WO2006085521A1 - Composition medicinale destinee a une absorption transdermique, contenant un antagoniste des recepteurs opioides, un procede de production de celui-ci et un procede destine a favoriser l’absorption transdermique de l’antagoniste - Google Patents

Composition medicinale destinee a une absorption transdermique, contenant un antagoniste des recepteurs opioides, un procede de production de celui-ci et un procede destine a favoriser l’absorption transdermique de l’antagoniste Download PDF

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Publication number
WO2006085521A1
WO2006085521A1 PCT/JP2006/302042 JP2006302042W WO2006085521A1 WO 2006085521 A1 WO2006085521 A1 WO 2006085521A1 JP 2006302042 W JP2006302042 W JP 2006302042W WO 2006085521 A1 WO2006085521 A1 WO 2006085521A1
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WO
WIPO (PCT)
Prior art keywords
fatty acid
acid ester
pharmaceutical composition
transdermal absorption
receptor antagonist
Prior art date
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PCT/JP2006/302042
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English (en)
Japanese (ja)
Inventor
Takayuki Furuishi
Kazuo Tomono
Toyofumi Suzuki
Toshiro Fukami
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Nihon University
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Publication of WO2006085521A1 publication Critical patent/WO2006085521A1/fr

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0014—Skin, i.e. galenical aspects of topical compositions
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/13—Amines
    • A61K31/135—Amines having aromatic rings, e.g. ketamine, nortriptyline
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/439—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom the ring forming part of a bridged ring system, e.g. quinuclidine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/485—Morphinan derivatives, e.g. morphine, codeine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/14—Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/26—Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/70—Web, sheet or filament bases ; Films; Fibres of the matrix type containing drug
    • A61K9/7023—Transdermal patches and similar drug-containing composite devices, e.g. cataplasms

