Transdermal administration of (2S)-(4E)-n-methyl-5-(3-(5-isopropoxypyridin)yl)-4-penten-2-amine

A kind of technology of propoxypyridine and methyl, applied in (2S)-(4E)-N-methyl-5-(3-(5-isopropoxypyridyl)yl)-4-pentene-2 -In the field of transdermal administration of amines, it is possible to solve problems such as administration

Inactive Publication Date: 2010-07-07
塔格赛普有限公司 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, some of these compounds undergo relatively rapid degradation in the body, making it difficult to deliver them to the site of action via a route first through metabolism in the liver

Method used

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  • Transdermal administration of (2S)-(4E)-n-methyl-5-(3-(5-isopropoxypyridin)yl)-4-penten-2-amine
  • Transdermal administration of (2S)-(4E)-n-methyl-5-(3-(5-isopropoxypyridin)yl)-4-penten-2-amine

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preparation example Construction

[0044] II. Preparation of active ingredients

[0045] (2S)-(4E)-N-Methyl-5-(3-(5-isopropoxypyridinyl)-4-penten-2-amine can be synthesized using, for example, the method described in U.S. Patent No. 6,958,399 method, the aforementioned patents are incorporated herein by reference. (2S)-(4E)-N-methyl-5-(3-(5-isopropoxypyridinyl) base)-4-pentene-2-amine salt can be synthesized by (2S)-(4E )-N-methyl-5-(3-(5-isopropoxypyridinyl)-4-penten-2-amine is combined with various inorganic acids and organic acids in a suitable solvent, as As set forth in US Patent No. 6,432,954 and PCT WO 06 / 053082, each of which is incorporated herein by reference. (2S)-(4E)-N-methyl-5-(3-(5-isopropoxypyridinyl) base)-4-penten-2-amine galactaric acid half salt (hemigalactarate) can Prepared using techniques described in US Patent No. 6,958,399, which is incorporated herein by reference.

[0046] III. Transdermal Compositions

[0047] Compositions for transdermal administration include (2S)-(4E)-N-meth...

Embodiment 1

[0152] Determination of Drug Absorption

[0153] The ability of transdermal compositions to deliver the active ingredient at pharmaceutically effective levels to a subject in need of such treatment can be evaluated by performing an in vitro drug permeation test on the abdominal skin of a guinea pig. These experiments can be performed using a diffusion chamber, such as a Franz Vertical Diffusion Cell. Skin can be obtained from 8-16 month old, ideally shaved and undamaged female guinea pigs. Sections of full-thickness abdominal skin can be surgically incised and placed with the epidermis facing up between sections of the vertical diffusion pool. The transdermal device is applied on the epithelial layer, and at the same time, the dermal layer is contacted with a receptor solution in PBS (or other suitable isotonic solution), with or without the addition of an appropriate amount of polyoxyethylene 20 oleyl ether (Oleth 20 ) or other surfactants to prevent foaming (pH 7.4). Th...

Embodiment 2

[0158] In Vitro Skin Penetration Studies Using Pig Ears

[0159] Bronaugh diffusion cells are used in in vitro permeation studies, which are performed to determine 14 C-The flux of active ingredient penetration (ie, the speed at which the compound penetrates through the skin) and the total cumulative amount. Compounds were dissolved in water at concentrations of 35 and 135 mg / g. The full-thickness skin of a pig's ear (the thickness of the skin is taken to be about 900 μm) was used as a membrane. The receiving chamber contained phosphate buffered saline (pH 7.4) and was maintained at 32°C. Apply the compound solution to the stratum corneum. Receptor chamber samples (2, 4, 8, 12 and 14h) were analyzed by liquid scintillation counting. Transdermal flux (μg / cm 2 / h) can be determined from the steady state slope of a plot of the cumulative amount of active ingredient permeated through the skin versus time. After the steady state has been established, the linear portion of t...

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Abstract

The present invention generally relates to the transdermal administration of (2S)-(4E)-N-methyl-5-(3-(5-isopropoxypyridin)yl)-4-penten-2-amine, or pharmaceutically acceptable salts thereof. The transdermal administration can be effected using transdermal drug delivery devices, semi-solid dosage forms, or iontophoresis. The drug delivery devices and / or semi-solid dosage forms can provide instantaneous release, sustained release, or combinations thereof, and can include permeation enhancers and other components to assist in drug transport across the dermis, especially the epidermis. The compositions can be used to treat and / or prevent any indication which the active ingredients are capable of treating and preventing, but deliver (2S)-(4E)-N-methyl-5-(3-(5-isopropoxypyridin)yl)-4-penten-2-amine, or pharmaceutically acceptable salts thereof, in an efficacious manner. Disorders that can be treated and / or prevented include central nervous system disorders, addictions, pain, and inflammation.

Description

[0001] References to related applications [0002] This application claims priority to US Provisional Patent Application Serial No. 60 / 953,062, filed July 31, 2007, the entire contents of which are incorporated herein by reference. technical field [0003] The present invention generally relates to the transdermal administration of (2S)-(4E)-N-methyl-5-(3-(5-isopropoxypyridinyl)-4-penten-2-amine, or Medicinal salt. Background technique [0004] The use of various metanicotine analogs has been proposed for the treatment of various conditions, mainly via oral administration. See, eg, US Patent No. 5,616,716, US Patent No. 5,861,423, US Patent No. 6,232,316, and US Patent No. 6,958,399, the contents of which are incorporated herein by reference. However, some of these compounds undergo relatively rapid degradation in the body, which makes it difficult to deliver them to the site of action via a route first through metabolism in the liver. For metabolized nicotinic analogs th...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/70A61K9/06A61K31/465A61K31/44
CPCA61K9/0009A61K9/7084A61K31/44A61K31/465A61P1/02A61P1/16A61P3/04A61P9/10A61P11/00A61P11/06A61P17/02A61P17/06A61P19/02A61P21/02A61P25/00A61P25/04A61P25/08A61P25/10A61P25/12A61P25/14A61P25/16A61P25/18A61P25/20A61P25/22A61P25/24A61P25/28A61P25/30A61P25/32A61P25/34A61P25/36A61P29/00A61P31/04A61P39/02
Inventor 梅罗勒·本谢里夫约翰·W·詹姆斯迈克尔·G·威廉姆斯约翰内斯·安东尼厄斯·玛丽亚·内莉斯森
Owner 塔格赛普有限公司
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