Journal of pharmaceutical sciences.
Publisher:
American Pharmaceutical Assn.. New York, NY : Elsevier (2016)
Frequency: Monthly
Country: United States
Language: English
Author(s):
American Pharmaceutical Association., American Pharmacists Association., Fédération internationale pharmaceutique., American Association of Pharmaceutical Scientists.
Start Year:1961 -
ISSN:
0022-3549 (Print)
1520-6017 (Electronic)
0022-3549 (Linking)
1520-6017 (Electronic)
0022-3549 (Linking)
Impact Factor
3.8
2022
| NLM ID: | 341145 |
| (DNLM): | J34360000(s) |
| (OCoLC): | 01754726 |
| Coden: | JPMSAE |
| LCCN: | 13021725 |
| Classification: | W1 JO829 |
Diclofenac Prodrugs for Intra-articular Depot Injectables: In Vitro Hydrolysis and Species Variation. Intra-articular depot injectables based on in situ suspension formation of ester prodrugs of nonsteroidal anti-inflammatory drugs are promising for management of joint pain. As candidates for this delivery approach, 5 diclofenac ester prodrugs comprising different imidazole-containing promoieties were synthesized and their physicochemical properties characterized. In vitro hydrolysis rates were investigated in buffer solutions, in 40% (v/v) human, equine, canine, and rat plasma, and in 80% (v/v) human and equine synovial fluid. Bioconversion of the prodrugs to diclofenac was found to be enzym...
Few Drugs Display Flip-Flop Pharmacokinetics and These Are Primarily Associated with Classes 3 and 4 of the BDDCS. This study was conducted to determine the number of drugs exhibiting flip-flop pharmacokinetics following oral (p.o.) dosing from immediate-release dosage forms and if they exhibit a common characteristic that may be predicted based on BDDCS classification. The literature was searched for drugs displaying flip-flop kinetics (i.e., absorption half-life larger than elimination half-life) in mammals in PubMed, via internet search engines and reviewing drug pharmacokinetic data. Twenty two drugs were identified as displaying flip-flop kinetics in humans (13 drugs), rat (nine drugs), monkey (three ...
In vitro and in vivo characteristics of celecoxib in situ formed suspensions for intra-articular administration. The objective of the present study was to explore the potential of using an in situ suspension forming drug delivery system of celecoxib to provide sustained drug exposure in the joint cavity following intra-articular administration. In vitro, precipitates were formed upon addition of a 400 mg/mL solution of celecoxib in polyethylene glycol 400 (PEG 400) to phosphate buffer, pH 7.4, or synovial fluid. The in vitro release profiles of the in situ formed suspensions were characterized by an initial fast release followed by a slower constant flux. In buffer solutions, these fluxes were comparable...
Identification of metabolites of azaperone in horse urine. Two metabolites of the tranquilizer azaperone were extracted from alkalinized horse urine after treatment with beta-glucuronidase/sulfatase from limpets (Patella vulgata). The metabolites were identified by a combination of independent chemical synthesis and GC/MS and 1H NMR analysis. The metabolites were identified as 1-(fluorophenyl)-4-[4-(5-hydroxy-2-pyridinyl)-1-piperazinyl]-1-butanol, designated as 5'-hydroxy-azaperol, and 1-(fluorophenyl)-4-[4-(5-hydroxy-2-pyridinyl)-1-piperazinyl]-1-butanone, designated as 5'-hydroxyazaperone. A TLC screening test was developed for detecting both metabo...
Species scaling of propafenone disposition and concentration–time relationships among eight mammalian species. Usually, smaller mammals have higher clearances per unit body mass than do larger mammalian species. When clearance and other pharmacokinetic parameters are correlated with internal physiological processes, species tend to dispose of drugs at a similar pace. The first application of this concept is pharmacokinetic time, expressed with different units: Kallynochron, Apolysichron, Dienetichron, and Syndesichron. The present work describes pharmacokinetic time in these units from data obtained with propafenone in eight animal species: mouse, rat, rabbit, dog, sheep, human, cow, and horse. Additio...
Prednisolone binding to plasma proteins in domestic species. The binding of prednisolone to total plasma proteins of dogs, horses, cows, and sheep was characterized using equilibrium dialysis. Prednisolone was bound to a first protein with high affinity but low capacity (transcortin) and to a second protein according to a nonsaturable mechanism (albumin). Interspecies differences were observed, with cows and dogs exhibiting the lowest, and sheep and horses the highest specific binding capacities. The results are in good agreement with known pharmacokinetic properties of prednisolone in domestic species.
In vitro evaluation of a sustained-release veterinary peroral pellet preparation. In a preceding in vivo study in horses, wide interindividual variation was found in the extent of bioavailability and time to reach peak concentration after peroral administration of one specific theophylline sustained-release dosage form. The purpose of the present study was to investigate the factors of potency, the pH of dissolution medium, the enzymes in the dissolution medium, and the crushing of the pellets on in vitro performance. The results show a wide variation in potency for the individual units, an increase in release rate with increasing pH, and an increase in release rate if the ...
Radioimmunoassay of oxfendazole in bovine, equine, or canine plasma or serum. A simple radioimmunoassay was developed for the determination of oxfendazole in plasma. Oxfendazole N-1(3)-valerate was coupled to polylysine via a carbodiimide reaction, and antiserum was developed in rabbits after inoculation with oxfendazole--polylysine conjugate. The assay was developed so that oxfendazole could be measured directly in a 0.1-ml aliquot of diluted or undiluted plasma. With the developed procedure, 200 pg of oxfendazole/ml of plasma can be determined quantitatively. Cross-reactivity was determined for closely related compounds and metabolites. The method was used to determin...