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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: 2012-07-25
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

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] Example 1 Preparation of raltitrexed for injection

[0025] Composition of prescription:

[0026]

[0027] Preparation Process:

[0028] (1) Weigh the prescription amount of disodium hydrogen phosphate dodecahydrate, add 50% of the total volume of water for injection to dissolve it, and then add the prescription amount of raltitrexed and stir to dissolve to obtain solution I;

[0029] (2) Weigh the prescribed amount of sodium chloride, add 45% of the total volume of water for injection, stir to dissolve it, weigh 0.1% of the prepared amount of activated carbon for needles into the solution, keep it at 60°C and stir for 30 minutes, filter and remove Carbon, get solution II;

[0030] (3) Add the said solution I to 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. Filter with 0.22μm microporous membrane;

[0031] (4) Filling the liquid med...

Embodiment 2

[0033] Example 2 Preparation of raltitrexed for injection

[0034] Composition of prescription:

[0035]

[0036] Preparation Process:

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

[0038] (2) Weigh the prescribed amount of sodium chloride, add 45% of the total volume of water for injection, stir to dissolve it, weigh 0.1% of the prepared amount of activated carbon for needles into the solution, keep it at 60°C and stir for 30 minutes, filter and remove Carbon, get solution II;

[0039] (3) Add the said solution I to 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. Filter with 0.22μm microporous membrane;

[0040] (4) Filling the liq...

Embodiment 3

[0042] Example 3 Preparation of raltitrexed for injection

[0043] Composition of prescription:

[0044]

[0045]

[0046] Preparation process: the same as in Example 2.

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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, and belongs 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-thenoyl]-L-glutamic acid, a thymus synthase inhibitor, belongs to a quinazoline folate analog. In the body, raltitrexed is actively taken up by cells and quickly metabolized by folate-based polymerized glutamate synthase into a series of polyglutamate. These metabolites have a stronger inhibitory effect on thymus synthase than raltitrexed, thus Inhibit the synthesis of cell DNA, and can stay in the cell for a long time. In the treatment of colorectal cancer, the efficacy is similar to that of fluorouracil, but the incidence of side effects with raltitrexed is low, the method is simple, and the patient is easy to accept. [0003] Although th...

Claims

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Application Information

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IPC IPC(8): A61K9/19A61K31/517A61K47/02A61P35/00
Inventor 冯艳
Owner NANJING CHIA TAI TIANQING PHARMA
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