Definitions

  • composition for percutaneous absorption containing an opioid receptor antagonist, method for producing the same, and method for promoting percutaneous absorption of said antagonist
  • the present invention relates to a pharmaceutical composition for transdermal absorption containing an obioid receptor antagonist, and more specifically, pentazocine and the like, and specific fatty acid esters and glycerin fatty acid esters as transdermal absorption accelerators.
  • the present invention relates to a pharmaceutical composition for transdermal absorption containing the like and a method for producing the same. Background art
  • Obioid receptor antagonists typified by pentazocine have been known as analgesics and have been administered to patients in dosage forms such as oral preparations, injections, and suppositories.
  • a powerful oral preparation has the disadvantage that the medicinal effect does not last for a long time
  • a powerful injection has the disadvantage that administration itself causes pain to the patient.
  • suppositories improve the above-mentioned drawbacks of oral and injectables, but the improvement effect is not sufficient, and patient discomfort due to the route of suppository administration is large. RU
  • Patent Document 1 one or more dermally selected from the group consisting of the above-mentioned drug, polyoxyethylene lauryl ether having 6 to 12 oxyethylene chains, hydroxycarboxylic acid having 2 to 8 carbon atoms, and lower alcohol with dicarboxylic acid.
  • a transdermal absorption patch in which an adhesive layer containing an absorption accelerator and an adhesive is laminated is disclosed.
  • an ovioid receptor antagonist having an analgesic effect is used for postoperative pain management and suppression of cancer pain.
  • injections and oral agents often have short blood half-life. It has been pointed out that it is inconvenient for patients because it requires multiple doses.
  • an object of the present invention is to provide a pharmaceutical composition for efficient transdermal absorption of an ovioid receptor antagonist represented by pentazocine and the like having analgesic activity in order to realize treatment that eliminates the above-mentioned drawbacks.
  • the present invention has been made in view of the above circumstances, and when the present inventors diligently studied a percutaneous absorption enhancer, the percutaneous absorption of an obioid receptor antagonist is a specific fatty acid ester.
  • the inventors By combining glycerin fatty acid ester and the like, the inventors have found that it can be remarkably improved, and have completed the present invention.
  • a pharmaceutical composition for percutaneous absorption comprising an obioid receptor antagonist, a fatty acid ester, and a glycerin fatty acid ester or a sorbitan fatty acid ester,
  • the fatty acid ester is a fatty acid ester having a fatty acid having 6 to 22 carbon atoms and an alcohol having 1 to 12 carbon atoms, [1 potato, a pharmaceutical composition for transdermal absorption according to [2], 4] The pharmaceutical composition for transdermal absorption according to any one of [1] to [3], wherein the fatty acid ester is isopropyl myristate,
  • the glycerin fatty acid ester or sorbitan fatty acid ester is C to C
  • the pharmaceutical composition for transdermal absorption according to any one of [1], [4], which is a medium-chain glycerin fatty acid ester or sorbitan fatty acid ester, [6]
  • the glycerin fatty acid ester or sorbitan fatty acid ester is also selected from the group power consisting of glyceryl prillate, glyceryl phosphonate, sorbitan caprate and glyceryl laurate, [1] to [5]
  • the glycerin fatty acid ester is selected from the group force consisting of mono-strength glyceryl prillate, mono-strength monophosphate, and glycerin mono-laurate, [1] to [6]
  • a pharmaceutical composition for skin absorption is selected from the group force consisting of mono-strength glyceryl prillate, mono-strength monophosphate, and glycerin mono-laurate, [1] to [6] A pharmaceutical composition for skin absorption,
  • composition is suitable for a dosage form in which a group strength consisting of a patch, a tape, a cream, a lotion, an ointment, and a gel is also selected. Any one of [1] to [7] A pharmaceutical composition for transdermal absorption as described in
  • a production method comprising a step of adding a fatty acid ester and a glycerin fatty acid ester or a sorbitan fatty acid ester to the ovoid receptor antagonist;
  • obioid receptor antagonist is selected from the group consisting of pentazocine, ebutazosin hydrobromide, buprenorphine hydrochloride, tramadol hydrochloride and butorphanol tartrate,
  • the fatty acid ester is a fatty acid ester having a fatty acid having 6 to 22 carbon atoms and an alcohol having 1 to 12 carbon atoms, [9] The production method according to [10],
  • the glycerin fatty acid ester or sorbitan fatty acid ester is C to C
  • the glycerin fatty acid ester or sorbitan fatty acid ester is composed of glyceryl prillate, glyceryl phosphonate, sorbitan caprate and glyceryl laurate.
