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9-nitrocamptothecin solid dispersant and preparation method

A technology of nitrocamptothecin and solid dispersion, which is applied in the direction of pharmaceutical formulations, drug combinations, anti-tumor drugs, etc., can solve the problems of gastrointestinal irritation, loss of activity, inability to increase drug stability, Increase solubility and reduce irritation effect

Inactive Publication Date: 2006-01-11
FUDAN UNIV +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The solubility of 9-nitrocamptothecin in water is extremely small, and its T 50 44.79min, T d 308.04min, unable to directly prepare qualified preparations from raw materials
The chemical stability of the drug is poor, it is easy to degrade when exposed to light, and when it encounters alkali and water, the lactone ring is easy to open and lose its activity
The absolute bioavailability of oral administration is low, only about 10%, and the oral administration is very irritating to the gastrointestinal tract

Method used

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  • 9-nitrocamptothecin solid dispersant and preparation method

Examples

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Comparison scheme
Effect test

Embodiment 1

[0049] Take 50mg of 9-nitrocamptothecin and 1000mg of poloxamer 188, grind and mix them evenly, put them in an evaporating dish, heat them in a water bath at about 55-60°C to melt, stir them vigorously, put them in an ice-salt bath, and cool them down rapidly to solidify. Put it in the freezer for 2 hours to fully solidify it, put it in the desiccator for 2 days, take it out, grind it, and pass it through an 80-mesh sieve.

Embodiment 2

[0051] Take 40mg of 9-nitrocamptothecin and 800mg of polyethylene glycol 6000, grind and mix evenly, place in an evaporating dish, heat in a water bath (about 60°C) to melt, stir vigorously, place in an ice-salt bath, cool and solidify rapidly, Put it in the freezer for 2 hours to fully solidify it, put it in the desiccator for 3 days, take it out, grind it, and pass it through an 80-mesh sieve.

Embodiment 3

[0053] Take some polyethylene glycol 6000, put it in a mortar and grind it, the rotation speed is 200rpm, the grinding time is 20min, and set aside. Take 40mg of 9-nitrocamptothecin and 800mg of polyethylene glycol 6000 (pulverized) and place them together in a mortar for grinding at a rotational speed of 200 rpm for 30 minutes. Pass through a 120-mesh sieve.

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Abstract

The present invention relates to a compound 9-nitrocamptothecine solid dispersion and its preparation method. Said invention adopts 9-nitrocamptothecine as medicine active componnet, and adds carrier material, and separately adopts grinding method, freeze-drying method, melting method and solvent method to prepare the invented product which can be made into capsule, table and drip pill. It can raise solubility of medicine, as compared with raw material medicine its resolution speed can be raised by 4-80 times, it can promote absorption, can reduce irritation of medicine to stomach and intestine and can raise stability of the medicine.

Description

technical field [0001] The invention belongs to the field of chemical pharmacy, and in particular relates to a compound 9-nitrocamptothecin solid dispersion 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. The camptothecin is a pentacyclic anticancer active alkaloid. It is known that it has significant curative effects on various animal tumors. It can treat gastric cancer, liver cancer and leukemia, etc. clinically, and has certain effects. However, du...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/4741A61K9/00A61P35/00
Inventor 方晓玲韩丽珠杨敏王明坤李君婵吴云绢朱宇江
Owner FUDAN UNIV
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