Transdermal administration preparation of a 9-aminocyclopenta (b

Details Transdermal administration preparation of a 9-aminocyclopenta (b Transdermal administration preparation of a 9-aminocyclopenta (b

1997-04-17

1999-02-09

Brouillette, D. Gabrielle

Drug, bio-affecting and body treating compositions

Preparations characterized by special physical form

Web, sheet or filament bases; compositions of bandages; or...

424448, 514944, 514969, A61F 1300

Patent

active

058690883

DESCRIPTION:

BRIEF SUMMARY
This application is a 371 of PCT/JP95/02183, filed Oct. 24, 1995.


TECHNICAL FIELD

The present invention relates to a transdermal administration preparation, more specifically a transdermal administration preparation containing a 9-amino-cyclopenta(b)quinoline as an active ingredient.


BACKGROUND ARTS

9-aminocyclopenta(b)quinolines, in particular, 9-amino-2,3,5,6,7,8-hexahydro-1H-cyclopenta(b)quinoline or its salts, as disclosed in Japanese Examined Patent Publication (Kokoku) No. 63-35611 and Japanese Examined Patent Publication (Kokoku) No. 3-54922, are compounds useful as medicines for the treatment of Alzheinier's disease and other dementia and as medicines for the treatment of peripheral nerve-muscle transmission disorders. It is described that these compounds are to be administered to patients orally or by injection etc. to achieve the desired pharmaceutical effects.
Japan has experienced a sharp rise in diseases peculiar to the aged along with the rapid aging of its population. In particular, senile dementia, especially Alzheimer's disease, have as major symptoms impairment of memory, disorientation, dyslogia, etc. In addition, many patients exhibit abnormal behavior such as poriomania. Further, some exhibit symptoms such as hallucinations or delusions. Therefore, the burden on the family members or medical personnel caring for them is high. Measures against this are becoming an important national issue.
Patients suffering from dementia, however, are unable in practice to control the frequency or amount of ingestion of a drug on their own volition even looking at a single administration of a drug. Further, even if a doctor or family member instructs the patients to take the medication, they often cannot understand the instructions or else will not follow the instructions even if understanding them. This is a major hurdle in treatment. Further, the aged generally have reduced swallowing power and, therefore, quite a few patients complain of suffering when ingesting solids such as tablets.
In this way, in patients suffering from senile dementia, oral administration of a drug often becomes difficult along with the progression of the disease. In this case, normally the drug is administered by non-oral methods, that is, injection etc., but in this case it is essential that this be done by a doctor or other expert. On top of this, patients suffering from senile dementia differ from other patients in that there are a large number of patients fared for at home where trips to the hospital are difficult, therefore it is becoming urgent to find a method of administration of drugs effective for these patients as well.
In view of this situation, in recent years, the transdermal method of administration has been studied in the field of dementia. For example, Japanese Unexamined Patent Publication (Kokai) No. 61-186317 and Japanese Unexamined Patent Publication (Kokai) No. 4-338325 propose transdermal administration preparations containing as an active ingredient tetrahydroaminoacridine etc. known as an antidementia drug.
That is, Japanese Unexamined Patent Publication (Kokai) No. 61-186317 discloses a transdermal absorption preparation composition (for treatment of dementia) comprising a basic drug composed of a combination of a cholinergic agent or anticholinergic agent and a low molecular weight fatty acid.
Further, Japanese Unexamined Patent Publication (Kokai) No. 4-338325 discloses a transdermal absorption preparation of a two-layer composite laminate comprising a silicone elastomer and a large-pore polyethylene slab and containing tetrahydroaminoacridine etc. as a drug.
However, these known preparations have the defects that the tetrahydroaminoacridine used as the active ingredient has strong side effects on the liver and further the frequency of occurrence of these side effects is extremely high, therefore cannot be safety used for patients suffering from dementia. No satisfactory therapeutic agent, has yet been found.


DISCLOSURE OF INVENTION

In view of the above situation, the present inventors eng

REFERENCES:
patent: 4550113 (1985-10-01), Lavretskaya et al.
patent: 4735953 (1988-04-01), Lavretskaya et al.
patent: 5019395 (1991-05-01), Mahjour et al.
patent: 5629007 (1997-05-01), Audia

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