JPWO2019229249A5 - - Google Patents

Claims (13)

With 0.1-8% by weight nicotine,
A liquid pharmaceutical preparation containing at least 65% by weight of water and one or more of flavoring agents, cosolubilizers and solubilizers.
The preparation contains a cosolubilizer and / or a solubilizer.
The nicotine is in the form of nicotine and nicotine salts of acids.
The pharmaceutical preparation is a liquid pharmaceutical preparation having a pH of 4.5 to 5.9, and the liquid pharmaceutical preparation can be aerosolized to form an inhalable preparation. The acids include acetic acid, acetylsalicylic acid, arginic acid, 2-aminoethanesulfonic acid (taurine), aminomethylphosphonic acid, arachidic acid, ascorbic acid, aspartic acid, azelaic acid, barbituric acid, benzylic acid, benzoic acid and butanoic acid. , Buty acid, capric acid, caproic acid, capric acid, carbonic acid, platinum chloride acid, cinnamic acid, citric acid, decanoic acid, dodecanoic acid, enanthic acid, ethanoic acid, folic acid, formic acid, fumaric acid, gallic acid, gentisic acid, glucon Acids, glutamic acid, glutaric acid, heptanic acid, hexanoic acid, hydrochloric acid, icosanoic acid, ketobutyric acid, lactic acid, lauric acid, levulinic acid, malic acid, maleic acid, malonic acid, margaric acid, methanic acid, 2-methylbutyric acid, 3 -Methylbutyric acid, 2-methylpropanoic acid, 3,7-dimethyl-6-octenoic acid, myristic acid, nonadesilic acid, nonadecanic acid, octadecanoic acid, octanoic acid, oleic acid, oxalic acid, 2-oxobutyric acid, palmitic acid, Pectic acid, pelargonic acid, pentadecanoic acid, pentadecylic acid, pentanic acid, phthalic acid, phenylacetic acid, picric acid, propanoic acid, propiolic acid, propionic acid, pyruvate, quinic acid, rosolic acid, salicylic acid, tonguestosilicic acid, sorbic acid, From stearate, succinic acid, sulfosalicylic acid, tannic acid, tartaric acid, tetradecanoic acid, p-toluenesulfonic acid, tridecanoic acid, tridecylic acid, trifluoroacetic acid, trifluoromethanesulfonic acid, undecanoic acid, undecylic acid, uric acid, and valerian acid. The pharmaceutical preparation according to claim 1, which is selected. The acids include lactic acid, 2-methylpropanoic acid, acetylsalicylic acid, 2-aminoethanesulfonic acid (taurine), aminomethylphosphonic acid, arachidic acid, ascorbic acid, azelaine acid, barbituric acid, benzylic acid, butanoic acid and caprin. Acid, caproic acid, capric acid, carbonic acid, cinnamic acid, decanoic acid, dodecanoic acid, enanthic acid, ethanoic acid, folic acid, fumaric acid, gluconic acid, glutaric acid, heptanic acid, hexanoic acid, icosanoic acid, ketobutyric acid, levulinic acid , Maleic acid, malonic acid, margaric acid, methanic acid, 3,7-dimethyl-6-octenoic acid, myristic acid, nonadecanic acid, nonadesilic acid, octadecanoic acid, octanoic acid, oleic acid, 2-oxobutyric acid, pelargonic acid, Pentadecanoic acid, pentadecylic acid, pentanic acid, propanoic acid, propiolic acid, quinic acid, rosolic acid, sorbic acid, stearic acid, succinic acid, tetradecanoic acid, p-toluenesulfonic acid, tridecanoic acid, tridecylic acid, trifluoroacetic acid, trifluo The pharmaceutical preparation according to claim 2, wherein the acid is preferably lactic acid, selected from a selection from romethanesulfonic acid, undecanoic acid, undecylic acid, and uric acid. The pharmaceutical preparation according to any one of claims 1 to 3, which comprises at least 75% water. The pharmaceutical preparation according to any one of claims 1 to 4, wherein the preparation is an aerosolized mist droplet. In the pharmaceutical preparation according to any one of claims 1 to 5,
