JP2016003196A - Percutaneous absorption preparation - Google Patents

Abstract

PROBLEM TO BE SOLVED: To provide a lidocaine-containing percutaneous absorption preparation which can be produced conveniently and can express lidocaine drug action rapidly.SOLUTION: The invention provides a percutaneous absorption preparation in which an adhesive layer containing an agent is formed on a support. The adhesive contains (a) lidocaine or a salt thereof, (b) lactic acid, (c) thermoplastic elastomer, and (d) liquid paraffin, wherein the molar content of the lactic acid (b) is more than 0.9 times to less than 1.0 times to the molar content of the lidocaine.

Description

  The present invention relates to a transdermally absorbable preparation using lidocaine as a drug. More specifically, the present invention relates to a transdermally absorbable preparation that improves the drug release by containing a specific amount of lactic acid.

  Lidocaine, a local anesthetic, has been studied for various external preparations such as ointments and patches. Pain for patients such as pain relief at the time of venous needle puncture and pain relief at skin laser irradiation therapy This medicine is indispensable to relieve However, conventional ointments and patches have the disadvantage that the analgesic effect does not appear unless they are applied to or stuck to the skin and wait for 30 minutes or longer.

  In recent years, the development of a physical percutaneous absorption promotion method has been actively studied as one means for promptly exerting a medicinal effect. For example, by a new transdermal delivery system using a soluble microneedle array chip as a preparation. It is known that the analgesic effect is exhibited within 5 minutes after administration (Patent Document 1). However, since the microneedle is a device with a special structure, there are problems in mass productivity and productivity, such as a complicated manufacturing process.

JP 2013-32324 A

  An object of the present invention is to provide a transdermally absorbable preparation that can be easily produced and can rapidly develop the efficacy of lidocaine.

As a result of intensive studies in view of the above problems, the present inventors have found that the above-described problems can be achieved by including a specific amount of lactic acid in lidocaine, and have completed the present invention.
That is, the present invention provides the following percutaneous absorption preparations (1) to (6).
(1) A percutaneous absorption preparation in which a pressure-sensitive adhesive layer containing a drug is formed on a support, wherein the pressure-sensitive adhesive in the pressure-sensitive adhesive layer is (a) lidocaine or a salt thereof, (b) lactic acid, (c ) A thermoplastic elastomer, and (d) liquid paraffin, and (b) transdermal where the lactic acid content is more than 0.9 to less than 1.0 times the lidocaine content. Absorption formulation.
(2) The percutaneous absorption preparation according to (1), wherein the thermoplastic elastomer (c) is a styrene-isoprene-styrene copolymer.
(3) The percutaneous absorption preparation according to (1) or (2), wherein the thermoplastic elastomer (c) is contained in an amount of 10 to 30% by weight based on the total amount of the pressure-sensitive adhesive.
(4) The transdermally absorbable preparation according to any one of (1) to (3), wherein (d) liquid paraffin contains 30 to 65% by weight of the total amount of the adhesive.
(5) The above (1) to (5), wherein the weight ratio C: D of the content C of the thermoplastic elastomer (c) and the content D of the liquid paraffin (d) is 3: 7 to 5: 5. (4) The transdermally absorbable preparation according to any one of (4).
(6) (b) The content molar amount of lactic acid is 0.92 to 0.98 times the content molar amount of lidocaine, according to any one of (1) to (5) above Percutaneous absorption preparation.

  The transdermal absorption preparation of the present invention has sufficient transdermal absorbability even with a single-layer matrix type patch by adding a specific amount of lactic acid to lidocaine, and shortens the onset of anesthetic effect. There is an advantage that you can.

It is the figure which showed the measurement result of the permeation | transmission speed | velocity | rate of the transdermal absorbability evaluation test which concerns on Test Example 1 of this invention. It is the figure which showed the result of the skin surface anesthetic effect test which concerns on Test Example 2 of this invention.

  The transdermally absorbable preparation of the present invention has a support and at least one pressure-sensitive adhesive layer provided on the support.

  The pressure-sensitive adhesive in the pressure-sensitive adhesive layer of the present invention contains (a) lidocaine or a salt thereof, (b) lactic acid, (c) a thermoplastic elastomer, and (d) liquid paraffin.

