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Abstract text
A film-shaped, mucoadhesive administration form having a content of at least one active agent. The active agent is a cannabis agent.
Claims
1. A film-shaped, mucoadhesive administration form containing a cannabis agent selected from the group consisting of cannabis extract and cannabis oil.
2. The administration form according to claim 1, wherein said administration form comprises a polymer matrix, said polymer matrix being an active substance reservoir and having mucoadhesive properties.
3. The administration form according to claim 2, wherein said polymer matrix contains at least one polymer being water-soluble and/or swellable in an aqueous media, said at least one polymer is selected from the group consisting of starch and starch derivatives, dextran, carboxymethyl cellulose, hydroxypropyl cellulose, hydroxyethyl cellulose, hydroxypropyl methyl cellulose, hydroxypropyl ethyl cellulose, sodium carboxymethyl cellulose, ethyl cellulose or propyl cellulose, polyacrylic acid, polyacrylates, polyvinyl pyrrolidones, polyethylene oxide polymers, polyacrylamides, polyethylene glycol, gelatine, collagen, alginates, pectins, pullulan, tragacanth, chitosan, alginic acid, arabinogalactan, galactomannan, agar-agar, agarose, carrageenan and natural gums, and wherein said administration form comprises said at least one polymer at a portion of 5 to 95%-wt.
4. The administration form according to claim 1, wherein said administration form contains said cannabis agent selected from the group consisting of cannabis extract and cannabis oil in an amount of 0.5 to 50%-wt.
5. The administration form according to claim 1, wherein said administration form further contains at least one substance selected from the group consisting of flavourings, odorous substances and aromatics.
6. The administration form according to claim 1, wherein the layer thickness is 0.01 to 2 mm.
7. The administration form according to claim 1, wherein said administration form further contains at least one inactive ingredient selected from the group consisting of fillers, colourants, emulsifiers, plasticizers, sweeteners, preservatives, pH regulators, permeation-enhancing substances, and antioxidants.
8. The administration form according to claim 1, wherein said administration form has a multilayer structure with at least one layer having an active agent content.
9. A method of treating conditions of pain in cases of carcinosis and as a result of chemotherapy; conditions of pain and "wasting" syndrome in connection with AIDS; nausea and vomiting, especially nausea and vomiting as side effects of a chemotherapy as well as in connection with AIDS or hepatitis; neuropathic pain; anorexia or cachexia, especially in connection with AIDS or carcinosis in the advanced stages; paralytic symptoms in connection with multiple sclerosis or traumatic transverse lesions; dystonic motor disturbance; bronchial asthma; epileptic attacks or generalized epilepsia; withdrawal symptoms in connection with alcohol dependence, benzodiazepine dependence and opiate dependence; Parkinson's disease; dementia, especially Alzheimer's disease; arthritis; glaucoma; migraine; dysmenorrhoea, said method comprising the step of: administering a film-shaped, mucoadhesive administration form containing a cannabis agent selected from the group consisting of cannabis extract and cannabis oil to an inflicted person.
10. A method of treating conditions of pain in cases of carcinosis and as a result of chemotherapy; conditions of pain and "wasting" syndrome in connection with AIDS; nausea and vomiting, especially nausea and vomiting as side effects of a chemotherapy as well as in connection with AIDS or hepatitis; neuropathic pain; anorexia or cachexia, especially in connection with AIDS or carcinosis in the advanced stages; paralytic symptoms in connection with multiple sclerosis or traumatic transverse lesions; dystonic motor disturbance; bronchial asthma; epileptic attacks or generalized epilepsia; withdrawal symptoms in connection with alcohol dependence, benzodiazepine dependence and opiate dependence; Parkinson's disease; dementia, especially Alzheimer's disease; arthritis; glaucoma; migraine; dysmenorrhoea, said method comprising the step of: administering a film-shaped, mucoadhesive administration form to an afflicted person, said administration form containing a cannabinoid active agent selected from the group of active agents consisting of tetrahydrocannabinol, cannabinol, cannabidiol and cannabichromen.
11. The method according to claim 9, wherein the administration form is a film-shaped, mucoadhesive administration form containing a cannabis agent selected from the group consisting of cannabis extract and cannabis oil, and wherein said administration form comprises a polymer matrix, said polymer matrix being an active substance reservoir and having mucoadhesive properties.
