Transdermal formulations

一种透皮、溶剂的技术，应用在无水透皮制剂领域，能够解决炎症、皮肤刺激等问题

Inactive Publication Date: 2015-12-23
劳瑞·罗伯特·巴特 +6
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

A problem with transdermal formulations is that these penetration enhancers can cause skin irritation and inflammation

Method used

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  • Transdermal formulations
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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0404] Example 1 - Stability Study

[0405] 1. Solvent stability

[0406] The purpose of these studies is to identify solvents and co-solvents to optimize active substance solubility and product physical / chemical stability.

[0407] In a certain range of solvents, the solubility and recovery of levamisole base and / or abactin after one month were determined, as shown in Table 1.

[0408] Table 1. Solubility data for solvents used alone to examine the stability of two actives, levamisole base and abactin

[0409]

[0410]

[0411]

[0412] 2. Abaktin stability

[0413] The purpose of this study was to examine the stability of abactin in a solvent-neutralized solvent system containing only glycerol formal (GF) and a solvent system comprising a complexing agent (eg PVP), an acidulant (eg malic acid) and Chelating agents such as EDTA are combined with glycerol formal.

[0414] Table 2. Stability data for levamisole base and abactin in solvent systems containing glycero...

Embodiment 2

[0456] Example 2 - In vitro studies

[0457] 5. Permeability studies

[0458] This example describes the use of a platform composition to deliver a range of different actives across the skin of a range of different animals (bovine, equine, rabbit).

[0459] The active substances investigated in this example are

[0460] ■Levamisole base (insect repellent)

[0461] ■ Macrolides (abactin and moxidectin) (insect repellants),

[0462] Hydrocortisone (steroidal anti-inflammatory agent),

[0463] ■ metoclopramide (antiemetic),

[0464] cetirizine (an antihistamine), and

[0465] ■ Diphenhydramine (antihistamine).

[0466] The properties of each active tested are shown in Table 7 below.

[0467] Table 7. Characteristics of the tested APIs

[0468]

[0469]

[0470] Formulations of the platform compositions are given in Table 8.

[0471] Table 8. Formulations for Abaktin / Levamisole Base Formulations

[0472]

[0473] Table 9. Formulations for Moxidectin / Levamisole B...

Embodiment 3

[0570] Example 3 - Clinical Study

[0571] Two clinical efficacy studies were conducted. The study design for each study is summarized below.

[0572] ■Study 1 - Winter Fur

[0573] ○ Control

[0574] ○ When there is no rain, test the composition

[0575] ○ Rain after 2 hours of application, test composition

[0576] ■Study 2 - Summer Fur

[0577] ○ Control

[0578] ○Test composition

[0579] ○Comparative product (Eclipse-combination dual pour-on with abactin and levamisole)

[0580] ○Single active substance comparison product

[0581] The purpose of Study 1 was to evaluate the efficacy of the test composition against gastrointestinal parasites in cattle with winter coats and to determine the effect of rain on the efficacy of the composition after application of the composition on the skin of cattle.

[0582] The purpose of Study 2 was to evaluate the efficacy of the test composition against gastrointestinal parasites in cattle with summer coats and to compare with th...

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PUM

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Abstract

The present invention relates to a non-aqueous composition that comprises a permeation enhancer such as a terpene, for delivering an active ingredient transdermally. The composition comprises at least on one active ingredient, a terpene, and a solvent, such as a non-hydroxyl containing solvent, non-heterocyclic ester solvent and / or a tripropylene glycol alkyl ether. The composition can be used to deliver a range of actives, such as anthelmintics. The present invention provides a platform composition and can be used to deliver a wide variety of active ingredients and combinations thereof transdermally to mammals.

Description

[0001] incorporated by reference [0002] All documents cited or referenced herein ("documents cited herein") and all documents cited or referenced in documents cited herein, together with any manufacturer of any product mentioned herein or in any document incorporated herein by reference The specifications, descriptions, product specifications, and product parameter tables of , are hereby incorporated by reference and may be used in the practice of the present invention. More particularly, all references are incorporated herein by reference to the same extent as if each individual document was specifically and individually indicated to be incorporated by reference. technical field [0003] The present invention relates to anhydrous transdermal formulations comprising terpenes, and more particularly to formulations suitable for transdermal delivery of active therapeutic agents to mammals. The present invention also relates to methods of making such compositions, and to the us...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/015A61K31/365A61K31/429A61P33/10
CPCA61K31/429A61K9/0014A61K47/06A61K47/08A61K47/10A61K31/506A61K31/365A61K47/14A61K31/7048A61K9/08A61K31/166A61K31/573A61K31/495A61K31/135A61K47/20A61K47/22A61K47/26
Inventor 劳瑞·罗伯特·巴特苏·韦恩凯琳·戴维斯大卫·安东尼·吉尔詹姆斯·罗伯特·法尔科内尔道格拉斯·罗伯特·克莱维利吴子梅
Owner 劳瑞·罗伯特·巴特
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