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A liquid pharmaceutical formulation comprising nicotine for the administration to the oral cavity

A technology of liquid medicine and nicotine, applied in the direction of drug combination, drug delivery, medical preparations of non-active ingredients, etc., can solve the problem that the means and methods do not satisfactorily meet the teachings of NRT, cannot provide nicotine, and do not meet the requirements of tobacco User addiction and other issues

Inactive Publication Date: 2010-04-14
麦克尼尔有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0028] The means and methods described do not satisfy the cravings experienced by some tobacco users
In particular, these means and methods generally do not provide a sufficiently rapid intake of nicotine without adverse effects
[0029] This means that none of the currently known means and methods satisfy satisfactorily the following known NRT teachings by Russel et al.:

Method used

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  • A liquid pharmaceutical formulation comprising nicotine for the administration to the oral cavity
  • A liquid pharmaceutical formulation comprising nicotine for the administration to the oral cavity
  • A liquid pharmaceutical formulation comprising nicotine for the administration to the oral cavity

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0160] 1000 ml of a formulation containing 10 mg nicotine / ml and approximately pH 8.5 was prepared.

[0161] Mixture 1

[0162] Into a beaker containing 800 ml of water at 90°C were added 0.7 g of methylparaben as a preservative, and 0.3 g of propylparaben as a preservative. Additives were dissolved during stirring for about 10 minutes. Then 10.45 g of sodium dihydrogen phosphate as a buffer and 0.5 g of EDTA as a chelating agent were added to the solution, and the solution was stirred for about 5 minutes. The solution was then cooled to 30°C during stirring.

[0163] mixture 2

[0164] To a beaker containing 15.9 g of ethanol as a solvent at room temperature was added 0.045 g of peppermint oil as a flavor. The liquid was mixed for 2 minutes.

[0165] final mixture

[0166] Mixture 2 was added to a beaker containing 150 ml of water during stirring. Slowly add 10 g of nicotine (base) to the beaker. Mixture 1 was then added to the beaker and stirred for 5 minutes. ...

Embodiment 2

[0168] 1000 ml of a formulation containing 10 mg nicotine / ml and approximately pH 7.0 is prepared.

[0169] Example 2 differs from Example 1 only in pH. The formulation of Example 2 contained a non-basifying buffer. This preparation is used for figure 2 Comparison.

[0170] Mixture 1

[0171] Into a beaker containing 800 ml of water at 90°C were added 0.7 g of methylparaben as a preservative, and 0.3 g of propylparaben as a preservative. Additives were dissolved during stirring for about 10 minutes. Then 10.45 g of sodium dihydrogen phosphate as a buffer and 0.5 g of EDTA as a chelating agent were added to the solution, and the solution was stirred for about 5 minutes. The solution was then cooled to 30°C during stirring.

[0172] mixture 2

[0173] To a beaker containing 15.9 g of ethanol as a solvent at room temperature was added 0.045 g of peppermint oil as a flavor. The liquid was mixed for 2 minutes.

[0174] final mixture

[0175] Mixture 2 was added to ...

Embodiment 3

[0177] 1000 ml of a formulation containing 10 mg nicotine / ml and approximately pH 6.0 is prepared.

[0178] Example 3 differs from Example 1 only in pH. The formulation of Example 3 included a non-basifying buffer. This preparation is used for figure 2 Comparison.

[0179] Mixture 1

[0180] Into a beaker containing 800 ml of water at 90°C were added 0.7 g of methylparaben as a preservative, and 0.3 g of propylparaben as a preservative. Additives were dissolved during stirring for about 10 minutes. Then 10.45 g of sodium dihydrogen phosphate as a buffer and 0.5 g of EDTA as a chelating agent were added to the solution, and the solution was stirred for about 5 minutes. The solution was then cooled to 30°C during stirring.

[0181] mixture 2

[0182] To a beaker containing 15.9 g of ethanol as a solvent at room temperature was added 0.045 g of peppermint oil as a flavor. The liquid was mixed for 2 minutes.

[0183] final mixture

[0184] Mixture 2 was added to a...

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PUM

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Abstract

A liquid pharmaceutical formulation comprising nicotine in any form for administration to the oral cavity being alkalized by buffering and / or pH regulation. The administration is preferably by spraying and most preferably by spraying under the tongue. A method for manufacturing said formulation. Use of said formulation in therapy, such as therapy for treating addiction to tobacco.

Description

technical field [0001] The present invention relates to a liquid pharmaceutical formulation for delivering nicotine to a recipient. The present invention also relates to a method and system for delivering nicotine and making and using the liquid pharmaceutical formulation. Background of the invention [0002] Tobacco Dependence and Its Reduction [0003] In recent years, with awareness of the harmful effects of smoking, many campaigns and programs have been undertaken by government agencies and various health groups and other interested organizations to disseminate information about the adverse health effects of smoking. Furthermore, as a result of the recognition of the harmful effects, there have been many programs involved in trying to reduce the incidence of smoking. [0004] Nicotine is an organic compound that is the main alkaloid of tobacco. Nicotine is the main active ingredient in tobacco used in cigarettes, cigars, snuff, etc. But nicotine is also an addictive...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/465A61P25/34A61K9/08A61K9/12A61K31/34A61K47/04A61K47/10A61K47/12A61K47/40
CPCA61K31/465A61K9/006A61K47/10A61P25/34A61K31/455
Inventor K·林德尔B·伯森G·伯根格兰A·施吕特
Owner 麦克尼尔有限公司