CA2422424A1 - Pharmaceutical compositions for rectal and vaginal administration - Google Patents

Pharmaceutical compositions for rectal and vaginal administration Download PDF

Info

Publication number
CA2422424A1
CA2422424A1 CA002422424A CA2422424A CA2422424A1 CA 2422424 A1 CA2422424 A1 CA 2422424A1 CA 002422424 A CA002422424 A CA 002422424A CA 2422424 A CA2422424 A CA 2422424A CA 2422424 A1 CA2422424 A1 CA 2422424A1
Authority
CA
Canada
Prior art keywords
dosage form
active ingredient
amount
effervescent
target area
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
CA002422424A
Other languages
French (fr)
Other versions
CA2422424C (en
Inventor
S. Indiran Pather
Joseph R. Robinson
Jonathan D. Eichman
Rajendra K. Khankari
John Hontz
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Cima Labs Inc
Original Assignee
Individual
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 Individual filed Critical Individual
Publication of CA2422424A1 publication Critical patent/CA2422424A1/en
Application granted granted Critical
Publication of CA2422424C publication Critical patent/CA2422424C/en
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

Links

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
    • A61K9/0002—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
    • A61K9/0031—Rectum, anus
    • 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
    • A61K9/0034—Urogenital system, e.g. vagina, uterus, cervix, penis, scrotum, urethra, bladder; Personal lubricants
    • 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
    • A61K9/02—Suppositories; Bougies; Bases therefor; Ovules

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Epidemiology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Reproductive Health (AREA)
  • Urology & Nephrology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Medicinal Preparation (AREA)

Abstract

The pharmaceutical compositions of the present invention comprise rectally a nd vaginally administerable dosage forms that contain effervescent agents as penetration enhancers for drugs. Effervescence occurs in the rectum or vagin a, once the dosage form is administered or at a predetermined time following administration. The effervescent agents can be used alone or in combination with pH adjusting substance, which further promote dissolution and absorptio n of the active ingredient.

Claims (28)

1. A dosage form adapted for rectal administration of a therapeutically effective amount of an active ingredient to a target area in the rectum of a mammal;
comprising:

(a) a therapeutically effective amount of an active ingredient; and (b) at least one effervescent penetration enhancer; wherein said at least one effervescent penetration enhancer is present in an amount sufficient to increase the penetration of said active ingredient across said target area of said rectum, and to permit delivery of a therapeutically effective amount of said active ingredient.
2. The dosage form of claim 1, wherein said amount of said at least one effervescent penetration enhancer is equal to about two times to about three times the amount of said drug.
3. The dosage form of claim 1, further comprising a pH adjusting substance.
4. The dosage form of claim 1, further comprising a bioadhesive, wherein said bioadhesive increases contact time between said active ingredient and a mucosa layer of said target area.
5. The dosage form of claim 4, wherein said bioadhesive is contained in a portion of said dosage form external to said active ingredient.
6. The dosage form of claim 1, further comprising at least one noneffervescent penetration enhancer.
7. The dosage form of claim 1, further comprising at least one noneffervescent disintegration agent.
8. The dosage form of claim 1, wherein said dosage form is a suppository.
9. The dosage form of claim 1, wherein said effervescent penetration enhancer comprises a pharmaceutically acceptable effervescent couple; said effervescent couple comprising an acid or equivalent thereof and a base or equivalent thereof.
10. The dosage form of claim 9 wherein said base or equivalent thereof is present in an amount equal to about two times to about three times the amount of said active ingredient; and said acid is present in an amount approximately equimolar to said base.
11. A method for delivering an active ingredient to a target area in the rectum of a mammal; comprising the steps of:
(a) administering in the rectum of a mammal a dosage form comprising a therapeutically effective amount of an active ingredient and at least one effervescent penetration enhancer present in an amount sufficient to increase absorption of said active ingredient across a mucosa layer of said target area, (b) causing said active ingredient and said effervescent penetration enhancer to release from said dosage form at said target area in said rectum and to provide effervescent action at said target area; so that said effervescent action promotes the absorption of a therapeutically effective amount of said active ingredient across said target area.
12. The method of claim 11 wherein said amount of said at least one effervescent penetration enhancer is about two times to about three times the amount of said active ingredient.
13. The method of any one of claim 11, further comprising the step of administering a suitable pH adjusting substance in said dosage form.
14. A dosage form adapted for vaginal administration of a therapeutically effective amount of an active ingredient to a target area in the vagina of a mammal;
comprising:

