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

A technology of nano-microspheres and preparations, which is applied in the direction of antineoplastic drugs, medical preparations containing active ingredients, and pharmaceutical formulas, and can solve problems such as unsatisfactory clinical efficacy, increased systemic toxic and side effects, and large dosage of gemcitabine. , to achieve the effects of prolonged residence time in the body, large toxic and side effects, and large dosage

Inactive Publication Date: 2010-06-16
AFFILIATED HUSN HOSPITAL OF FUDAN UNIV
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  • Abstract
  • Description
  • Claims
  • Application Information

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, a

Method used

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

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Experimental program
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Effect test

Embodiment 1

[0039] Dissolve 20mg albumin in 1mL water for injection, adjust the pH value to 8.5 with 1M NaOH solution, dissolve 1.25mg gemcitabine hydrochloride in 100μL water for injection, adjust the pH value to about 9.0 with 1M NaOH solution, add the drug solution under stirring To the albumin solution, add 3.0 mL of ethanol at a rate of 1.0 mL / min under stirring to form a blue opalescence. After stirring for 10 minutes, add 2.5 μL of the cross-linking agent glutaraldehyde, and continue stirring for 12 hours to promote the cross-linking of the nanoparticles After solidification, the ethanol was removed by evaporation under reduced pressure at 40° C., and then freeze-dried to obtain gemcitabine albumin nanospheres.

Embodiment 2

[0041] Dissolve 50mg of albumin and 10mg of gemcitabine hydrochloride in 2mL of normal saline, adjust the pH to 9.0 with 1M NaOH solution, add 5.0mL of absolute ethanol at a rate of 1.0mL / min under stirring to form a latex colloidal suspension, stir Under the circumstances, 15 μL of glutaraldehyde was added, continuously stirred for 6 hours to promote the cross-linking and solidification of albumin nanoparticles, the ethanol was evaporated under reduced pressure at 30° C., and the mixture was freeze-dried to obtain gemcitabine albumin nanospheres.

Embodiment 3

[0043] Dissolve 100mg albumin and 10mg gemcitabine hydrochloride in 2mL normal saline, adjust the pH to 9.0 with 1M NaOH solution, add 5mL acetone solution at 1.0mL / min while stirring to form a latex colloidal suspension, under stirring Add 30 μL of glutaraldehyde, continue stirring for 8 hours to promote cross-linking and solidification of albumin nanoparticles, evaporate acetone under reduced pressure at 30°C, and freeze-dry to obtain gemcitabine albumin nanospheres.

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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...

Claims

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Application Information

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IPC IPC(8): A61K9/16A61K31/7068A61K47/42A61P35/00
Inventor 倪泉兴傅德良侯惠民金忱虞先浚徐近龙江蒋永剑李骥狄扬
Owner AFFILIATED HUSN HOSPITAL OF FUDAN UNIV
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