Abstract:
:Hydrolytic degradation products of cefdinir were studied in acidic (pH 1), neutral (pH 6), and basic (pH 9) solutions. Seven major degradation products were isolated by preparative and/or high-performance liquid chromatography and characterized by UV, IR, 1H-NMR, and mass spectra. To clarify degradation pathways in each pH solution, kinetic and product analyses during hydrolysis of cefdinir were carried out along with the followup reaction of representative degradation products. Cefdinir was shown to degrade via two major degradation routes: beta-lactam ring-opening and pH-dependent isomerizations (lactonization, epimerization at C-6 or C-7, syn-anti isomerization of N-oxime function).
journal_name
J Pharm Scijournal_title
Journal of pharmaceutical sciencesauthors
Okamoto Y,Kiriyama K,Namiki Y,Matsushita J,Fujioka M,Yasuda Tdoi
10.1021/js950446rsubject
Has Abstractpub_date
1996-09-01 00:00:00pages
976-83issue
9eissn
0022-3549issn
1520-6017pii
S0022-3549(15)50134-2journal_volume
85pub_type
杂志文章abstract::Oxidation of 7,8-dimethoxy-1,2,3,4-tetrahydroisoquinoline with potassium permanganate in acetone afforded 7,8-dimethoxy-3,4-dihydroisoquinoline as the primary product. Hence, oxidation of the appropriate secondary nonphenolic 7,8-dioxygenated tetrahydroisoquinoline alkaloid is thus a facile method for the generation o...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600731137
更新日期:1984-11-01 00:00:00
abstract::Topical lidocaine has been recently marketed as a new treatment for post-herpetic neuralgia. The aim of our study was to characterize the absorption profile of and systemic exposure to lidocaine from patch and gel formulations in normal volunteers, patients with post-herpetic neuralgia, and patients with acute herpes ...
journal_title:Journal of pharmaceutical sciences
pub_type: 临床试验,杂志文章
doi:10.1002/jps.10133
更新日期:2002-05-01 00:00:00
abstract::A series of 3-substituted indeno[1,2-c]pyrazol-4(1H)-one-2-acetic acids (3a-e) and 3-substituted indeno[1,2-c]pyrazol-4(1H)-one-1-acetic acids (4a-e) were synthesized as semirigid analogues of tolmetin (1). These compounds were evaluated for their anti-inflammatory action by investigating their ability to block arachi...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600780417
更新日期:1989-04-01 00:00:00
abstract::A rapid, simple, and accurate high-performance liquid chromatographic procedure using an amino-bonded microparticulate column is reported for the determination of chlorpromazine hydrochloride (I) and its two oxidation products, the sulfoxide (II) and the sulfone (III), in commercially available pharmaceutical dosage p...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600690217
更新日期:1980-02-01 00:00:00
abstract::Adsorption of proteins to solid-fluid interfaces is often empirically found to promote formation of soluble aggregates and larger, subvisible, and visible particles, but key stages in this process are often difficult to probe directly. Aggregation mediated by adsorption to water-silicon oxide (SiOx) interfaces, akin t...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.24429
更新日期:2015-06-01 00:00:00
abstract::The present work describes the development of a novel formulation of amorphous agomelatine (AGM) that exhibits enhanced in vitro dissolution rate and bioavailability, as well as improved storage stability. AGM was loaded on a mixture of microcrystalline cellulose with a high specific surface area excipient, namely col...