(a) a therapeutically effective amount of an active ingredient; and (b) at least one effervescent penetration enhancer; wherein said at least one effervescent penetration enhancer is present in an amount sufficient to increases the penetration of said active ingredient across said target area of said vagina.
15. The dosage form of claim 14, wherein said amount of said at least one effervescent penetration enhancer is equal to about two to about three times the amount of said active ingredient.
16. The dosage form of claim 14, further comprising a pH adjusting substance.
17. The dosage form of claim 14, further comprising a bioadhesive, wherein said bioadhesive increases contact time between said active ingredient and a mucosa layer of said target area.
18. The dosage form of claim 17, wherein said bioadhesive is contained in a portion of said dosage form external to said active ingredient.
19. The dosage form of claim 14, further comprising at least one noneffervescent penetration enhancer.
20. The dosage form of claim 14, further comprising at least one noneffervescent disintegration agent.
21. The dosage form of claim 14, wherein said dosage form is a suppository.
22. The dosage form of claim 14, wherein said dosage form is a tablet.
23. The dosage form of claim 14, wherein said dosage form is a capsule.
24. The dosage form of claim 14, wherein said effervescent penetration enhancer comprises a pharmaceutically acceptable effervescent couple; said effervescent couple comprising an acid or equivalent thereof and a base or equivalent thereof.
25. The dosage form of claim 24 wherein said base or equivalent thereof is present in an amount equal to about two to about three times the amount of said active ingredient;
and said acid is present in an amount approximately equimolar to said base.
26. A method for delivering an active ingredient to a target area in the vagina of a mammal; comprising the steps of:

(a) administering in the vagina of a mammal a dosage form comprising a therapeutically effective amount of an active ingredient and at least one effervescent penetration enhancer present in an amount sufficient to increase absorption.
of said active ingredient across a mucosa layer of said target area, (b) causing said active ingredient and said effervescent penetration enhancer to release from said dosage form at said target area in said vagina and to provide effervescent action at said target area; so that said effervescent action promotes the absorption of a therapeutically effective amount of said active ingredient across said target area.
27. The method of claim 26 wherein said amount of said at least one effervescent penetration enhancer is about two times to about three times the amount of said active ingredient.
28. The method of claim 26, further comprising the step of administering a suitable pH adjusting substance in said dosage form.
CA002422424A 2000-09-19 2000-09-19 Pharmaceutical compositions for rectal and vaginal administration Expired - Fee Related CA2422424C (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
PCT/US2000/025634 WO2002024170A1 (en) 2000-09-19 2000-09-19 Pharmaceutical compositions for rectal and vaginal administration

Publications (2)

Publication Number Publication Date
CA2422424A1 true CA2422424A1 (en) 2002-03-28
CA2422424C CA2422424C (en) 2009-12-01

Family

ID=21741785

Family Applications (1)

Application Number Title Priority Date Filing Date
CA002422424A Expired - Fee Related CA2422424C (en) 2000-09-19 2000-09-19 Pharmaceutical compositions for rectal and vaginal administration

Country Status (5)

Country Link
EP (1) EP1318790A4 (en)
JP (1) JP2004509142A (en)
AU (1) AU7384700A (en)
CA (1) CA2422424C (en)
WO (1) WO2002024170A1 (en)

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1872775A1 (en) * 2006-06-29 2008-01-02 Polichem S.A. Use of a hydrophilic matrix comprising a polyacrylic acid derivative, a cellulose ether and a disintegrant for the manufacture of a medicament for treating female genital disorders

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB1212704A (en) * 1967-11-21 1970-11-18 Prodotti Antibiotici Spa Vaginal suppositories
US3888976A (en) * 1972-09-21 1975-06-10 William P Mlkvy Zinc and strontium ion containing effervescent mouthwash tablet
NL7302521A (en) * 1973-02-23 1974-08-27 Foaming, effervescent capsules - contg. therapeutic agents for rectal and vaginal use
JPS58152809A (en) * 1982-03-05 1983-09-10 Eisai Co Ltd Stable foaming vaginal suppository
IT1251114B (en) * 1991-07-26 1995-05-04 Farcon Ag ANTIVIRAL PHARMACEUTICAL FORMS FOR VAGINAL APPLICATION
DE4139883A1 (en) * 1991-11-29 1993-06-03 Michael Prof Dr Dittgen Prodn. of bio-adhesive medicament, e.g. oral or vaginal tablet - comprises mixing drug with swellable, bio-adhesive polymer, dispersant and opt. binder
GB9523136D0 (en) * 1995-11-11 1996-01-10 Procter & Gamble Silicone-containing powders
US5646151A (en) * 1996-03-08 1997-07-08 Adolor Corporation Kappa agonist compounds and pharmaceutical formulations thereof
US6071539A (en) * 1996-09-20 2000-06-06 Ethypharm, Sa Effervescent granules and methods for their preparation
EP2127642A3 (en) * 1998-08-13 2010-02-24 Cima Labs, Inc. Microemulsions as solid dosage forms for oral administration

Also Published As

Publication number Publication date
EP1318790A1 (en) 2003-06-18
JP2004509142A (en) 2004-03-25
WO2002024170A1 (en) 2002-03-28
AU7384700A (en) 2002-04-02
CA2422424C (en) 2009-12-01
EP1318790A4 (en) 2006-02-01
AU2000273847B2 (en) 2006-09-14

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MKLA Lapsed

Effective date: 20160919