CA2548915A1 - Generally linear effervescent oral fentanyl dosage form and methods of administering - Google Patents

Generally linear effervescent oral fentanyl dosage form and methods of administering Download PDF

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Publication number
CA2548915A1
CA2548915A1 CA002548915A CA2548915A CA2548915A1 CA 2548915 A1 CA2548915 A1 CA 2548915A1 CA 002548915 A CA002548915 A CA 002548915A CA 2548915 A CA2548915 A CA 2548915A CA 2548915 A1 CA2548915 A1 CA 2548915A1
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CA
Canada
Prior art keywords
dosage form
fentanyl
amount
tablet
max
Prior art date
Legal status (The legal status 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 status listed.)
Granted
Application number
CA002548915A
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French (fr)
Other versions
CA2548915C (en
Inventor
Derek Moe
Vikas Agarwal
Walid Habib
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Cima Labs Inc
Original Assignee
Cima Labs Inc.
Derek Moe
Vikas Agarwal
Walid Habib
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Application filed by Cima Labs Inc., Derek Moe, Vikas Agarwal, Walid Habib filed Critical Cima Labs Inc.
Publication of CA2548915A1 publication Critical patent/CA2548915A1/en
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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
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2072—Pills, tablets, discs, rods characterised by shape, structure or size; Tablets with holes, special break lines or identification marks; Partially coated tablets; Disintegrating flat shaped forms
    • A61K9/2086—Layered tablets, e.g. bilayer tablets; Tablets of the type inert core-active coat
    • A61K9/209—Layered tablets, e.g. bilayer tablets; Tablets of the type inert core-active coat containing drug in at least two layers or in the core and in at least one outer layer
    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • 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
    • A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
    • A61K31/22—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin
    • 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
    • A61K31/60—Salicylic acid; Derivatives thereof
    • A61K31/612—Salicylic acid; Derivatives thereof having the hydroxy group in position 2 esterified, e.g. salicylsulfuric acid
    • A61K31/616—Salicylic acid; Derivatives thereof having the hydroxy group in position 2 esterified, e.g. salicylsulfuric acid by carboxylic acids, e.g. acetylsalicylic acid
    • 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
    • A61K9/0002—Galenical forms characterised by the drug release technique; Application systems commanded by energy
    • A61K9/0007—Effervescent
    • 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
    • A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
    • A61K9/006—Oral mucosa, e.g. mucoadhesive forms, sublingual droplets; Buccal patches or films; Buccal sprays
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A61P29/02—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] without antiinflammatory effect
    • 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
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin

Abstract

Fentanyl containing dosage forms and methods using same are described. These dosage forms include substantially less fentanyl by weight than know oral formulation and have advantages in terms of cost and side effects. These dosage forms are intended for oral administration of fentanyl across the oral mucosa.

Claims (52)