12. The method according to claim 9, wherein the treatment is effected by application of the administration form to the oral mucosa.
13. A medicinal product for treating conditions of pain in cases of carcinosis and as a result of chemotherapy; conditions of pain and "wasting" syndrome in connection with AIDS; nausea and vomiting, especially nausea and vomiting as side effects of a chemotherapy as well as in connection with AIDS or hepatitis; neuropathic pain; anorexia or cachexia, especially in connection with AIDS or carcinosis in the advanced stages; paralytic symptoms in connection with multiple sclerosis or traumatic transverse lesions; dystonic motor disturbance; bronchial asthma; epileptic attacks or generalized epilepsia; withdrawal symptoms in connection with alcohol dependence, benzodiazepine dependence and opiate dependence; Parkinson's disease; dementia, especially Alzheimer's disease; arthritis; glaucoma; migraine; dysmenorrhoea, said medicinal product comprising a film-shaped, muco-adhesive administration form containing a cannabis agent selected from the group consisting of cannabis extract and cannabis oil.
14. A medicinal product for treating conditions of pain in cases of carcinosis and as a result of chemotherapy; conditions of pain and "wasting" syndrome in connection with AIDS; nausea and vomiting, especially nausea and vomiting as side effects of a chemotherapy as well as in connection with AIDS or hepatitis; neuropathic pain; anorexia or cachexia, especially in connection with AIDS or carcinosis in the advanced stages; paralytic symptoms in connection with multiple sclerosis or traumatic transverse lesions; dystonic motor disturbance; bronchial asthma; epileptic attacks or generalized epilepsia; withdrawal symptoms in connection with alcohol dependence, benzodiazepine dependence and opiate dependence; Parkinson's disease; dementia, especially Alzheimer's disease; arthritis; glaucoma; migraine; dysmenorrhoea, said medicinal product comprising a film-shaped, mucoadhesive administration form containing a cannabinoid active agent selected from the group of active agents consisting of tetrahydrocannabinol, cannabinol, cannabidiol and cannabichromen.
15. The medicinal product according to claim 14, wherein the administration form is a film-shaped, mucoadhesive administration form containing a cannabis agent selected from the group consisting of cannabis extract and cannabis oil, and wherein said administration form comprises a polymer matrix, said polymer matrix being an active substance reservoir and having mucoadhesive properties, said reservoir containing said cannabis extract or cannabis oil.
16. The medicinal product according to claim 13, wherein the administration form is an administration form for application on the oral mucosa.
17. The administration form according to claim 3, wherein said administration form comprises said polymer at a portion of 15 to 75%-wt.
18. The administration form according to claim 4, wherein said administration form contains said cannabis agent selected from the group consisting of cannabis extract and cannabis oil in an amount of 1 to 30%-wt.
19. The administration form according to claim 5, wherein said flavourings, odorous substances and aromatics are selected from the group consisting of menthol, eucalyptol, limonene, phenyl ethanol, camphene, pinene, n-butyl phthalide, cineol, eucalyptus oil, thyme oil, methyl salicylate, turpentine oil, camomile oil, ethyl vanillin, 6-methyl coumarin, citronellol, and acetic acid n-butyl ester.
20. (canceled)
21. The administration form according to claim 6, wherein the layer thickness is 0.05 to 0.5 mm.
22. The method according claim 12, wherein the application of the administration form to the oral mucosa is selected from the group consisting of sublingual application and buccal application.
23. The method according to claim 10, wherein the administration form is a film-shaped, mucoadhesive administration form containing a cannabinoid agent selected from the group consisting of tetrahydrocannabinol, cannabinol, cannabidiol and cannabichromen and wherein said administration form comprises a polymer matrix, said polymer matrix being an active substance reservoir and having mucoadhesive properties.
24. The method according to claim 10, wherein the treatment is effected by application of the administration form to the oral mucosa.
25. The method according claim 24, wherein the application of the administration form to the oral mucosa is selected from the group consisting of sublingual application and buccal application.
26. The medicinal product according claim 16, wherein the application of the administration form to the oral mucosa is selected from the group consisting of sublingual application and buccal application.
27. The medicinal product according to claim 14, wherein the administration form is an administration form for application on the oral mucosa.
28. The medicinal product according claim 27, wherein the application of the administration form to the oral mucosa is selected from the group consisting of sublingual application and buccal application.