journal_title:Journal of pharmaceutical sciences
pub_type: 临床试验,杂志文章,随机对照试验
doi:10.1016/j.xphs.2017.09.017
更新日期:2018-01-01 00:00:00
abstract::Exposure of 4-methoxy-2-(3-phenyl-2-propynyl)phenol (CO/1828) to air and light (accelerated by temperature) yields 1-(2-hydroxy-5- methoxyphenyl)-3-phenylpropynone as the major degradation product. With extraction, this product rapidly degrades to 5-methoxyaurone and 6-methoxyflavone. In addition, a mixture of dimeric...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600810818
更新日期:1992-08-01 00:00:00
abstract::The chemical shifts of the methyl groups of 2,4-dimethylbenzo[g]quinoline are defined with respect to concentration, showing that the methyl resonances are reversed from their expected positions in concentrations normally used in NMR spectroscopy. The phenomenon is explained in terms of the probably "fixation" of bond...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600660839
更新日期:1977-08-01 00:00:00
abstract::The adsorption of quinidine onto kaolin was studied as a function of pH in aqueous solutions in which the ionic strength was adjusted to 0.1. The interaction of quinidine with pectin also was investigated in water and in phosphate buffer; the buffer pH and ionic strength were adjusted to 6.5 and 0.1, respectively. The...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600700907
更新日期:1981-09-01 00:00:00
abstract::The pharmaceutical preparation, chromatography, and biological distribution of a series of new chemical analogs of palmitic acid and diethylenetriaminepentaacetic acid, ethylenediaminetetraacetic acid, or diethylenetriamine are described. The biological distribution in rabbits 30 min after intravenous administration o...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600660223
更新日期:1977-02-01 00:00:00
abstract::(13)C labeling was used to enhance the sensitivity of (13)C solid-state NMR to study the effect of tabletting on the polymorphism of a steroidal drug. The steroidal drug Org OD 14 was (13)C labeled and formulated into tablets containing only 0.5-2.5% active ingredient. The tablets were subsequently studied by solid-st...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.20236
更新日期:2005-02-01 00:00:00
abstract::Anthralin and its decomposition products were separated by both column chromatographic and TLC techniques. Two decomposition products were characterized by TLC, melting-point data, and UV and IR spectroscopy. Pure anthralin and its decomposition products also were determined quantitatively. ...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600680340
更新日期:1979-03-01 00:00:00
abstract::The objective of this study was to generate a water-soluble thiolated chitosan to enable the permeation-enhancing effect of chitosan at pH of at least 5.5 without losing the advantages of improved mucoadhesive properties. Therefore, the thiol-bearing polyoxyethylene ligand {O-(3-carboxylpropyl)-O'-[2-[3-mercaptopropio...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.23832
更新日期:2014-02-01 00:00:00
abstract::This study reports, for the first time, development of tyrosine kinase inhibitor-loaded, thermosensitive liposomes (TKI/TSLs) and their efficacy for treatment of renal cell carcinoma when triggered by focused ultrasound (FUS). Uptake of these nanoparticles into renal cancer cells was visualized with confocal and fluor...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1016/j.xphs.2017.01.027
更新日期:2017-05-01 00:00:00
abstract::A method is presented for determining the equilibrium solubility of a drug in a solid polymer at or near room temperature, which represents a typical storage temperature. The method is based on a thermodynamic model to calculate the Gibbs energy change ΔG(SS) associated with forming a binary drug-polymer solid solutio...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.23319
更新日期:2012-12-01 00:00:00
abstract::A model is presented for transdermal drug delivery from single-layered silicone matrix systems. The work is based on our previous results that, in particular, extend the well-known Higuchi model. Recently, we have introduced a numerical transient model describing matrix systems where the drug dissolution can be non-in...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.24052
更新日期:2014-08-01 00:00:00
abstract::The in vitro uptake study was performed using the isolated cells of human oral mucosa, buccal and the dorsum of the tongue, to investigate the mechanisms of glucose uptake. The uptake of D-glucose was much larger in cells of the dorsum of the tongue than in buccal cells and was inhibited more extensively by 2-deoxy-D-...
