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Hydroxycamptothecine injection and its prepn process

A technology for hydroxycamptothecin and alkali injection, which can be used in pharmaceutical formulations, drug combinations, antitumor drugs and other directions, can solve the problems of affecting the curative effect, inaccurate content determination, increased toxicity, etc., and achieves a simple and feasible preparation process. The effect of strong control and high safety

Inactive Publication Date: 2006-03-01
四川标新医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In the 1970s, the domestic Shanghai Institute of Materia Medica made HCPT sodium salt injection and put it on the market for the treatment of primary liver cancer, gastrointestinal cancer, leukemia, head and neck glandular skin cancer, and bladder cancer. Alkali is insoluble in water, and its injections have always used NaOH solution as a solvent, so that the physical and chemical properties of the preparation are not stable enough, easy to oxidize, the toxicity increases after oxidation, the solution changes color, and affects the curative effect; and the quality control method adopts ultraviolet spectrophotometry. Interference, inaccurate content determination

Method used

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  • Hydroxycamptothecine injection and its prepn process
  • Hydroxycamptothecine injection and its prepn process

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] R x1 50ml: 10mg

[0032] Hydroxycamptothecin 0.10g

[0033] L-Arginine 0.390g

[0034] Sodium chloride 4.27g

[0035] Hydrochloric acid (1mol / L) appropriate amount

[0036] Add water for injection to 500ml

[0037] Preparation process: Take L-arginine and add 250ml of water for injection to dissolve, add hydroxycamptothecin, stir, add sodium chloride after the solution is clear, stir and mix well, adjust the pH to about 8.3 with hydrochloric acid, then add water for injection to 500ml , measure the content and pH value, filter through a 0.45 μm microporous membrane after passing the test, potting, and autoclave at 115° C. for 30 minutes to obtain the product.

[0038] Detection method::

[0039] Instrument: (Shimadzu) LC-10A liquid chromatograph

[0040] Chromatographic column ALTEX ULTRSPHERE-ODS (4.6×150mm, 5um)

[0041] The mobile phase is methanol-0.4% phosphoric acid aqueous solution (57:43)

[0042] Detection wavelength 342nm Column temperature 40℃ Flow ...

Embodiment 2

[0045] R x1 100ml: 9mg

[0046] Hydroxycamptothecin 0.09g

[0047] L-Arginine 0.43g

[0048] Sodium chloride 9.30g

[0049] Hydrochloric acid (1mol / L) appropriate amount

[0050] Add water for injection to 1000ml

[0051] The preparation process is the same as in Example 1.

Embodiment 3

[0053] R x1 250ml: 11mg

[0054] Hydroxycamptothecin 0.11g

[0055] L-Arginine 0.47g

[0056] Sodium chloride 22.48g

[0057] Hydrochloric acid (1mol / L) appropriate amount

[0058] Add water for injection to 2500ml

[0059] The preparation process is the same as in Example 1.

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Abstract

The hydroxycamptothecine injection has the active components comprising hydroxycamptothecine in 0.9-1.1 molar portions, and L- arginine or arginine hydrochloride in 1-75 molar portions. The present invention provides the preparation process and quality control method of the hydroxycamptothecine injection. The present invention overcomes the water solubility problem of hydroxycamptothecine, and the hydroxycamptothecine injection has high stability, lowered toxicity and high antitumor activity.

Description

technical field [0001] The invention relates to an antitumor drug, in particular to an injection containing hydroxycamptothecin, belonging to the field of drugs. Background technique [0002] Camptothecin is an alkaloid extracted from Doveiaceae plants, which has high anti-tumor activity and has obvious effect on inhibiting tumor pain. However, the toxicity of camptothecin affects its clinical application. The clinical toxicity is mainly manifested in the urinary system, cardiovascular system and digestive system. The urinary system is the most prominent, such as frequent urination, dysuria and hematuria. Hydroxycamptothecin (HCPT) also has significant anti-tumor activity, has the characteristics of broad anti-cancer spectrum, remarkable curative effect, and small toxic and side effects, especially for primary liver cancer, gastrointestinal cancer, bladder cancer, head and neck skin cancer, It has a significant curative effect on malignant tumors such as leukemia and cervic...

Claims

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Application Information

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IPC IPC(8): A61K31/475A61K9/08A61P35/00
Inventor 吴四灵
Owner 四川标新医药科技有限公司
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