[Adhesive]
(A) Lidocaine or a salt thereof Lidocaine that can be used in the present invention may be a free form of lidocaine or a pharmaceutically acceptable salt of lidocaine. The pharmaceutically acceptable salt is not particularly limited, and may be an inorganic salt or an organic salt.
Examples of inorganic salts of lidocaine include hydrochloride, hydrobromide, nitrate, sulfate, phosphate, etc., and examples of organic acid salts include formate, acetate, trifluoroacetate, propionic acid. Salt, lactate, tartrate, oxalate, fumarate, maleate, citrate, malonate, methanesulfonate and the like can be mentioned.
Among the above-mentioned lidocaine and lidocaine salts, free lidocaine or lidocaine hydrochloride can be preferably used from the viewpoint of easy availability, and free lidocaine can be used from the viewpoint of dispersibility in an adhesive and the like. It is particularly preferable to use it.

  The compounding amount of lidocaine or a salt thereof is 10% to 30% by mass based on the total mass of the pressure-sensitive adhesive layer, from the viewpoint that the medicinal effect can be sufficiently obtained and the physical properties such as the adhesive property of the pressure-sensitive adhesive layer. In particular, it is preferable to add 10% by weight to 20% by weight. Furthermore, it is most preferable to blend 13 to 16% by weight.

(B) Lactic acid The lactic acid that can be used in the present invention is not particularly limited, and those that are commercially available can be used, and are L-forms or D-forms that are enantiomers, and racemates. Any lactic acid in the DL-form can be used.

  The molar amount of lactic acid is more than 0.9 times to less than 1.0 times the molar amount of lidocaine in terms of excellent lidocaine permeation rate, and 0.92 times in terms of particularly excellent permeation rate. ˜0.98 times are preferable, and 0.93 times to 0.95 times are particularly preferable.

(C) Thermoplastic elastomer The thermoplastic elastomer that can be used in the transdermally absorbable preparation of the present invention is not particularly limited as long as it becomes a base of the pressure-sensitive adhesive layer. And silicon-based polymers.

  Examples of the rubber polymer include styrene-isoprene-styrene block copolymer, polyisobutylene, styrene-butadiene-styrene block copolymer, natural rubber, butyl rubber, polyisoprene and polybutene.

Examples of the acrylic polymer include acrylic acid / octyl acrylate ester copolymer, 2-ethylhexyl acrylate / vinyl pyrrolidone copolymer solution, acrylate-vinyl acetate copolymer, 2-ethylhexyl acrylate-methacrylic acid. Acid 2-ethylhexyl / dodecyl methacrylate copolymer, methyl acrylate-acrylic acid 2-ethylhexyl copolymer resin emulsion, adhesive such as acrylic polymer contained in acrylic resin alkanolamine liquid, DURO-TAK acrylic adhesive Series (made by National Starch and Chemical Co., Ltd.), Eudragit series (Higuchi Shokai) and the like.
Examples of the silicon polymer include dimethylsiloxane / methylsiloxane copolymer and dimethylpolysiloxane.

  Preferred thermoplastic elastomers include styrene-isoprene-styrene block copolymers, polyisobutylenes, styrene-polymers from the viewpoints of sufficient adhesiveness and low skin irritation, as well as availability and handling properties for skin application. A rubber polymer such as a butadiene-styrene block copolymer, and the most preferable thermoplastic elastomer includes a styrene-isoprene-styrene block copolymer. In addition, these thermoplastic elastomers may be used alone or in combination of two or more.

  The content of the thermoplastic elastomer is not particularly limited as long as it does not impair the effects of the present invention, such as pressure-sensitive adhesive and drug release properties, but it is based on the total amount of the pressure-sensitive adhesive component in terms of excellent pressure-sensitive adhesiveness and workability. It is preferably 10% by weight to 30% by weight, and particularly preferably 15% by weight to 25% by weight.

(D) Liquid paraffin Although the liquid paraffin which can be used by this invention is not specifically limited, A commercially available thing can be used conveniently.

  The content of the liquid paraffin is not particularly limited as long as it does not impair the effects of the present invention, such as the pressure-sensitive adhesive and drug release properties. 30 wt% or more and 65 wt% or less is preferable, and 35 wt% or more and 60 wt% or less is particularly preferable.

