Method for preparing nicotine containing oral dosage form

A technology of nicotine and lozenges, applied in the field of preparation of oral dosage forms containing nicotine, can solve problems such as rapid relief of addiction

Inactive Publication Date: 2008-11-12
SMITHKLINE BECKMAN CORP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Furthermore, the inventors are aware that commercial tablets are designed to have a long dissolution period so that the release of the craving may not be as rapid as desired

Method used

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  • Method for preparing nicotine containing oral dosage form

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0075] Nicotine lozenges were prepared as follows. In a 500ml beaker, combine 100g of ISOMALT powder, 25g of water and 0.4g of menthol. Heat the mixture using a hot plate while stirring until all of the ISOMALT is melted. Continue mixing and heating to about 165°C. Continue stirring and lower the temperature to about 120°C. At about 120°C, add about 1.2 g of sodium carbonate to adjust the pH to about 7.5-9.0 (pH can be measured from a solution of 0.1 g of this mixture in 10 ml of deionized water), and all other desired optional ingredients such as flavoring and / or vitamins. At about 120°C, 185 g of nicotine bitartrate dihydrate (equivalent to 60 mg of nicotine free base) was added to the mixture, mixed well and the molten mixture maintained at about 120°C. This mixture is pushed through a confectionery former to produce nicotine lozenges. Alternatively, the mixture may be deposited in suitable molds, cooled and demolded to obtain nicotine lozenges. By the time it solidif...

Embodiment 2

[0077] The 4-mg nicotine lozenges of Formulations A and B below were prepared.

[0078] Formulation A ingredients:

weight%

nicotine polacrilex (18 wt% nicotine potency)

0.47

Anhydrous sodium carbonate, NF

1.70

ISOMALT M type

96.83

Sesame oil, NF

1.0

[0079] Formulation B ingredients:

weight%

Nicotine bitartrate dihydrate (33% nicotine potency by weight)

0.86

Anhydrous sodium carbonate, NF

1.70

ISOMALT M type

96.44

Sesame oil, NF

1.0

[0080] Mix 75% ISOMALT and 25% purified water by weight. While mixing, heat the ISOMALT / water mixture until all the ISOMALT is melted. Continue mixing and heating to about 165°C. Continue mixing and lower the temperature to about 120°C. At about 120°C, sodium carbonate was added to adjust the pH to about 7.5-9.0 (pH can be measured on a solution of 0.1 g of this mixture dissolved in 10 ml of deioniz...

Embodiment 3

[0083] The in vitro dissolution profile of the lozenges was determined using a VanKel model VK7000 Dissolution Bath under the following conditions:

[0084] a.USP instrument I (Basket)

[0085] b. Dissolving medium: 900ml USP phosphate buffer (pH=7.4)

[0086] c. Dissolving temperature: 37℃+ / -0.5℃

[0087] d. Shaft peripheral speed: 100rpm

[0088] e. per container, at each predetermined time interval (e.g., 5, 10, 20, and 30 minutes, and 1, 2, 3, 4, 5, 6, 7, and 8 hours, until 100% or steady-state release is achieved), A 2ml sample was collected with an automatic sampling device. The removed media was replaced with 2 ml of phosphate buffered saline at each time interval.

[0089] f. directly analyzing the nicotine content of the sample by HPLC method.

[0090] The in vitro dissolution curve of the lozenge prepared according to Example 2 is shown in figure 1 . Such as figure 1 As shown, the nicotine is completely released within about 20 minutes; at least about 50% is ...

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Abstract

The present invention relates to a preparing method of oral dosage forms including nicotine, specifically to glassy matrix solid oral dosage forms useful for transmucosal oral administration of a nicotine active.

Description

[0001] This application is a divisional application of Chinese patent application 02807333.9 (which is an application for PCT / US02 / 08914 entering the national phase, the filing date is March 22, 2002, and the invention name is "oral dosage form containing nicotine"). technical field [0002] The present invention relates to solid oral dosage forms containing a nicotine active which are useful for reducing or preventing nicotine craving caused by oral transmucosal administration of a nicotine active. The invention also relates to methods of reducing or preventing nicotine craving or tobacco use using said compositions. Background technique [0003] Active as well as passive smoking of herbal products such as cigarettes, cigars and pipe tobacco are known to pose serious health hazards to users and second-hand smokers. The use of other forms of tobacco, such as chewing tobacco, is also known to pose serious health risks to users. In addition, the use of tobacco products in pub...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K9/20A61K31/465A61K47/36A61K47/26A61P25/34A61K9/00A61K47/02A61K47/10
CPCA61K31/465A61K47/26A61K9/0056A61P25/34
Inventor J·刘S·J·莱赫S·普拉特考
Owner SMITHKLINE BECKMAN CORP
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