Nasally administrable compositions

Details Nasally administrable compositions Nasally administrable compositions

1999-08-20

2001-03-06

Kishore, Gollamudi S. (Department: 1615)

Drug, bio-affecting and body treating compositions

Preparations characterized by special physical form

Implant or insert

C514S002600, C514S003100, C514S021800, C514S057000, C424S489000, C424S494000, C424S499000

Reexamination Certificate

active

06197328

ABSTRACT:

BACKGROUND OF THE INVENTION
1. Field of the Invention
The present invention relates to a nasally administrable composition containing a physiologically active ingredient, and more particularly, to a nasally administrable composition containing a physiologically active compound with a mixture of unique carrier which adhere to the mucous membrane of the nasal cavity, and cellulose derivatives as absorption accelerator.
2. Description of the Prior Art
Hitherto, there have been developed nasally administrable preparations for physiologically active compounds unlikely to be administered orally. As one example of the preparations, an aerosol in the form of a suspension has been developed for nasal inhalation of calcitonin, in which a fluorinated hydrocarbon is used as a spouting agent. As another means for nasal administration of calcitonin, a liquid spray preparation has also been proposed. However, nasally administrable preparations so far proposed cannot be sufficient because of poor absorbability of physiologically active compounds or local irritability.
The inventor of the present invention has actively been studying a nasally administrable preparations of physiologically active peptides unlikely to be administered orally such as insulin, calcitonin. parathyroid hormone (PTH), human growth hormone (HGH) and so on. As a result of intensive studies, he has proposed nasally administrable composition using a unique carrier, wherein the physiologically active peptide is dispersed and absorbed homogeneously onto the carrier, and is highly absorbable into the body via nasal route.
Through further extensive studies and researches, the inventor of the present invention has found that the amounts of absorbed physiologically active compound into a body via nasal route well proportion to size of surface area of the carrier. Further, the inventor has found that the absorbability of the physiological peptide into a body via nasal route increase when the carrier adhere and stay on the mucous so membrane of the nasal cavity.
SUMMARY OF THE INVENTION
Accordingly, the object of the present invention is to provide a nasally administrable composition that can nasally administer physiologically active compound with higher bioavailability with less irritability than the preparations so far proposed using the carrier, wherein the carrier adhere to the mucous membrane of the nasal cavity.
One aspect of the present invention is to provide the nasally administrable composition comprising:
(a) an effective amount of physiologically active compound;
(b) fine particulate of carrier having a mean particle size from 15 &mgr;m to 300 &mgr;m, and particle surface area from 0.1 m
2
/g to 0.4 m
2
/g, which adhere to the mucous membrane of the nasal cavity; and
(c) cellulose derivatives as absorption accelerator, wherein said physiologically active compound is dispersed homogeneously in and adsorbed homogeneously onto the mixture of said carrier and the cellulose derivatives.
In the specific embodiment of the present invention is the nasally administrable composition comprising:
(a) an effective amount of physiologically active compound selected from the group consisting of insulin, calcitonin and prostaglandin (PG) derivative;
(b) fine particulate of carrier having a mean particle size from 15 &mgr;m to 300 &mgr;m, and particle surface area from 0.1 m
2
/g to 0.4 m
2
/g, which adhere to the mucous membrane of the nasal cavity; and
(c) high substituted hydroxypropylcellulose having 53.4% to a 77.5% of hydroxypropyl group in the compound (HPC—H) as absorption accelerator, wherein said physiologically active compound is dispersed homogeneously in and adsorbed homogeneously onto the mixture of said carrier and HPC—H.
In still another specific embodiment of the present invention is the composition in which HPC—H is contained at a rate of from 5.0% to 70.0%, per the loot total weight of the composition.
The other aspect of the present invention is to provide a mixed carrier to be used for nasally administrable composition comprising:
(a) fine particulate of aluminum compound, calcium compound or magnesium compound having a mean particle size from 15 &mgr;m to 300 &mgr;m, and particle surface area from 0.1 m
2
/g to 0.4 m
2
/g, which adhere to the mucous membrane of the nasal cavity, and
(b) high substituted hydroxypropylcellulose having 53.4% to 77.5% of hydroxypropyl group in the compound (HPC—H).
In still another aspect of the present invention, use of high substituted hydroxypropylcellulose having 53.4% to 77.5% of hydroxypropyl group in the compound (HPC—H) as absorption accelerator for nasally administrable composition containing physiologically active compound such as insulin, calcitonin, prostaglandin (PG) derivatives, monoclonal antibodies, interleukin derivatives (IL) and so on, is provided.


REFERENCES:
patent: 5183802 (1993-02-01), Aliverti et al.
patent: 5578567 (1996-11-01), Cardinaux et al.
patent: 5603943 (1997-02-01), Yanagawa
patent: 5908824 (1999-06-01), Yanagawa

Affiliated with

Also associated with

Rating

Nasally administrable compositions does not yet have a rating. At this time, there are no reviews or comments for this patent.

If you have personal experience with Nasally administrable compositions, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Nasally administrable compositions will most certainly appreciate the feedback.

Rate now

Comments { 0 }

Profile ID: LFUS-PAI-O-2503216