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Stable dosage forms of arterolane and piperaquine

A stable, dosage-form technology, applied in the field of stable dosage forms of artemisinin and piperaquine, which can solve problems such as poor efficacy, reduced efficacy, and poor compliance

Inactive Publication Date: 2014-07-16
RANBAXY LAB LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

As mentioned above, this increases the chances of missing some doses and subsequent loss of efficacy due to noncompliance, and can even lead to the development of drug resistance
[0016] Therefore, there is an urgent and unmet need for antimalarial combination drugs with simplified daily dosing regimens to reduce the burden of medication and improve patient compliance
[0017] In addition to simplifying the dosing regimen, formulators are still limited in developing trioxolane-containing formulations, starting with their susceptibility to degradation in the presence of moisture leading to reduced shelf life
The second is their bitter taste, which leads to poor compliance with the regimen or selection of another, possibly less effective therapeutic agent

Method used

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  • Stable dosage forms of arterolane and piperaquine
  • Stable dosage forms of arterolane and piperaquine
  • Stable dosage forms of arterolane and piperaquine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0162]

[0163] process:

[0164] 1. Sieve Active Compound I with the intragranular portion of microcrystalline cellulose through a sieve BSS #44 and mix in a double cone mixer to form a homogeneous mixture.

[0165] 2. Add the sieved intragranular portion of the magnesium stearate to the mixture of step 1 and mix for about 5 minutes.

[0166] 3. Compact the mixture from step 2 in a roller compactor, then sieve through a BSS #22 sieve to form granules.

[0167] 4. Sieve the microcrystalline cellulose, croscarmellose sodium and magnesium stearate of the extragranular fraction through a sieve BSS#44 and blend with the granules from step 3.

[0168] 5. The mixture of step 4 is compressed using a punching machine of appropriate size to obtain compressed tablets.

[0169] 6. The tablets obtained in step 5 are coated with Perform coating.

[0170] The tablets prepared in Example 1 were subjected to a stability study for 6 months at 25°C / 60% relative humidity, 30°C / 65% rela...

Embodiment 2

[0179]

[0180] process:

[0181] 1. Sieve Active Compound I, microcrystalline cellulose, croscarmellose sodium and magnesium stearate through sieve BSS #44.

[0182] 2. Mix the sieved Active Compound I, microcrystalline cellulose and croscarmellose sodium in a double cone mixer for about 15 minutes to form a homogeneous mixture.

[0183] 3. Add the sieved magnesium stearate to the mixture from step 2 and mix for approximately 5 minutes.

[0184] 4. The mixture obtained in step 3 is directly compressed using capsule-shaped punches of appropriate size to obtain compressed tablets.

Embodiment 3 and 4

[0186]

[0187]

[0188] process:

[0189] 1. Sieve the intragranular fraction of Active Compound I, piperaquine phosphate and microcrystalline cellulose and cross-linked polyvinylpyrrolidone through a sieve BSS #44, then mix in a double cone mixer to form a homogeneous mixture.

[0190] 2. Add the intragranular portion of the sieved magnesium stearate to the mixture of step 1 and mix for about 5 minutes.

[0191] 3. The mixture from step 2 was compacted in a roller compactor, then sieved through a BSS #18 sieve to form granules.

[0192] 4. Sieve the microcrystalline cellulose and cross-linked polyvinylpyrrolidone in the extragranular portion through a sieve BSS#44, then mix with the granules from step 3.

[0193] 5. Sieve the magnesium stearate extragranular portion through a sieve BSS #44 and blend with the mixture from step 4 in a double cone blender for about 5 minutes.

[0194] 6. The blend of step 5 is compressed using appropriate sized punches to obtain compr...

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PUM

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Abstract

The field of the invention relates to stable oral dosage forms comprising, (a) cis-adamantane-2-spiro-3'-8'-[[[(2'-amino-2'-methylpropyl)amino]carbonyl]-methyl]-l',2',4'-trioxaspiro[4.5]decane hydrogen maleate(Active compound I); (b) piperaquine; and (c) one or more pharmaceutically acceptable excipients; and processes for their preparation, especially wherein the dosage form is prepared by a dry process.

Description

technical field [0001] The field of the invention relates to stable oral dosage forms comprising spiro or dispiro 1,2,4-trioxolane antimalarials, or pharmaceutically acceptable salts, prodrugs and analogs thereof, and methods for their preparation. Background technique [0002] Malaria, the most common parasitic disease in humans, remains a major health and economic burden in most tropical countries. Wide areas of Central and South America, Hispaniola (Haiti and the Dominican Republic), Africa, the Middle East, the Indian subcontinent, Southeast Asia, and Oceania are considered malaria risk areas. This results in a heavy toll in disease and death, especially among children and pregnant women. According to the World Health Organization, it is estimated that 400 million people are infected with the disease each year, and approximately two to three million people die from malaria each year. There are four classes of malaria parasites that infect humans: Plasmodium falciparum,...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/357A61K31/496A61K9/20A61P33/06
CPCA61K9/2054A61K9/2077A61K9/2095A61K31/357A61K31/496A61P33/06A61P43/00Y02A50/30A61K2300/00
Inventor A·A·伊诺斯H·K·马丹S·马丹A·特里汉P·太吉V·K·阿罗拉S·巴塔查里亚A·罗伊
Owner RANBAXY LAB LTD
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