  In addition, (c) thermoplastic elastomer and (d) liquid paraffin are (c) thermoplastic elastomer content C and (d) liquid paraffin content D in terms of particularly excellent tackiness and workability. It is preferable that the weight ratio C: D is mixed in the range of 3: 7 to 5: 5. In addition, in the transdermally absorbable preparation of the present invention, by adopting the contents of the above-mentioned (c) thermoplastic elastomer and (d) liquid paraffin, it exhibits good adhesiveness even without adding a tackifier. There are cases where it is possible.

  As used herein, “tackifier” is a tackifier that is generally used in the field of patches, such as rosin resins, polyterpene resins, coumarone-indene resins, petroleum resins, terpene-phenol resins, Examples include alicyclic saturated hydrocarbon resins. From the viewpoint of reducing skin irritation and the like, it is most preferable not to contain a tackifier, but when it is included, the content of the tackifier is preferably 20% by weight or less, preferably based on the total amount of the adhesive component. Is 10% by weight or less, more preferably 5% by weight or less.

(E) Other components Further, the pressure-sensitive adhesive contains (e1) a surfactant, (e2) an absorption accelerator, (e3) alcohols, (e4) an antioxidant, (e5) a filler, etc., as necessary. Can be included.

(E1) Surfactant Examples of the surfactant include nonionic surfactants, anionic surfactants, cationic surfactants, and amphoteric surfactants.

  Nonionic surfactants include, for example, sorbitan monolaurate, sorbitan monopalmitate, sorbitan sesquioleate, glycerol monooleate, glycerol monostearate, decaglyceryl monolaurate, hexaglycerin polyricinoleate, polyoxyethylene (9) Lauryl ether, polyoxyethylene (2) lauryl ether, polyoxyethylene (4,2) lauryl ether, polyoxyethylene (5) nonylphenyl ether, polyoxyethylene (7,5) nonylphenyl ether, polyoxy Ethylene (10) nonylphenyl ether, polyoxyethylene (3) octylphenyl ether, polyoxyethylene (10) octylphenyl ether, polyoxyethylene (10) oilylamine, polyoxyethylene (10) Oxy (5) oleylamine, polyoxy (5) oleic acid amide, polyoxyethylene (2) monolaurate, monoglyceride stearate, polyoxyethylene castor oil (hardened castor oil), and the like.

  Examples of the anionic surfactant include sodium lauryl sulfate, potassium lauryl sulfate, triethanolamine lauryl sulfate, sodium cetyl sulfate, sodium lauroyl sarcosine, di-2-ethylhexyl sodium sulfosuccinate, polyoxyethylene (10) lauryl ether phosphorus Examples thereof include sodium acid, polyoxyethylene (4) sodium lauryl ether phosphate, polyoxyethylene (5) sodium cetyl ether phosphate, polyoxyethylene (6) sodium ether oil phosphate and the like.

  Examples of the cationic surfactant include stearyl trimethyl ammonium chloride, distearyl dimethyl ammonium chloride, benzalkonium chloride, stearyl dimethyl benzyl ammonium chloride, and the like.

  Examples of the amphoteric surfactant include lauryldimethylaminoacetic acid betaine, 2-alkyl-N-carboxymethyl-N-hydroxyethylimidazolinium betaine, and the like. In addition to the above, lauroyl diethanolamide can also be used. Among these, nonionic surfactants are preferable, and sorbitan monolaurate, sorbitan monopalmitate, sorbitan sesquioleate, glycerol monooleate, and glycerol monostearate are more preferable.

  The surfactants may be used alone or in combination of two or more. When a surfactant is contained, it is contained in an amount of 5% by weight or less, preferably 3% by weight or less, based on the total amount of the pressure-sensitive adhesive component, from the viewpoint of maintaining a sufficient permeation rate and sufficient cohesive strength as a transdermal absorption preparation. I can do it.

(E2) Absorption accelerating agent As the absorption accelerating agent, for example, isopropyl isostearate, methyl stearate, butyl stearate, butyl myristate, ethyl linoleate, isopropyl linoleate, ethyl olive oleate, myristyl myristate, cetyl isoctanate Octyldodecyl myristate, diisopropyl adipate, cetyl palmitate, retinol palmitate, methyl laurate, methyl myristate, methyl caproate, methyl palmitate, isopropyl myristate, isopropyl palmitate, diethyl sebacate, diethyl adipate, etc. Fatty acid monohydric alcohol esters such as glyceryl monooleate, glyceryl monocaprate, glycerin dioleate, propylene glycol monostearate And fatty acid polyhydric alcohol esters such as decaoleic acid decaglycerol, for example, fatty acid cyclic polyhydric alcohol esters such as sorbitan monostearate, sorbitan monolaurate, sorbitan monooleate, sorbitan trioleate, ascorbyl palmitate, such as lactic acid Lactic acid esters such as cetyl and myristyl lactate, carbonate esters such as propylene carbonate, and pyrrolidone derivatives such as N-methyl-2-pyrrolidone.

