Stable dosage forms of spiro and dispiro 1,2,4-trioxolane antimalarials

a technology of trioxolane and spiro, which is applied in the direction of antiparasitic agents, drug compositions, active ingredients of phosphorous compounds, etc., can solve the problems of malaria, the most common parasitic disease of humans, and the characteristic paroxysm of the disease, and achieves the effect of death, reducing the risk of infection, and improving the effect of anti-malarial

Inactive Publication Date: 2009-02-12
RANBAXY LAB LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0016]In another aspect there is provided a stable oral solid dosage form of a therapeutically effective amo

Problems solved by technology

Malaria, the most common parasitic disease of humans, remains a major health and economic burden in most tropical countries.
It leads to a heavy toll of illness and death especially amongst children and pregnant women.
This process continues, destroying a significant number of blood cells and causing the characteristic paroxysm (“chills and fever”) associated with the disease.
The downside to quinine and its derivatives is that they are short-acting and have bitter taste.
Further, they fail to prevent disease relapses and are also associated with side effects commonly known as ‘Chinchonism syndrome’ characterized by nausea, vomiting, dizziness, vertigo and deafness.
However, in recent years, with the emergence of drug-resistant strains of parasite and insecticide-resistant strains of vector, the treatment and/or contr

Method used

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  • Stable dosage forms of spiro and dispiro 1,2,4-trioxolane antimalarials
  • Stable dosage forms of spiro and dispiro 1,2,4-trioxolane antimalarials
  • Stable dosage forms of spiro and dispiro 1,2,4-trioxolane antimalarials

Examples

Experimental program
Comparison scheme
Effect test

example 1

[0066]

Ingredients% w / wIntragranularMaleate salt of a compound of Formula II (active43.2compound)Microcrystalline Cellulose46.67Magnesium stearate0.75ExtragranularMicrocrystalline Cellulose5.63Croscarmellose sodium3.0Magnesium stearate0.75CoatingOpadry ® OY SS 58910 white2.5Waterq.sTotal weight615Water content

Procedure:

[0067]1. Active compound and intragranular portion of microcrystalline cellulose were sieved through sieve BSS# 44 and mixed together in a double cone blender to form a uniform blend.

[0068]2. To the blend of step 1, intragranular portion of sifted magnesium stearate was added and blended for about 5 minutes.

[0069]3. The blend of step 2 was compacted in a roller compactor and was sifted through sieve BSS # 22 to form granules.

[0070]4. Extragranular portion of microcrystalline cellulose, croscarmellose sodium and magnesium stearate were sieved through sieve BSS # 44 and blended with the granules of step 3.

[0071]5. The blend of step 4 was compressed using suitable size pu...

example 2

[0075]

Ingredients% w / w1Maleate salt of a44.33compound of Formula II(active compound)2Microcrystalline Cellulose51.173Magnesium stearate1.54Croscarmellose sodium3.0Total weight600 mgWater content

Procedure:

[0076]1. Active compound, microcrystalline cellulose, croscarmellose sodium and magnesium stearate were sifted through sieve BSS# 44.

[0077]2. Sifted active compound, microcrystalline cellulose, and croscarmellose sodium were mixed in a double cone blender for about 15 minutes to form a uniform blend.

[0078]3. To the blend of step 2, sifted magnesium stearate was added and mixed for about 5 minutes.

[0079]4. The blend obtained in step 3 was directly compressed using suitable size capsule shape punches to obtain compressed tablets.

examples 3 and 4

[0080]

IngredientsExample 3 % w / wExample 4 % w / wIntragranularMaleate salt of a compound of7.6813.8Formula II (active compound)Piperquine phosphate61.8055.5Microcrystalline Cellulose20.3921.05Magnesium stearate0.440.39Crospovidone2.211.99ExtragranularMicrocrystalline Cellulose4.423.99Crospovidone2.211.99Magnesium stearate1.051.09CoatingOpadry ® O2B53782 orange2.52.5Waterq.sq.sTotal weight (mg)1332.5738Water content

Procedure:

[0081]1. Active compound, piperaquine phosphate and intragranular portion of microcrystalline cellulose and crospovidone were sieved through sieve BSS # 44 and mixed together in a double cone blender to form a uniform blend.

[0082]2. To the blend of step 1, intragranular portion of sifted magnesium stearate was added and blended for about 5 minutes.

[0083]3. The blend of step 2 was compacted in a roller compactor and was sifted through sieve BSS # 18 to form granules.

[0084]4. Extragranular portion of microcrystalline cellulose and crospovidone were sieved through sie...

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Abstract

The field of the invention relates to stable dosage forms comprising spiro or dispiro 1,2,4-trioxolane antimalarials, or their pharmaceutically acceptable salts, prodrugs and analogues, and processes for their preparation. The water content of the dosage form is not more than 6.5% w/w.

Description

FIELD OF THE INVENTION[0001]The field of the invention relates to stable dosage forms comprising spiro or dispiro 1,2,4-trioxolane antimalarials, or their pharmaceutically acceptable salts, prodrugs and analogues, and processes for their preparation.BACKGROUND OF THE INVENTION[0002]Malaria, the most common parasitic disease of humans, remains a major health and economic burden in most tropical countries. Large 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 as malaria-risk areas. It leads to a heavy toll of illness and death especially amongst children and pregnant women. According to the World Health Organization, it is estimated that the disease infects about 400 million people each year, and around two to three million people die from malaria every year. There are four kinds of malaria parasites that infect human: Plasmodium falciparum, Plasmodium vivax,...

Claims

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Application Information

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IPC IPC(8): A61K31/70A61K31/343A61K31/47A61K31/505A61K31/66A61P33/02A61K31/4709A61K31/36A61K31/4706A61K31/65
CPCA61K9/1652A61K9/2027A61K9/2054A61K9/2077A61K9/2866A61K9/4866A61K31/335A61K31/357A61K31/4706A61K31/496A61K31/498A61K45/06A61P33/02A61P33/06C07D323/02Y02A50/30A61K2300/00
Inventor ENOSE, ARNO APPAVOOMADAN, HARISH KUMARMADAN, SUMITTREHAN, ANUPAMTYAGI, PUNEETARORA, VINOD KUMAR
Owner RANBAXY LAB LTD
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