Intravaginal preparation containing physiologically active pepti

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Peptide containing doai

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Details

424433, 514 3, 514 12, 514 21, 514784, 514785, 514808, 514967, A61K 902, A61K 3800, A61K 4712, A61K 4714

Patent

active

057768862

DESCRIPTION:

BRIEF SUMMARY
TECHNICAL FIELD

This invention relates to an intravaginal preparation containing a physiologically active peptide. More particularly, it relates to an improved intravaginal preparation comprising a physiologically active peptide and as an absorption promoter a combination of a sucrose fatty acid ester and an organic acid, by which the active peptide can be effectively absorbed via vaginal mucous membrane with safety to human body.


PRIOR ART

The study on physiologically active peptides has recently been developed and benefitfed by the recent significant development of science. The results of the fundamental studies include production of highly pure peptides on a large scale, clarification of the mechanism of the pharmacological activities including clarification of the structure of the drug-receptor in the therapy with the peptides, creation or improvement of animals useful as a model for studying diseases and thereby finding of new physiological activities, which are owing to the development of genetic engineering technique and purification technique. With such development, the physiologically active peptides are expected to be useful as a very important medicament in therapy of various diseases in the future, and nowadays, intensive studies have been done in order to use them clinically.
The representative peptides which have already been clinically used are insulin and calcitonin. The main diseases in which these peptides participate are diabetes and osteoporosis. It is considered that these diseases become significant by increase in population of old ages and are owing to the unbalanced diet resulting from the recent easy and rich dietary life, and population of patients suffering from such diseases has been increased, which is one of the social problems.
Insulin participates in permeation through membrane of saccharide, amino acids and potassium ion in muscles and the liver, activation of glycogen synthetic enzyme ribosome, promotion of synthesis of proteins and fatty acids, promotion of utilization of saccharides and inhibition of new production thereof, promotion of membrane permeability of saccharides in the fatty tissues, and promotion of synthesis of fatty acids, and it has clinically been used in the therapy of insulin-dependent diabetes and in the shock therapy of schizophrenia.
It is known that calcitonin participates in calcium metabolic homeostasis which is important to biobody, and it has clinically been used in the therapy of pain of osteoporosis in aged persons, especially in aged females, hypercalcemia and Paget's disease of bone. It has also been found that calcitonins participate in locomotorium disorder, diseases of digestive organs, endocrinic pathobolism, blood dyscrasias, cardiovascular disease, and the like, and hence it has been studied as to the possibility to use as a medicament in the therapy of various diseases.
However, these peptides are water-soluble high molecular compounds which are easily decomposed by gastric juice or proteases such as pepsin and trypsin, and hence, when they are administered by oral route, they are hardly absorbed and cannot exhibit their activities. In order to exhibit their pharmacological activities, they are usually administered by injection. According to the administration method, the peptide preparation must be administered regularly and frequently for the therapy of the above chronic diseases, which disadvantageously forces the patient frequent attendance to hospitals. Moreover, injection causes pain at the injection site and psychic pain. Besides, injection possibly causes topical allergic reaction or muscular contracture to the patients. Accordingly, it has been desired to find an improved preparation which can easily be administered by the patients themselves.
It has been studied how to administer the peptides by other means than injection, for example, intrarectal, intranasal, oral, or intravaginal administration. It has been found that when the peptides are administered through mucous membrane, they are usually not absorbed alone, but t

REFERENCES:
patent: 5482706 (1996-01-01), Igari et al.
Remington's Pharmaceutical Sciences, 18th ed. pp. 245-246, 1990.

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