Tape formulation for percutaneous administration containing fent

Details Tape formulation for percutaneous administration containing fent Tape formulation for percutaneous administration containing fent

1998-01-13

2000-10-31

Criares, Theodore J.

Drug, bio-affecting and body treating compositions

Preparations characterized by special physical form

Web, sheet or filament bases; compositions of bandages; or...

424446, 424448, 424445, 424449, 514352, A61L 970, A61L 1516, A61L 1500, A61L 3138

Patent

active

061398667

DESCRIPTION:

BRIEF SUMMARY
TECHNICAL FIELD

The present invention relates to a tape formulation for percutaneous administration containing fentanyl (chemical name: 1-phenethyl-4-N-proplonyl-anilino-piperidine) or a salt thereof, which is very excellent in transdermal permeable property and which has a low irritative property to skins. The tape formulation for percutaneous administration containing fentanyl of the present invention is greatly expected to be utilized as a prolonged-action anesthetic and analgesic.


BACKGROUND ART

Fentanyl, in particular fentanyl citrate is known as a pharmaceutical having a high analgesic effect. However, there was no useful administration method of the pharmaceutical for relatively long lasting pains such as carcinomatous pains, since its elimination half life is short and thus its effects does not last though it is utilized for the constant rate instillation before and after operation.
In the USA, a prolonged-action patch formulation containing fentanyl base (trade name: DURAGESIC) is put on the market. However, it has the disadvantage of being highly irritative to administered regions (The PII value showing a primary irritant index to rabbit skins of the patch formulation is 2.2, which is a very high value compared with that of the formulation of the present invention which is 0.3 to 0.8 (see Table 3).
Further, although the attempts to formulate fentanyl citrate into a tape formulation for percutaneous administration have been made, it could not be used clinically, since the solubility of fentanyl citrate in nonaqueous base is low and thus the transdermal permeable property of the formulation, in which fentanyl is contained in a nonaqueous base, is very low.
Therefore, an object of the present invention is to dissolve the above problems in connection with the prior arts, and to provide a tape formulation for percutaneous administration containing fentanyl, which has a low irritative property to skin, which is extremely excellent in the transdermal permeable property of fentanyl, and which is stable during the storage period.
The present inventors have researched earnestly in order to achieve the above object, and as the results, they found that a tape formulation for percutaneous administration which is extremely excellent in transderaml permeable property and which has a low irritative property to skin, can be prepared, by adding sodium acetate to a pressure sensitive adhesive base containing fentanyl or a salt thereof, and thus completed the present invention.


DISCLOSURE OF INVENTION

Thus the present invention relates to a tape formulation for percutaneous administration containing fentanyl which comprises fentanyl or a salt thereof, a pressure sensitive adhesive and sodium acetate.
The present invention also relates to the tape formulation for percutaneous administration containing fentanyl, which comprises 0.05 to 20%(w/w) of fentanyl or a salt thereof, 0.1 to 98%(w/w) of a pressure sensitive adhesive and 0.01 to 15%(w/w) of sodium acetate.
The present invention also relates to the tape formulation for percutaneous administration containing fentanyl, wherein the salt of fentanyl is fentanyl citrate.
The present invention also relates to the tape formulation for percutaneous administration containing fentanyl, wherein the weight ratio of formulation of fentanyl citrate and sodium acetate is (1 to 5):(0.5 to 2.5).
The present invention also relates to the tape formulation for percutaneous administration containing fentanyl, wherein the weight ratio of formulation of fentanyl citrate and sodium acetate is (3 to 5):(1.5 to 2.5).
The present invention also relates to the tape formulation for percutaneous administration containing fentanyl, wherein the weight ratio of formulation of fentanyl citrate and sodium acetate is 2:1.
The present invention also relates to the tape formulation for percutaneous administration containing fentanyl, which further comprises an oil and/or a tackifier.
The present invention also relates to the tape formulation for percutaneous administration containing fentanyl,

REFERENCES:
patent: 5176916 (1993-01-01), Yamanaka et al.
patent: 5462744 (1995-10-01), Gupte et al.
patent: 5484913 (1996-01-01), Stillwell

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