  The absorption accelerator may be used alone or in combination of two or more.

  When an absorption accelerator is contained, it is contained at 15% by weight or less, preferably 10% by weight or less, based on the total amount of the pressure-sensitive adhesive component, from the viewpoint of maintaining a sufficient permeation rate and sufficient cohesive strength as a transdermal absorption preparation. I can do it.

(E3) Alcohols Examples of alcohols include aliphatic alcohols such as ethanol, isopropanol, lauryl alcohol, 2-octyldodecanol, 2-hexyldecanol, ethylene glycol, propylene glycol, 1,3-butanediol, and glycerin, such as salicylic acid. Aromatic alcohols such as glycol and benzyl alcohol can be mentioned. Preferred are aliphatic alcohols, and more preferred are lauryl alcohol, 2-octyldodecanol, 2-hexyldecanol, propylene glycol, 1,3-butanediol and the like. Alcohols may be used alone or in combination of two or more.

  When alcohols are contained, they should be contained in an amount of 15% by weight or less, preferably 10% by weight or less, based on the total amount of the pressure-sensitive adhesive component, from the viewpoint of maintaining a sufficient permeation rate and sufficient cohesive strength as a transdermal absorption preparation. I can do it.

(E4) Antioxidant Examples of the antioxidant include dibutylhydroxyl toluene, 4-dioxyphenol, EDTA-2Na, and the like. Of these, dibutylhydroxyl toluene is preferable. Antioxidants may be used alone or in admixture of two or more.

  When an antioxidant is contained, it is 10% by weight or less, preferably 5% by weight or less, more preferably 5% by weight or less based on the total amount of the pressure-sensitive adhesive component, from the viewpoint of maintaining a sufficient permeation rate and sufficient cohesive strength as a transdermal absorption preparation. Can be contained in an amount of 2% by weight or less.

(E5) Filler A filler can be included in order to control the flexibility of the pressure-sensitive adhesive layer.
Examples of the filler include kaolin, titanium oxide, talc, calcium carbonate, magnesium carbonate, silicate, silicic acid, aluminum hydrate, barium sulfate, and calcium sulfate. The fillers may be used alone or in combination of two or more.

  When a filler is contained, it is 10% by weight or less, preferably 5% by weight or less, more preferably 5% by weight or less based on the total amount of the pressure-sensitive adhesive component, from the viewpoint of maintaining a sufficient permeation rate and sufficient cohesive strength as a transdermal absorption preparation. It can mix | blend at 2 weight% or less.

[Support]
The support of the present invention is not particularly limited, and those generally used can be used. For example, polyester films, polyethylene films, polypropylene films, polyvinyl chloride films, polycarbonate films, polyurethane films and cellophane films and other non-woven fabrics, woven fabrics and knitted fabrics made of foam, polyester fibers, polyethylene fibers, polypropylene fibers, etc. Examples thereof include cloth base materials such as these, and laminates thereof. Among these, nonwoven fabrics, woven fabrics, and knitted fabrics are preferable in terms of stretchability, and plastic films having transparency in terms of usability are preferable.

[Method for preparing adhesive]
The pressure-sensitive adhesive can be adjusted by mixing and stirring the components of the pressure-sensitive adhesive. That is, the pressure-sensitive adhesive can be obtained by mixing and stirring (a) lidocaine or a salt thereof, (b) lactic acid, (c) a thermoplastic elastomer, and (d) liquid paraffin.

The order of mixing may be the above (a) to (d) added sequentially, or the (a) and (b) are mixed in advance and added to the mixture of (c) and (d). And may be mixed.
Moreover, it is preferable to heat at the time of mixing and stirring at the point which is easy to mix uniformly. The heating temperature is not particularly limited as long as the adhesive component does not deteriorate or volatilize, but is preferably 50 ° C to 100 ° C, and more preferably 80 ° C to 90 ° C.

