WO2001093868A1 - Bande adhesive contenant de la buprenorphine - Google Patents

Bande adhesive contenant de la buprenorphine Download PDF

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Publication number
WO2001093868A1
WO2001093868A1 PCT/JP2001/004624 JP0104624W WO0193868A1 WO 2001093868 A1 WO2001093868 A1 WO 2001093868A1 JP 0104624 W JP0104624 W JP 0104624W WO 0193868 A1 WO0193868 A1 WO 0193868A1
Authority
WO
WIPO (PCT)
Prior art keywords
patch
buprenorphine
drug
sensitive adhesive
adhesive layer
Prior art date
Application number
PCT/JP2001/004624
Other languages
English (en)
Japanese (ja)
Inventor
Susumu Maruo
Satoshi Murakami
Osafumi Hidaka
Original Assignee
Teijin Limited
Teysan Pharmaceuticals Co.,Ltd.
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Teijin Limited, Teysan Pharmaceuticals Co.,Ltd. filed Critical Teijin Limited
Priority to AU2001262683A priority Critical patent/AU2001262683A1/en
Publication of WO2001093868A1 publication Critical patent/WO2001093868A1/fr

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Classifications

    • 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
    • A61K9/703—Transdermal patches and similar drug-containing composite devices, e.g. cataplasms characterised by shape or structure; Details concerning release liner or backing; Refillable patches; User-activated patches
    • A61K9/7038—Transdermal patches of the drug-in-adhesive type, i.e. comprising drug in the skin-adhesive layer
    • A61K9/7046—Transdermal patches of the drug-in-adhesive type, i.e. comprising drug in the skin-adhesive layer the adhesive comprising macromolecular compounds
    • A61K9/7053—Transdermal patches of the drug-in-adhesive type, i.e. comprising drug in the skin-adhesive layer the adhesive comprising macromolecular compounds obtained by reactions only involving carbon to carbon unsaturated bonds, e.g. polyvinyl, polyisobutylene, polystyrene
    • A61K9/7061—Polyacrylates
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids

