scholarly journals Hydrogel medicinal systems of prolonged action

2007 ◽  
pp. 118-122 ◽  
Author(s):  
Yu. Samchenko ◽  
Z. Ulberg ◽  
N. Pertsov
Keyword(s):  
Prolonged Action

METABOLISM OF 17α-HYDROXYPROGESTERONE-4-14C-17α-CAPROATE BY HOMOGENATES OF RAT LIVER AND HUMAN PLACENTA

1961 ◽  
Vol 36 (4) ◽  
pp. 511-519 ◽  
Author(s):  
Margaret Wiener ◽  
Charles I. Lupa ◽  
E. Jürgen Plotz
Keyword(s):  
Rat Liver ◽  
Human Placenta ◽  
Steric Hindrance ◽  
Placental Tissue ◽  
Caproic Acid ◽  
Major Product ◽  
Side Chain ◽  
Anaerobic Conditions ◽  
Prolonged Action ◽  
Long Acting

ABSTRACT 17α-hydroxyprogesterone-4-14C-17α-caproate (HPC), a long-acting progestational agent, was incubated with homogenates of rat liver and human placenta. The rat liver was found to reduce Ring A of HPC under anaerobic conditions to form allopregnane-3β,17α-diol-20-one-17α-caproate and pregnane-3β,17α-diol-20-one-17α-caproate, the allopregnane isomer being the major product. The caproic acid ester was neither removed nor altered during the incubation. Placental tissue did not attack HPC under conditions where the 20-ketone of progesterone was reduced. It is postulated that this absence of attack on the side chain is due to steric hindrance from the caproate ester, and that this may account for the prolonged action of HPC.

Evaluation of the effectiveness of the drug prolonged action Lipomaс 2% for helminthosis of small cattle

2020 ◽  
Vol 23 (05) ◽  
pp. 35-37
Author(s):  
K.F. Fatakhov ◽  
◽  
D.A. Devrishov ◽  
O.B. Litvinov ◽  
A.D. Devrishov ◽  
...  
Keyword(s):  
Prolonged Action

BIOPOLYMER PRESOWING TREATMENT OF SEEDS ENSURING THE PROLONGED ACTION

2018 ◽  
Vol 0 (4) ◽  
pp. 90-94
Author(s):  
S.P. Chetverikov ◽  
◽  
R.K. Bikkuzina ◽  
D.V. Chetverikova ◽  
◽  
...  
Keyword(s):  
Prolonged Action ◽  
Presowing Treatment

Fluorinated tricyclic neuroleptics with prolonged action: 8-Methoxy, 8-ethoxy, 8-ethylthio and 8-hydroxy derivatives of 3-fluoro-10-(4-methylpiperazino)-10,11-dihydrodibenzo[b,f]thiepin

1982 ◽  
Vol 47 (5) ◽  
pp. 1382-1391 ◽  
Author(s):  
Jiří Jílek ◽  
Josef Pomykáček ◽  
Jiřina Metyšová ◽  
Miroslav Protiva
Keyword(s):  
Acetic Acid ◽  
Polyphosphoric Acid ◽  
Prolonged Action ◽  
Substitution Reactions ◽  
Methoxy Derivative ◽  
Chloro Derivatives ◽  
Boron Tribromide ◽  
Derivatives Of ◽  
Central Depressant ◽  
Boiling Toluene

Acids IIa-c were prepared by reactions of (4-fluoro-2-iodophenyl)acetic acid with 4-methoxythiophenol, 4-ethoxythiophenol and 4-(ethylthio)thiophenol and cyclized with polyphosphoric acid in boiling toluene to dibenzo[b,f]thiepin-10(11H)-ones IIIa-c. Reduction with sodium borohydride afforded the alcohols IVa-c which were treated with hydrogen chloride and gave the chloro derivatives Va-c. Substitution reactions with 1-methylpiperazine resulted in the title compounds Ia-c out of which the methoxy derivative Ia was transformed by demethylation with boron tribromide to the phenol Id. Compounds Ia-d are very potent neuroleptics exhibiting a clear prolongation of the central depressant and some prolongation of the cataleptic activity.