  • composition is suitable for a dosage form in which a group strength consisting of a patch, a tape, a cream, a lotion, an ointment, and a gel is also selected. Any one of [9] to [15] The manufacturing method described in
  • the present invention provides
  • a method of promoting comprising the step of coexisting a fatty acid ester and a glycerin fatty acid ester or a sorbitan fatty acid ester together with the above-mentioned opioid receptor antagonist, [18]
  • the above-mentioned opioid receptor antagonist is pentazocine, ebazosin hydrobromide, buprenorphine hydrochloride,
  • the accelerating method according to [17] selected from the group consisting of tramadol hydrochloride and butorphanol tartrate,
  • the glycerin fatty acid ester or sorbitan fatty acid ester is C to C
  • the glycerin fatty acid ester or sorbitan fatty acid ester is selected from the group force consisting of glyceryl prillate, glyceryl purinate, sorbitan caprate, and glyceryl laurate, and any one of [17] to [21]
  • the skin absorptivity of pentazocine is remarkably improved, and a sufficient amount of pentazocine can be permeated through the skin for a long period of time, resulting in a higher analgesic effect. Is realized.
  • the pharmaceutical composition for percutaneous absorption comprises an ovioid receptor antagonist represented by pentazocine and a percutaneous absorption enhancer comprising a fatty acid ester and a fatty acid glycerin ester.
  • ovioid receptor antagonist represented by pentazocine
  • a percutaneous absorption enhancer comprising a fatty acid ester and a fatty acid glycerin ester.
  • specific examples of the obioid receptor antagonist used in the present invention include, but are not limited to, pentazocine, eptazocine hydrobromide, buprenorphine hydrochloride, tramadol hydrochloride, and butorphanol tartrate.
  • fatty acid esters constituting the transdermal absorption enhancer used in the present invention are not limited to the following, but fatty acids having 6 to 22 carbon atoms and carbon atoms having 1 to 12 carbon atoms. Fatty acid esters that have an alcohol power. Specific examples of fatty acids having 6 to 22 carbon atoms include caproic acid, enanthic acid, force prillic acid, force puric acid, undecylenic acid, lauric acid, myristic acid, palmitic acid, margaric acid, stearic acid, oleic acid, linol. Examples thereof include monocarboxylic acids such as acids, and dicarboxylic acids such as adipic acid and sebacic acid.
  • alcohols having 1 to 12 carbon atoms include methanol, ethanol, propanol, isopropanol, butanol, tert-butanol, hexanol, and octanol. Therefore, specific examples of fatty acid esters include diisopropyl adipate, decyl sebacate, isopropyl myristate, isopropyl palmitate.
  • Examples include pill, isopropyl stearate, butyl stearate, octyldodecyl myristate, butyl myristate, hexyl laurate, octyl palmitate, ethyl oleate, and the like. Among them, isopropyl myristate is preferable.
  • These fatty acid esters can be used alone or in admixture of two or more.
  • glycerin fatty acid ester or sorbitan fatty acid ester constituting the transdermal absorption enhancer used in the present invention are not limited to the following, but include c to c medium chain fatty acid glycerin.
  • Esters or sorbitan fatty acid esters are not limited to the following, but include c to c medium chain fatty acid glycerin.
  • glyceryl prillate glyceryl purinate, glyceryl laurate, glyceryl palmitate, glycol oleate, glyceryl stearate, glyceryl dicaprylate, glyceryl triphosphate, glyceryl triphosphate
  • glyceryl triphosphate examples include glycerin and strong sorbitan purinate. More preferably, glyceryl monophosphate, glyceryl monocaprate, and glyceryl monolaurate are used. These glycerin fatty acid esters or sorbitan fatty acid esters may be used alone or in combination of two or more.
  • the blending amount of the ovioid receptor antagonist in the pharmaceutical composition for transdermal absorption according to the present invention varies depending on the dosage form described below, etc. Preferably, it is 0.05 to 5.0% by weight, and more preferably 0.1 to 3.0% by weight.
  • the amount of fatty acid ester and glycerin fatty acid ester or sorbitan fatty acid ester of the pharmaceutical composition for transdermal absorption according to the present invention varies depending on the dosage form described later, but is 0. It is preferably 1 to 40% by weight. When the amount is less than 1% by weight, the effect of promoting the percutaneous absorption of the drug is lowered. On the other hand, when the amount is more than 40% by weight, the compatibility in the composition is deteriorated.
  • the dosage form of the pharmaceutical composition for percutaneous absorption according to the present invention is not particularly limited, and can be various dosage forms that absorb the drug from the skin.
  • Specific examples of powerful dosage forms include patches, tapes, creams, lotions, ointments and gels.
  • the pharmaceutical composition for transdermal absorption according to the present invention comprises, in a conventional manner, each component constituting the pharmaceutical composition, components necessary for the dosage form to be produced, that is, a base, an adjuvant, and an additive. Etc. can be manufactured by combining them as necessary.
