Nano microsphere preparation used for chemotherapy of tumors and preparation method thereof

Abstract

The invention belongs to the technical field of the pharmacy of medicine, which relates to a gemcitabine-albumin nano microsphere preparation used for the chemotherapy of the tumors of pancreatic cancer and the like and a preparation method thereof. The invention uses an ethanol precipitation-glutaric dialdehyde crosslinking denaturation method to prepare a slow-release gemcitabine biodegradable albumin nano microsphere. By animal experiments, the result confirms that the invention can obviously enhance the slow-release property and the tissue retention property of the medicine, enhances the concentration of gemcitabine in tumors and other target organs effectively, prolongs the effective acting time of the gemcitabine and reduces the side effect of the medicine. The nano microsphere can be used for the chemotherapy and the interventional chemotherapy of pancreatic cancer and non-small cell lung cancer and is suitable for the venous chemotherapy, the arterial interventional treatment, the local tumor injection interstitial chemotherapy, the celiac chemotherapy and the oral chemotherapy of tumor patients with gemcitabine adaptive diseases.

Description

Technical field [0001] The invention belongs to the technical field of medicine and pharmacy, and relates to a new dosage form of tumor chemotherapy drug-nano microspheres, in particular to a gemcitabine-albumin nanomicrosphere preparation used for tumor chemotherapy such as pancreatic cancer and a preparation method thereof. Background technique [0002] Gemcitabine [gemcitabine, GCB; 2'-deoxy-2', 2'-difluorocytidine monohydrochloride (β isomer); dFdC] is a pyrimidine cell cycle specific anti-tumor drug with a molecular weight of 263.1. GCB is currently the main chemotherapeutic drug for pancreatic cancer and non-small cell lung cancer. It is the only first-line drug approved by the FDA for the treatment of advanced pancreatic cancer. Relevant studies have disclosed that the efficacy comparison with traditional 5-FU is: 23.8% vs 4.8%, P = 0.0022, showing that GCB chemotherapy has obvious advantages. [0003] Gemcitabine hydrochloride lyophilized powder injections are currently us...

AI Technical Summary

Problems solved by technology

[0003] The gemcitabine preparations currently in clinical use are all gemcitabine hydrochloride freeze-dried powder injections. Clinical practice shows that this dosage form has three more serious shortcomings: (1) fast metabolism, short plasma half-life of only about 17 minutes, and insufficient sustained release; ( 2) Small molecular weight, strong hydrophilicity, poor tissue retention and poor targeting of important organs such as tumors, pancreas, liver, spleen, and lungs; (3) The combination of the above two characteristics leads to a large dosage of gemcitabine, and the clinical efficacy reaches If it is less than the satisfactory level, the systemic side effects will also increase

This method of changing the chemical structure can certainly increase the drug loading and stability of the gemcitabine microparticle system, and at the same time partially maintain the drug toxicity of gemcitabine, but the pharmacodynamics, pharmacokinetics, and safety of gemcitabine after changing the structure Both need to be re-evaluated. Clinical treatment practice shows that the above drug delivery systems cannot replace the original gemcitabine.

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