Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Peptide containing doai
Patent
1996-04-15
1998-08-04
Russel, Jeffrey E.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Peptide containing doai
424 851, 424 852, 424 854, 424 941, 514 12, 514 18, 514 19, 514 21, 514946, 514947, A61K 3802, A61K 3806, A61K 4710
Patent
active
057893756
DESCRIPTION:
BRIEF SUMMARY
TECHNICAL FIELD
This invention relates to a pernasal composition (pernasally administrable composition) and a pernasal preparation (pernasally administrable preparation) and more particularly to a novel composition and a novel preparation which are very low in irritation to nasal mucosae and enable their pharmacologically active ingredients to be highly pernasally absorbed.
The pernasally administrable composition and preparation are hereinafter referred to respectively as "pernasal composition" and "pernasal preparation" for brevity.
BACKGROUND TECHNIQUES
It has heretofore been known that pharmaceutical compounds having high hydrophilicity and a low oil/water distribution ratio are not absorbable through digestive tracts or are extremely difficultly absorbable therethrough. In general, a peptide or protein having a physiological activity is extremely difficultly absorbable through the digestive tracts since it not only has high hydrophilicity and a low oil/water distribution ratio but also is subject to decomposition with enzymes present in the digestive tracts or on the wall thereof.
Further, since many medicines absorbed through the digestive tracts are subject to an initial passage effect in a liver, it has hitherto been necessary to administer a medicine such as a peptide or protein having a physiological activity by injection in order to expect full efficacy from the medicine so administered. However, since administration of such a medicine by injection is not allowed to be executed by those other than specialists in the art and is also accompanied with pain given to the administered, there is demanded a medicinal preparation which may be administered in a more expedient and more feasible manner especially in a case where frequent administration of the preparation is required.
Pernasal administration of preparations adapted for pernasal absorption has recently been noted as a substitute for administration by injection.
Nasal mucosae have abundant capillary vessels and are satisfactory in absorption of medicines therethrough as compared with vaginal mucosae, and, in addition, medicines absorbed directly into the capillary vessels are advantageous in that, for example, they can avoid the initial passage effect in a liver.
The medicines pernasally administered are not necessarily sufficient in their biological availability and, therefore, the necessary dosage of a peptide or protein having a physiological activity must be large even if pernasally administered as compared with that administered by injection. Further, the physiological variation (such as common cold and an allergy) of nasal mucosae will disadvantageously affect the absorbability of medicines when administered.
Thus, fusigic acid derivatives, phospholipids, alkyl glucosides, saccharide fatty acid esters and surface-active agents proposed respectively in Japanese Pat. Appln. Laid-Open Gazettes Nos. Sho 61-33126 (or No. 33126/86), Hei 1-501550, Sho 63-243033, Sho 63-39882 and Sho 52-25013, and the like have been used in attempts to enhance the absorbability of pernasally administered medicines and reduce the dispersion of absorption thereof. These compositions and absorption accelerators so proposed in the above Japanese Gazettes have, in addition to beneficial effects, a serious side-effect which is irritation to nasal mucosae, and, therefore, they are now still not put to practical use. Moreover, a part of antiseptics and preservatives which have been used in many conventional pernasally administrable preparations have surface-activity and, therefore, a problem as to local irritation caused by said surface-activity begins to be raised (J. pharm. pharmacol, 1990, 42, 145-151).
Further, Japanese Patent Gazette No. Hei 3-38255 (No. 38255/91) describes that the use of hydroxypropylcellulose having a predetermined viscosity will enhance the retentivity of a medicine at the nasal mucosae and increase the absorbability thereof, whereas it cannot necessarily be said to be sufficiently effective.
It is thus eagerly sought to develop a pernasal
REFERENCES:
patent: 4504470 (1985-03-01), Uda et al.
patent: 4882359 (1989-11-01), Nakagawa et al.
patent: 4948588 (1990-08-01), Kamiya et al.
patent: 5112804 (1992-05-01), Kowarski
patent: 5397771 (1995-03-01), Bechgaard et al.
patent: 5428006 (1995-06-01), Bechgaard et al.
Itoh Kohki
Mizumachi Mitsuhiro
Mukae Katsuya
Hisamitsu Pharmaceutical Co. Inc.
Russel Jeffrey E.
LandOfFree
Pernasal composition and pernasal preparation containing the sam does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Pernasal composition and pernasal preparation containing the sam, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Pernasal composition and pernasal preparation containing the sam will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-1177182