journal_title:Journal of pharmaceutical sciences
pub_type: 临床试验,杂志文章
doi:10.1021/js980298f
更新日期:1999-08-01 00:00:00
abstract::Lipids were extracted from human stratum corneum and the remaining corneocytes were reaggregated with different lyotropic liquid crystals. Water transport through the reaggregated stratum corneum was determined using a diffusion chamber according to Smith and Blank. The permeability constant for the reaggregated strat...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600800506
更新日期:1991-05-01 00:00:00
abstract::This investigation was designed to quantitate and compare in the rat the oral absorption characteristics of micronized griseofulvin from a corn oil-in-water emulsion dosage form containing suspended drug and a control aqueous suspension after single-dose (50 mg/kg) and multiple-dose (50 mg/kg every 12 hr for five dose...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600640910
更新日期:1975-09-01 00:00:00
abstract::After intravenous administration of MK-826, a new carbapenem antibiotic, the compound exhibited nonlinear pharmacokinetics in rats and monkeys. In both species, time-averaged plasma clearance (based on total concentrations) increased about 5-fold over the 10- to 180-mg/kg dose range. MK-826 was extensively plasma prot...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1021/js980232k
更新日期:1999-02-01 00:00:00
abstract::Nonionic block copolymers are surfactants synthesized using propylene oxide and ethylene oxide, and they can be designed so that individual copolymers have unique vaccine adjuvant properties. We have designed and produced nonionic block copolymers based on high molecular weight (MW), 9-15 kDA, cores of poly(oxypropyle...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1021/js980072c
更新日期:1998-11-01 00:00:00
abstract::The critical micellar concentration (cmc) values of some mixed systems containing two bile salts were determined by a maximum pressure bubble method and compared with those derived from a theoretical model developed for nonionic surfactants to assess the applicability of this model to such systems. Some assumptions on...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600840514
更新日期:1995-05-01 00:00:00
abstract::The objective of this study was to examine the ocular absorption behavior of an amphiphilic prodrug after instillation onto the cornea of rabbits. A micellar solution of O-palmitoyl tilisolol (PalTL), an amphiphilic prodrug, was prepared. After instillation of tilisolol (TL) and PalTL, the drug concentrations in the t...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.1162
更新日期:2001-12-01 00:00:00
abstract::Samples of ethacrynic acid were treated with methanol-hydrochloric acid or with diazomethane. GLC and mass spectrometric analysis indicated that the methanol-hydrochloric acid reaction gave the expected methyl ester, whereas diazomethane treatment gave a compound containing an additional 14 mass units. Accurate mass m...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600670728
更新日期:1978-07-01 00:00:00
abstract::To characterize and evaluate human serum albumin-encapsulated nanoparticles for drug delivery of a tyrosine kinase inhibitor combined with induction of photothermal ablation combination therapy of renal cell carcinoma (RCC), nanoparticles of varying preparations and concentrations were characterized via zeta potential...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1016/j.xphs.2015.11.017
更新日期:2016-01-01 00:00:00
abstract::We have used rheological and thermal methods to study the colloidal characteristics of a widely used technical latex. The dispersions of poly(methacrylic acid-ethyl acrylate) (Eudragit L100-55) were found to be stabilized by a combination of electrostatic and steric mechanisms termed as electrosteric stabilization. Th...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1021/js9803555
更新日期:1999-04-01 00:00:00
abstract::A new quantitative GLC method for analysis of lidamidine hydrochloride (I) was developed. The method was based on derivatization of I to 1-(2,6-dimethylphenyl)-4-methylamino-dihydro-1,3,5-triazin-2-one (II) using dimethylformamide dimethylacetal reagent. Compound II was synthesized and characterized by IR, NMR, mass s...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600710327
更新日期:1982-03-01 00:00:00
abstract::The potential binding interaction(s) of the anti-thyroid drug methimazole (MMZ) with the protein bovine serum albumin (BSA) has been studied using isothermal titration calorimetry (ITC) and UV-Visible, fluorescence and circular dichroism (CD) spectroscopic techniques. The binding of MMZ to BSA has been studied in both...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.21140
更新日期:2008-06-01 00:00:00
abstract::Both nonequilibrium and equilibrium models were proposed to explain the optimal biological response to a set of congeners with respect to the oil-water partition coefficient (P). A detailed analysis of the kinetic model proposed by Hansch demonstrates the bilinear form of the model, with the initial slope of the logar...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600700110
更新日期:1981-01-01 00:00:00
abstract::The viscosity and surface tension of systems containing small amounts of salicylic acid in aqueous solutions of cetrimide were determined. An abrupt increase in viscosity was observed, and the molar ratio of salicylic acid to certrimide at which this viscosity increase occurred was 1:2. The surface tension of these sy...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600661236
更新日期:1977-12-01 00:00:00