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Iontophoretic transdermal delivery of nicotine salts

A nicotine salt and nicotine technology, applied in electrotherapy, medical preparations containing active ingredients, treatment, etc., can solve problems such as undesired attention, difficult to conceal places, uncomfortable patches, etc.

Inactive Publication Date: 2009-03-11
SMITHKLINE BECKMAN CORP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] However the relatively large patch may attract the attention of some users, as it is difficult to place in a hidden place, thus attracting unwanted attention
Alternatively, some users may find the patch uncomfortable due to the large area of ​​skin in contact with the irritating nicotine
It is known that the delivery of certain compounds through the skin may be increased when delivered under the impetus of a small electrical current (eg, iontophoresis)

Method used

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  • Iontophoretic transdermal delivery of nicotine salts
  • Iontophoretic transdermal delivery of nicotine salts
  • Iontophoretic transdermal delivery of nicotine salts

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] Example 1: Transdermal Delivery of Nicotine Base by Passive Diffusion and Iontophoresis

[0022] Studying the Permeation of Nicotine Base in Two Different Setup Conditions

[0023] i) Nicotine in 50 mM HEPES ([4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid) buffer (pH 5.5) containing 50 mM NaCl.

[0024] ii) Nicotine in 500 mM citrate buffer (pH 8) containing 50 mM NaCl.

[0025] Nicotine is a binary base with pKa values ​​of 3.4 and 8.2. At pH greater than 9, it is a free base. At pH 4.8-7.5, it is in the form of free base and single cation. Nicotine is more passively transported at pH 8, where the drug is present primarily in the nonionic form, compared to the monocationic form at pH 5.5. In both cases evaluated above, iontophoresis enhanced nicotine penetration compared to passive diffusion nicotine delivery (Figures 1 and 2).

Embodiment 2

[0026] Example 2: Transdermal Delivery of Nicotine Salts by Passive Diffusion and Iontophoresis in 500 mM Citrate Donor Buffer

[0027] Study of passive diffusion and iontophoresis of nicotine salts (equivalent to 1% nicotine), especially nicotine bitartrate and nicotine hemisulfate, in 500 mM citrate buffer containing 50 mM NaCl . The iontophoresis current was stopped after 4 hours. The iontophoretic flux of nicotine was similar in both salt forms, which was less than that of passive delivery of nicotine base at pH 8 (Figure 3). The pH of the donor solution was checked after the experiment, and it was found that the pH of the donor solution did not change.

Embodiment 3

[0028] Example 3: Comparison of Iontophoretic Delivery of Nicotine Bitartrate in 50 mM HEPES Donor Buffer vs. 500 mM Citrate Donor Buffer

[0029] Iontophoresis of nicotine bitartrate was studied in 50 mM HEPES buffer (pH 5.5). Nicotine bitartrate lowered the pH of the HEPES buffer to about 3.5, which was then adjusted to about 5.5 with NaOH.

[0030] As can be seen from the comparative graph (Figure 3), the flux of nicotine from the 50 mM HEPES buffer is higher than that from the 500 mM citrate buffer. It appears that the higher buffer strength citrate buffer contributed more buffer ions, which competed with drug ions for passage through the skin, thus reducing nicotine penetration. This has some indication in the conductivity test. 500 mM citrate buffer has a conductivity of 66400 μmhos / cm compared to 16300 μmhos / cm for 50 mM HEPES buffer. A final pH check of the experiment in a 50 mM HEPES solution showed no significant change in pH.

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Abstract

The present invention relates to iontophoretic transdermal delivery of nicotine salts useful for nicotine replacement therapy for an individual in need thereof. The present invention further relates to the iontophoretic transdermal delivery of nicotine maleate and nicotine citrate. Methods of reducing skin irritation generally caused by transdermal nicotine delivery by iontophoretic transdermal delivery of nicotine salts are also disclosed.

Description

field of invention [0001] The present invention relates to iontophoretic transdermal delivery of nicotine salts. More specifically, the present invention relates to iontophoretic transdermal delivery of nicotine maleate and nicotine citrate for use in nicotine replacement therapy for individuals in need thereof. Background of the invention [0002] It is well known that active as well as passive inhalation of tobacco products, such as cigars, cigarettes, and pipe tobacco, pose serious health risks to users and inhalers of second-hand smoke. The use of other forms of tobacco, such as chewing tobacco, is also known to pose serious health risks to users. In fact, it has been shown that cigarettes alone kill over 400,000 Americans each year and that smoking is responsible for 30% of all cancer deaths in the United States. Another 50,000 Americans die from exposure-related diseases (ie, lung cancer, cardiovascular disease) due to second-hand smoke (people exposed to environment...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61N1/30A61K9/70
CPCA61K9/0009A61K9/7023A61K31/4439A61P25/26A61P25/34
Inventor 帕梅拉·M·莱
Owner SMITHKLINE BECKMAN CORP
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