Definitions

  • the present invention relates to a patch containing buprenorphine. More particularly, the present invention relates to a cancer patient or a postoperative patient, particularly to a cancer patient.
  • Cancer is the leading cause of death from Japanese illness, and cancer pain is occurring in many cancer patients. Therefore, alleviating cancer pain is very important in the treatment of cancer itself as well as in reducing the pain of patients.
  • Drugs for cancer pain relief are prescribed according to each stage based on the guideline issued by WH0.
  • the first stage of pain is mainly non-steroid anti-inflammatory drugs
  • the second stage of pain with further increased pain is a weak opiate pain agent
  • the third stage of final pain is morphine.
  • Each of the strong opiates is prescribed.
  • One of the drugs prescribed in these second and third stages is buprenorphine.
  • Buprenorphine has about 30 times the analgesic effect of morphine, and has serious side effects compared to morphine, such as respiratory depression, mental dependence, and And have little physical dependence.
  • a patch of buprenorphine can be obtained by administering a specific amount of buprenorphine from the skin. Is disclosed.
  • Japanese Patent Application Laid-Open Nos. Hei 4-2-179626, Hei 7-10754, Japanese Patent Laid-Open Hei 7-304672, and Japanese Patent Publication No. Hei 10-51 In Japanese Patent Publication No. 25551, a patch is proposed that improves the skin permeability of buprenorphine by using various absorption enhancers.
  • the property required as a patch is not only that the drug is administered from the skin, but also that a therapeutically effective amount of the drug can be administered continuously over a long period of time.
  • buprenorphine has fewer serious side effects than morphine, it does cause side effects once, and if treatment is delayed, it can lead to fatal accidents and irreparable physical disability. If the required amount of drug cannot be administered stably and continuously, there is no medical significance. Disclosure of the invention
  • the purpose of the present invention is to provide a long-lasting,
  • An object of the present invention is to provide a patch which can administer prenorphin and can efficiently administer a required amount of buprenorphine to the skin without leaving a large amount of buprenorphine in the patch.
  • the present inventors have conducted intensive studies and found that a patch having a buprenorphine-containing pressure-sensitive adhesive layer provided on one surface of a support, comprising a patch having a specific drug amount and a specific drug elution rate, The inventors have found that the object of the present invention can be solved, and arrived at the present invention.
  • a first aspect of the present invention is a patch comprising a flexible support and an adhesive layer containing a drug (buprenorphine) provided on one surface thereof, and the patch in one administration.
  • the buprenorphine content is 2 to 12 mg
  • the buprenorphine elution rate is 25% to 45% in 5 minutes, 45% to 80% in 15 minutes, and 120% in 120 minutes.
  • the purpose of the present invention is to provide a patch having a content of 75% or more.
  • a second aspect of the present invention is a patch comprising a flexible support and a buprenorphine-containing pressure-sensitive adhesive layer provided on one surface thereof, wherein the buprenorphine in the patch in one administration is provided.
  • puprenorphine (hereinafter may be referred to as “BN”) may be one whose action in the body is based on buprenorphine.
  • BN puprenorphine hydrochloride Buprenorphine salts such as buprenorphine sulfate are also included.
  • the BN content in one patch in the first and second embodiments of the present invention is 2 to 12 mg.
  • the BN content of a commercially available BN-containing preparation is 0.2 mg or 0.4 mg for an injection (eg, Otsuka Pharmaceutical Lepetan Injection) and a suppository (eg, Otsuka Pharmaceutical). In lepetan suppositories) is 0.2 mg or 0.3 mg.
  • the degree of pain that occurs in cancer patients and postoperative patients varies depending on the degree and sensitivity of the underlying disease and the difference in the drug metabolizing ability of the patients. Therefore, there is no optimal dose for all patients with all diseases. Therefore, it is preferable that the BN-containing preparation for the above-mentioned pain is formulated in accordance with the symptoms and the constitution of the patient, etc.
  • the present inventors have suggested that the dose of BN having a high medical effect is 2 mg to l 2 mg, particularly preferably a 3 mg to 8 mg formulation, to respond to symptoms The result is that it is preferable to be able to increase or decrease the number of times.
  • BN is therapeutically effective depends on the patient's BN concentration in the blood, so even if the BN content in a single patch is more than 12 mg, if the absorption is reduced, it is in principle possible. The same therapeutic effect can be expected. However, it is not preferable that the BN content in a single patch is more than 12 mg in order to guarantee the safety of unspecified number of patients in various lifestyles. Further, it is not economically preferable that the BN content is more than 12 mg because BN is an expensive drug.
  • the BN content of the BN patch is important, and the rate of dissolution of BN from the patch is also specified in order to enhance and maintain the therapeutic effect safely. I found it necessary.
  • the above dissolution rate refers to the test performed in accordance with the Dissolution Test Method 2 of the Japanese Pharmacopoeia.
  • the dissolution test solution is 0.25% sodium peryl sodium sulfate solution, and the solution is rotated. The number is performed at 100 revolutions per minute.
  • the BN elution rate of the patch in the first embodiment of the present invention is 25% to 45% in 5 minutes, 45.% to 80% in 15 minutes, It is important that it is 70% or more in 120 minutes.