29. A film-shaped, mucoadhesive administration form containing a cannabis agent selected from the group consisting of cannabis extract and cannabis oil, wherein said administration form comprises a polymer matrix, said polymer matrix being an active substance reservoir and having mucoadhesive properties, wherein said administration form contains said cannabis agent selected from the group consisting of cannabis extract and cannabis oil in an amount of 0.5 to 50%-wt, and wherein the layer thickness is 0.01 to 2 mm.
30. The administration form according to claim 29, wherein said polymer matrix contains at least one polymer being water-soluble and/or swellable in an aqueous media, said at least one polymer is selected from the group consisting of starch and starch derivatives, dextran, carboxymethyl cellulose, hydroxypropyl cellulose, hydroxyethyl cellulose, hydroxypropyl methyl cellulose, hydroxypropyl ethyl cellulose, sodium carboxymethyl cellulose, ethyl cellulose or propyl cellulose, polyacrylic acid, polyacrylates, polyvinyl pyrrolidones, polyethylene oxide polymers, polyacrylamides, polyethylene glycol, gelatine, collagen, alginates, pectins, pullulan, tragacanth, chitosan, alginic acid, arabinogalactan, galactomannan, agar-agar, agarose, carrageenan and natural gums, and wherein said administration form comprises said at least one polymer at a portion of 5 to 95%-wt.
31. The administration form according to claim 30, wherein said administration form has a multilayer structure with at least one layer having an active agent content.
32. The administration form according to claim 29, wherein the administration form is a film-shaped, mucoadhesive administration form containing a cannabinoid agent selected from the group consisting of tetrahydrocannabinol, cannabinol, cannabidiol and cannabichromen and wherein said administration form comprises a polymer matrix, said polymer matrix being an active substance reservoir and having mucoadhesive properties.
33. The medicinal product according to claim 13, wherein said administration form comprises a polymer matrix, said polymer matrix being an active substance reservoir and having mucoadhesive properties, said reservoir containing said active agent selected from the group consisting of tetrahydrocannabinol, cannabinol, cannabidiol and cannabichromen.
Description
CROSS REFERENCE TO RELATED APPLICATIONS
[0001] This application is a National Stage application of International Application No. PCT/EP03/04807, filed on May 8, 2003, which claims priority of German application number 102 26 494.5, filed on Jun. 14, 2002.
BACKGROUND OF THE INVENTION
[0002] 1. Field of the Invention
[0003] The present invention relates to film-shaped, mucoadhesive administration forms which have a content of cannabis agents and which are suitable for administration of cannabis agents for therapeutic purposes. The invention further relates to the use of the said administration forms for treating conditions of disease in humans or animals.
[0004] 2. Description of the Prior Art
[0005] The components of the Indian hemp plant (Cannabis sativa L.) have numerous pharmacological effects, of which the psychotropic effect is most widely known. Apart from this, cannabis components also have anti-emetic, anticonvulsive, muscle-relaxing, analgesic, sedative and appetite-increasing effects.
[0006] Because of the psychotropic or euphorizing effect and the dependency potential associated therewith, the therapeutic application of cannabis components is subject to severe restrictions.
[0007] It has long been known that cannabis components can be used beneficially for treating insomnia, neuralgias and painful rheumatism, as well as gastric and intestinal disorders. A favourable therapeutic effect of cannabis components has furthermore been observed for the following indications:
[0008] Conditions of pain in cases of carcinosis and as a result of chemotherapy; conditions of pain and "wasting" syndrome in connection with AIDS; nausea and vomiting as side effects of chemotherapy as well as in connection with AIDS or hepatitis; neuropathic pain; anorexia or cachexia, especially in connection with AIDS or carcinosis in the advanced stages.
[0009] A favourable therapeutic effect of cannabis components has also been observed in connection with paralytic symptoms in connection with multiple sclerosis or traumatic transverse lesions; dystonic motor disturbance; bronchial asthma; epileptic attacks or generalized epilepsia; withdrawal symptoms in connection with alcohol dependence, benzodiazepine dependence and opiate dependence; Parkinson's disease; dementia, especially Morbus Alzheimer; nausea; arthritis; glaucoma; migraine; and dysmenorrhoea.
