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Tegafur and gimeracil compound injecta

A technology of injection and tegafur, which is applied in the field of injection, can solve the problems of large differences in individual drug absorption, difficult preparation technology, and drug malabsorption, etc., so as to alleviate the weight loss of the small intestine, achieve good therapeutic effect, and reduce gastrointestinal side effects Effect

Active Publication Date: 2012-01-11
TIANJIN JINYAO GRP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Mainly, however, we found that due to the gastrointestinal toxicity of the drug, the malabsorption of the drug caused by the disorder of the digestive system caused by the change of the gastrointestinal environment in patients with gastrointestinal tumors, and the large difference in individual drug absorption, the above-mentioned compound preparations in the There are still some defects when it is used to treat tumors, especially gastrointestinal tumors
Since gimelast and oteracil potassium are raw materials that are not easily soluble in water and can only be dissolved in strong alkali solutions, there are technical difficulties in the preparation of injections containing gimelast and oteracil potassium

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0013] Tegafur 10g, Gimexast 2.18g 0.1M Potassium Hydroxide Solution, Sodium Sulfite 1g

[0014] Water for injection to 1000ml, the water for injection is pre-adjusted to pH 10 with 0.1M potassium hydroxide

[0015] Take 800ml of water for injection with adjusted pH, heat it to 40°C, add active ingredients such as tegafur and gimexast, stir to dissolve, add sodium sulfite, add water for injection with adjusted pH to the prescribed amount, filter and sterilize, and pack To 100 ampoules, each bottle contains 100mg tegafur, 21.8mg gimexast.

Embodiment 2

[0017] Tegafur 5g, Gemelast 1.09g, 0.1M Potassium Hydroxide Solution

[0018] Water for injection to 1000ml, the water for injection is pre-adjusted to pH 10 with 0.1M potassium hydroxide

[0019] Take 800ml of water for injection with adjusted pH, heat it to 40°C, add active ingredients such as tegafur and gimexast, stir to dissolve, make up the water for injection with adjusted pH to the prescribed amount, filter and sterilize, and pack into 100 ampoules Each dose contains 50mg of tegafur and 10.9mg of gimelast.

Embodiment 3

[0021] Tegafur 10g, Gemelast 2.18g, 1M Potassium Carbonate Solution

[0022] Water for injection to 1000ml, the water for injection is pre-adjusted to pH 10 with 1M potassium carbonate solution

[0023] Take 800ml of water for injection with adjusted pH, heat it to 40°C, add active ingredients such as tegafur and gimexast, stir to dissolve, make up the water for injection with adjusted pH to the prescribed amount, filter and sterilize, and pack into 100 ampoules Each dose contains 100mg tegafur and 21.8mg gimelast.

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PUM

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Abstract

The invention discloses tegafur and gimeracil compound injecta, comprising tegafur, gimeracil, one or several kinds of auxiliaries suitable for injecta, and the balance of water for injection, wherein the tegafur and the gimeracil serve as active constituents, and the tegafur and gimeracil compound injecta is characterized in that the molar ratio of tegafur to gimeracil to oteracil potassium is 1:(0.2-0.4):1.

Description

[0001] The invention relates to an injection, in particular to a compound injection of tegafur and gimester. Background technique [0002] Tegafur (Tegafur, CAS: 17902-23-7) is the prodrug of the antineoplastic drug fluorouracil, which has good therapeutic activity on gastrointestinal tumors, head and neck tumors and breast cancer. In comparison, the toxicity of tegafur is only 1 / 7-1 / 4 of that, while the chemotherapy index has been doubled. The currently commercially available tegafur preparations include tegafur injection (5ml, 0.2g) and oral preparations. Tegafur tablets (50mg), the dosage when using Tegafur alone for treatment is 8000-1200mg / d. Japan's Dapeng Pharmaceutical Co., Ltd. has developed a tegafur compound preparation with the trade name TS-1, which consists of tegafur, gimexast (CAS: 103766-25-2, CDHP for short) and oteracil potassium (CAS : 2207-75-2, also known as potassium oxonate, referred to as OXO) according to the molar ratio of 1:0.4:1 composition, for t...

Claims

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Application Information

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IPC IPC(8): A61K31/513A61K31/4412A61K9/08A61P35/00
Inventor 孙亮陈松赵琳
Owner TIANJIN JINYAO GRP
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