  • the patch of the present invention can be used to determine the amount of BN in a single product and to determine the BN dissolution rate based on the results of clinical tests using humans and preliminary tests using animals. This is a patch. Such patches are highly safe and can be expected to have sufficient clinical efficacy.
  • Patches with a BN dissolution rate below the above range have the following problems: First, it is difficult to achieve the BN concentration in blood required for treatment, and second, the duration of the drug effect. Is not sufficient, and thirdly, The time stability is not sufficient, and the residual amount of the drug in the patch after application to the skin increases.
  • the blood concentration of the drug temporarily rises above the effective therapeutic dose in the early stage of administration, second, it is more likely to cause side effects, and third, the duration is shorter. That is.
  • a more preferable range of the elution rate is 25 to 40% in 5 minutes, 48 to 75% in 15 minutes, and 75% or more in 120 minutes. It is.
  • the dissolution rate in the present invention indicates the ratio of the amount of BN released into the eluate for a predetermined period of the effective BN amount contained in the preparation.
  • the drug content in one patch is 2 to 12 mg, and the drug dissolution rate is 25% to 45% in 5 minutes, and 4% in 15 minutes. It is important that it is 5% to 80%, and 70% or more in 120 minutes. Patches that satisfy this condition have high treatment efficiency without causing serious side effects.
  • a general method for controlling the drug release from the preparation can be used.
  • a method of maintaining the concentration of buprenorphine in the adhesive layer at 1% to 30% a method of adding a plasticizer for the adhesive, a method of adding a desired buprenorphine dissolution aid or an absorption promoter, or Examples of the method include a method of laminating a drug release controlling film on a drug-containing pressure-sensitive adhesive layer.
  • the drug content in one patch is 2 to It is important that the drug concentration be 12 mg and that the blood concentration of the drug in humans be between 40 and 150 pg Zml over 48 hours. And in the blood of drugs in humans? It is preferable that the viscosity be 50 to 100 p / m1 over 48 hours or more.
  • the blood concentration or duration of the drug is less than the above range, the following problems occur. First, it is difficult to provide the drug concentration in the blood necessary for treatment.Second, the duration of the drug effect is not sufficient. Furthermore, the amount of drug remaining in the patch after application to the skin is low. That is a lot.
  • the blood concentration of the drug exceeds the above range, the following problems occur.Firstly, the blood concentration of the drug temporarily exceeds the effective therapeutic amount in the early stage of administration, and second, side effects occur. And thirdly, the duration of the drug's blood concentration is reduced.
  • the drug content in one patch is 2 to 12 mg
  • the blood concentration of the drug in human is 40 to 150 pg
  • the patch that satisfied the above was able to obtain a continuous analgesic effect without causing any serious side effects.
  • particularly preferred conditions are when the BN content in the patch is 3 to 8 mg and the blood concentration is 50 to 500 pg / ml. At this time, the analgesic effect was obtained with high efficiency and few side effects.
  • the relationship between the drug concentration C in human blood 48 hours after application of the patch and the maximum blood concentration C max of the drug should be l / 6 C max ⁇ C ⁇ C max. Is preferred. That is, the ratio of C max to C (drug blood concentration 48 hours later) is important.
  • the effective BN blood concentration for analgesic effect varies from individual to individual, but since buprenorphine has serious side effects, the blood concentration is 40-150 pg / ml. Even so, it is not desirable to fluctuate greatly in that range.
  • the maximum value of the blood concentration when the analgesic effect is exerted at a preferable dose is defined as C max, and C is preferably a release tape which is about 1/6 of C max.
  • BN 'concentration C in human blood 48 hours after administration of the patch is less than 1-6 CmaX. These problems are: firstly, decreased treatment efficiency; second, it is difficult to sustain treatment for a long period of time; and third, because the blood concentration of the drug exceeds the suitable blood concentration range, side effects occur. Is more likely to occur.
  • the pressure-sensitive adhesive constituting the pressure-sensitive adhesive layer of the present invention is not particularly limited as long as it has adhesiveness to the skin, and is conventionally known. Can be used.
  • Vinyl-based pressure-sensitive adhesives; acrylate-based pressure-sensitive adhesives containing alkyl acrylate as a main component can be used.
  • acrylate-based pressure-sensitive adhesives are preferred from the viewpoints of pressure-sensitive properties, economy, and stability.
  • carbon number 4 (Meth) acrylic acid obtained by copolymerizing at least 80 to 98 mol% of (meth) acrylic acid alkyl ester of ⁇ 20 and (meth) acrylic acid of 2 to 20 mol%.
  • Alkyl ester copolymers are preferred.
  • alkyl (meth) acrylate examples include, for example, butyl (meth) acrylate, amyl (meth) acrylate, hexyl (meth) acrylate, and heptyl.
  • BN is a salt such as buprenorphine hydrochloride
  • 0.1 to 1 molar equivalent of the amine such as monoethanolamine, diethanolamine, diisopropanolamine or the like with respect to the salt.
  • the release of drugs is improved when inorganic compounds such as inorganic compounds such as sodium hydroxide, calcium hydroxide, calcium hydroxide and sodium hydrogen carbonate are added. I do.