[0010] At present, only the synthetically produced cannabis agent R-(6a, 10a)-Δ-9-tetrahydrocannabinol (Dronabinol) is marketable. This isomer of tetrahydrocannabinol (THC) is sold under the product name Marinol. This medicament is administered orally in the form of capsules. Marinol is used for treating severe loss of weight in AIDS patients and cancer patients who, as a result of chemotherapy, suffer from heavy vomiting.
[0011] Apart from the aforementioned THC isomer, cannabis extracts and cannabis oils for therapeutic treatment purposes are also suitable. Application is usually effected via the oral route, e.g. in the form of capsules.
[0012] Cannabis extracts contain as pharmacologically active ingredients tetrahydrocannabinol (predominantly Δ-9-tetrahydrocannabinol, in small proportion: Δ-8-tetrahydrocannabinol), cannabidiol, cannabinol and cannabichromen. These active agents are also called cannabinoids (see the list "The Merck Index", 12th ed., 1996, page 285, No. 1794, as well as page 1573, No. 9349).
[0013] Oral administration of cannabis agents, especially of R-(6a, 10a)-Δ-9-tetrahydrocannabinol, in the form of capsules, tablets, pills or other solid, oral administration forms, or in the form of orally administered liquid preparations is disadvantageous for a variety of reasons: [0014] Since on use of the aforementioned administration forms, the absorption of the active agent takes place in the gastrointestinal tract, the time of onset of action is delayed. This is disadvantageous especially with respect to the indications mentioned, which generally require a quick onset of action (e.g. pain therapy). [0015] Cannabis agents are at least partially degraded and inactivated during the passage through the stomach and intestines under the influence of acid and enzymes, so that only part of the administered dose is absorbed and is systemically available. [0016] In this connection, unwanted plasma peak values may occur which are frequently the cause of side effects. [0017] In addition, after oral administration a significant portion of the active substance is already metabolised during the first passage through the liver ("first pass effect").
[0018] These disadvantages are particularly important with respect to the acceptance with which these medicaments are met in the above indicated indications. With the mentioned oral administration forms, it is also disadvantageous that patients, in a particular given situation, regard the extended retention, e.g. of a tablet or capsule (filled with an oily solution) in the mouth as particularly unpleasant.
Source: Film-Shaped Mucoadhesive Administration Forms For Administering Cannabis Agents - US Patent Application 20060039959 Full Text
A film-shaped, mucoadhesive administration form having a content of at least one active agent. The active agent is a cannabis agent.
Claims
1. A film-shaped, mucoadhesive administration form containing a cannabis agent selected from the group consisting of cannabis extract and cannabis oil.
2. The administration form according to claim 1, wherein said administration form comprises a polymer matrix, said polymer matrix being an active substance reservoir and having mucoadhesive properties.
3. The administration form according to claim 2, wherein said polymer matrix contains at least one polymer being water-soluble and/or swellable in an aqueous media, said at least one polymer is selected from the group consisting of starch and starch derivatives, dextran, carboxymethyl cellulose, hydroxypropyl cellulose, hydroxyethyl cellulose, hydroxypropyl methyl cellulose, hydroxypropyl ethyl cellulose, sodium carboxymethyl cellulose, ethyl cellulose or propyl cellulose, polyacrylic acid, polyacrylates, polyvinyl pyrrolidones, polyethylene oxide polymers, polyacrylamides, polyethylene glycol, gelatine, collagen, alginates, pectins, pullulan, tragacanth, chitosan, alginic acid, arabinogalactan, galactomannan, agar-agar, agarose, carrageenan and natural gums, and wherein said administration form comprises said at least one polymer at a portion of 5 to 95%-wt.
4. The administration form according to claim 1, wherein said administration form contains said cannabis agent selected from the group consisting of cannabis extract and cannabis oil in an amount of 0.5 to 50%-wt.
5. The administration form according to claim 1, wherein said administration form further contains at least one substance selected from the group consisting of flavourings, odorous substances and aromatics.
6. The administration form according to claim 1, wherein the layer thickness is 0.01 to 2 mm.
7. The administration form according to claim 1, wherein said administration form further contains at least one inactive ingredient selected from the group consisting of fillers, colourants, emulsifiers, plasticizers, sweeteners, preservatives, pH regulators, permeation-enhancing substances, and antioxidants.
8. The administration form according to claim 1, wherein said administration form has a multilayer structure with at least one layer having an active agent content.
