Tape preparation
View Patent ↗It is intended to provide a preparation for percutaneous administration of 2-(4-ethyl-1-piperazinyl)-4-(4-fluoro-phenyl)-5,6,7,8,9,10-hexahydrocycloocta[b]pyridine (Compound A), which inhibits the generation of a metabolite and is capable of continuously maintaining a blood drug level. Specifically, a tape preparation comprising an adhesive layer formed on one surface of a support, characterized in that the adhesive layer contains (1) Compound A or a physiologically acceptable acid addition salt thereof, and (2) an acrylic adhesive, or (1) Compound A or a physiologically acceptable acid addition salt thereof, (2) an acrylic adhesive, and (3) a permeation enhancer is provided.
1. A tape preparation comprising an adhesive layer formed on one surface of a support, wherein the adhesive layer comprises:
(1) 2-(4-ethyl-1-piperazinyl)-4-(4-fluorophenyl)-5,6,7,8,9,10-hexahydrocycloocta[b]pyridine (hereinafter referred to as “Compound A”) or a physiologically acceptable acid addition salt thereof,
(2) an acrylic adhesive, and
(3) lactic acid as a first permeation enhancer in a concentration of 0.1% to about 40% by weight,
wherein Compound A is the only active ingredient in the adhesive layer.
2. The tape preparation of claim 1 wherein the adhesive layer further comprises (4) a second permeation enhancer besides (3) lactic acid as the first permeation enhancer, and
the total concentration of said first and second permeation enhancers is about 0.3% to about 40% by weight.
3. The tape preparation of claim 1 wherein Compound A is present in a concentration of about 0.1% to about 50% by weight.
4. The tape preparation of claim 1 wherein the acrylic adhesive (2) is at least one selected from the group consisting of a (co)polymer mainly containing an alkyl (meth)acrylate, and a copolymer of an alkyl (meth)acrylate and a functional monomer.
5. The tape preparation of claim 2 wherein the second permeation enhancer (4) is at least one selected from the group consisting of a saturated or unsaturated C 7-22 aliphatic alcohol, diisopropyl adipate, medium chain fatty acid triglyceride, propylene glycol, oleic acid, crotamiton, N-methyl-2-pyrrolidone, olive oil, soybean oil, myristic acid, glycerin, macrogol 200, squalane, liquid paraffin, polyoxyethylene(160)polyoxypropylene(40)glycol, polyoxyethylene-nonylphenyl ether, lauromacrogol, α-monoisostearyl glyceryl ether, polyoxyethylene hydrogenated castor oil 10, isopropyl myristate, diethyl sebacate, sorbitan sesquioleate, polyoxyl 40 stearate, polyethylene glycol monolaurate, cetanol.polyethyleneglycol monostearate mixed wax, liquid lanolin, acetic acid, cetyl lactate, oleyl oleate, cetyl 2-ethylhexanoate, n-butyl acetate, l-menthol, methylisobutyl ketone and triacetin.
6. The tape preparation of claim 1 whose target disease is schizophrenia.
7. The tape preparation of claim 1 wherein Compound A is present in a concentration of about 0.5% to about 30% by weight.
8. A tape preparation comprising an adhesive layer formed on one surface of a support, wherein the adhesive layer comprises:
(1) 2-(4-ethyl-1-piperazinyl)-4-(4-fluorophenyl)-5,6,7,8,9,10-hexahydrocycloocta[b]pyridine (hereinafter referred to as “Compound A”) or a physiologically acceptable acid addition salt thereof,
(2) an acrylic adhesive,
(3) lactic acid as a first permeation enhancer, and
(4) a second permeation enhancer,
wherein the total concentration of said first and second permeation enhancers is about 0.01% to about 50% by weight, and
wherein Compound A is the only active ingredient in the adhesive layer.