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9-nitrocamptothecin freeze-dried powder injection and preparation method thereof

A technology of nitrocamptothecin and freeze-dried powder injection, which is applied in the direction of freeze-dried delivery, powder delivery, non-effective ingredients of polymer compounds, etc. Poor stability and other problems, to achieve the effect of improving drug safety, cost-free pollution, and simple method

Inactive Publication Date: 2011-08-17
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] The purpose of the present invention is to provide a 9-nitrocamptothecin that can be completely dissolved in clinical application, and has a biological Freeze-dried powder for injection of 9-nitrocamptothecin with high utilization and good stability and preparation method thereof

Method used

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  • 9-nitrocamptothecin freeze-dried powder injection and preparation method thereof
  • 9-nitrocamptothecin freeze-dried powder injection and preparation method thereof
  • 9-nitrocamptothecin freeze-dried powder injection and preparation method thereof

Examples

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Embodiment 1

[0055] Prepare 5ml of 10mM hydroxypropyl-β-cyclodextrin aqueous solution, add 1.5mg of 9-nitrocamptothecin, stir at 50°C in the dark for 2 hours, filter, add 5% mannitol, and freeze-dry to obtain light yellow loose powder.

Embodiment 2

[0057] Prepare 5ml of 10mM glucose-β-cyclodextrin aqueous solution, add 1.5mg of 9-nitrocamptothecin, stir at room temperature in the dark for 5h, filter, add 10% glucose, and freeze-dry to obtain light yellow loose powder.

Embodiment 3

[0059] Prepare 5ml of 8mM β-cyclodextrin phosphate buffer (pH5.0), add 2ml of 9-NC saturated ethanol solution, stir for 3h at room temperature in the dark, remove ethanol by rotary evaporation, filter, add 1% dextran, and freeze-dry to obtain Light yellow loose powder.

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Abstract

The invention belongs to the field of chemical pharmacy, and relates to a compound 9-nitrocamptothecin freeze-dried powder injection and a preparation method thereof. In the invention, 9-nitrocamptothecin is used as the active pharmaceutical ingredient, is mixed with an inclusion material, and is respectively treated by an unsaturated water solution method, a grinding method and a suspension method, thus obtaining the 9-nitrocamptothecin freeze-dried powder injection. The invention overcomes the defects of extremely low water solubility, poor chemical stability, low absolute bioavailability for oral administration, strong stimulus to the gastrointestinal tract and the like of the 9-nitrocamptothecin in the prior art; and the prepared freeze-dried powder injection can be completely dissolved in clinical application and has obviously improved bioavailability. The method has the advantages of simple operation process, low cost and no pollution; and the inclusion compound is easy to store, and is nontoxic and harmless.

Description

technical field [0001] The invention belongs to the field of chemical pharmacy, and in particular relates to a compound 9-nitrocamptothecin freeze-dried powder for injection and a preparation method thereof. Background technique [0002] 9-Nitrocamptothecin (English name: 9-Nitro-20(s)-camptothecin, Latin name: Rubitecan) is a camptothecin derivative and a broad-spectrum antineoplastic drug. Its chemical name is 4-ethyl-4-hydroxy-(s)-10-nitro-1Hpyrano[3,4:6,7]indeno[1,2-b]quinoline-3 , 14(4H,12H)-diketone, molecular formula: C 20 h 15 N 3 o 6 ; Molecular weight: 393.35, with the following chemical structure, [0003] [0004] In the 1970s, Wall first isolated and extracted Camptothecin (CPT) from Camptotheca Acuminata Decsne, Nyssacene. It is a pentacyclic anti-cancer active alkaloid. It is known that it has a significant effect on a variety of animal tumors. It can be used to treat gastric cancer, liver cancer and leukemia, etc. clinically, and has certain effects,...

Claims

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Application Information

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IPC IPC(8): A61K9/19A61K31/4745A61K47/40A61P35/00
Inventor 方晓玲蒋晔沙先谊
Owner FUDAN UNIV
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