9. A method of treating conditions of pain in cases of carcinosis and as a result of chemotherapy; conditions of pain and "wasting" syndrome in connection with AIDS; nausea and vomiting, especially nausea and vomiting as side effects of a chemotherapy as well as in connection with AIDS or hepatitis; neuropathic pain; anorexia or cachexia, especially in connection with AIDS or carcinosis in the advanced stages; paralytic symptoms in connection with multiple sclerosis or traumatic transverse lesions; dystonic motor disturbance; bronchial asthma; epileptic attacks or generalized epilepsia; withdrawal symptoms in connection with alcohol dependence, benzodiazepine dependence and opiate dependence; Parkinson's disease; dementia, especially Alzheimer's disease; arthritis; glaucoma; migraine; dysmenorrhoea, said method comprising the step of: administering a film-shaped, mucoadhesive administration form containing a cannabis agent selected from the group consisting of cannabis extract and cannabis oil to an inflicted person.
10. A method of treating conditions of pain in cases of carcinosis and as a result of chemotherapy; conditions of pain and "wasting" syndrome in connection with AIDS; nausea and vomiting, especially nausea and vomiting as side effects of a chemotherapy as well as in connection with AIDS or hepatitis; neuropathic pain; anorexia or cachexia, especially in connection with AIDS or carcinosis in the advanced stages; paralytic symptoms in connection with multiple sclerosis or traumatic transverse lesions; dystonic motor disturbance; bronchial asthma; epileptic attacks or generalized epilepsia; withdrawal symptoms in connection with alcohol dependence, benzodiazepine dependence and opiate dependence; Parkinson's disease; dementia, especially Alzheimer's disease; arthritis; glaucoma; migraine; dysmenorrhoea, said method comprising the step of: administering a film-shaped, mucoadhesive administration form to an afflicted person, said administration form containing a cannabinoid active agent selected from the group of active agents consisting of tetrahydrocannabinol, cannabinol, cannabidiol and cannabichromen.
11. The method according to claim 9, wherein the administration form is a film-shaped, mucoadhesive administration form containing a cannabis agent selected from the group consisting of cannabis extract and cannabis oil, and wherein said administration form comprises a polymer matrix, said polymer matrix being an active substance reservoir and having mucoadhesive properties.
12. The method according to claim 9, wherein the treatment is effected by application of the administration form to the oral mucosa.
13. A medicinal product for treating conditions of pain in cases of carcinosis and as a result of chemotherapy; conditions of pain and "wasting" syndrome in connection with AIDS; nausea and vomiting, especially nausea and vomiting as side effects of a chemotherapy as well as in connection with AIDS or hepatitis; neuropathic pain; anorexia or cachexia, especially in connection with AIDS or carcinosis in the advanced stages; paralytic symptoms in connection with multiple sclerosis or traumatic transverse lesions; dystonic motor disturbance; bronchial asthma; epileptic attacks or generalized epilepsia; withdrawal symptoms in connection with alcohol dependence, benzodiazepine dependence and opiate dependence; Parkinson's disease; dementia, especially Alzheimer's disease; arthritis; glaucoma; migraine; dysmenorrhoea, said medicinal product comprising a film-shaped, muco-adhesive administration form containing a cannabis agent selected from the group consisting of cannabis extract and cannabis oil.
14. A medicinal product for treating conditions of pain in cases of carcinosis and as a result of chemotherapy; conditions of pain and "wasting" syndrome in connection with AIDS; nausea and vomiting, especially nausea and vomiting as side effects of a chemotherapy as well as in connection with AIDS or hepatitis; neuropathic pain; anorexia or cachexia, especially in connection with AIDS or carcinosis in the advanced stages; paralytic symptoms in connection with multiple sclerosis or traumatic transverse lesions; dystonic motor disturbance; bronchial asthma; epileptic attacks or generalized epilepsia; withdrawal symptoms in connection with alcohol dependence, benzodiazepine dependence and opiate dependence; Parkinson's disease; dementia, especially Alzheimer's disease; arthritis; glaucoma; migraine; dysmenorrhoea, said medicinal product comprising a film-shaped, mucoadhesive administration form containing a cannabinoid active agent selected from the group of active agents consisting of tetrahydrocannabinol, cannabinol, cannabidiol and cannabichromen.
15. The medicinal product according to claim 14, wherein the administration form is a film-shaped, mucoadhesive administration form containing a cannabis agent selected from the group consisting of cannabis extract and cannabis oil, and wherein said administration form comprises a polymer matrix, said polymer matrix being an active substance reservoir and having mucoadhesive properties, said reservoir containing said cannabis extract or cannabis oil.