  In addition, from the point which is excellent in the handleability of an adhesive, and the point which is easy to mix uniformly, it is preferable to add a solvent further to an adhesive component and to make an adhesive solution.

  The solvent that can be used in the present invention is not particularly limited as long as it can dissolve the pressure-sensitive adhesive component, but organic solvents such as toluene, hexane, ethyl acetate, and N-methyl-2-pyrrolidone are used. Toluene can be particularly preferably used because it can be preferably used and is soluble or easily dried.

[Method for preparing transdermal absorption preparation]
As a method for producing the transdermally absorbable preparation of the present invention, a method of coating the pressure-sensitive adhesive layer on a support can be suitably used.

  As a method for producing the transdermally absorbable preparation of the present invention, the same method as that for the pressure-sensitive adhesive tape can be employed. For example, a hot melt coating method in which a pressure-sensitive adhesive is heated and melted and coated on a support, or a pressure-sensitive adhesive composition. Examples thereof include a solvent coating method in which a pressure-sensitive adhesive solution obtained by dissolving a product in an organic solvent is coated on a support and dried.

  In addition, as a method for producing the transdermally absorbable preparation of the present invention, the pressure-sensitive adhesive is once coated on the release paper and then peeled off from the release paper and transferred and adhered to the support, or the coated surface is not peeled off. It is also possible to use a method of transferring and adhering to the substrate.

  The release paper is used for the purpose of protecting the pressure-sensitive adhesive layer, and can be appropriately selected depending on the purpose in consideration of easy release from the pressure-sensitive adhesive layer, air permeability, water permeability, flexibility, and the like. Preferably, a film made of a polymer material such as polyethylene, polypropylene and polyester is used, and the film surface can be treated with silicon or fluorocarbon in order to enhance the peelability.

  In the transdermally absorbable preparation of the present invention, the pressure-sensitive adhesive layer may be a single layer or a multilayer of two or more layers. In the case of a multilayer, at least one layer contains lidocaine or a salt thereof and lactic acid. It only has to be.

  Hereinafter, the present invention will be described more specifically with reference to examples and test examples, but the present invention is not limited to these examples.

(Example 1)
23.73 g of styrene-isoprene-styrene block copolymer (hereinafter sometimes referred to as SIS copolymer, product name: JSR SIS 5229) as a thermoplastic elastomer, and 55.37 g of liquid paraffin (Sonneborn) (Product name: Kaydol) was charged with 44.30 g of toluene, mixed, heated and stirred at 80 to 90 ° C. for 120 minutes to completely dissolve, and cooled to 20 to 30 ° C. to obtain solution A. . Next, 11.07 g of 15 g of lidocaine (manufactured by Tokyo Chemical Industry Co., Ltd., product name: Lidocaine) and 5.9 g of L-lactic acid (manufactured by Wako Pure Chemical Industries, Ltd., product name: L-lactic acid, purity: 90%) A solution mixed with toluene was added to the obtained solution A and mixed and stirred at room temperature to obtain a uniform pressure-sensitive adhesive solution. The adhesive solution was applied to an 80 μm-thick polyethylene terephthalate (PET) film (Fujimori Kogyo Co., Ltd., product name: 75E-0010 BD) whose surface was silicon-treated with an applicator, and toluene was heated at 60 ° C. in a hot air oven. After drying and removing for 120 minutes or more and forming a pressure-sensitive adhesive layer having a thickness of 600 to 700 μm after drying, a 60 μm-thick PET film (manufactured by OG Corporation, product name: PET16 white NR embossing) is formed on the surface of the pressure-sensitive adhesive layer. 280 mm) was laminated to prepare the intended percutaneous absorption preparation. The components of the adhesive and the weight ratio (%) are shown in Table 1.

(Examples 2-3, Comparative Examples 1-2)
A percutaneous absorption preparation was prepared in the same manner as in Example 1 except that lidocaine, SIS copolymer, liquid paraffin, and 90% lactic acid were mixed at the ratio shown in Table 1.

