Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Peptide containing doai
Patent
1990-11-30
1991-09-24
Schain, Howard E.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Peptide containing doai
530362, 530363, 514776, A61K 4742, A61K 3700, A61K 3100
Patent
active
050514067
DESCRIPTION:
BRIEF SUMMARY
TECHNICAL FIELD
The present invention relates to a pharmaceutical composition using albumin as a carrier, as well as to a process for producing the pharmaceutical composition. More particularly, the present invention relates to a pharmaceutical composition wherein the side effect undesirable to the human body, of the drug contained therein has been alleviated and further the absorption, light stability, etc. of the drug has been improved, as well as to a process for producing the pharmaceutical composition.
BACKGROUND ART
For the alleviation of the side effect of drugs, there have been proposed pharmaceutical compositions comprising a drug and a carrier or the like. As an example, non-steroidal anti-inflammatory agents show a strong anti-inflammatory action to inflamation-affected parts, but they are known to give serious side effects to the central nervous system and the digestive system and to cause hemorrhage and ulcer in the digestive system, in particular; in order to alleviate these side effects, there was proposed, for example, a pharmaceutical composition comprising a non-steroidal anti-inflammatory agent or a salt thereof and 0.2-50 parts by weight, based on 1 part by weight of the former, of salicylic acid and/or an alkali metal salicylate as an activating agent [Japanese Patent Application Kokai (Laid-Open) No. 82715/1976). Further, it was proposed to include Indometacin, a non-steroidal anti-inflammatory agent in a biodegradable carrier selected from collagen and gelatin (Japanese Patent Application Kokai (Laid-Open) No. 84213/1985), or to include Indometacin in cyclodextrin to enable the sustained release of Indometacin (Japanese Patent Application Kokai (Laid-Open) Nos. 62313/1979 and 117018/1979). Furthermore, there was proposed in Japanese Patent Application Kokai (Laid-Open) No. 110334/1979 a method wherein Indometacin is mixed with a benzodiazepine compound to thereby reduce the administration amount of Indometacin and to inhibit the expression of its serious side effect.
Though these conventional methods are superior in sustained release of drug, they are poor in absorption of drug into human body, take a long time before the drug exhibits an anti-inflammatory action, and hardly show sufficient effects for the alleviation of the side effect of the drug to the digestive system.
There were also proposed pharmaceutical compositions using albumin as a carrier, such as a composite of a 5-fluorouracil derivative and albumin [Japanese Patent Application Kokai (Laid-Open) No. 151988/1979) and a drug-albumin composite of sustained release type (Japanese Patent Application Kokai (Laid-Open) No. 162595/1983). These pharmaceutical compositions using albumin as a carrier described in the above patent documents, however, have drawbacks in that in their preparation, the binding property of the carrier albumin must be improved in advance at a pH of 6-11 at a temperature of 30.degree. C. or below using a cyanogen halide or a perhalogenic acid, or the affinity of the carrier albumin must be improved in advance using a spacer of a functional compound or the like, thus requiring many preparation steps and making the preparation procedure complex.
The present invention has been made in order to solve the above-mentioned problems of prior arts. The first object of the present invention is to provide a pharmaceutical composition which can alleviate the side effect of the drug contained therein to the skin and mucous membrane, particularly the digestive system and can improve the absorption, light stability, etc. of the drug. The second object of the present invention is to provide a process which can produce a pharmaceutical composition having the above advantages according to a simple procedure.
DISCLOSURE OF THE INVENTION
The present invention has been made in order to achieve the above objects. The present invention relates to a pharmaceutical composition of high drug content characterized by containing 1-200 parts by weight of a drug having a protein binding property and 100 parts by weight of album
REFERENCES:
patent: 3933996 (1976-01-01), Charlton
patent: 4578391 (1986-03-01), Kawata et al.
patent: 4702918 (1987-10-01), Ushimaru et al.
Asano et al., Kokai publication, No. 57-106610, 7/2/82.
Freedman; J. Kokai Pat. No. Sho 62(1987)-207217.
Fujoka et al., 61-236729 (A), JP.
Kuwayama et al., 57-108020 JP.
Kikazawa et al., 57-26615 JP.
Kaetsu et al., 56-115713 JP.
Koh Choon
Nippon Hypox Laboratories Incorporated
Schain Howard E.
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