16. The medicinal product according to claim 13, wherein the administration form is an administration form for application on the oral mucosa.
17. The administration form according to claim 3, wherein said administration form comprises said polymer at a portion of 15 to 75%-wt.
18. The administration form according to claim 4, wherein said administration form contains said cannabis agent selected from the group consisting of cannabis extract and cannabis oil in an amount of 1 to 30%-wt.
19. The administration form according to claim 5, wherein said flavourings, odorous substances and aromatics are selected from the group consisting of menthol, eucalyptol, limonene, phenyl ethanol, camphene, pinene, n-butyl phthalide, cineol, eucalyptus oil, thyme oil, methyl salicylate, turpentine oil, camomile oil, ethyl vanillin, 6-methyl coumarin, citronellol, and acetic acid n-butyl ester.
20. (canceled)
21. The administration form according to claim 6, wherein the layer thickness is 0.05 to 0.5 mm.
22. The method according claim 12, wherein the application of the administration form to the oral mucosa is selected from the group consisting of sublingual application and buccal application.
23. The method according to claim 10, wherein the administration form is a film-shaped, mucoadhesive administration form containing a cannabinoid agent selected from the group consisting of tetrahydrocannabinol, cannabinol, cannabidiol and cannabichromen and wherein said administration form comprises a polymer matrix, said polymer matrix being an active substance reservoir and having mucoadhesive properties.
24. The method according to claim 10, wherein the treatment is effected by application of the administration form to the oral mucosa.
25. The method according claim 24, wherein the application of the administration form to the oral mucosa is selected from the group consisting of sublingual application and buccal application.
26. The medicinal product according claim 16, wherein the application of the administration form to the oral mucosa is selected from the group consisting of sublingual application and buccal application.
27. The medicinal product according to claim 14, wherein the administration form is an administration form for application on the oral mucosa.
28. The medicinal product according claim 27, wherein the application of the administration form to the oral mucosa is selected from the group consisting of sublingual application and buccal application.
29. A film-shaped, mucoadhesive administration form containing a cannabis agent selected from the group consisting of cannabis extract and cannabis oil, wherein said administration form comprises a polymer matrix, said polymer matrix being an active substance reservoir and having mucoadhesive properties, wherein said administration form contains said cannabis agent selected from the group consisting of cannabis extract and cannabis oil in an amount of 0.5 to 50%-wt, and wherein the layer thickness is 0.01 to 2 mm.
30. The administration form according to claim 29, wherein said polymer matrix contains at least one polymer being water-soluble and/or swellable in an aqueous media, said at least one polymer is selected from the group consisting of starch and starch derivatives, dextran, carboxymethyl cellulose, hydroxypropyl cellulose, hydroxyethyl cellulose, hydroxypropyl methyl cellulose, hydroxypropyl ethyl cellulose, sodium carboxymethyl cellulose, ethyl cellulose or propyl cellulose, polyacrylic acid, polyacrylates, polyvinyl pyrrolidones, polyethylene oxide polymers, polyacrylamides, polyethylene glycol, gelatine, collagen, alginates, pectins, pullulan, tragacanth, chitosan, alginic acid, arabinogalactan, galactomannan, agar-agar, agarose, carrageenan and natural gums, and wherein said administration form comprises said at least one polymer at a portion of 5 to 95%-wt.
31. The administration form according to claim 30, wherein said administration form has a multilayer structure with at least one layer having an active agent content.
32. The administration form according to claim 29, wherein the administration form is a film-shaped, mucoadhesive administration form containing a cannabinoid agent selected from the group consisting of tetrahydrocannabinol, cannabinol, cannabidiol and cannabichromen and wherein said administration form comprises a polymer matrix, said polymer matrix being an active substance reservoir and having mucoadhesive properties.
33. The medicinal product according to claim 13, wherein said administration form comprises a polymer matrix, said polymer matrix being an active substance reservoir and having mucoadhesive properties, said reservoir containing said active agent selected from the group consisting of tetrahydrocannabinol, cannabinol, cannabidiol and cannabichromen.
Description
CROSS REFERENCE TO RELATED APPLICATIONS
[0001] This application is a National Stage application of International Application No. PCT/EP03/04807, filed on May 8, 2003, which claims priority of German application number 102 26 494.5, filed on Jun. 14, 2002.