1. A dosage form comprising: about 100 to about 800 micrograms of fentanyl, calculated as fentanyl free base or an equivalent amount of a salt thereof, an effervescent couple in an amount of about 5 to about 85% by weight of the dosage form, a pH
adjusting substance in an amount of about 0.5 to about 25% by weight of the dosage form, and a starch glycolate in an amount of about 0.25 to about 20% by weight of the dosage form, said dosage form being suitable for delivery of said fentanyl across the oral mucosa of a patient by buccal, gingival or sublingual administration.
2. The dosage form of claim 1 wherein said pH adjusting substance is selected and provided in an amount capable of providing a change in localized pH of at least 0.5 pH units.
3. The dosage form of claim 2 wherein said pH adjusting substance is a carbonate or bicarbonate.
4. The dosage form of claim 1 further comprising a filler.
5. The dosage form of claim 4 wherein said filler is present in an amount of between about 10 and about 80% w/w.
6. The dosage form of claim 4 wherein said filler is mannitol.
7. The dosage form of claim 1 being a compressed tablet.
8. The dosage form of claim 1 having a C max which is comparable to that of an ACTIQ® dosage form having about 80% more fentanyl
9. The dosage form of claim 8 having a C max which is highly comparable to that of an ACTIQ® dosage form having about 80% more fentanyl.
10. The dosage form of claim 9 having a C max which is very highly comparable to that of an ACTIQ® dosage form having about 80% more fentanyl.
11. The dosage form of claim 1 having a linear relationship between dose and C max.
12. The dosage form of claim 1 wherein the ratio of C max to dose is between about 2.0 and about 4.0 picograms/mL/microgram.
13. The dosage form of claim 12 wherein the ratio of C max to dose is between about 2.5 and about 3.5 picograms/mL/microgram.
14. The dosage form of claim 13 wherein the ratio of C max to dose is between about 2.7 and about 3.5 picograms/mL/microgram.
15. A dosage form comprising: about 100 to about 800 micrograms of fentanyl, calculated as fentanyl free base or an equivalent amount of a salt thereof, an effervescent couple, a pH
adjusting substance said adjusting substance selected and provided in an amount capable of providing a change in localized pH of at least 0.5 pH units, and a starch glycolate, said dosage form being suitable for delivery of said fentanyl across the oral mucosa of a patient by buccal, gingival or sublingual administration and providing a ratio of C max to dose is between about 2.0 and about 4.0 picograms/mL/microgram, a linear relationship between dose and C max or a C max which is comparable to that of an ACTIQ® dosage form having about 80% more fentanyl.
16. The dosage form of claim 15 providing a ratio of C max to dose is between about 2.7 and about 3.5 picograms/mL/microgram.
17. The dosage form of claim 16 further providing a linear relationship between dose and C max.
18. The dosage form of claim 15 providing a C max which is comparable to that of an ACTIQ® dosage form having about 80% more fentanyl.
19. The dosage form of claim 18 further providing a linear relationship between dose and C max.
20. The dosage form of any one of claims 15, 17 and 19 wherein said effervescent couple is present in an amount of about to about 85% by weight of said dosage form, said pH adjusting substance is present in an amount of about 0.5 to about 25% by weight of said dosage form, and said starch glycolate is present in an amount of about 0.25 to about 20% by weight of the dosage form.
21. The dosage form of claim 20 wherein said effervescent couple is present in an amount of about 15 to about 60% by weight of said dosage form, said pH adjusting substance is present in an amount of about 2 to about 20% by weight of said dosage form, and said starch glycolate is present in an amount of about 0.5 to about 15% by weight of the dosage form.
22. The dosage form of claim 20 further comprising a filler.
23. The dosage form of claim 22 wherein said filler is present in an amount of between about 10 and about 80% w/w.
24. The dosage form of claim 23 wherein said filler is mannitol.
25. The dosaqe form of claims 1 or 15 packaged in an F1 package.
26. A method of treating pain in a patient in need thereof comprising the steps of: placing a dosage form comprising about 100 to about 800 micrograms of fentanyl, calculated as fentanyl free base or an equivalent amount of a salt thereof, an effervescent couple, a pH adjusting substance said adjusting substance selected and provided in an amount capable of providing a change in localized pH of at least 0.5 pH units, and a starch glycolate, said dosage form being suitable for delivery of said fentanyl across the oral mucosa of a patient by buccal, gingival or sublingual administration and providing a ratio of C max to dose is between about 2.0 and about 4.0 picograms/mL/microgram, a linear relationship between dose and C max or a C max which is comparable to that of an ACTIQ® dosage form having about 80% more fentanyl into the mouth of a patient in contact with said patient's oral mucosa, and maintaining said dosage form in intimate contact with said oral mucosa for a time sufficient to deliver a therapeutically effective amount of said fentanyl across said oral mucosa.
27. The method of claim 26 wherein said dosage form is held in contact with said oral mucosa for a period of between about 10 and about 30 minutes.
28. The method of claim 26 wherein said dosage form is held in contact with said oral mucosa for a period of time sufficient to provide absorption of at least about 75% of said fentanyl dose into the blood stream of said patient.
29. The method of claim 26 wherein said pain is selected from the group consisting of breakthrough cancer pain, back pain, neuropathic pain, surgical pain, or post operative pain.
