Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Peptide containing doai
Patent
1996-10-23
1998-06-09
Davenport, Avis M.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Peptide containing doai
514 16, 530315, 530327, 530328, 530300, A61K 3800, A61K 3802, C07K 500, C07K 700
Patent
active
057634050
DESCRIPTION:
BRIEF SUMMARY
This application is a 371 of PCT/SE95/00249 filed Mar. 9, 1995.
The present invention relates to pharmaceutical compositions in solid form for oral administration of small and medium size peptides, particularly vasopressin, oxytocin, and their analogues. The present invention also relates to a method for manufacture of a single dose of said composition for oral administration of small and medium-size peptides, particularly vasopressin, oxytocin, and their analogues.
The invention further relates to a method for administration of said composition to a patient.
BACKGROUND
A number of medicines for treatment of a variety of diseases contain, as active principle, naturally occurring peptides or their synthetic analogues.
Because of the instability of small and medium size peptides, particularly vasopressin, oxytocin, and their analogues, in the environment of the gastrointestinal tract their uptake, when given as a medicine or for similar reasons, is still very unsatisfactory. Thus, better delivery systems for non-parenteral, particularly for oral, administration of peptides and their analogues are desirable, cf. Davies, S.: "Developing delivery systems for peptides and proteins", Scrip Magazine 1992, 34-38.
It is an object of the present invention to provide a pharmaceutical composition of the kind known in the art and mentioned above which provides for better absorption of said small or medium-size peptides, particularly vasopressin, oxytocin, and their analogues.
It is another object of the present invention to provide a method of manufacture of a single dose of said pharmaceutical composition for oral administration of small and medium-size peptides, particularly vasopressin, oxytocin, and their analogues.
It is a further object of the invention to provide a method for administration of said composition to a patient.
Additional objects of the present invention will become evident by study of the detailed description of preferred embodiments of the invention.
SUMMARY OF THE INVENTION
The above and other objects of the invention are provided by a pharmaceutical composition of the kind described above, said composition comprising a small and medium size peptide, particularly vasopressin, oxytocin, or an analog of vasopressin or oxytocin, an enteric coat, and a pharmaceutically acceptable carrier containing a buffering agent buffering at a pH of from 2 to 6, more preferred from 4 to 5,5, most preferred at about pH 5. It is preferred for the peptide to be chosen from DDAVP (desmopressin), oxytocin, CAP (atosiban), and carbetocin. Particularly preferred is DDAVP. For full sequences of these peptides, see Table 1 at the end of the DETAILED DESCRIPTION section. Another group of peptides preferred for oral administration by incorporation into the composition according to the invention comprises GnRH-analogues (gonadotropin-releasing hormone analogues) such as gonadorelin and triptorelin.
It is preferred for the the pharmaceutically acceptable carrier to further comprise one or several agents selected from the group consisting of carbohydrates and modified carbohydrates and derivatives thereof, polyethylene and/or polypropylene glycol and derivatives thereof, inorganic fillers or lubricating agents, fatty acids and their esters and salts, preservatives and coating agents. Suitable pharmaceutical acceptable carriers comprise a wide variety of carriers for production of pharmaceutical formulations in tablet or capsule form, e.g. the carrier of the antidiuretic composition containing DDAVP disclosed in the European patent no. 163 723. Especially preferred are multiparticle systems, such as systems for administration in soft and hard gelatin capsules; preferred particle sizes for spheres containing peptide and/or protease inhibitor are below about 2 mm.
According to a preferred aspect of the invention the enteric coat is designed for release of its contents in the small intestine. It is particularly preferred for the particles contained in the tablets or capsules to be coated with an enteric coating for delayed re
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Ahlm-Soderberg Christina
Fjellestad-Paulsen Anne
Davenport Avis M.
Ferring B.V.
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