High dose oral pharmaceutical compositions of artemether and lumefantrine

A technology of artemether and composition, applied in the field of high-dose oral pharmaceutical composition, can solve the problems of patient non-compliance, low reliability, mental confusion and the like

Inactive Publication Date: 2009-07-08
RANBAXY LAB LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0011] Therefore, as evidenced by the table above, the burden of taking medication during the day is very heavy
Additionally, this dosing regimen may result in confusion, low reliability, and patient noncompliance

Method used

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  • High dose oral pharmaceutical compositions of artemether and lumefantrine
  • High dose oral pharmaceutical compositions of artemether and lumefantrine
  • High dose oral pharmaceutical compositions of artemether and lumefantrine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

(80+480mg) artemether 80.0 benzefantrine 480.0 Microcrystalline Cellulose (MCC 112) 250.0 Hydroxypropylmethylcellulose 20.0 Croscarmellose Sodium 120.0 Colloidal silica 20.0 Magnesium stearate 30.0 Tablet weight 1000.0

[0054] 1. Artemether and lumefantrine are sieved through a specific sieve together with microcrystalline cellulose, hydroxypropyl methylcellulose and croscarmellose sodium, and blended in a double-cone mixer to obtain a blend compound.

[0055] 2. Blend the blend of step 1 with the sieved colloidal silicon dioxide and magnesium stearate to obtain the final blend.

[0056] 3. Compress the final blend of step 2 using approved processing methods to obtain tablets.

Embodiment 2-4

80+480mg Intragranular artemether 40.0 60.0 80.0 benzefantrine 240.0 360.0 480.0 microcrystalline cellulose 42.6 63.9 85.2 Croscarmellose Sodium 56.0 84.0 112.0 Hydroxypropylmethylcellulose 8.0 12.0 16.0 Colloidal silica 10.0 15.0 20.0

[0059] Extragranular microcrystalline cellulose 20.0 30.0 40.0 Polysorbate 80 1.0 1.5 2.0 microcrystalline cellulose 56.4 84.6 112.8 Colloidal silica 6.0 9.0 12.0 Magnesium stearate 20.0 30.0 40.0 total 500.0 750.0 1000.0

[0060] 1. Artemether and lumefantrine are sieved through a specific sieve and mixed geometrically to obtain a mixture.

[0061] 2. Add microcrystalline cellulose, hydroxypropylmethylcellulose, croscarmellose sodium and colloidal silicon dioxide to the mixture obtained in step 1 to obtain a blend.

[0062] 3. Compress the blend obtained in step 2 to obtain a pre-compressed tablet, det...

Embodiment 2

[0078] The experimental value of embodiment 2

[0079]

Example 2

Test (%w / w) artemether 103.93 benzefantrine 100.07

[0080] Table 4

[0081] The dissolution curve of embodiment 2

[0082] Artemether: Dissolution curve obtained by USPI type II method at 100 rpm in 1800 ml pH 7.0 phosphate buffer + 3.0% sodium lauryl sulfate.

[0083] Benefantrine: Dissolution curve in 1800 ml 0.1N HCl + 3.0% benzalkonium chloride using USP Type II method at 75 rpm.

[0084]

[0085] While specific high dose oral pharmaceutical compositions have been described above, it will be apparent that various modifications and combinations can be made to the compositions detailed herein without departing from the spirit and scope of the invention. For example, other exemplary tablet formulations were contemplated for preparing high dose oral pharmaceutical compositions of artemether and lumefantrine, as described in Examples 5-12.

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PUM

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Abstract

The present invention relates to high dose oral pharmaceutical compositions of artemether and lumefantrine, and process for preparation thereof. The compositions comprise of artemether and lumefantrine comprising artemether in an amount of from about 40 mg to about 80 mg, lumefantrine in an amount of from about 240 mg to about 480 mg. The compositions are useful for treatment of uncomplicated infections with Plasmodium falciparum, including strains from multi-drug-resistant areas.

Description

field of invention [0001] The invention relates to a high-dose oral pharmaceutical composition of artemether and lumefantrine and a manufacturing method thereof. The composition comprises artemether and lumefantrine, wherein the content of artemether is from about 40 mg to about 80 mg, and the content of lumefantrine is from about 240 mg to about 480 mg. The composition can be used for treating non-complicated Plasmodium falciparum infection, including varieties in various drug-resistant regions. Background of the invention [0002] Malaria is a parasitic disease transmitted by mosquitoes. It infects millions of people worldwide and causes high morbidity and mortality. Symptoms of uncomplicated malaria are fever, headache, muscle aches, and vomiting. The parasite has developed resistance to many previously effective drugs, so drug combinations have been employed in an attempt to prevent further resistance. Artemether-lumefantrine is one member of this drug combination, w...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/35A61K31/137A61P33/06
CPCA61K31/35A61K31/137A61P33/06Y02A50/30A61K2300/00
Inventor S·马丹V·巴特拉A·A·伊诺斯V·阿罗拉
Owner RANBAXY LAB LTD
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