Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Peptide containing doai
Patent
1996-12-02
1999-10-19
Sayala, Chhaya D.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Peptide containing doai
514 2, 514 8, 514 12, 514 21, 514802, A61K 3817, A61K 3809, A61K 3810, A61K 3816
Patent
active
059688998
DESCRIPTION:
BRIEF SUMMARY
TECHNICAL FIELD
This invention relates to a medicinal composition, and more specifically to a medicinal composition which makes it possible to absorb a peptide, which is susceptible to decomposition and has a low absorption rate, at a high rate through a mucosa or the like and further to prolong its pharmacological effects over a long time.
BACKGROUND ART
Peptides have conventionally been employed for the treatment or the like of various diseases. For example, calcitonin, insulin, interferon and erythropoietin are used for the improvement of osteoporosis and pains associated with osteoporosis and the treatment of diseases such as hypercalcemia, for the treatment of diseases such as diabetes, for the treatment of diseases such as hepatitis and renal carcinoma, and for the treatment of diseases such as anemia, respectively.
As an administration method of peptides, administration by injection is usual because of the difficulty in having them absorbed through the digestive tract. However, this injection-reliant administration is not an administration method which permits self-administration by a patient, so that regular outpatient treatment is required. It also involves the problem of administration being accompanied by painful discomfort.
On the other hand, from the standpoint of economy, oral administration is accompanied by a problem because the absorption rate of a peptide through the digestive tract is low and moreover, the peptide is subjected to decomposition, first-pass effect and the like by proteinases and hence, the peptide has to be administered in a very large quantity to have it absorbed in an effective amount through the digestive tract.
Concerning the administration form of peptides, a great deal of research is now under way to overcome the above-described problems. Intranasal sprays containing peptides as effective ingredients have already been developed in Europe. However, they are accompanied by problems such as insufficient absorption of the peptides and are not satisfactory.
With a view to increasing the absorbability of peptides, it has heretofore been attempted to formulate them into preparations with the addition of a bile acid salt or a surfactant [Japanese Patent Application Laid-Open (Kokai) No. SHO 59-130820, Japanese Patent Application Laid-Open (Kokai) No. SHO 59-89619, and Japanese Patent Application Laid-Open (Kokai) No. SHO 63-39822] or to use a proteinase inhibitor for promoting permucosal absorption [J. Pharmacobiodin. 14(2), S4, 1991, and Japanese Patent Application Laid-Open (Kokai) No. HEI 3-48627). The absorption enhancers employed in these preparations are all accompanied by one or more safety problems such as excessively strong mucosal irritation, so that none of them have been put into practice.
From the foregoing circumstances, there is an outstanding desire for the development of a preparation which is free of the above-described problems .
DISCLOSURE OF THE INVENTION
With the foregoing circumstances in view, the present inventors have conducted extensive research with a view to developing a medicinal composition excellent in absorbability and safety despite its easily-applicable administration form. As a result, it has been found that the above object can be achieved by adding a peptide to a base containing epsilon aminocaproic acid or tranexamic acid and an ethylene oxide-propylene oxide block copolymer represented by the below-described formula (I), leading to the completion of the present invention.
Namely, an object of the present invention is to provide a medicinal composition comprising a peptide, epsilon aminocaproic acid or tranexamic acid, and an ethylene oxide-propylene oxide block copolymer represented by the following formula (I): O).sub.c H (I)
BEST MODES FOR CARRYING OUT THE INVENTION
No particular limitation is imposed on the peptide for use in the medicinal composition according to the present invention insofar as it is a peptide having pharmacological effects. Its specific examples can include calcitonin, insulin, proinsulins, epidermal gr
REFERENCES:
patent: 5578324 (1996-11-01), Dohi et al.
Tau et al., Biomaterials, vol. 14 (11), p. 823-833, 1993.
Pluromic (Information Brochure), Wyandotte Chem. Corp., pp. 1-14, 1952.
Pec et al., J. Pharm. Sci., vol. 81 (7), p. 626-630, 1992.
The United States Pharmacopeia, 16.sup.th Edn, pp. 1491-1493, 1985.
Parsons et al., Br. 13 J. Pharm., vol. 66, pp. 25-32, 1979.
Manning et al., Pharm. Res., vol. 6 (11), pp. 903-918, 1989.
Johnston et al., Pharm. Res., vol. 9(3), pp. 425-434, 1992.
Wang et al., J. Parenteral. Sci & Tech., vol. 42(2s) p. S3 to S26, 1988.
Duncan et al., Int. J. Pharm., vol. 120, pp. 179-188, 1995.
Ishikawa Kazuyuki
Kimura Takayoshi
Nakai Yoshinobu
Sekine Takashi
Sayala Chhaya D.
Tsumura & Co.
LandOfFree
Medicinal compositions of peptides with EACA or tranexamic acid does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Medicinal compositions of peptides with EACA or tranexamic acid , we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Medicinal compositions of peptides with EACA or tranexamic acid will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-2055416