Medicine composition containing raltitrexed and preparation method of medicine composition

A technology of raltitrexed and its composition, which is applied in the field of pharmaceutical composition containing raltitrexed and its preparation, can solve the problems of clinical popularization and application limitations, sensitivity to light, humidity, heat, and unresolved stability problems, etc. Reach the effect of good resolubility and stability and reduce cost

Active Publication Date: 2013-12-04
NANJING CHIA TAI TIANQING PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Although the anti-colorectal cancer pharmacological activity of raltitrexed has great market competitiveness, the physical and chemical properties of raltitrexed are unstable, sensitive to light, humidity and heat, and almost insoluble in water, which gives the Clinical use of compounds poses great difficulties
At present, although the clinically approved powder injection solves the solubility problem, the stability problem has not been solved, and the product must be kept at a temperature below 8°C, which has brought certain restrictions to the clinical application of the drug.

Method used

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  • Medicine composition containing raltitrexed and preparation method of medicine composition
  • Medicine composition containing raltitrexed and preparation method of medicine composition
  • Medicine composition containing raltitrexed and preparation method of medicine composition

Examples

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Effect test

Embodiment 1

[0024] The preparation of embodiment 1 injection raltitrexed

[0025] Prescription composition:

[0026]

[0027] Preparation Process:

[0028] (1) Take by weighing the disodium hydrogen phosphate dodecahydrate of prescription quantity, after adding the water for injection of total volume 50% amount to dissolve clearly, then add the prescription quantity of raltitrexed and stir to dissolve, obtain solution I;

[0029] (2) Take by weighing the sodium chloride of recipe quantity, add the water for injection of total volume 45% amount, stir to make it dissolve, take by weighing 0.1% activated carbon for needles of preparation amount and add in this solution, keep stirring at 60 ℃ for 30min, filter and remove carbon, to obtain solution II;

[0030] (3) Add the solution I into the solution II, stir evenly, adjust the pH=7.6-7.8 with 0.1mol / L sodium hydroxide, add the remaining amount of water for injection cooled to below 30°C and mix to obtain the medicinal solution, and then...

Embodiment 2

[0033] The preparation of embodiment 2 injection raltitrexed

[0034] Prescription composition:

[0035]

[0036] Preparation Process:

[0037] (1) Take by weighing the disodium hydrogen phosphate dodecahydrate of the prescription amount, add 50% of the total volume of water for injection to dissolve it, then add the prescription amount of raltitrexed and azacitidine (Azacitidine) and stir to dissolve, to obtain Solution I;

[0038] (2) Take by weighing the sodium chloride of recipe quantity, add the water for injection of total volume 45% amount, stir to make it dissolve, take by weighing 0.1% activated carbon for needles of preparation amount and add in this solution, keep stirring at 60 ℃ for 30min, filter and remove carbon, to obtain solution II;

[0039] (3) Add the solution I into the solution II, stir evenly, adjust the pH=7.6-7.8 with 0.1mol / L sodium hydroxide, add the remaining amount of water for injection cooled to below 30°C and mix to obtain the medicinal so...

Embodiment 3

[0042] The preparation of embodiment 3 injection raltitrexed

[0043] Prescription composition:

[0044]

[0045]

[0046] Preparation process: with embodiment 2.

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PUM

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Abstract

The invention relates to a medicine composition containing raltitrexed and a preparation method of the medicine composition. Raltitrexed freeze-dried injection is preferably selected as the medicine composition. The preparation method comprises the steps of: weighing sodium phosphate dibasic dodecahydrate, adding injection water for dissolving, adding raltitrexed for stirring and dissolving to obtain a solution I; weighing sodium chloride, adding injection water for dissolving, removing carbon through filtering to obtain a solution II; adding the solution I into the solution II, uniformly stirring, regulating the pH to be 7.6-7.8 by using sodium hydroxide, filtering after constant volume; and filling a medicine solution, partially plugging, loading in a tray, and drying through freezing. According to the invention, the defect of poor stability of the medicine composition is effectively overcome while the problem of the solubility of the raltitrexed is solved.

Description

technical field [0001] The invention relates to a pharmaceutical composition containing raltitrexed and a preparation method thereof, belonging to the technical field of western medicine preparations. Background technique [0002] The chemical name of Raltitrexed is N-[5-[N-methyl-N-(2-methyl-4-oxo-3,4-dihydroquinazolin-6-ylmethyl )amino]-2-thienyl]-L-glutamic acid, a thymus synthase inhibitor, belongs to the class of quinazoline folate analogues. In vivo, after being actively taken up by cells, raltitrexed is quickly metabolized into a series of polyglutamic acids by folate-based polyglutamic acid synthase, and these metabolites have a stronger inhibitory effect on thymus synthase than raltitrexed, thereby Inhibits the synthesis of cellular DNA, and can be retained in cells to exert an inhibitory effect for a long time. In the treatment of colorectal cancer, the curative effect is similar to that of fluorouracil, but the incidence of side effects of raltitrexed is low, th...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/19A61K31/517A61K47/02A61P35/00
Inventor 冯艳
Owner NANJING CHIA TAI TIANQING PHARMA
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