Quantitative relations between structure and antiinflammatory activity of aryloxoalkanoic acids

1988 ◽  
Vol 53 (8) ◽  
pp. 1862-1872 ◽  
Author(s):  
Miroslav Kuchař ◽  
Eva Maturová ◽  
Bohumila Brunová ◽  
Jaroslava Grimová ◽  
Hana Tomková ◽  
...  
Keyword(s):  
Regression Analysis ◽  
Structural Changes ◽  
Antiinflammatory Activity ◽  
Structural Parameters ◽  
Considerable Effect ◽  
Antiinflammatory Effect ◽  
Prolonged Action ◽  
Preclinical Development ◽  
Indicator Variables ◽  
Inhibitory Activities

The antiinflammatory effect of a series of aryloxoalkanoic acids II and of their biphenyl derivatives III was examined by measuring the inhibition of the development of carageenan- and adjuvant-induced edemas. The quantitative relations between the antiinflammatory effect and physicochemical and structural parameters of the compounds tested were evaluated. The equations obtained by the method of regression analysis showed a significant linear dependence of both inhibitory activities on the lipophilicity of the compounds and a considerable effect of some structural changes as expressed by indicator variables. The antiinflammatory effect is especially enhanced in both tests by the presence of a cyclic substituent at the aromatic ring. The high antiinflammatory effect of biphenylyl derivatives III is paralleled by their prolonged action. The prolongation of the effect is most likely a result of a suitable biotransformation of acid III to an efficient metabolite. The structural requirements which resulted from both the regression analysis and from the hypothesis of biotransformation of acids III were utilized in the synthesis of suitably substituted biphenylyloxoalkanoic acids. By this approach derivatives IIIe-i were obtained some of which showed a high antiinflammatory and also protracted effect. 4-(2',4'-Difluorbiphenylyl)-4-oxo-2-methylbutanoic acid (VÚFB-16 066, Flobufen) was chosen for further preclinical development.

Biological and chemical properties of two glucagon preparations with prolonged action

1969 ◽  
Vol 7 (2) ◽  
pp. 206-210 ◽  
Author(s):  
F. Trading ◽  
P. Nielsen ◽  
M. Pingel ◽  
Aa. Vølund
Keyword(s):  
Chemical Properties ◽  
Prolonged Action ◽  
And Chemical Properties

Trypsinolysis of Polyurethane Particles Based on Сyclodextrin with Encapsulated Moxifloxacin

2021 ◽  
Vol 37 (5) ◽  
pp. 72-79
Author(s):  
L.R. Yakupova ◽  
А.А. Skuredina ◽  
Е.V. Kudryashova
Keyword(s):  
Enzymatic Degradation ◽  
Dosage Forms ◽  
Oral Dosage ◽  
Hydrodynamic Diameter ◽  
Prolonged Action ◽  
Cyclodextrin Complexes ◽  
Acidic Media ◽  
Drug Molecules ◽  
Oral Dosage Forms ◽  
Average Hydrodynamic Diameter

Abstract-Moxifloxacin encapsulation in polymer cyclodextrin-based particles with an average hydrodynamic diameter of 150--200 nm has led to the formation of potential delivery systems with a degree of moxifloxacin inclusion of more than 80%. Cross-linking of the moxifloxacin-cyclodextrin complexes caused a pronounced slowdown in the release of the drug molecules in acidic media to less than 10% per day. In the presence of trypsin, the drug release was accelerated by 15--20% within 90 min. It was shown by Fourier-transform infrared spectroscopy that this acceleration was due to the partial enzymatic degradation of the urethane bonds of the polymer matrix near the surface of the particles. The results obtained are important for the development of highly effective oral dosage forms of prolonged action. Key words: fluoroquinolones, cyclodextrins, FTIR spectroscopy, trypsin

PHARMACODYNAMIC PROPERTIES OF PENICILLIN PREPARATIONS WITH PROLONGED ACTION

1948 ◽  
Vol 215 (5) ◽  
pp. 498-505
Author(s):  
N. Ercoli ◽  
W. C. Hueper ◽  
L. Landis ◽  
Mary M. Lewis ◽  
B. S. Schwartz
Keyword(s):  
Prolonged Action
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