(I) The preparation comprises a flavoring agent, optionally the flavoring agent is a tobacco, mint or fruit flavored flavoring agent and / or (ii) the preparation is an additional sweetener. Including pharmaceutical preparations. The preparation contains a cosolubilizer, which is propylene glycol, polyethylene glycol, glycerin, polyethylene glycol / polypropylene glycol copolymer, polyvinylpyrrolidone, 1,2-hexanediol, and the like. The cosolubilizer is preferably selected from 1,2-pentanediol, diethylene glycol monoethyl ether, dimethyl isosorbide, ethanol, n-butanol, n-pentanol, and combinations thereof. The pharmaceutical preparation according to any one of claims 1 to 6, which is propylene glycol, glycerin, or a mixture thereof. The preparation contains a solubilizer, which is polyoxyethylene (40) castor oil, Poroxummer 407 ™ (poly (ethylene glycol) -block-poly (propylene glycol) -block-. Poly (ethylene glycol), polyoxyl (35) castor oil, polyoxyl (40) castor oil, polyoxyl (40) castor oil mixed with PPG-1-PEG 9 lauryl glycol ether, PPG-1-PEG 9 lauryl. Glycol ether, polyoxyethylated 12-hydroxystearic acid, PEG300, PEG400, dioleic acid PEG600 ester, heptyl glucoside, isostearic acid monoisopropanolamide, coconut fatty acid diethanolamide, coconut fatty acid glycol ester, coconut fatty acid monoethanolamide, Coconut fatty acid PEG200 ester, coconut fatty acid PEG600 ester, oleic acid PEG600 ester, oleic acid C12-C14 alkyl ester, oleic acid diethanolamide, oleic acid monoisopropanolamide, oleic acid PEG1000 ester, oleic acid PEG200 ester, rapeseed oil diethanolamide, tall oil Fatty acid diethanolamide, tall oil fatty acid monoisopropanolamide, tall oil PEG200 ester, tall oil PEG600 ester, polysorbate 20, polysorbate 40 (polyoxyethylene sorbitan monopalmitate / Tween ™ 40), polysorbate 60, polysorbate 65, Polysorbate 80 (Tween ™ 80), Polysorbate 85, sorbitan lauric acid monoester, sorbitan monopalmitate, sorbitan monostearate, sorbitan oleic acid monoester, sorbitan monoisostearate, sorbitan tristearate, Cosmacol ™. The liquid pharmaceutical preparation according to any one of claims 1 to 7, which is selected from N119 (C12 to C13Pareth 9) and a mixture thereof. In the pharmaceutical preparation according to any one of claims 1 to 8, the preparation is
With 75-85% by weight of water,
With 0.1-8% by weight nicotine,
With 0.1-15% by weight cosolubilizer,
With 0.5-1.5% by weight of sweetener,
A pharmaceutical preparation containing 0.05 to 1.5% by weight of a flavoring agent. It ’s a way to send nicotine to the subject,
A step of preparing an aerosolizing preparation comprising 0.1-8% by weight of nicotine, at least 65% by weight of water , and one or more of flavoring agents, cosolubilizers, and solubilizers .
The step of administering the aerosolized preparation agent by inhalation comprises.
The preparation comprises a co-solubilizer and / or a solubilizer; the nicotine is in the form of a nicotine salt of nicotine and an acid, and the preparation has a pH of 4.5-5.9.
Method. Further, a step of preparing a liquid preparation containing 0.1 to 8% by weight of nicotine and at least 65% by weight of water, and a step of atomizing the liquid preparation to form the aerosolization preparation. Equipped with, optionally,
10. The method of claim 10, wherein the liquid preparation is atomized by supplying oxygen, compressed air or ultrasonic power to form the aerosolization preparation. A cartridge used for an e-cigarette and containing the preparation according to any one of claims 1 to 9 . An e-cigarette comprising the cartridge according to claim 12.