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A kind of artemether suppository and preparation method thereof

A technology for artemether and suppositories, which is applied in the field of artemether suppositories and its preparation, which can solve the problems of affecting absorption and drug efficacy, small drug loading, and easy slipping of cataplasms, and achieve high bioavailability, ease of use and ease of use. Easy to carry and avoid the first-pass effect

Active Publication Date: 2020-06-19
KPC PHARM INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Artemether transdermal drug delivery technology is currently available, but the patch for direct skin drug delivery has a small drug load, which affects absorption and drug efficacy, and cataplasms are easy to slip off when pasted on the skin. The rate-limiting process affects the efficacy of the drug, etc.

Method used

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Examples

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Effect test

preparation example Construction

[0037] The preparation method of the artemether suppository of the present invention comprises the steps of oil phase preparation, water phase preparation and suppository preparation, specifically comprising:

[0038] A. Oil phase preparation: add artemether that has been finely ground and passed through a 80-120 mesh sieve to the peanut oil in the formula ratio at 25-45°C, stir and dissolve to obtain oil phase a;

[0039] B. Preparation of water phase: Take the polyethylene glycol 400, polyethylene glycol 4000 and polyoxyethylene monostearate in the proportion of the formula, melt them completely at 45~65°C, and mix them uniformly to obtain the water phase b;

[0040] C. Suppository preparation: Take the Tween-80, poloxamer and additives in the formula ratio and pour them into the fully melted matrix water phase b, stir and mix, then add the oil phase a, stir evenly to obtain emulsion c, and mix the emulsion c. Pour it into a plug mold, cool it in an environment below 30°C, a...

Embodiment 1

[0125] Artemether 1 g, polyethylene glycol 400 5 g, polyethylene glycol 4000 12 g, peanut oil 6 g, Tween-80 0.8 g, polyoxyethylene (40) monostearate 1 g, porol Sham 1 g

[0126] In a water bath at 25°C, gradually add artemether that has been finely ground and passed through a 80-mesh sieve to peanut oil, and stir as it is added to dissolve the main ingredient completely, and use it as the oil phase; take PEG400, PEG4000, polyoxyethylene (40) Monostearic acid esters are completely melted in a water bath at 50°C, and mixed evenly, as the water phase; an appropriate amount of Tween-80, poloxamer and other additives are slowly poured into the completely melted matrix, and continuously Stir to make the matrix and emulsifier completely mixed; slowly add the oil phase to the water phase matrix mixed with emulsifier, add slowly, and keep stirring at a speed of 60r / s for a certain period of time to make it a uniform emulsion; It is advisable to pour the above-mentioned molten plug int...

Embodiment 2

[0128] Artemether 90 g, Macrogol 400 300 g, Macrogol 4000 500 g, Peanut Oil 240 g, Tween-8060 g

[0129] At 45°C, gradually add artemether that has been finely ground and passed through a 120-mesh sieve into peanut oil, and stir as it is added, so that the main ingredient is completely dissolved and used as the oil phase; take PEG400 and PEG4000, melt them completely at 60°C, and Mix evenly and use it as the water phase; weigh an appropriate amount of Tween-80 and slowly pour it into the completely melted matrix, and keep stirring to completely mix the matrix and the emulsifier; slowly add the oil phase to the mixture mixed with the emulsifier Slowly add to the aqueous phase matrix, and stir for a certain period of time to make it a uniform emulsion; pour the above-mentioned molten plug into the plug mold, and it is advisable to pour it until the mold mouth overflows slightly; cool it in an environment below 30°C, and take it out , Gently scrape off the excess, take out the ar...

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Abstract

The invention discloses an artemether suppository and a preparation method thereof. The artemether suppository is prepared from, by weight, 0.8-5 parts of artemether, 3-15 parts of polyethylene glycol 400, 5-25 parts of polyethylene glycol 4000, 3-10 parts of peanut oil, 0.6-5 parts of tween-80, 0-20 parts of polyoxyethylene monostearate, 0.5 parts of poloxamer and 0-5 parts of additives. The preparation method comprises the steps of oil phase preparation, water phase preparation and suppository preparation. The artemether suppository prepared through the method can be prevented from interacting with digestive tracts such as the stomach and the intestines to make drugs inactivated or enable the drugs to irritate the intestines and the stomach, the bioavailability is high, after the artemether suppository is absorbed by the rectum, the first pass effect caused by the liver can be avoided, and using and carrying are both convenient.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to an artemether suppository and a preparation method thereof. Background technique [0002] Malaria is a global acute parasitic infectious disease caused by Plasmodium and transmitted by Anopheles mosquitoes as the main vector. The number of deaths due to malaria is between 1 million and 3 million, most of whom are children. [0003] Colorectal cancer in cancer is also called colorectal cancer, including colon cancer and rectal cancer, and its incidence is mainly related to factors such as lifestyle. At present, for rectal cancer, surgery is the main method, supplemented by comprehensive treatment of chemotherapy and radiotherapy. However, surgical operations are often faced with the difficult choice of "keeping the anus and saving life", which is more harmful to the patient; moreover, the drug treatment of rectal cancer is mainly chemically synthesized drugs, but its...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/02A61K31/357A61K47/44A61K47/10A61K47/26A61K47/14A61P33/06A61P35/00
CPCA61K9/0031A61K9/02A61K31/357A61K47/10A61K47/14A61K47/26A61K47/44
Inventor 普俊学张恒张伟屈云莲马珍琼代玉玲郭明里
Owner KPC PHARM INC