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Compositions for oral adminstration of active principles requiring masking of taste

a technology of oral administration and active principles, applied in the field of pharmaceutical compositions, can solve the problems of unsuitable pediatric or oral formulation preparation, unacceptable organoleptic properties, and extremely prejudicial, or even vital, consequences

Inactive Publication Date: 2010-01-14
AVENTIS PHARMA SA (US)
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

The formulation effectively masks unpleasant tastes and textures, allowing for acceptable oral administration, with high dissolution rates at acidic pH conditions, reducing bitterness and sandy mouthfeel, and ensuring effective release of active principles in the stomach.

Problems solved by technology

Some active principles exhibit unacceptable organoleptic properties and, as a result, are unsuitable for preparing pediatric or oral formulations intended for individuals in whom swallowing is difficult and can pose problems.
For these reasons, some major products are deprived of a pediatric formulation and, in addition, some individuals are deprived of treatment using these active principles, which may have extremely prejudicial, or even vital, consequences.
The problem of masking taste has always been a considerable problem for the pharmaceutical industry.
Antibiotics, often given to children for numerous childhood illnesses, are particularly plagued with this problem.
Many systems have been tried, but in the case of active principles which are too bitter, coating systems have mostly proved to be insufficient and particulate systems, when they are more effective, exhibit drawbacks of too great a particle size, leading to a sandy aspect in the mouth and to the patient refusing the medicinal product.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

example 1

[0029]2 400 g of precirol melted beforehand in an incubator at 60° C. are introduced into a jacketed reactor, the set jacket temperature of which is fixed at 75° C. 78 g of soybean lecithin are added. When the soybean lecithin is dissolved, the set temperature is lowered to 65° C. and 540 g of pristinamycin are added. Stirring is carried out for 20 minutes at 300 rpm, and then the suspension is passed over a bore mill.

[0030]1 248 g of the ground suspension are then sprayed via a two-fluid nozzle in a prilling tower precooled with a current of cold nitrogen. At the beginning of spraying the temperature is 0° C. at the top of the tower and −20° C. at the bottom of the tower. The air pressure on the two-fluid nozzle is 1.5 bar, which produces a spray-air flow rate of 2.3 m3 / h. The flow rate of liquid is 4.7 kg / h.

[0031]At the end of spraying, the product is then fluidized for 20 minutes at −20° C., and then for 2 hours at 32° C.

[0032]The particle size of the product obtained, measured b...

example 2

[0039]704 g of precirol are introduced into a jacketed reactor, the set jacket temperature of which is fixed at 75° C. When the precirol is molten, 18 g of soybean lecithin are added. When the soybean lecithin is dissolved, 182 g of pristinamycin premicronized in an air jet micronizer, and exhibiting, after grinding, a median diameter of 2 μm, are added. Stirring is carried out for 45 minutes at 800 rpm in order to obtain a homogeneous suspension.

[0040]The suspension is then sprayed via a two-fluid nozzle in a prilling tower precooled with a current of cold nitrogen. At the beginning of spraying, the temperature is −14° C. at the top of the tower and −42° C. at the bottom of the tower. The air pressure on the two-fluid nozzle is 1.5 bar, which produces a spray-air flow rate of 2.3 m3 / h. The flow rate of liquid is 10.8 kg / h.

[0041]The particle size of the product obtained, measured by sieving, is:[0042]30% of particles between 0 and 100 μm[0043]54% of particles between 100 and 315 μm[...

example 3

[0048]907 g of precirol are added to a jacketed reactor, the set jacket temperature of which is fixed at 70° C. When the precirol is molten, 23 g of soybean lecithin are added. When the soybean lecithin is dissolved, 207 g of unground telithromycin exhibiting a median diameter of 114 μm are introduced. Stirring is carried out for 50 minutes at 500 rpm in order to obtain a homogeneous liquid: the telithromycin is visibly soluble in the precirol.

[0049]The suspension is then sprayed via a two-fluid nozzle in a prilling tower precooled with a current of cold nitrogen. At the beginning of spraying, the temperature is 0° C. at the top of the tower and −20° C. at the bottom of the tower. The air pressure on the two-fluid nozzle is 1.3 bar, which produces a spray-air flow rate of 4 m3 / h. The flow rate of liquid is 8.5 kg / h.

[0050]The particle size of the product obtained, measured by sieving, is:[0051]59% of particles between 0 and 100 μm[0052]38% of particles between 100 and 315 μm[0053]3% ...

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Abstract

Composition intended for the oral administration of active principles with unacceptable taste, which comprises from about 15% to about 30% of organoleptically unpleasant active ingredient (principle) that is mixed with from about 60% to about 80% of an ester of glycerol or of a fatty acid, to which a wax is optionally added and to which a surfactant is added, and in that it is prepared by a spray-cooling process which can produce a particle size of less than 350 μm.

Description

CROSS-REFERENCE TO RELATED APPLICATIONS[0001]This application is a continuation of U.S. application Ser. No. 10 / 743,244, filed on Dec. 22, 2003, now pending, which is incorporated herein by reference in its entirety; which claims the benefit of U.S. Provisional Application No. 60 / 455,796, filed Mar. 19, 2003 with a right of priority of French Patent Application No. 02 / 16,521, filed Dec. 23, 2002.FIELD OF THE INVENTION[0002]The present invention relates generally to compositions intended for the oral administration of active principles with unacceptable taste, and also to the preparation thereof. In particular, the present invention relates to pharmaceutical compositions which by their nature exhibit bitter or bad tasting organoleptic characteristics.BACKGROUND OF THE INVENTION[0003]Some active principles exhibit unacceptable organoleptic properties and, as a result, are unsuitable for preparing pediatric or oral formulations intended for individuals in whom swallowing is difficult a...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K9/14A61K9/16B01J2/04
CPCA61K9/1617B01J2/04A61K9/1694A61P1/04A61P1/06A61P9/00A61P11/06A61P11/14A61P25/00A61P29/00A61P31/04A61P31/10A61P31/12A61P33/00A61P35/00A61P37/08A61P43/00
Inventor CHACORNAC, ISABELLEPROBECK, PATRICIA
Owner AVENTIS PHARMA SA (US)