  • the pharmaceutical group according to the present invention The composition can be prepared by arbitrarily adding each component and mixing them.
  • the patch to which the pharmaceutical composition according to the present invention is applied comprises a support, a pressure-sensitive adhesive layer capable of releasing a drug, and a release film for protecting the paste layer.
  • a pressure-sensitive adhesive layer capable of releasing a drug
  • a release film for protecting the paste layer.
  • Each component of the pharmaceutical composition for transdermal absorption according to the present invention is blended in the plaster layer, and further, a base for patch is also blended.
  • the patch base contains an adhesive component. Examples of such components include natural or synthetic rubbers, superabsorbent polymers, and hydrophilic polymers.
  • the tape to which the pharmaceutical composition according to the present invention is applied is a flexible support comprising a plaster obtained by mixing each component of the pharmaceutical composition for transdermal absorption according to the present invention with an adhesive. It can be manufactured by applying it on top.
  • Specific examples of the pressure-sensitive adhesive used in the present invention are not limited to the following, but include acrylic ester-based, rubber-based, and silicon-based adhesives.
  • the cream to which the pharmaceutical composition according to the present invention is applied has a carbonic acid such as higher fatty acid esters such as palmitic acid esters and fluidized roseffins in each component of the pharmaceutical composition for transdermal absorption according to the present invention. It can be produced by adding hydrogen, purified water, emulsifiers such as polyoxyethylene alkyl ethers, and the like. In the case of a liquid preparation, it can be produced by adding each of the above components to a liquid higher fatty acid, vegetable oil or the like.
  • the lotion to which the pharmaceutical composition according to the present invention is applied comprises dissolving, emulsifying or embedding each component of the pharmaceutical composition for percutaneous absorption according to the present invention in a lower alcohol such as ethyl alcohol and / or purified water. It can be produced by suspending.
  • the ointment to which the pharmaceutical composition according to the present invention is applied includes each component of the pharmaceutical composition for transdermal absorption according to the present invention, an ointment base such as petrolatum, macrogol, paraffin, light water-free It can be produced by adding an auxiliary agent such as cai acid, a surfactant, a stabilizer such as dibutylhydroxytoluene, and a pH adjuster if necessary.
  • an auxiliary agent such as cai acid, a surfactant, a stabilizer such as dibutylhydroxytoluene, and a pH adjuster if necessary.
  • the gel to which the pharmaceutical composition according to the present invention is applied includes each component of the pharmaceutical composition for transdermal absorption according to the present invention, a lower alcohol such as ethyl alcohol, purified water, a carboxyvinyl polymer, It can be produced by containing a gelling agent such as ethyl cellulose and a neutralizing agent such as triethanolamine.
  • a lower alcohol such as ethyl alcohol
  • purified water purified water
  • a carboxyvinyl polymer It can be produced by containing a gelling agent such as ethyl cellulose and a neutralizing agent such as triethanolamine.
  • Example [0026] The present invention will be described in more detail with reference to the following examples and comparative examples of the present invention. These are illustrative, and the present invention is not limited to the following specific examples. Those skilled in the art can implement the present invention by making various modifications to the examples shown below, and such modifications are encompassed in the scope of the claims of the present application.
  • PTZ pentazocine
  • IPM isopropyl myristate
  • the receptor phase was filled with isotonic phosphate buffer (PBS, pH 7.4) heated to 32 ° C, and 0.5 mL of the receptor phase PBS in the cell was collected over time. These were used as measurement samples. In addition, PBS was supplemented with 0.5 mL after collection. The measurement sample was quantified by high performance liquid chromatography under the following conditions.
  • PBS isotonic phosphate buffer
  • UV absorbance meter (measurement wavelength: 278nm)
  • the donor phase was prepared using the above test except that 5 mg of PTZ was only dissolved in 490 L of IPM. Performed similarly to the preparation of the donor phase described in the method.
  • a donor phase was prepared using IPM and citrate as a transdermal absorption enhancer.
  • a donor phase was prepared using IPM and N-methyl-2-pyrrolidone as a transdermal absorption enhancer.
  • a donor phase was prepared using IPM and 1-menthol as a transdermal absorption enhancer.
  • a donor phase was prepared using IPM and lactic acid as a transdermal absorption enhancer.
