WO2006099877A1 - Rectal and vaginal suppositories containing bioadhesive bromocriptine and poloxamer - Google Patents

Rectal and vaginal suppositories containing bioadhesive bromocriptine and poloxamer Download PDF

Info

Publication number
WO2006099877A1
WO2006099877A1 PCT/EG2005/000032 EG2005000032W WO2006099877A1 WO 2006099877 A1 WO2006099877 A1 WO 2006099877A1 EG 2005000032 W EG2005000032 W EG 2005000032W WO 2006099877 A1 WO2006099877 A1 WO 2006099877A1
Authority
WO
WIPO (PCT)
Prior art keywords
rectal
bromocriptine
poloxamer
vaginal suppositories
suppositories containing
Prior art date
Application number
PCT/EG2005/000032
Other languages
French (fr)
Inventor
Atef Mohammed Mostafa Darwish
Original Assignee
Atef Mohammed Mostafa Darwish
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 Atef Mohammed Mostafa Darwish filed Critical Atef Mohammed Mostafa Darwish
Publication of WO2006099877A1 publication Critical patent/WO2006099877A1/en

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Classifications

    • 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
    • A61K31/48—Ergoline derivatives, e.g. lysergic acid, ergotamine
    • 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

Definitions

  • Bromocriptine methylate is a water insoluble drug. It is associated with a lot of side effects that lead to 10% discontinuation rate. Its solubility and subsequently absorption could be increased by adding pluronics as demonstrated in a previous study ( Darwish et al. Fertility and sterility- April, 2005 (755)
  • the previous formula is mixed with bioadhesive polymers including caobopol 974P, chitosan and is created in a suppository form suitable for both male ( rectal ) and female ( vaginal ) usage to extend the scope of this treatment modality.
  • bioadhesive polymers including caobopol 974P, chitosan

Abstract

The present invention refers to suppositories, which can be applied rectally or vaginally, containing bromocryptine mesylate and poloxamer. For achieving bioadhesivity the formulation contains carbomer or chitosan.

Description

Rectal and vaginal suppositories containing bioadhesive bromocriptine and pluronic
Technical Field:
Bromocriptine methylate is a water insoluble drug. It is associated with a lot of side effects that lead to 10% discontinuation rate. Its solubility and subsequently absorption could be increased by adding pluronics as demonstrated in a previous study ( Darwish et al. Fertility and sterility- April, 2005 (755)
Background Art:
Trials of vaginal use of the commercial tablets resulted in significant decline of the prolactin level after 1 month of therapy. However, the patient acceptability was very low as they were convienced that tablets can be effective if inserted vaginally. Many patients feel that the previous formula was inconvenient due to excessive vaginal discharge and easy dislodgement from the vagina.
Disclosure of the invention:
In the current modification, the previous formula is mixed with bioadhesive polymers including caobopol 974P, chitosan and is created in a suppository form suitable for both male ( rectal ) and female ( vaginal ) usage to extend the scope of this treatment modality.
Best mode for carrying out the invention:
Manufacturing this new formulation in a suppository form to be suited for vaginal as well as rectal application.
Industrial applicability:
It is easily manufactured in a suppository fonn.

Claims

Calims
- Creation of bromocriptive methylate suppositories. - Adding bioadhesive and pluronic substances.
PCT/EG2005/000032 2005-03-24 2005-10-01 Rectal and vaginal suppositories containing bioadhesive bromocriptine and poloxamer WO2006099877A1 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EG2005030150 2005-03-24
EG2005030150 2005-03-24

Publications (1)

Publication Number Publication Date
WO2006099877A1 true WO2006099877A1 (en) 2006-09-28

Family

ID=37023380

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EG2005/000032 WO2006099877A1 (en) 2005-03-24 2005-10-01 Rectal and vaginal suppositories containing bioadhesive bromocriptine and poloxamer

Country Status (1)

Country Link
WO (1) WO2006099877A1 (en)

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3752814A (en) * 1968-05-31 1973-08-14 Sandoz Ltd 2-bromo-alpha-ergocryptine
US6267985B1 (en) * 1999-06-30 2001-07-31 Lipocine Inc. Clear oil-containing pharmaceutical compositions

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3752814A (en) * 1968-05-31 1973-08-14 Sandoz Ltd 2-bromo-alpha-ergocryptine
US6267985B1 (en) * 1999-06-30 2001-07-31 Lipocine Inc. Clear oil-containing pharmaceutical compositions

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