  • the acrylic ester-based pressure-sensitive adhesive is preferred from the viewpoint that the drug release property is significantly improved when the above-mentioned alcoholic compound is added to the acrylate-based pressure-sensitive adhesive.
  • the adhesive strength of the pressure-sensitive adhesive layer is not particularly limited as long as it does not peel off when applied to the skin and does not cause pain when peeled off.
  • the adhesive strength is preferably from 40 g to 400 g in the adhesive strength test of the adhesive plaster of Japanese Pharmacopoeia.
  • the adhesive strength is preferably 80 g to 300 g from the viewpoint that pain upon removal of the drug is small. .
  • the BN concentration in the pressure-sensitive adhesive layer of the present invention is not particularly limited.
  • the only condition required for such BN concentration is that the BN elution rate falls within the above range.
  • the preferred BN concentration is 4 to 25 wt%, particularly preferably 5 to ⁇ 8 wt%.
  • the BN concentration is less than 4 wt%, problems such as thickening of the adhesive layer, skin irritation due to the large area of application, and difficulty in obtaining sufficient skin permeability of the drug occur. This is not preferred.
  • the BN concentration is higher than 25 wt%, the internal cohesive force of the pressure-sensitive adhesive composition, which is one of the important properties of the pressure-sensitive adhesive, is reduced. For this reason, a phenomenon in which a part of the adhesive remains on the skin after the patch is removed from the human, that is, a so-called glue residue increases, which is not preferable. Further, when the BN concentration is higher than 25 wt%, the amount of the residual drug in the patch after use tends to increase, which is not preferable.
  • the following conventionally known methods can be employed as a method for incorporating a drug into an adhesive.
  • a method of preparing a drug-containing pressure-sensitive adhesive layer by premixing a drug solution with a solution-type pressure-sensitive adhesive, or by not impregnating, transferring, spraying, or the like to contain a drug or to sufficiently
  • a method in which a drug is contained in an adhesive layer which does not contain a sufficient amount for transdermal absorption are appropriately adopted depending on the physical properties of the drug to be used.
  • the thickness of the BN-containing pressure-sensitive adhesive layer of the present invention is not particularly limited, but is preferably 3 to 100 m.
  • the amount is preferably from 7 to 50 m, and more preferably from 7 to 20 m, from the viewpoint of reducing the amount of BN used.
  • BN is further added to the first pressure-sensitive adhesive layer.
  • Pressure-sensitive adhesive layer consisting of other pressure-sensitive adhesive base material that does not contain or contains a very small amount
  • the thickness of the pressure-sensitive adhesive layer substantially containing BN, that is, the first pressure-sensitive adhesive layer and the second pressure-sensitive adhesive layer, is reduced. It can be 7 to 50 m.
  • the first pressure-sensitive adhesive layer is a patch in which a patch is used in combination with another support or auxiliary material for the purpose of handling, heat retention, moisture permeability, etc.
  • it refers to a BN-containing pressure-sensitive adhesive layer provided for transdermal absorption by directly facing human skin.
  • the embodiment of the first pressure-sensitive adhesive layer is not particularly limited as long as it contains a drug and can be adhered to the skin. The following embodiments can be exemplified.
  • a substance obtained by dissolving or dispersing a drug in an adhesive polymer a layer obtained by laminating layers having different drug contents, a layer obtained by laminating a drug-containing layer, a drug permeability control layer and an adhesive polymer, or a substance obtained by laminating a drug in an adhesive polymer.
  • a mixture of hollow fibers a substance obtained by dissolving or dispersing a drug in an adhesive polymer, a layer obtained by laminating layers having different drug contents, a layer obtained by laminating a drug-containing layer, a drug permeability control layer and an adhesive polymer, or a substance obtained by laminating a drug in an adhesive polymer. And a mixture of hollow fibers.
  • conventionally known absorption promoters, stabilizers, antioxidants, fragrances, preservatives, pH adjusters, and the like can be added to the pressure-sensitive adhesive of the present invention as necessary.
  • alcohols such as ethyl alcohol, lauryl alcohol, and benzyl alcohol; propylene glycol, hexanetriol, glycerin, polyethylene glycol, polypropylene glycol, and poly (oxyethylene propylene)
  • Polyhydric alcohols such as glycols; polyhydric alcohols such as monoacetin, triacetin, glycerin triisooctanoate, sorbitan monocaprolate, sorbitan monooleate, polyethylene glycol sorbitan monooleate Derivatives; linolenic acid, Higher fatty acids such as linoleic acid, oleic acid, and capric acid; fats and oils such as olive oil and castor oil; fatty acid esters such as isopropyl
  • the size of the patch of the present invention is not particularly limited.
  • the preferred size of the patch in the present invention is from 10 to 150 cm 2 from the viewpoint of handleability and QOL of the patient. Cancer patients are often bedridden, and considering that nurses administer medication, small preparations are not always preferred. Considering this point, the size of the patch particularly preferred in the present invention is 15 to 100 cm 2 .
  • the support used in the present invention is particularly suitable for its material and shape. No restrictions.
  • the elements required for the support of the present invention are that the pressure-sensitive adhesive layer is adhered to the support and that the support has self-shape retention.