  • a donor phase was prepared using IPM and urea as transdermal absorption enhancers.
  • a donor phase was prepared using IPM and propylene glycol as transdermal absorption enhancers.
  • a donor phase was prepared using IPM and ethanol as a transdermal absorption enhancer.
  • a donor phase was prepared using IPM and 1-octadecanol as a transdermal absorption enhancer Reference Example 9
  • a donor phase was prepared using IPM and polyoxyethylene lauryl ether as transdermal absorption enhancers.
  • a donor phase was prepared using IPM and sodium hyaluronate as a transdermal absorption enhancer Example 1
  • the donor phase was prepared using IPM and mono force glyceryl prillate as a transdermal absorption enhancer.
  • a donor phase was prepared using IPM and mono-powered glyceryl monophosphate as a transdermal absorption enhancer.
  • a donor phase was prepared using IPM and glyceryl monolaurate as transdermal absorption enhancers.
  • FIG. 1 The results of permeation rate, rise time, and cumulative permeation rate for various compounds that promote percutaneous absorption of pentazocine are shown.
  • the cumulative permeation amount shown in Fig. 1 represents the permeation amount of total pentazocine per unit area up to 24 hours after the measurement. From the results shown in Fig. 1, it was found that IPM and monostrength glyceryl prillate, glyceryl monoprinate and glyceryl monolaurate have the group power of choice.
  • the selected compound significantly improves the transdermal absorption of pentazocine.
  • the transdermal absorption enhancer consisting of IPM and glyceryl monophosphate, improved the onset of pentazocine permeation and increased the permeation rate of pentazocine more than 3 times. This also suggests that by improving the permeability of pentazocine through the skin, pentazocine is quickly transferred into the blood through the skin, and the blood concentration of pentazocine is maintained at a higher level.
  • FIG. 2 is a graph showing the cumulative transmission values obtained in the control over time, Example 1 and Comparative Example. As is clear from FIG. 2, it can be seen that the pharmaceutical composition for percutaneous absorption according to Example 1 of the present invention is markedly improved compared to the control and comparative examples.
  • Fig. 3 is a graph showing the cumulative transmission amount obtained in the control over time, Examples 1 to 3. According to the results shown in FIG. 3, the cumulative permeation amount of the pharmaceutical composition for transdermal absorption according to Examples 1 to 3 is increased with respect to the control. In particular, the cumulative permeation amount of Example 1 is notable. It is improved. [0032] Next, for the purpose of further enhancing skin permeability, a sample in which PTZ was suspended in a solution of IPM solution with or without glyceryl monophosphate (10% W / W), ie, PTZ concentration A test was conducted on a sample that was saturated. Fig.
  • FIG. 4 shows the results of cumulative permeation amount of PTZ of IPM solution with and without added monoglyceryl monophosphate (GMC: 10% W / W) over time.
  • FIG. 5 shows specific values for the transmission speed, the rise time, and the accumulated transmission amount obtained from the results shown in FIG. From the results shown in Fig. 4 and Fig. 5, when dariserine monophosphate is added, the penetration rate is about 7 times that of the case without addition, and PTZ skin penetration is increased by increasing the PTZ concentration. It became clear that the property improved.
  • FIG. 6 shows the results of a hairless mouse skin permeability test of the tape prepared in the present invention. From the permeation profile shown in FIG. 6, it was found that permeation of the pharmaceutical composition for transdermal absorption according to the present invention using GMC can last up to 48 hours.
  • the tape preparation shown in FIG. 6 had a permeation rate of 13.3 ⁇ g / cm 2 / hr and a cumulative permeation rate of 347.9 mg / cm 2 .
  • the skin absorptivity of pentazocine is remarkably improved, and a sufficient amount of pentazocine can be permeated through the skin for a long time, so that it has a higher analgesic effect. Is realized.
  • FIG. 1 shows the results of permeation rate, rise time, and cumulative permeation rate in various compounds that promote percutaneous absorption of pentazocine according to the present invention.
  • FIG. 2 is a graph showing cumulative permeation values obtained in control over time, Example 1 and Comparative Example. Each figure is an average of 4 times.
  • FIG. 3 is a graph showing cumulative permeation values obtained in Examples 1 to 3 for control over time. Each figure is an average of 4 times.
  • Fig. 4 shows the cumulative PTZ of the IPM solution with and without GMC (10% W / W) over time. The result of the product permeation amount is shown. Each figure is an average of 4 times.
  • FIG. 5 shows specific values of permeation speed, rise time, and cumulative permeation amount obtained from the results shown in FIG.
  • FIG. 6 shows the results of a hairless mouse skin permeability test of the tape prepared in the present invention. Each figure is an average of 4 times.

