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Transdermal delivery system

a technology of transdermal delivery and delivery system, which is applied in the direction of bandages, biocide, drug compositions, etc., can solve the problems of high variability in performance, system failure, undesired burst, etc., and achieve the effect of small area

Inactive Publication Date: 2016-01-14
LTS LOHMANN THERAPIE-SYST AG
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

The present invention is about a transdermal therapeutic system for the buprenorphine base that can provide pain relief for a long period of time (about 168 hours) with a small amount of buprenorphine contained therein. The system uses a self-adhesive layer structure that is free of active agent and larger in area than the active agent-containing structure, which has additional area adhering to the skin and enhances the overall adhesive properties of the system. The system also uses a viscosity-increasing substance that increases the viscosity of the mixture of buprenorphine and carboxylic acid. The manufacturing process of the system is also provided.

Problems solved by technology

The manufacturing of several batches, however, shows a high variability in the performance.
Large deposits release the drug too fast and provide for an undesired burst in the beginning of the dosing period and a failure of the system after three to four days.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

example 3

[0285]The composition of the buprenorphine base-containing adhesive mixture is summarized in Table 3 below.

TABLE 3Ingredient (Trade Name)Amt / unit (g)Buprenorphine base7.44Levulinic acid5.24Ascorbyl palmitate0.14Polyvinylpyrrolidone (PVP)1.88Ethanol10.77Polysiloxane adhesive in n-heptane82.47Solids content of 73% by weight(BIO-PSA 7-4201 from Dow CorningHealthcare)n-heptane1.73Total109.67

[0286]In a suitable vessel, 37.86 g of polyvinylpyrrolidone and 113.57 g of ethanol were dissolved to form a 25% PVP pre-solution. The prescribed amount of the PVP pre-solution, Levulinic acid and Ascorbyl palmitate were suspended with stirring and afterwards the remaining part of Ethanol and the Buprenorphine was added to form a buprenorphine containing solution by stirring until a solution is formed. 82.50 g of a polysiloxane adhesive in the form of a solution in n-heptane having a solids content of 73% by weight and 1.74 g of heptane were added. The mixture was stirred to give 109.67 g of a bupren...

example 4

[0290]The composition of the buprenorphine base-containing adhesive mixture is summarized in Table 4 below.

TABLE 4Ingredient (Trade Name)Amt / unit (kg)Buprenorphine base1.368Levulinic acid0.958Polyvinylpyrrolidone (PVP)0.342Ascorbyl palmitate0.027Ethanol1.938Polysiloxane adhesive in n-heptane15.048Solids content of 73% by weight(BIO-PSA 7-4201 from Dow CorningHealthcare)n-heptane0.319Total20

[0291]In a 10 l vessel, 1.00 kg of polyvinylpyrrolidone and 3.00 g of ethanol were dissolved to form a 25% PVP pre-solution. In a homogenizing / mixing vessel: Becomix Lab mixer RW 30 Ex, 1.368 kg of PVP pre-solution, 0.958 kg levulinic acid, 0.027 kg of Ascorbyl palmitate and the main part of 0.912 kg of Ethanol were suspended by stirring. The prescribed amount of buprenorphine was weighed and added to the homogenizing / mixing vessel followed by rinsing the weighing container used for buprenorphine with the remaining part of Ethanol. The mixture was kept under stirring for at least 1 h until a bupre...

example 5

[0297]The composition of the buprenorphine base-containing adhesive mixture and the process of manufacture was as described for Example 4. After the mixing step forming a buprenorphine containing mixture, the buprenorphine base-containing adhesive mixture was additionally homogenized at a homogenizing speed of 2000 rpm-2500 rpm before coated on a polyethylene terephthalate film (e.g. Scotchpak from 3M).

[0298]In Example 5, films with two different coating weights of the matrix layer were prepared:

TABLE 5Coating weight of theExample 5matrix layer [g / m2]Example 5.1120Example 5.290

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Abstract

The invention relates to transdermal therapeutic system for the transdermal administration of buprenorphine, comprising a buprenorphine-containing self-adhesive layer structure comprising A) a buprenorphine-impermeable backing layer, and B) a buprenorphine-containing pressure-sensitive adhesive layer on said buprenorphine-impermeable backing layer, the adhesive layer comprising a) at least one polymer-based pressure-sensitive adhesive, b) an analgesically effective amount of buprenorphine base or a pharmaceutically acceptable salt thereof, c) a viscosity-increasing substance in an amount of about 0.1% to about 8% of said buprenorphine-containing pressure-sensitive adhesive layer, and d) a carboxylic acid selected from the group consisting of oleic acid, linoleic acid, linolenic acid, levulinic acid and mixtures thereof, in an amount sufficient so that said analgesically effective amount of buprenorphine is solubilized therein to form a mixture including said viscosity-increasing substance, and wherein the carboxylic acid-, buprenorphine- and viscosity-increasing substance-containing mixture forms dispersed deposits in the said pressure-sensitive adhesive, and wherein said buprenorphine-containing pressure-sensitive adhesive layer is the skin contact layer.

Description

TECHNICAL FIELD OF THE INVENTION[0001]The present invention relates to a transdermal therapeutic system (TTS) for the transdermal administration of buprenorphine, and processes of manufacture, uses thereof, and corresponding methods of treatment therewith.BACKGROUND OF THE INVENTION[0002]The active ingredient buprenorphine (5R,6R,7R,9R,13S,14S)-17-Cyclopropylmethyl-7-[(S)-3,3-dimethyl-2-hydroxybutan-2-yl]-6-methoxy-4,5-epoxy-6,14-ethanomorphinan-3-ol) is a partially synthetic opiate with high potency. Cancer patients may be treated with daily doses of around 1 mg. Despite its rather high molecular weight of 467.64 daltons, it is currently used for transdermal administration. The commercial TTS product Norspan®, also known as BuTrans®, delivers buprenorphine to the skin sufficiently to treat patients in pain for a time period of 7 days (about 168 hours) and allows therefore a use of the TTS over a time period of 7 days and allows in a fixed dosing regimen a once-weekly TTS exchange. ...

Claims

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Application Information

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IPC IPC(8): A61K9/70A61F13/02A61K9/00A61K31/485
CPCA61K9/7053A61F13/0256A61K9/0014A61K31/485A61K9/7069A61K31/4748A61P25/00A61P25/04A61K47/12A61K47/32
Inventor HILLE, THOMASWAUER, GABRIELSEIBERTZ, FRANKWEINHEIMER, SHU-LUN
Owner LTS LOHMANN THERAPIE-SYST AG
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