30. A method of treating episodes of breakthrough cancer pain comprising the steps of providing an initial dose of about 100 micrograms of fentanyl calculated as a fentanyl free base or an equivalent amount of a salt thereof, in a dosage form comprising an effervescent couple in amount of about 5 to about 85% by weight of the dosage form, a pH adjusting substance in an amount of about 0.5 to about 25% by weight of the dosage form, and a starch glycolate in the amount of 0.25 to about 20% by weight of the dosage form, said dosage form being suitable for delivery of said fentanyl across the oral mucosa of a patient, and placing said dosage form in the mouth of said patient between the cheek and the upper or lower gum, for a time sufficient to deliver a therapeutically effective amount of said fentanyl across said oral mucosa.
31. A method of making a tablet for buccal, gingival or sublingual administration of fentanyl comprising the steps of:
providing fentanyl or a salt thereof in an amount of between about 100 and about 800 micrograms per dose measured as fentanyl base, or an equivalent amount of a salt thereof, providing an effervescent couple in an amount of about 5 to about 85% by weight of the dosage form, a pH adjusting substance in an amount of about 0.5 to about 25% by weight of the dosage form, and a starch glycolate in an amount of about 0.25 to about 20% by weight of the dosage form, blending said fentanyl, effervescent couple, pH adjusting substance and said starch glycolate, and compressing the resulting blend into at least one tablet.
32. The method of claim 31 further comprising the step of packaging said tablet in an F1 package.
33. The method of claim 31 further comprising the step of providing a filler in an amount of between about 10 and about 80%
by weight of the dosage form and blending same with said fentanyl, effervescent couple, pH adjusting substance and said starch glycolate prior to compressing the resulting blend into at least one tablet.
34. The method of claim 33 wherein said filler is mannitol.
35. The method of claim 34 wherein said mannitol is spray dried mannitol.
36. The method of claim 33 further comprising the step of adding a lubricant to said blend prior to compressing same into at least one tablet.
37. The method of clam 36 further comprising the step of blending said lubricant with said fentanyl, effervescent couple, pH adjusting substance, starch glycolate and said filler prior to compressing the resulting blend into at least one tablet.
38. The method of claim 37 wherein said tablet is compressed to a hardness of between about 5 and about 100 Newtons.
39. The method of claim 38 further comprising the step of packaging said tablet in an F1 package.
40. The method of claim 31 wherein said tablet is compressed to a hardness of between about 15 and about 100 Newtons.
41. The method of claim 40 further comprising the step of packaging said tablet in an F1 package.
42. A method of making a tablet for buccal, gingival or sublingual administration of fentanyl comprising the steps of:
providing about 100 to about 800 micrograms of fentanyl, calculated as fentanyl free base or an equivalent amount of a salt thereof, providing an effervescent couple, a pH adjusting substance said pH adjusting substance selected and provided in an amount capable of providing a change in localized pH of at least 0.5 pH units, and a starch glycolate, blending said fentanyl, effervescent couple, pH adjusting substance and said starch glycolate, and compressing the resulting blend into at least one tablet, said dosage form being suitable for delivery of said fentanyl across the oral mucosa of a patient by buccal, gingival or sublingual administration
43. The method of claim 42 further comprising the step of packaging said tablet in an F1 package.
44. The method of claim 42 further comprising the step of providing a filler in an amount of between about 10 and about 80%
by weight of the dosage form and blending same with said fentanyl, effervescent couple, pH adjusting substance and said starch glycolate prior to compressing the resulting blend into at least one tablet.
45. The method of claim 44 wherein said filler is mannitol.
46. The method of claim 45 wherein said mannitol is spray dried mannitol.
47. The method of claim 44 further comprising the step of adding a lubricant to said blend prior to compressing same into at least one tablet.
48. The method of claim 47 further comprising the step of blending said lubricant with said fentanyl, effervescent couple, pH adjusting substance, starch glycolate and said filler prior to compressing the resulting blend into at least one tablet.
49. The method of claim 48 wherein said tablet is compressed to a hardness of between about 5 and about 100 Newtons.
50. The method of claim 49 further comprising the step of packaging said tablet in an F1 package.
51. The method of claim 42 wherein said tablet is compressed to a hardness of between about 5 and about 100 Newtons.
52. The method of claim 51 further comprising the step of packaging said tablet in an F1 package.
CA2548915A 2003-12-31 2004-12-30 Generally linear effervescent oral fentanyl dosage form and methods of administering Active CA2548915C (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US53361903P 2003-12-31 2003-12-31
US60/533,619 2003-12-31
US61566504P 2004-10-04 2004-10-04
US60/615,665 2004-10-04
PCT/US2004/043703 WO2005065319A2 (en) 2003-12-31 2004-12-30 Generally linear effervescent oral fentanyl dosage form and methods of administering

Publications (2)

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CA2548915A1 true CA2548915A1 (en) 2005-07-21
CA2548915C CA2548915C (en) 2012-10-16

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US (3) US7862832B2 (en)
EP (1) EP1708686B1 (en)
JP (2) JP2007517054A (en)
KR (1) KR101184138B1 (en)
CN (1) CN102078310B (en)
AT (1) ATE498395T1 (en)
AU (1) AU2004311880B2 (en)
BR (1) BRPI0418228B8 (en)
CA (1) CA2548915C (en)
CY (1) CY1111458T1 (en)
DE (1) DE602004031462D1 (en)
DK (1) DK1708686T3 (en)
EA (1) EA010826B1 (en)
HK (1) HK1100480A1 (en)
HR (1) HRP20110336T1 (en)
IL (1) IL176449A (en)
ME (1) ME01300B (en)
NO (1) NO338714B1 (en)
NZ (1) NZ548216A (en)
PL (1) PL1708686T3 (en)
PT (1) PT1708686E (en)
RS (1) RS51713B (en)
WO (1) WO2005065319A2 (en)

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