BACKGROUND OF THE INVENTION
[0002] 1. Field of the Invention
[0003] The present invention relates to film-shaped, mucoadhesive administration forms which have a content of cannabis agents and which are suitable for administration of cannabis agents for therapeutic purposes. The invention further relates to the use of the said administration forms for treating conditions of disease in humans or animals.
[0004] 2. Description of the Prior Art
[0005] The components of the Indian hemp plant (Cannabis sativa L.) have numerous pharmacological effects, of which the psychotropic effect is most widely known. Apart from this, cannabis components also have anti-emetic, anticonvulsive, muscle-relaxing, analgesic, sedative and appetite-increasing effects.
[0006] Because of the psychotropic or euphorizing effect and the dependency potential associated therewith, the therapeutic application of cannabis components is subject to severe restrictions.
[0007] It has long been known that cannabis components can be used beneficially for treating insomnia, neuralgias and painful rheumatism, as well as gastric and intestinal disorders. A favourable therapeutic effect of cannabis components has furthermore been observed for the following indications:
[0008] Conditions of pain in cases of carcinosis and as a result of chemotherapy; conditions of pain and "wasting" syndrome in connection with AIDS; nausea and vomiting as side effects of chemotherapy as well as in connection with AIDS or hepatitis; neuropathic pain; anorexia or cachexia, especially in connection with AIDS or carcinosis in the advanced stages.
[0009] A favourable therapeutic effect of cannabis components has also been observed in connection with paralytic symptoms in connection with multiple sclerosis or traumatic transverse lesions; dystonic motor disturbance; bronchial asthma; epileptic attacks or generalized epilepsia; withdrawal symptoms in connection with alcohol dependence, benzodiazepine dependence and opiate dependence; Parkinson's disease; dementia, especially Morbus Alzheimer; nausea; arthritis; glaucoma; migraine; and dysmenorrhoea.
[0010] At present, only the synthetically produced cannabis agent R-(6a, 10a)-Δ-9-tetrahydrocannabinol (Dronabinol) is marketable. This isomer of tetrahydrocannabinol (THC) is sold under the product name Marinol. This medicament is administered orally in the form of capsules. Marinol is used for treating severe loss of weight in AIDS patients and cancer patients who, as a result of chemotherapy, suffer from heavy vomiting.
[0011] Apart from the aforementioned THC isomer, cannabis extracts and cannabis oils for therapeutic treatment purposes are also suitable. Application is usually effected via the oral route, e.g. in the form of capsules.
[0012] Cannabis extracts contain as pharmacologically active ingredients tetrahydrocannabinol (predominantly Δ-9-tetrahydrocannabinol, in small proportion: Δ-8-tetrahydrocannabinol), cannabidiol, cannabinol and cannabichromen. These active agents are also called cannabinoids (see the list "The Merck Index", 12th ed., 1996, page 285, No. 1794, as well as page 1573, No. 9349).
[0013] Oral administration of cannabis agents, especially of R-(6a, 10a)-Δ-9-tetrahydrocannabinol, in the form of capsules, tablets, pills or other solid, oral administration forms, or in the form of orally administered liquid preparations is disadvantageous for a variety of reasons: [0014] Since on use of the aforementioned administration forms, the absorption of the active agent takes place in the gastrointestinal tract, the time of onset of action is delayed. This is disadvantageous especially with respect to the indications mentioned, which generally require a quick onset of action (e.g. pain therapy). [0015] Cannabis agents are at least partially degraded and inactivated during the passage through the stomach and intestines under the influence of acid and enzymes, so that only part of the administered dose is absorbed and is systemically available. [0016] In this connection, unwanted plasma peak values may occur which are frequently the cause of side effects. [0017] In addition, after oral administration a significant portion of the active substance is already metabolised during the first passage through the liver ("first pass effect").
[0018] These disadvantages are particularly important with respect to the acceptance with which these medicaments are met in the above indicated indications. With the mentioned oral administration forms, it is also disadvantageous that patients, in a particular given situation, regard the extended retention, e.g. of a tablet or capsule (filled with an oily solution) in the mouth as particularly unpleasant.
Source: Film-Shaped Mucoadhesive Administration Forms For Administering Cannabis Agents - US Patent Application 20060039959 Full Text