[Percutaneous absorption evaluation test using Franz diffusion cell]
(Test Example 1)
The percutaneous absorption preparation produced in Example 1 by attaching the abdominal extracted skin of a male Wister rat (5 weeks old) with hair removal to a vertical Franz diffusion cell (product number: TP-8s). Was punched out into a circle with a diameter of 1.0 cm and pasted on the rat skin of a Franz diffusion cell.
The test was conducted at a buffer temperature of 32 ° C. using 0.01 mol / L phosphate buffered saline (pH 7.2 to 7.4) containing 10% ethanol as a buffer. 0.5, 1, 2, 3, 5, 7 hours after the start of the test, a part of the buffer was extracted, and the amount of lidocaine that permeated the rat skin in the buffer was quantified by HPLC, and the permeation rate of lidocaine was determined from the result. Was calculated. FIG. 1 shows the results of plotting the lidocaine permeation rate.

(Test Examples 2 to 5)
The permeation rate of lidocaine was calculated in the same manner as in Test Example 1 except that the percutaneous absorption preparations prepared in Example 2, Example 3, Comparative Example 1, and Comparative Example 2 were used, and the results are shown in FIG. Indicated.

(Test Example 6)
The same as Test Example 1 except that a commercially available lidocaine transdermal absorption preparation (manufactured by Yutoku Pharmaceutical Co., Ltd., product name: Yupatch (R) tape) containing SIS copolymer, liquid paraffin and 10% by weight lidocaine was used. The permeation rate of lidocaine was calculated by the method, and the results are shown in FIG.
As is apparent from FIG. 1, Test Examples 1 to 3 (lactic acid is 0.92 to 0.98 equivalent) are compared with Test Example 4 (0.9 equivalent) or Test Example 5 (1.0 equivalent). Thus, the permeation speed in the elapsed time 1 to 3 hours is remarkably improved. Furthermore, Test Example 1 to Test Example 3 have a permeation rate of about 5 times or more in the elapsed time 1 to 3 hours as compared with Test Example 6 (commercially available lidocaine patch). In addition, from FIG. 1, Test Examples 1 to 3 tend to have a constant permeation rate when the maximum value of the permeation rate is exceeded. This is due to overdosing caused by an increase in the blood concentration of the local anesthetic. There is an advantage that it becomes easy to control.

[Test on anesthesia of guinea pig skin surface by transdermal preparation]
(Test Example 7)
The percutaneously absorbable preparation prepared in Example 3 was applied to the back of a 5-6 week old Hartley male guinea pig from which hair had been removed, fixed with surgical tape to prevent peeling, and applied for 60 minutes. After peeling the percutaneously absorbable preparation, the presence or absence of a skin contraction reaction when stimulated with a mandolin wire at five predetermined measurement points in the peeled portion was confirmed. The reaction rate% (measurement point showing shrinkage reaction / 5 × 100) was calculated, and the result is shown in FIG.

(Test Example 8)
The same as Test Example 7 except that a commercially available lidocaine transdermal absorption preparation (manufactured by Yutoku Pharmaceutical Co., Ltd., product name: Yupatch (R) tape) containing SIS copolymer, liquid paraffin and 10% by weight lidocaine was used. The reaction rate (%) was calculated by the method, and the results are shown in FIG.
As is clear from FIG. 2, it can be seen that Test Example 7 (transdermal absorption preparation of the present invention) exhibits an anesthetic effect earlier than Test Example 8 (commercial lidocaine patch).

Claims (6)

A transdermally absorbable preparation in which a pressure-sensitive adhesive layer containing a drug is formed on a support, wherein the pressure-sensitive adhesive in the pressure-sensitive adhesive layer is (a) lidocaine or a salt thereof, (b) lactic acid, (c) thermoplasticity A transdermally absorbable preparation containing an elastomer and (d) liquid paraffin, wherein (b) the molar amount of lactic acid is more than 0.9 to less than 1.0 times the molar amount of lidocaine. The percutaneous absorption preparation according to claim 1, wherein the thermoplastic elastomer (c) is a styrene-isoprene-styrene copolymer. The percutaneous absorption preparation according to claim 1 or 2, wherein (c) the thermoplastic elastomer is contained in an amount of 10 to 30% by weight based on the total amount of the pressure-sensitive adhesive. The transdermally absorbable preparation according to any one of claims 1 to 3, wherein (d) liquid paraffin contains 30 to 65% by weight of the total amount of the adhesive. The weight ratio C: D of (c) thermoplastic elastomer content C and (d) liquid paraffin content D is from 3: 7 to 5: 5. A transdermally absorbable preparation according to 1. The percutaneous absorption preparation according to any one of claims 1 to 5, wherein the molar amount of lactic acid (b) is 0.92 to 0.98 times the molar content of lidocaine. .