer and other tumors. It is the third-generation platinum compound after cisplatin and carboplatin. The international common name is Platinum oxalate has a molecular formula of C8Hl4N2O4Pt and a molecular weight of 397.3. L-OHP has high anti-cancer activity and a broad anti-cancer spectrum. It has a unique intracellular target molecular mechanism and stronger cytotoxicity. It is stronger than cisplatin and carboplatin in inhibiting DNA, has a synergistic effect with 5-Fu, has no cross-resistance with other platinums, and is also effective against 5-Fu, cisplatin, irinotecan and other drug-resistant tumors, and is toxic. Side effects are mild. A large number of international mu...

AI Technical Summary

Problems solved by technology

However, the traditional oxaliplatin preparations are all in the form of freeze-dried powder, and there are still obvious shortcomings when they are configured as aqueous solutions for chemotherapy. The relevant drug instructions state: "Give oxaliplatin 130mg / m After 2 hours of intravenous infusion, 15% of the platinum exists in the systemic circulation, and the remaining 85% rapidly diffuses into the tissue or is excreted with urine; after the end of 2 hours, no complete drug can be detected in the plasma ultrafiltrate”

Therefore, it can be seen that the drug metabolism is fast, the action time is limited, and the sustained release is poor.

The combination of rapid metabolism and small molecular weight can lead to poor tissue deposition and lymphatic guidance, resulting in insufficient targeting of important target organs such as tumors, liver, and lymphatic system; it also causes damage to the whole body. Toxic side effects of non-target organ tissues are relatively increased

Images