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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: 2013-12-25
AFFILIATED HUSN HOSPITAL OF FUDAN UNIV
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  • Summary
  • 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, 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.

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

Examples

Experimental program
Comparison scheme
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 Add 3.0 mL of ethanol to the albumin solution at a rate of 1.0 mL / min while stirring until blue opalescence is formed. After stirring for 10 min, add 2.5 μL of cross-linking agent glutaraldehyde, and continue stirring for 12 h to promote the cross-linking of nanoparticles Solidified, evaporated to remove ethanol under reduced pressure at 40°C, and 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 value to 9.0 with 1M NaOH solution, add 5.0mL of absolute ethanol at a speed of 1.0mL / min while stirring to form a milky colloidal suspension, stir In some cases, 15 μL of glutaraldehyde was added, stirring continuously for 6 hours to promote cross-linking and solidification of albumin nanoparticles, evaporation of ethanol under reduced pressure at 30°C, and freeze-drying to obtain gemcitabine albumin nanoparticles.

Embodiment 3

[0043]Dissolve 100mg of albumin and 10mg of gemcitabine hydrochloride in 2mL of normal saline, adjust the pH value to 9.0 with 1M NaOH solution, add 5mL of acetone solution at a speed of 1.0mL / min under stirring to form a milky colloidal suspension, under stirring Add 30 μL of glutaraldehyde, stir continuously 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 nanoparticles.

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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 chemotherapeutic drugs-nano microspheres, in particular to a gemcitabine-albumin nano microsphere preparation for pancreatic cancer and other tumor chemotherapy 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 antineoplastic drug with a molecular weight of 263.1. GCB is currently the main chemotherapeutic drug for clinical pancreatic cancer and non-small cell lung cancer and other tumors. It is the only first-line drug approved by the FDA for the treatment of advanced pancreatic cancer so far. The results of the comparison with the traditional 5-FU curative effect are disclosed in relevant studies: 23.8% vs 4.8%, P=0.0022, showing that GCB chemotherapy has obvious advantages. [0003] The gem...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/16A61K31/7068A61K47/42A61P35/00
Inventor 金忱李骥傅德良蒋永剑狄扬侯惠民倪泉兴
Owner AFFILIATED HUSN HOSPITAL OF FUDAN UNIV
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