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Chemical & Pharmaceutical Bulletin Aug 2000Prednisolone 21-hemisuccinate/beta-cyclodextrin (beta-CyD) amide conjugate was prepared by binding prednisolone 21-hemisuccinate covalently to the amino group of...
Prednisolone 21-hemisuccinate/beta-cyclodextrin (beta-CyD) amide conjugate was prepared by binding prednisolone 21-hemisuccinate covalently to the amino group of mono(6-deoxy-6-amino)-beta-CyD through amide linkage. Prednisolone 21-hemisuccinate was intramolecularly transformed to prednisolone 17-hemisuccinate, and the parent drug, prednisolone, was slowly released from the 21-hemisuccinate with a half life of 69 h in pH 7.0 at 37 degrees C; the drug release at 25 degrees C was less than 10% for 48 h. In sharp contrast, the hydrolysis of prednisolone 21-hemisuccinate/beta-CyD amide conjugate was significantly faster (half life of 6.50 min at 25 degrees C) and gave prednisolone and mono(6-deoxy-6-succimino)-beta-CyD as products. The hydrolysis of the beta-CyD amide conjugate was subject to a specific-base catalysis in the alkaline region. The rapid hydrolysis of the conjugate can be ascribed to the involvement of an intramolecular nucleophilic catalysis of the amide group in the reaction. The succinic acid, bound to a drug through ester linkage at one carboxylic group and bound to a pro-moiety through amide linkage at another carboxylic group, may be useful as a spacer for construction of the immediate release type prodrugs of CyDs.
Topics: Amides; Catalysis; Cyclodextrins; Half-Life; Hydrogen-Ion Concentration; Hydrolysis; Kinetics; Prednisolone; beta-Cyclodextrins
PubMed: 10959575
DOI: 10.1248/cpb.48.1125 -
Fortschritte Der Medizin Sep 1982The prednisolone sparing effect of benoxaprofen has been examined in only 13 cases of rheumatoid arthritis. The examination was terminated prematurely because of an...
The prednisolone sparing effect of benoxaprofen has been examined in only 13 cases of rheumatoid arthritis. The examination was terminated prematurely because of an accumulation of side effects of the skin. The results of these 13 cases are not significant, but the drug seems to show a relatively high mean value of its prednisolone sparing effect but it seems to cause a high proportion of side effects, especially of the skin. This preliminary result should be reported in regard to possibly following studies with simular observations.
Topics: Anti-Inflammatory Agents; Arthritis, Rheumatoid; Dose-Response Relationship, Drug; Drug Therapy, Combination; Humans; Prednisolone; Propionates
PubMed: 7129310
DOI: No ID Found -
Deutsche Medizinische Wochenschrift... Nov 2014
Topics: Female; Glucocorticoids; Humans; Immunotherapy; Male; Mycobacterium; Pericarditis, Tuberculous; Prednisolone
PubMed: 25409398
DOI: 10.1055/s-0033-1353927 -
Arztliche Forschung Jul 1958
Topics: Humans; Internal Medicine; Prednisolone
PubMed: 13559057
DOI: No ID Found -
Journal of the American Medical... Nov 1958
Topics: Methylprednisolone; Prednisolone
PubMed: 13587198
DOI: 10.1001/jama.1958.03000090038008 -
Acta Crystallographica. Section C,... Jun 2017Prednisolone acetate {systematic name:...
Prednisolone acetate {systematic name: 2-[(8S,9S,10R,13S,14S,17R)-11,17-dihydroxy-10,13-dimethyl-3-oxo-6,7,8,9,10,11,12,13,14,15,16,17-dodecahydro-3H-cyclopenta[a]phenanthren-17-yl]-2-oxoethyl acetate}, is an ophthalmic drug that belongs to the class of corticosteroids. Its crystal structure was refined using the classical independent atom model (IAM) and a transferred multipolar atom model using the ELMAM2 database. The results of both refinements have been compared. The ELMAM2 refinement was found to be superior in terms of the refinement statistics. It has been shown that certain electron-density-derived properties can be calculated on the basis of the transferred parameters for crystals which diffract to ordinary resolution. The procedure proves helpful in understanding the mode of action of the drug molecule.
Topics: Anti-Inflammatory Agents; Crystallography, X-Ray; Hydrogen Bonding; Models, Chemical; Models, Molecular; Molecular Structure; Prednisolone; Static Electricity
PubMed: 28579562
DOI: 10.1107/S2053229617006556 -
Metabolism: Clinical and Experimental Jul 1958
Topics: Methylprednisolone; Prednisolone; Treatment Outcome
PubMed: 13565402
DOI: No ID Found -
Die Pharmazie Nov 1990A method for the quantitative determination of prednisolone in ointment preparations is described. It uses TLC and UV spectrophotometry in combination. Solutions and...
A method for the quantitative determination of prednisolone in ointment preparations is described. It uses TLC and UV spectrophotometry in combination. Solutions and ointments are chromatographed using silica gel GF 254 and various solvent systems, the layers containing the active ingredient are eluted and the substance determined at 240 nm.
Topics: Chromatography, Thin Layer; Gels; Ointments; Prednisolone; Solvents; Spectrophotometry, Ultraviolet
PubMed: 2100341
DOI: No ID Found -
Arzneimittel-Forschung Feb 1987Plasma levels of prednisolone and prednisolone hemisuccinate of volunteers were measured with HPLC following i.v. injections of 1200 and 75 mg of prednisolone, given as...
Plasma levels of prednisolone and prednisolone hemisuccinate of volunteers were measured with HPLC following i.v. injections of 1200 and 75 mg of prednisolone, given as the water-soluble hemisuccinate ester. The hemisuccinate ester is hydrolyzed relatively quickly with a plasma half-life between 18 and 25 min, and the resulting prednisolone has a plasma half-life of 3.5-3.7 h. The dose dependency of the pharmacokinetic parameters indicates a partial saturation of the metabolizing enzymes as consequence of the application of the high dose of prednisolone. In saliva no hemisuccinate could be detected. The prednisolone saliva concentration corresponds with those of non-protein-bound prednisolone in plasma measured at the same time. Only minor quantities of intact ester (1-8%) or intact prednisolone (2-4%) are excreted in urine. Following the application of 1200 mg prednisolone the endogenous cortisol level is partially suppressed only 24 h after the i.v. injection; 48 h later the difference from the basis value is not statistically significant. Leukocytosis and granulocytosis are at maximum 24 h after the injection of the high dose, and after 48 h normal values are observed. Lymphocytes and monocytes fall below normal levels for a longer time after 1200 mg compared to 75 mg, the minimum is between 4 and 8 h. Glucose levels are enhanced dose-dependently. They are normalized even after the extremely high dose at 24 h. Sodium, potassium, calcium, plasma proteins, urea, creatinine, hematocrit and hemoglobin showed no significant differences within 48 h following the injections.
Topics: Adult; Biotransformation; Blood Glucose; Dose-Response Relationship, Drug; Electrolytes; Female; Humans; Hydrocortisone; Injections, Intravenous; Kinetics; Leukocyte Count; Male; Prednisolone; Saliva
PubMed: 3580023
DOI: No ID Found -
The British Journal of Dermatology Oct 1990
Clinical Trial Randomized Controlled Trial
Topics: Administration, Oral; Double-Blind Method; Humans; Lichen Planus; Prednisolone
PubMed: 2095191
DOI: 10.1111/j.1365-2133.1990.tb01468.x