  • Supports having such elements include, for example, polymer films such as polyesters, polyolefins, polyurethanes, ethylene vinyl acetate copolymer films and cellulose esters; polyesters, polyolefins, polyurethanes, cellulose esters and polyamides. Woven or knitted fabrics or non-woven fabrics and papers made of fibers such as polyesters; porous membranes made of polyester, polyolefin cellulose ester, polyurethane or polyamide; and laminates made of a combination of two or more of these. You can choose from.
  • the thickness of the support of the present invention is not particularly limited, but is preferably 1 to 200 m, and particularly preferably 1 to 500 Am. Polyester is also preferred as a support because it has sufficient sealing properties to enhance transdermal absorbability, and has high stability and safety. Among them, polyethylene terephthalate film is preferred, and the preferred thickness is 1 to 12 microns. Further, a film in which a polyethylene terephthalate film and an ethylene acetate vinyl copolymer film, or a composite film of a polyethylene terephthalate film and a urethane or the like may be used. When such a composite film is used, it is possible to obtain the sealing property of a polyethylene terephthalate film and the handling property of another flexible and thick material.
  • a 9 cm 2 patch containing BN was removed from the hair and applied to the back of the hair slide, and blood was collected 24 and 48 hours after application (paste test), and then blood was collected
  • the concentration of buprenorphine in plasma was quantified by GC_MS method according to the method described in the literature (Juorna 1 of Chromatography, 338 (1989) 89-98).
  • the number of hairless rats used in the sticking test was 3.
  • Example 1 As an acrylic adhesive, a polyacrylic acid alkyl ester copolymer consisting of 90% 2-ethylhexyl acrylate, 7.5% methyl methacrylate, and 2.5% acrylic acid To 124 parts of the combined solution (solid content 6%), 0.12 parts of preprenorphin, 0.375 parts of 2% sodium hydroxide, and 3 parts of methanol were added. Next, this was coated on a silicone-coated release film so that the thickness of the dried adhesive layer became 10 ⁇ m, dried at 6 Ot for 30 minutes, and then dried. A patch was obtained by laminating a 1.3-layer PET film and a knitted fabric composed of polyester fiber as a support on one surface of the sample.
  • the resulting patch was cut to 9 cm 2 , applied to the back of a hairless rat from which hair had been removed, and blood was collected 24 and 48 hours later, and BN was quantified by GC-MS.
  • the results showed that, as shown in Table 1, good BN release was sustained over a long period of time.
  • Polyacrylic acid alkyl ester copolymer consisting of 90% 2-ethylhexyl acrylate, 7.5% methyl methacrylate, and 2.5% acrylic acid as an acrylic adhesive
  • the procedure of Example 1 was repeated, except that 0.02 part of oleic acid was added to 14.2 parts of the solution (solid content: 6%).
  • Polyacrylic acid alkyl ester copolymer consisting of 90% 2-ethylhexyl acrylate, 7.5% methyl methacrylate, and 2.5% acrylic acid as an acrylic adhesive Solution (solid content 6%) 1
  • Example 1 was repeated, except that 0.15 parts of buprenorphine, 0.469 parts of 2% sodium hydroxide, and 3.75 parts of methanol were added to 4.0 parts. Table 1 shows the results.
  • acrylic adhesive a polyacrylic acid alkyl ester copolymer consisting of 90% 2-ethylhexyl acrylate, 7.5% methyl methacrylate, and 2.5% acrylic acid Combined solution (solid content 6%) 1
  • Example 1 The procedure was performed in the same manner as in Example 1 except that 0.025 part of buprenorphine, 0.25 part of 2% sodium hydroxide and 2 parts of methanol were added to 5.25 parts. Table 1 shows the results.
  • Example 1 was carried out in the same manner as in Example 1 except that sodium hydroxide was not added.
  • this patch had a low BN elution rate and a low BN concentration in rat blood.
  • Example 2 was carried out in the same manner as in Example 1 except that benzalkonium chloride was used instead of oleic acid. As shown in Table 1, BN concentration in rat blood was low.
  • Polyacrylic acid alkyl ester copolymer consisting of 90% 2-ethylhexyl acrylate, 7.5% methyl methacrylate, and 2.5% acrylic acid as an acrylic adhesive Solution (solid content 6%) 1
  • Example 2 6.3 1 part of preprenorphin 0.02 parts, 2% sodium hydroxide The same procedure as in Example 1 was performed except that 0.063 part and methanol 0.5 part were added. As shown in Table 1, the BN elution rate was good, but the rat blood BN concentration was low.
  • a patch was obtained in the same manner as in Example 1. This was cut into 50 cm 2 to obtain a preparation having a BN content of 6 mg. This was applied to the upper arm of a healthy adult male for 48 hours, and the blood concentration was measured. Table 2 shows the results. As shown in Table 2, the therapeutically effective blood concentration was maintained for a long time.
  • Example 5 The procedure was performed in the same manner as in Example 5 except that the patch was cut into 33.3 cm 2 to obtain a preparation having a BN content of 4 mg. Table 2 shows the results.
  • Example 5 The procedure of Example 5 was repeated, except that the patch was cut into 66.7 cm 2 to obtain a preparation having a BN content of 8 mg. Table 2 shows the results.
  • Example 5 The procedure of Example 5 was repeated, except that the patch was cut into 8.3 cm 2 to obtain a preparation having a BN content of 1 mg. Table 2 shows the results.
  • Table 3 shows the efficacy of the formulations used in Examples 5-7 and Comparative Example 4 in clinical trials. As shown in Table 3, the BN content was in the range of 2 to 12 mg. The formulation in the box showed good analgesic effect.
  • the above-mentioned formulation efficacy rate is the proportion of patients who achieved a pain-reducing effect by administering the drug.
  • the BN content in the patch for application is 2 to 12 mg, and (1) the BN dissolution rate is 20% to 45% in 5 minutes, 45% to 80% in 15 minutes, By using a patch that is 70% or more in 120 minutes,

