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Camptothecin medicament injection solution and injection and preparation method thereof

A technology of camptothecin and injections, which is applied in the field of medicine, can solve problems such as difficulty in making injections, and achieve the effects of improving safety and effectiveness, improving stability, and increasing dispersion

Inactive Publication Date: 2010-05-19
SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The active ingredient of the medicine used in the present invention is a camptothecin drug mainly in the form of a lactone ring, which can improve the therapeutic activity of the drug and reduce toxic and side effects; the used dispersion medium is an emulsion for injection, which can increase the concentration of the camptothecin drug. Dispersion solves the problem that camptothecin drugs are difficult to make into injections because of their poor water solubility; the present invention packs camptothecin drug injection solutions and injection emulsions separately and stores them, and mixes them evenly before use for intravenous injection. Administration, which can improve the stability of long-term storage drug

Method used

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  • Camptothecin medicament injection solution and injection and preparation method thereof
  • Camptothecin medicament injection solution and injection and preparation method thereof
  • Camptothecin medicament injection solution and injection and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0055] Embodiment 1 prepares 10-hydroxycamptothecin injection solution and injection thereof

[0056] 1. Preparation of 10-hydroxycamptothecin injection solution

[0057] Weigh 1.0 g of 10-hydroxycamptothecin and 0.0005 g of disodium edetate, add it to an appropriate amount of polyethylene glycol 400, stir and dissolve at 40°C, and then dilute to 100 ml with polyethylene glycol 400 ; use citric acid to adjust the pH value to 4.15; add 0.50 grams of activated carbon for needles, absorb at a temperature of 30 ° C for 25 minutes, then filter with a 0.22 μm microporous membrane, pack in plastic or glass bottles, seal, Sterilize with circulating steam at 100°C for 30 minutes, and store for future use. Keep away from light during the whole preparation process.

[0058] 2. Preparation of Emulsion for Injection

[0059] Take 100 grams of caprylic triglyceride for injection and 100 grams of soybean oil, heat it in a water bath to 75°C, add 12 grams of egg yolk phospholipids for inje...

Embodiment 2

[0066] Embodiment 2 prepares 10-hydroxycamptothecin injection solution and injection thereof

[0067] 1. Preparation of 10-hydroxycamptothecin injection solution

[0068] Take 1.1 g of 10-hydroxycamptothecin, add it to an appropriate amount of polyethylene glycol 400, stir and dissolve at 35 ° C, and then use polyethylene glycol 400 to make the volume to 100 ml; adjust the pH value to 4.28 with citric acid; add 0.2 g of activated carbon for needles, adsorbed at 25°C for 35 minutes, then filtered with a 0.22 μm microporous membrane, packed in plastic or glass bottles, sealed, and sterilized in a rotary autoclave at 115°C for 20 minutes , store for later use. Keep away from light during the whole preparation process.

[0069] 2. Preparation of Emulsion for Injection

[0070] Take 200 grams of soybean oil for injection, heat it to 75°C in a water bath, add 12 grams of egg yolk phospholipids for injection, stir to dissolve to obtain an oil phase; take 700 ml of water for inject...

Embodiment 3

[0075] Embodiment 3 prepares 10-hydroxycamptothecin injection solution and injection thereof

[0076] 1. Preparation of 10-hydroxycamptothecin injection solution

[0077] Take 0.7 g of 10-hydroxycamptothecin and 0.01 g of vitamin E, add it to an appropriate amount of polyethylene glycol 400, stir and dissolve at 45 ° C, then use polyethylene glycol 400 to make the volume to 100 ml; adjust the pH with citric acid value to 3.95; add 0.8 g of activated carbon for needles, absorb at 45°C for 60 minutes, then filter with a 0.22 μm microporous membrane, pack in plastic or glass bottles, seal, and sterilize at 121°C for 15 minutes. Store for later use. Keep away from light during the whole preparation process.

[0078] 2. Preparation of Emulsion for Injection

[0079] Take 50 grams of soybean oil and 50 grams of caprylic triglyceride, mix them, heat in a water bath to 60°C, add 12 grams of egg yolk phospholipids for injection, cut and dissolve to obtain an oil phase; take 800 ml o...

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Abstract

The invention relates to the technical field of medicaments, in particular to a camptothecin medicament injection solution and an injection and a preparation method thereof. The invention provides a camptothecin medicament injection which is good in stability, high in curative effect and low in toxicity and consists of the camptothecin medicament injection solution and a disperse medium, wherein the camptothecin medicament injection solution consists of a medicament active component, a stabilizing agent, a pH value regulator and an injection solvent. The medicament active component of the camptothecin medicament injection solution is a camptothecin medicament mainly existing in the form of a lactonic ring, which can improve the curative activity of the medicament and reduce toxic side effects; and the disperse medium is an injection emulsion, which can improve the dispersion degree of the camptothecin medicament and solve the problem that the camptothecin medicament is difficult to be prepared into the injection due to poor water solubility. The camptothecin medicament injection solution and the injection emulsion are packed and then stored respectively, and are mixed uniformly before use for intravenous administration, so the stability of the medicaments stored for a long time can be improved. The invention provides an intravenous injection which has low toxicity and is save and convenient to store for camptothecin medicaments.

Description

technical field [0001] The invention relates to the technical field of medicine, and relates to a camptothecin drug injection solution, an injection and a preparation method thereof. Background technique [0002] Camptothecins are a kind of indole alkaloids with anti-tumor effect extracted and isolated from the trunk, bark and fruit of Camptotheca involucrata, which is a kind of topoisomerase I. Inhibitor. At present, it is mainly used in the treatment of malignant tumors such as bladder cancer, rectal cancer, liver cancer, gastric cancer, ovarian cancer, and leukemia. The α-hydroxylactone ring on the E ring in the chemical structure of camptothecin drugs has two forms: open ring and closed ring, both of which are active forms of camptothecin drugs, but the activities of the two are quite different. Slichemeyer et al. (J.Natl.Cancer.Inst.(1993) 85,271-291.) reported that the inhibitory effect of camptothecins in the form of lactone rings on topoisomerase I is much greater ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/08A61K9/107A61K31/4745A61K47/34A61K47/12A61K47/18A61K47/22A61K47/44A61P35/00A61K47/10
Inventor 陈建明陈明顾芃高保安邓莉刘文丽张佳良黄硕孙靖杨秋霞刘薇张莹莹
Owner SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
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