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Compound antimalarial composition

A composition and compound technology, applied in the field of pharmaceutical preparations, can solve the problems of affecting the antimalarial effect of drugs, low bioavailability, and obvious first-pass effect, and achieve the advantages of drug safety, simple preparation process, and low energy consumption.

Inactive Publication Date: 2014-12-24
INST OF CHINESE MATERIA MEDICA CHINA ACAD OF CHINESE MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, in the use of conventional artemisinin preparations, there are problems such as fast drug metabolism in the body, low bioavailability, and obvious first-pass effect, and multiple consecutive administrations are required to maintain the effective blood drug concentration. [3,4] , not only the patient's compliance is low, but also affects the antimalarial effect of the drug

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0061] Embodiment 1: Preparation of compound antimalarial elastosome gel ointment of the present invention

[0062]

[0063]

[0064]

[0065]

[0066] Preparation of artesunate ethosome / etobutan ethosome gel ointment:

[0067] (1) Preparation of artesunate ethosome:

[0068] Equipment and materials

[0069] Magnetic stirrer: C-MAG HS4 magnetic stirrer (IKA, Germany); analytical balance: BSA224S CW electronic analytical balance (Sartorius, Germany); filter: disposable syringe filter (Ф13, 0.22 μm , PTFE) (Tianjin Jinteng Experimental Equipment Co., Ltd.).

[0070] Take each component of each prescription amount, first artesunate and cholesterol are added in the 25ml tool sieve Erlenmeyer flask, and in Erlenmeyer flask, add whole recipe amount low-molecular alcohol, adopt magnetic stirrer to stir (stirring condition: 25 -40°C, 200-800 rpm), after the artesunate and cholesterol are dissolved, add the antioxidant to the low-molecular alcohol solution, and stir unde...

Embodiment 2

[0079] Example 2: Characterization of artesunate ethosomes and ethotoplasts

[0080] (1) Measurement of the particle size of artesunate ethotoplasts and ethotoplasts

[0081] Test Equipment

[0082] Zetasizer Nano ZS nanoparticle size analyzer (Malvern, UK); DTS0012 sample cell.

[0083] Test object

[0084] In Example 1, artesunate ethosomes and ethotoplasts for gel ointment 8 were prepared.

[0085] testing method

[0086] Add 1ml of artesunate ethosome and ethotoplast stock solution to DTS0012 sample cell respectively, and place the sample cell in Zetasizer Nano ZS to measure the particle size of the two.

[0087] Test Results

[0088] In Example 1, the particle diameters of artesunate ethosomes and ethotoplasts used to prepare gel ointment 8 are respectively: 26.48 ± 0.12nm and 28.58 ± 0.24nm (see figure 1 and figure 2 ).

[0089] Using the same method as above, the particle diameters of artesunate ethosomes and ethotoplasts of other gel pastes 1-7 and 9-10 were...

Embodiment 3

[0100] Example 3: Research on transdermal performance of compound antimalarial elastosome gel ointment of the present invention

[0101] Comparative study on the drug transdermal performance of artesunate ethosome / ethotoplast gel ointment and artesunate / ethotoplast gel ointment under the same drug loading.

[0102] sample preparation

[0103] (1) Preparation of artesunate / ephrine gel ointment

[0104] Prepare the gel paste matrix according to the gel paste base preparation method of gel paste 8 in Example 1; take each adjuvant and medicine according to the artesunate ethosome prescription and ethotoplast prescription in gel paste 8 , but the ethosome preparation process is not carried out, only the auxiliary materials (including drugs) are mixed with the gel paste base, so as to prepare the ordinary artesunate / emodestrin gel paste.

[0105] (2) Preparation of artesunate ethosome / ethotoplast gel ointment

[0106] According to the prescription and preparation method of gel oi...

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Abstract

The invention relates to a compound antimalarial composition. Particularly, the invention relates to a compound antimalarial composition containing artesunate and febrifugine and in particular relates to a compound antimalarial ethosome composition containing artesunate ethosomes and febrifugine ethosomes, a compound antimalarial ethosome gel paste as well as a preparation method and an application of the compound antimalarial ethosome gel paste. The compound antimalarial ethosome gel paste is prepared from the following components including a gel paste matrix, the artesunate ethosomes, the febrifugine ethosomes, a backing and an antisticking layer. According to the compound antimalarial ethosome gel paste disclosed by the invention, by utilizing the carrier permeation enhancing property of the ethosomes, the percutaneous permeability of an antimalarial medicament and the antimalarial effect of the medicament are improved; in addition, with the adoption of the compound antimalarial ethosome gel paste, the preparation technology is simple, high-temperature heating is not needed in the preparation process, and a harmful organic solvent is avoided.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, in particular to a compound antimalarial composition containing artesunate and ethotoplasts, in particular to a compound antimalarial ethosome containing artesunate ethosomes and ethotoplasts Composition and compound antimalarial plastosome gel ointment, preparation method and application thereof. Background technique [0002] Malaria is a vector-borne disease transmitted by mosquito bites. Statistics show that in 2010, about 219 million people worldwide were infected with malaria, and the death toll reached 660,000 [1] . Malaria is still one of the major diseases threatening human health worldwide, especially in underdeveloped tropical regions. In the 1970s, Chinese pharmaceutical workers isolated a sesquiterpene lactone compound with a powerful killing effect on malaria parasites——artemisinin from Artemisia annua L. [2] . With the deepening of research, a series of deri...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/517A61P33/06A61K9/127A61K9/06A61K31/357
CPCY02A50/30
Inventor 刘淑芝沈硕梁爱华张宇实杜茂波宋立华叶祖光
Owner INST OF CHINESE MATERIA MEDICA CHINA ACAD OF CHINESE MEDICAL SCI
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