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Drug formulation having improved oral tolerability

A technology for irritating and oral mucosa, applied in the direction of pharmaceutical formulas, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc.

Inactive Publication Date: 2010-01-06
PROCTER & GAMBLE CO
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Often results in a burning sensation if the level of cooling agent is increased enough to overcome the irritation produced by the agent

Method used

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Examples

Experimental program
Comparison scheme
Effect test

example 1

[0033] Example 1: Cough Treatment Composition

[0034] Element

weight percentage

Dextromethorphan base

2.20

Propylene Glycol

42.45

(Poloxymer) Poloxamer 1

29.71

pure water

12.08

Ethanol (100% by weight)

10.91

Sodium metabisulfite

0.10

Disodium edetate

0.10

Eucalyptus

0.45

Coolant:

-----

Menthol

0.20

N-ethyl-p-menthane-3-carboxamide 2

0.15

1-Menthone- / d-Isomenthone Glycerol Ketal 3

0.30

3-1-menthoxypropane-1,2-diol 4

0.10

Sweetener:

-----

sodium saccharin

0.60

Acesulfame Potassium

0.50

Monoammonium glycyrrhizinate

0.15

[0035] 1 Polyether F127 is available from BASF Special Chemicals, Mount Olive, NJ, USA.

[0036] 2WS-3 is available from Millennium Specialty Chemicals.

[0037] 3MGA is available from Haarmann and Rei...

example 2

[0043] Example 2: Composition for treating cough

[0044] Element

weight percentage

Dextromethorphan base

2.75

Propylene Glycol

79.41

Menthol (100% by weight)

10.00

pure water

5.00

Sodium metabisulfite

0.10

Disodium edetate

0.10

artificial orange flavor

0.50

Coolant ：

-----

Menthol

0.10

N-ethyl-p-menthane-3-carboxamide 1

0.12

1-Menthone- / d-Isomenthone Glycerol Ketal 2

0.10

Sweetener:

-----

1’,4,6’-Sucralose 3

1.20

sodium saccharin

0.20

Acesulfame Potassium

0.40

Monoammonium glycyrrhizinate

0.02

[0045] 1 WS-3 is available from Millennium Specialty Chemicals.

[0046] 2 MGA is available from Haarmann and Reimer.

[0047] 3 Sucralose, also known as Splenda TM , available from McNeil Specialty Products Co.

[0048] preparation :

...

example 3

[0050] Example 3: Cough Treatment Composition

[0051] Element

weight percentage

Dextromethorphan base

1.69

Propylene Glycol

42.58

(Poloxymer) Poloxamer 1

29.80

pure water

12.77

Ethanol (100% by weight)

10.91

Sodium metabisulfite

0.10

Disodium edetate

0.10

artificial grape flavor

0.55

Coolant:

-----

Menthol

0.10

N-ethyl-p-menthane-3-carboxamide 2

0.15

1-Menthone- / d-Isomenthone Glycerol Ketal 3

0.25

Sweetener:

-----

1’,4,6’-Sucralose 4

0.80

Acesulfame Potassium

0.20

[0052] 1 Polyether F127 is available from BASF Specialty Chemicals, Mount Olive, NJ, USA.

[0053] 2 WS-3 is available from Millennium Specialty Chemicals.

[0054] 3 MGA is available from Haarmann and Reimer.

[0055] 4 Sucralose, also known as Splenda TM , available from McNei...

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PUM

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Abstract

Oral compositions containing therapeutical agents wherein the undesirable consumer aesthetics associated with these agents are mitigated using coolants and sweeteners.

Description

technical field [0001] The present invention is an oral composition comprising a therapeutic agent that generally has an unpleasant consumer sensibility. These compositions comprise compositions in various forms, including liquids and solids, which contain the pharmaceutically active ingredient. Liquid compositions include, but are not necessarily limited to, elixirs, syrups, liquid-filled chewable capsules, suspensions, sprays and suspensions. technical background [0002] Irritation to the nerves in the mouth occurs when spices or chemicals can easily irritate the nerves in the mouth. Oral compositions containing therapeutic agents, such as pharmaceutically active ingredients, often contain unpleasant-tasting or poor-tasting ingredients. These compositions are taken orally and are often designed to deliver the agent through the intestinal mucosa into the bloodstream. These formulations are not designed to deliver their therapeutic agents through the mucous membranes of ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/485A61K31/425A61K31/54A61K31/704A61K31/045A61K31/16A61K31/357A61K31/047A61K47/10A61K9/00A61K9/20A61K31/40A61K47/12A61K47/14A61K47/16A61K47/22A61K47/26A61K47/42A61P11/14
CPCA61K31/485A61K9/2059A61K9/0034A61K9/2054A61K9/2018A61P11/14
Inventor K·-C·M·李
Owner PROCTER & GAMBLE CO