Self-emulsifying agent of compound artemether

A technology of self-emulsifier and artemether, which is applied in the field of pharmaceutical preparations, can solve the problems of large variation, limited actual effect, and discount of drug treatment effect, and achieve the effects of promoting absorption, simple preparation process, and improving bioavailability

Inactive Publication Date: 2007-02-21
GUANGZHOU PHARMACEUTICAL INDUSTRIAL RESEARCH INSTITUTE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In fact, it is difficult for the patient to fully follow the doctor's advice, which leads to a great reduction in the actual therapeutic effect of the drug, and the variation is particularly large, and the absorption delay time can even reach 2 hours
The usage method of AL tablets in the drug instruction manual is to take 2 times on the first day, 4 tablets each time, and 1 time on the second and third day, 4 tablets each time (in areas with relatively low drug resistance, the total oral Dose of artemether is 320mg, lumefantrine up to 1840mg), or 6 doses are taken in 3 days (in multi-drug resistant areas, the total oral dose is 480mg of artemether, lumefantrine up to 2880mg), in an attempt to pass Taking larger doses and frequent daily doses to make up for the above-mentioned defects in biopharmacokinetics of pharmaceutical preparations, but the actual effect is still limited. In order to overcome the above-mentioned defects of compound artemether tablets, it is necessary to develop new dosage forms

Method used

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  • Self-emulsifying agent of compound artemether
  • Self-emulsifying agent of compound artemether
  • Self-emulsifying agent of compound artemether

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0066] Composition of raw materials Amount (mg / grain) Weight ratio

[0067] Artemether 20 3%

[0068] Benefenol 120 20%

[0069] Coconut Oil 45 8%

[0070] Glyceryl Linoleate 120 20%

[0071] Polyglyceryl Laurate 30 5%

[0072] Cremophor EL35 (polyoxyethylene triricinoleic acid

[0073] Glycerides) 150 25%

[0074] Glyceryl monoacetate 115 19%

[0075] Total 600 100%

[0076] Preparation method: at room temperature, mix 4.5 grams of coconut oil, 3 grams of polyglyceryl laurate, 12 grams of glyceryl linoleate, 11.5 grams of glycerol monoacetate, and 15 grams of Cremophor EL35, and then mix 12 grams of this Add 2 grams of fluorenol and artemether to it, oscillate and completely dissolve the artemether to form a homogeneous solution, which is the compound artemether self-emulsifier.

[0077] The self-microemulsifying agent can be further made into hard capsules or soft capsules as required.

[0078] Process 1: Calculate according to the specification that each capsule co...

Embodiment 2

[0082] Composition of raw materials Amount (mg / grain) Weight ratio

[0083] Artemether 8 2%

[0084]Benefantrine 48 13%

[0085] Coconut Oil Medium Chain Fatty Acid Glycerides 110 30%

[0086] Tween 85 45 12%

[0087] Labrasol (mono-, di-, tri-caprylic / capric (C8-C10) glycerin 110 30%

[0088] oily esters and mono-, di-caprylyl / capric polyethylene glycol ester mixtures)

[0089] Gelucire 44 / 14 (Coconut Oil C8 / C10 Carboxylated Polyethylene 15 4%

[0090] alcohol glycerides)

[0091] Propylene Glycol 30 8%

[0092] Total 366 100%

[0093] Contents of each capsule 0.366g Specifications: Each capsule contains 8mg of artemether and 48mg of lumefantrine

Embodiment 3

[0095] Composition of raw materials (mg / grain) weight ratio

[0096] Artemether 30 4%

[0097] Benefantrine 120 16%

[0098] Sunflower oil 180 24%

[0099] Capmul MCM (single and double coconut oil C8 / C10 carboxyglycerin

[0100] 45 6%

[0101] ester)

[0102] Captex 355 (triple coconut oil C8 / C10 carboxyglycerides) 95 13%

[0103] Tween 80 100 13%

[0104] Diethylene glycol monoethyl ether 190 25%

[0105] Total 760 100%

[0106] Contents of each capsule 0.76g Specifications: Each capsule contains 30mg of artemether and 120mg of lumefantrine

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Abstract

A self-emulsifying compound artemether in the form of capsule able to be automatically emulsified in the body fluid of stomach and intestine is proportionally prepared from artemether, benflumetol, oil, non-ionic surfactant and assistant.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to an improved preparation of compound artemether. Background technique [0002] Artemisinin derivative artemether has a strong killing effect on Plasmodium schizonts, and has a significant effect on multidrug-resistant malaria and chloroquine-resistant falciparum malaria. However, it has the disadvantages of short duration of action and high recurrence rate. The World Health Organization recommends using them in combination with other antimalarial drugs to improve cure rates and delay the emergence of pathogen resistance. Benefantrine kills malaria parasites cleanly and thoroughly, with an effective rate of more than 95% and a recurrence rate of less than 5%, but the onset of action is slow. And after compounding the two medicines, they can synergize and complement each other. It overcomes the shortcomings of high artemether reactivation rate an...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K9/107A61K9/48A61K31/357A61K31/133A61K47/44A61K47/30A61P33/06
Inventor 朱少璇温新国张霖泽刘学斌李云峰刘文坚倪庆纯卢克伟王晓玲
Owner GUANGZHOU PHARMACEUTICAL INDUSTRIAL RESEARCH INSTITUTE
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