Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Implant or insert
Patent
1998-07-08
2000-10-24
Azpuru, Carlos A.
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Implant or insert
424DIG15, 514966, A61F 902
Patent
active
061363375
DESCRIPTION:
BRIEF SUMMARY
BACKGROUND OF THE INVENTION
1. Field of the Invention
This invention relates to a composition for rectal administration, more particularly to a composition for rectal administration suitable for local curing such as curing of hemorrhoids or the like, which composition comprises an acrylic acid polymer, a vasoconstrictor and a rectal tissue-curing agent, with which the concentration of the curing agent in the rectal tissue is increased and the potency of the curing agent continues so as to be "long acting."
2. Background Art
It is known that conventional preparations for rectal administration, such as a suppository and the like, when administered to an anorectal region, spread with time from the administered site to the upper region of the rectum because a base in the preparation is melted at the body temperature to become a liquid state. For the purpose of local curing, such as curing of hemorrhoids or the like, the spreading of the preparation to the upper region of the rectum results in a decrease in the amount of the preparation present in the vicinity of the affected region. Therefore, reports have been made on innovations in preparations for rectal administration for the purpose of preventing the spread of the preparation in the rectum and allowing the preparation to remain in the vicinity of the affected region.
For example, JP-A-54-26325 discloses a preparation for rectal administration which remains in the vicinity of the affected region of the rectum and which contains a metal salt of polyacrylic acid. A mixture of polyacrylic acid and polyvinylpyrrolidone for such a purpose is disclosed in JP-A-6-40889 and the use of a carboxyvinyl polymer for such a purpose is disclosed in JP-A-63-280016 and JP-A-1-143825.
SUMMARY OF THE INVENTION
The present inventors have made various studies of compositions for rectal administration and have consequently found that a preparation in the form of a composition comprising an acrylic acid polymer, a vasoconstrictor and a rectal tissue-curing agent not only remains in the vicinity of the affected region in the rectum but also inhibits the curing agent from diffusing from the rectal tissue, increases the concentration of the curing agent in the tissue and has long acting potency.
That is to say, this invention is a long acting composition for rectal administration which comprises an acrylic acid polymer, a vasoconstrictor and a rectal tissue-curing agent.
BRIEF DESCRIPTION OF DRAWINGS
FIG. 1 is a graph showing the results of determination of the amount of lidocaine in 1 g of rectal tissue of a section of 10 cm from the anal region.
FIG. 2 is a graph showing the results of determination of the amount of hydrocortisone acetate in 1 g of rectal tissue of a section of 10 cm from the anal region.
DESCRIPTION OF THE PREFERRED EMBODIMENTS
In this invention, the terminology "acrylic acid polymer" means a polyacrylic acid, a polyacrylic acid salt, a partially cross-linked polyacrylic acid or its salt. The average molecular weight thereof is 100,000 to 10,000,000 and the content of carboxyl group thereof is preferably 50 to 70%, more preferably 58 to 63%. The particle size is preferably 500 microns or less, more preferably 250 microns or less. Suitable partially cross-linked polyacrylic acids, include, for example, carboxyvinyl polymer, carbomer and polycarbofil, and preferably carboxyvinyl polymer. As a salt of polyacrylic acid, there are mentioned alkali metal salts such as sodium salt, potassium salt and the like; alkaline earth metal salts such as calcium salt and the like; trivalent metal salts such as aluminum salt and the like; and ammonium salt. Preferable are potassium polyacrylate, sodium polyacrylate, calcium polyacrylate and ammonium polyacrylate.
The amount of the acrylic acid polymer formulated is 0.1 to 20% by weight based on the total amount of the composition for rectal administration. Among the acrylic acid polymers, most preferable is carboxyvinyl polymer and the amount of the same formulated is 0.2 to 15% by weight, more preferably 1 to 10% by we
REFERENCES:
patent: 4292300 (1981-09-01), Byrne et al.
Webster's II new Riverside University Distionary, p 75.
Chemical Abstracts, vol. 124, No. 12 Mar. 18, 1996 # 156068.
Fujimori Tomoko
Kondo Osamu
Tanaka Shigeo
Urushizaki Fumio
Azpuru Carlos A.
Taisho Pharmaceutical Co. Ltd.
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