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Abstract

La présente invention concerne une composition médicinale destinée à l’absorption transdermique efficace d’un antagoniste des récepteurs opioïdes, représenté par la pentazocine, dotée notamment d’un effet analgésique. La composition médicinale pour absorption transdermique contient un antagoniste des récepteurs opioïdes, un ester d’acide gras ainsi qu’un ester d’acide gras de glycérol ou un ester d’acide gras de sorbitane. De manière plus spécifique, l’ester d’acide gras décrit ci-dessus est préparé à partir d’un acide gras ayant de 6 à 22 atomes de carbone ainsi que d’un alcool ayant de 1 à 12 atomes de carbone, de préférence le myristate d’isopropyle. L’ester d’acide gras de glycérol ou de sorbitane décrit ci-dessus est sélectionné à partir du groupe se composant de caprylate de glycérol, caprate de glycérol, caprate de sorbitane et laurate de glycérol. Il convient que cette composition médicinale pour absorption transdermique se présente sous une forme posologique sélectionnée parmi le groupe composé d’un timbre transdermique, d’un sparadrap, d’une crème, d’une lotion, d’un onguent et d’un gel.
PCT/JP2006/302042 2005-02-10 2006-02-07 Composition medicinale destinee a une absorption transdermique, contenant un antagoniste des recepteurs opioides, un procede de production de celui-ci et un procede destine a favoriser l’absorption transdermique de l’antagoniste WO2006085521A1 (fr)

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Cited By (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2008105445A1 (fr) * 2007-03-01 2008-09-04 Nihon University Composition pharmaceutique transdermique
WO2011059037A1 (fr) 2009-11-12 2011-05-19 学校法人日本大学 Composition phatmaceutique pour usage externe/
JP2015051961A (ja) * 2013-06-05 2015-03-19 国立大学法人九州大学 経皮吸収基材
JP2016504359A (ja) * 2012-12-28 2016-02-12 テイコク ファーマ ユーエスエー インコーポレーテッド 持続性ブプレノルフィン経皮送達組成物およびそれの使用方法
US9700552B2 (en) 2008-02-28 2017-07-11 Syntropharma Limited Pharmaceutical compositions for treatment of addiction

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JPH02503672A (ja) * 1987-06-01 1990-11-01 ワーナー‐ランバート・コンパニー 水性の系における浸透促進剤としての脂肪酸およびその短鎖エステル
JPH03163014A (ja) * 1989-06-28 1991-07-15 Teisan Seiyaku Kk 貼付剤及びその製造法
WO1994002119A1 (fr) * 1992-07-23 1994-02-03 Hisamitsu Pharmaceutical Co., Inc. Composition de base administrable par injection percutanee et composition de medicament derivee
JPH07304672A (ja) * 1994-05-06 1995-11-21 Nitto Denko Corp 経皮吸収製剤
JPH1036265A (ja) * 1996-07-19 1998-02-10 Nitto Denko Corp ブプレノルフィン経皮吸収製剤

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WO2008105445A1 (fr) * 2007-03-01 2008-09-04 Nihon University Composition pharmaceutique transdermique
JP5230596B2 (ja) * 2007-03-01 2013-07-10 学校法人日本大学 経皮吸収用医薬組成物
US9700552B2 (en) 2008-02-28 2017-07-11 Syntropharma Limited Pharmaceutical compositions for treatment of addiction
US10729686B2 (en) 2008-02-28 2020-08-04 Libero Pharma Limited Pharmaceutical compositions
WO2011059037A1 (fr) 2009-11-12 2011-05-19 学校法人日本大学 Composition phatmaceutique pour usage externe/
CN102781473A (zh) * 2009-11-12 2012-11-14 学校法人日本大学 外用药物组合物
JPWO2011059037A1 (ja) * 2009-11-12 2013-04-04 学校法人日本大学 外用医薬組成物
US9050247B2 (en) 2009-11-12 2015-06-09 Nihon University Pharmaceutical composition for external use
JP2015145429A (ja) * 2009-11-12 2015-08-13 学校法人日本大学 外用医薬組成物を用いた貼付剤
JP2016504359A (ja) * 2012-12-28 2016-02-12 テイコク ファーマ ユーエスエー インコーポレーテッド 持続性ブプレノルフィン経皮送達組成物およびそれの使用方法
JP2015051961A (ja) * 2013-06-05 2015-03-19 国立大学法人九州大学 経皮吸収基材

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