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Pharmaceutical composition for transdermal administration of perospirone

A technology of perospirone and perospirone hydrochloride, applied in the field of pharmaceutical compositions for systemic transdermal administration, capable of solving problems such as not being able to make transdermal preparations

Inactive Publication Date: 2007-10-17
SUMITOMO DAINIPPON PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In other words, many drugs are known not to be formulated transdermally due to their inherent properties

Method used

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  • Pharmaceutical composition for transdermal administration of perospirone
  • Pharmaceutical composition for transdermal administration of perospirone
  • Pharmaceutical composition for transdermal administration of perospirone

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0068] Preparation of Perospirone Tape

[0069] Styrene-isoprene-styrene block copolymer (Quintac 3421) (2.00g), liquid paraffin (3.00g), polybutene (NISSEKI polybutene HV-300) (1.50g) and alicyclic A saturated hydrocarbon resin (Alcon P-100) (2.50 g) was dissolved in hexane to prepare a binder solution. Perospirone was added thereto so that its content in the matrix layer was 10%, and the mixture was fully stirred. Then, the mixture was spread on a carrier to a thickness of about 100 µm, dried, adhered with a release liner and cut into a size of 4 cm x 4 cm to prepare a perospirone tape (Formulation 1).

Embodiment 2

[0071] Preparation of perospirone hydrochloride adhesive tape

[0072] Styrene-isoprene-styrene block copolymer (Quintac 3421) (2.00g), liquid paraffin (3.00g), polybutene (NISSEKI polybutene HV-300) (1.50g) and alicyclic Group saturated hydrocarbon resin (Alcon P-100) (2.50g) is dissolved in hexane, prepares adhesive solution, and perospirone hydrochloride is added wherein, and make its content in matrix layer be 10%, will The mixture is stirred well. Then, the mixture was spread on a support to a thickness of about 100 µm, dried, glued with a release liner and cut into a size of 4 cm x 4 cm to prepare perospirone hydrochloride tape (Formulation 2).

Embodiment 3

[0074] Preparation of Perospirone Aqueous Ointment

[0075] Perospirone (0.15 g) was added to polyethylene glycol 400 (NOF Corporation) (1.425 g) to dissolve, and the resulting mixture was heated to 70°C. The resulting solution (1.05 g) was mixed with polyethylene glycol 4000 (NOF Corporation) (0.95 g) dissolved at 70° C. to prepare perospirone aqueous ointment (formulation 3).

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Abstract

The present invention provides a medicinal composition for percutaneous administration which contains either perospirone, which is represented by the formula (1): (1) or a pharmaceutically acceptable acid addition salt thereof. Use of the composition can inhibit metabolite generation and maintain a concentration in the blood over long.

Description

technical field [0001] The present invention relates to a pharmaceutical composition for transdermal administration containing perospirone or its pharmaceutically acceptable acid addition salt. More specifically, the present invention relates to making perospirone or its pharmaceutically acceptable acid addition salt A pharmaceutical composition for systemic transdermal administration in which the salt is absorbed transdermally and delivered continuously to the central tissue through the circulatory system. Background technique [0002] Perospirone represented by formula (1) (cis-N-[4-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl}butyl}cyclohexane- 1,2-diimide) has been described in Patent Document 1. [0003] [0004] Perospirone or its pharmaceutically acceptable acid addition salt is a 5-hydroxytryptamine-stimulating agent that exhibits strong binding activity and antagonistic action on dopamine 2 (D2) receptors and 5-hydroxytryptamine 2 (5-HT2) receptors. Dopamine anta...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/496A61K9/06A61K9/08A61K9/10A61K9/70A61P25/18A61P43/00
CPCA61K31/496A61K9/0014A61P25/18A61P43/00A61K9/06A61K9/70
Inventor 前田弘雄大原长夫喜池田友纪
Owner SUMITOMO DAINIPPON PHARMA CO LTD