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  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Dermatology (AREA)
  • Biomedical Technology (AREA)
  • Pain & Pain Management (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Emergency Medicine (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

L'invention concerne une bande adhésive comprenant un support souple et une couche adhésive sensible à la pression contenant de la buprénorphine, formée sur une surface du support. La quantité de buprénorphine contenue par bande adhésive est de l'ordre de 2 à 12 mg et les pourcentages d'exsudation de la buprénorphine hors de la bande adhésive, calculés pour 5, 15 et respectivement 120 minutes sont compris entre 25 et 45 %, 45 et 80 %, et 70 % ou davantage.
PCT/JP2001/004624 2000-06-02 2001-05-31 Bande adhesive contenant de la buprenorphine WO2001093868A1 (fr)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU2001262683A AU2001262683A1 (en) 2000-06-02 2001-05-31 Buprenorphine-containing patch

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Application Number Priority Date Filing Date Title
JP2000-165809 2000-06-02
JP2000165809 2000-06-02

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Publication Number Publication Date
WO2001093868A1 true WO2001093868A1 (fr) 2001-12-13

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Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2007500133A (ja) * 2003-07-25 2007-01-11 ユーロ−セルティーク エス．エイ． 術後痛の術前治療
US9745274B2 (en) 2013-07-03 2017-08-29 Shin Nippon Biomedical Laboratories, Ltd. Compound, organic cation transporter 3 detection agent, and organic cation transporter 3 activity inhibitor

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0680754A2 (fr) * 1994-05-06 1995-11-08 Nitto Denko Corporation Préparation pour absorption percutanée contenant de la buprenorphine
JPH09143062A (ja) * 1995-11-21 1997-06-03 Mikasa Seiyaku Kk 経皮用粘着剤組成物及びその製法
US5968547A (en) * 1997-02-24 1999-10-19 Euro-Celtique, S.A. Method of providing sustained analgesia with buprenorphine

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0680754A2 (fr) * 1994-05-06 1995-11-08 Nitto Denko Corporation Préparation pour absorption percutanée contenant de la buprenorphine
JPH09143062A (ja) * 1995-11-21 1997-06-03 Mikasa Seiyaku Kk 経皮用粘着剤組成物及びその製法
US5968547A (en) * 1997-02-24 1999-10-19 Euro-Celtique, S.A. Method of providing sustained analgesia with buprenorphine

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2007500133A (ja) * 2003-07-25 2007-01-11 ユーロ−セルティーク エス．エイ． 術後痛の術前治療
US9745274B2 (en) 2013-07-03 2017-08-29 Shin Nippon Biomedical Laboratories, Ltd. Compound, organic cation transporter 3 detection agent, and organic cation transporter 3 activity inhibitor

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