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Artemether-containing pharmaceutical composition and its preparation and use

A pharmaceutical preparation and composition technology, which is applied in the direction of drug combination, medical preparations containing active ingredients, drug delivery, etc., can solve the problems of malaria parasite cell structure and function destruction

Inactive Publication Date: 2014-06-11
KPC PHARM INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Oxygen bridge is covered by Fe 2+ After catalytic cleavage, oxygen free radicals are first produced, and then converted into more active carbon free radicals through molecular rearrangement. Alkylation of macromolecules in many organisms, so artemisinin is now thought to be more likely to be active through carbon free radicals

Method used

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  • Artemether-containing pharmaceutical composition and its preparation and use
  • Artemether-containing pharmaceutical composition and its preparation and use
  • Artemether-containing pharmaceutical composition and its preparation and use

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] Example 1: Effect of artemether lyophilized powder preparation on the growth of human tumor cells (compared with other artemisinin derivatives)

[0036] (1) Materials and methods

[0037] 1. Test sample and preparation

[0038] (1) Test sample

[0039] Artemether freeze-dried powder preparation, artemether API, artemisinin, dihydroartemisinin, and artesunate were provided by the Research Institute of Kunming Pharmaceutical Group Co., Ltd.

[0040] (2) Sample and preparation

[0041] ① Preparation of test samples

[0042] Five test concentrations of 2, 10, 50, 250 and 500 μM were set for the five artemisinin derivatives. Artemether raw materials, artemisinin, dihydroartemisinin, and artesunate are dissolved in dimethyl sulfoxide (DMSO), and artemether lyophilized powder preparations are dissolved in normal saline (N.S.), and then a certain amount of RPMI 1640 complete culture solution is prepared into high-concentration solution, and each low-concentration solution ...

Embodiment 2

[0078] Example 2: Effect of artemether freeze-dried powder preparation on the growth of transplanted tumor in mice

[0079] (1) Effect on the growth of transplanted sarcoma S180 in mice

[0080] 1. Materials and methods

[0081] (1) Test sample

[0082] The artemether freeze-dried powder preparation was provided by the Research Institute of Kunming Pharmaceutical Group Co., Ltd.

[0083] (2) Preparation of artemether freeze-dried powder preparation (the amount tested is the amount of the artemether raw material contained in it, the same below)

[0084] Weigh a certain amount of artemether freeze-dried powder, dissolve it with normal saline (N.S), and give it at the rate of 0.2ml / 10g body weight

[0085] Drug volume, 20mg / kg high dose is prepared into a solution of the corresponding concentration, and the medium and low doses are prepared by diluting the high dose concentration solution with N.S solution in proportion.

[0086] (3) Experimental method

[0087] ①Establishment...

Embodiment 3

[0144] Example 3: Effect of artemether freeze-dried powder preparation on the growth of transplanted tumors in nude mice with human gastric cancer

[0145] (1) Materials and methods

[0146] 1. Test sample and preparation

[0147] (1) Test sample

[0148] Freeze-dried artemether powder was provided by the Research Institute of Kunming Pharmaceutical Group Co., Ltd.

[0149] (2) Preparation of test samples

[0150]Weigh a certain amount of artemether freeze-dried powder H freeze-dried powder and dissolve it with N.S. According to the administration volume of 0.15ml / 10g body weight, prepare a solution with a corresponding concentration of 30mg / kg at a high dose. Low and medium doses (3, 10mg / kg ) is prepared by diluting proportionally with N.S solution at a high dosage concentration.

[0151] (3) Preparation of positive control

[0152] Take 5-fluorouracil (5-Fu) stock solution at a dose of 10mg / kg, and dilute it with N.S to the required concentration according to the admin...

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Abstract

The invention relates to the field of medicine and discloses an artemether-containing pharmaceutical composition and its preparation and use in preparation of drugs for treating tumors. The artemether-containing pharmaceutical composition for treating tumors contains artemether or dihydroartemisinin and a chalybeate.

Description

technical field [0001] The invention relates to the field of medicine, in particular to a pharmaceutical composition and preparation containing artemether and its use in the preparation of medicines for treating tumors. Background technique [0002] Artemether, chemical name is (3R, 5αS, 6R, 8αS, 9R, 10S, 12R, 12αR)-decahydro-10-methoxy-3,6,9-trimethyl-3,12-oxo -12H-pyrano[4,3-j]-1,2-benzodisepin, the molecular formula is C 16 h 26 o 5 , the structural formula is as follows: [0003] [0004] It is used for various types of malaria, mainly for the treatment of anti-chloroquine falciparum malaria and the first aid of dangerous type falciparum malaria. [0005] Artemisinin and its derivatives have recognized antimalarial efficacy. Studies have found that the in vivo metabolic active product of artemisinin and its derivatives is dihydroartemisinin, which has high antimalarial activity and low toxicity. Many scholars have conducted detailed studies on the peroxygen brid...

Claims

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Application Information

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IPC IPC(8): A61K33/26A61K31/357A61K31/366A61P35/00
CPCA61K31/357A61K9/19A61K33/26A61K9/0019A61K9/2081A61P35/00A61P43/00A61K2300/00
Inventor 卿晨陈云建代晓阳张雁丽陈亚娟刘一丹杨兆祥杨旭娟朱泽
Owner KPC PHARM INC