Polar drug of prodrug compositions with extended shelf-life stor

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Carbohydrate doai

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Details

514169, 514385, 536103, A61K 31715, A61K 3156, A61K 31415

Patent

active

061332488

ABSTRACT:
The present invention is drawn to pharmaceutical composition comprising cyclodextrin and a pharmaceutically active agent or prodrug, wherein the cyclodextrin is present at less than 75% equimolar amounts of the above agent or prodrug. The present invention is further drawn to a method of extending the shelf-life of a pharmaceutically active agent or prodrug by adding one or more cyclodextrins a less than 75% equimolar amounts to said pharmaceutically active agent or prodrug.

REFERENCES:
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patent: 5134127 (1992-07-01), Stella et al.
patent: 5324718 (1994-06-01), Loftsson
patent: 5376645 (1994-12-01), Stella et al.
Rajewski et al. "Preliminary Safety Evaluation f Parenterally Administered Sulfoalkyl Ether beta-Cyclodextrin Derivatives", Journal of Pharmaceutical Sciences, vol. 84(8): 927-932, Aug. 1995.
Kazuto Okimoto et al. "The Interaction of Charged and Uncharged Drugs with Neutral (HP-B-CD) and Anionically Charged (SBE7-B-CD) B-Cyclodextrins", Pharmaceutical Research, vol. 13, No. 2 (1996) pp. 256-264.
Thorsteinn Loftsson et al. "Pharmaceutical Applications of Cyclodextrins. 1. Drug Solubilization and Stabilization", Journal of Pharmaceutical Sciences, vol..85, No. 10 (Oct. 1996) pp. 1017-1025.
S.A. Varia et al. "Phenytoin Prodrugs IV: Hydrolysis of Various 3-(Hydroxymethyl) phenytoin Esters", Journal of Pharmaceutical Sciences, vol. 73, No. 8 (Aug. 1984) pp. 1074-1080.
Loftsson et al., "Effects of cyclodextrins on the chemical stability of drugs in aqueous solutions", Drug Stability, vol. 1, No. 1 (1995) pp. 22-33.
Menard et al., "Studies of the Effect of pH, Temperature and Ring Size on the Complexation of Phenytoin with Cyclodextrins", Pharmaceutica Acta Helvetiae, vol. 63, No. 11 (1988) pp. 303-308.
Stella, "A case for prodrugs: Fosphenytoin", Advanced Drug Delivery Reviews, vol. 19, No. 2. (1996) pp. 311-330.
Muller et al., "Determination of the position of the ester bond in a micellar prodrug of phenytoin", International Journal of Pharmaceutics, vol. 102 (1994) pp. 109-116.

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