Parathyroid hormone-containing emulsion for nasal administration

Details Parathyroid hormone-containing emulsion for nasal administration Parathyroid hormone-containing emulsion for nasal administration

1994-05-16

1995-04-18

Griffin, Ronald W.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Peptide containing doai

514 12, 514947, A61K 3724, A61K 9107, A61K 4726

Patent

active

054079110

DESCRIPTION:

BRIEF SUMMARY
FIELD OF THE INVENTION

The present invention relates to an emulsion for nasal administration containing a parathyroid hormone or its analogue (hereinafter generally designates as PTH) as an active ingredient. More particularly, it relates to such emulsion for nasal administration, having superior stability, and being so improved that the PTH is absorbed safely and efficiently through spraying administration in the nasal cavity.


PRIOR ARTS

Physiologically active peptides are becoming one of the fields where the most progressive development is effected as future therapeutic drugs. However, the present conventional route of administration for the peptide drugs are almost limited to injection. Thus, a more simple administrating preparation which can be adminsitered by self-medication has been desired, especially in the treatments of the chronic disorders, to avoid the inconvenient of going to hospital regularly, and for the purpose of diminishing pain and anguish at the site of injection.
Recently, there have been many attempts to develop alternative administration, e.g. rectal, nasal, oral, etc., instead of injection route. It has been found that absorption of peptides, which are poorly absorbed through mucosain the form of a normal drug preparation, can be enhanced by addition of surface active agents, and accordingly several absorption promoters have been found. For example, among the report on nasal administration of physiologically active peptides, nasal adminsitration of aqueous insulin preparation using sodium glycodeoxycholate as an absorption promoter has been known. [Proc. Natl. Acad. Sci. U.S.A., 82 (21), 7419-7423 (1985)]. Further nasal administration of polypeptide using biel acid such as cholic acid, deoxycholic acid and taurocholic acid, has known (Japanese Patent Unexamined Publication, No. 63-2932). A powdery nasal administration preparation consisting of physiologically active peptides and aqueous absorbable and water-less-soluble base ingredients has also known. (Japanese Patent Unexamined Publication, No. 60-224616) However, these preparations are not satisfactory due to the inferior absorbability and local irritation and are not yet practically employed.
Among various physiologically active peptides, parathyroid homons are generally known as a peptide hormone having serum calcium elevating activity, and are used clinically as diagnostic agent for hypoparathyroidism. But, it has been known that PTH are a highly hydrophillic peptide with a higher molecular weight (approximately 4,000-10,000) and much poorly absorbed through the gastrointestinal tract.


PROBLEMS TO BE SOLVED BY THE INVENTION

Azacycloalkane derivatives was disclosed to exhibit superior absorption promoting effect. (Japanese Patent Unexamined Publication, No. 62-238261) It was found that these derivativs have much stronger absorption promoting effect with physiological properties different from those absorption promotors used in the conventional preparations for nasal administration. Accordingly, PTH preparations for nasal administration were prepared using such derivatives as the absorption promotor, however, satisfactory results were not obtained since the emulsifying agent required for emulsification, heretofore used, were insufficiently effected.
Also many studies have been conducted recently on emulsions which are a liquid preparation containing water and oil in homogeneous state. Many emulsifying agents have been developed, and much stable emulsions have been broadly used, owing to the significant progress in emulsifying techniques.
However, the majority of the emulsions are those using a nonionic surface active agent having a polyoxyethylene chain, or an ionic surface active agent, as the emulsifying agent, many of which are, in turn, had a strong suspicion about the safety to human body. Further, egg-york lecithin and soybean lecithin may be referred to as the emulsifying agent commonly used for fatty emulsions for intravenous injection. These emulsions have, however, certain problems in their insufficient stabili

REFERENCES:
patent: 4695465 (1987-09-01), Kigasawa et al.
patent: 4882359 (1989-11-01), Nakagawa et al.
patent: 5059587 (1991-10-01), Yamamoto et al.
patent: 5238917 (1993-08-01), Fujii et al.
patent: 5281580 (1994-01-01), Yamamoto et al.

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