Organic compounds -- part of the class 532-570 series – Organic compounds – Carbohydrates or derivatives
Patent
1995-06-06
1997-03-04
Kight, John
Organic compounds -- part of the class 532-570 series
Organic compounds
Carbohydrates or derivatives
5361231, 514 58, 540349, C08B 3716, A61K 31715, C07D48708
Patent
active
056080522
ABSTRACT:
Described is a new process for the preparation of alkali clavulanate from an aqueous solution of crude clavulanic acid, which is obtained in a conventional manner after the fermentation with a clavulanic-acid-producing microorganism, extracted with an ethyl acetate solution of a hydrophobic .beta.-cyclodextrin derivative such as heptakis-(2,3,6-tri-O-acetyl)-.beta.-cyclodextrin in at least equimolar ratio with regard to clavulanic acid. The resulting novel inclusion complexes of clavulanic acid and hydrophobic .beta.-cyclodextrin derivative in a molar ratio about 1:1 are isolated, purified and then converted with an alkali base or alkali alkanoate to the desired alkali clavulanate, which is isolated. Furthermore, there are described new inclusion complexes of clavulanic acid and of its pharmaceutically acceptable alkali salts both with hydrophilic .beta.-cyclodextrin derivatives and with hydrophobic .beta.-cyclodextrin derivatives, processes for the preparation thereof and the use thereof for the preparation of galenic forms with immediate as well as with sustained action, in combination with amoxicillin trihydrate, which are valuable medicaments in the therapy of infectious diseases.
REFERENCES:
patent: 4454069 (1984-06-01), Cook et al.
patent: 4525353 (1985-06-01), Cole et al.
patent: 4647659 (1987-03-01), Cook et al.
patent: 4869904 (1989-09-01), Uekama et al.
patent: 5310898 (1994-05-01), Copar
Lenga, Robert, The Sigma-Aldrich Library of Chemical Safety Data, Edition 1, 1985, p. 310.
Bekers et al., Cyclodextrins in the Pharmaceutical Field, Drug Development and Industrial Pharmacy, vol. 17, No. 11 (1991) pp. 1503-1549.
Hedges, Allan, Minutes of the Sixty international Symposium on Cyclodextrins, Symposium organized by American Maize-Products Company (1992), pp. 1-8.
Matsubara et al., Possible Use of Triacetylated Cyclodextrins in the Preparation of Sustained-Release Oily Injection of LHRH Agonist, Buserelin Acetate, pp. 547-550, (1992).
Hendrickson et al., Organic Chemistry, 3rd Edition, (1970), pp. 98, 1156-1157.
Szejtli, Cyclodextrin Technology, Kluwer Academic Publishers (1988), pp. 48-65.
Yamamoto et al., Some physiochemical properties of branched .beta.-cyclodextrins and their inclusion characteristics, International Journal of Pharmaceutics, vol. 49 (1989), pp. 163-171.
Catalogue Aldrich, USA, 1994, pp. 750, 790, 809, 941 and 1367.
A pamphlet by the producer of different CD derivatives Cyclolab R & D Laboratory, Budapest, Hungary, Jan. 1995.
Chemical Abstracts, The American Chemical Society, vol. 101, No. 21 (1984), p. 808.
Fer cej-Temeljotov Darja
Kotnik Sonja
Kova ci c Mateja
Verhnjak Katarina
Zmitek Janko
Kight John
Lek, Tovarna Farmacevtskih in Kemicnih
White Everett
LandOfFree
Inclusioin complexes of clavulanic acid and of alkali salts ther does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Inclusioin complexes of clavulanic acid and of alkali salts ther, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Inclusioin complexes of clavulanic acid and of alkali salts ther will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-2146995