Abstract：
:Using two UV-spectrophotometric methods, the hydrolysis of tinidazole was studied at pH 1.00-8.45 at 80 degrees C. The reaction followed apparent first-order kinetics throughout the studied range. No kinetic salt effect was detected, indicating that at least one of the reacting partners forming the transition state has a charge of 0. The reaction rate macro constants M(1)-M(4) were calculated to be 3.35 x 10(-2) M(-1) h(-1), 1.45 x 10(-2) h(-1), 3.76 x 10(-6) M h(-1), and 2.85 x 10(-11) M(2) h(-1), respectively. At pH >or= 7, the uncharged tinidazole was decomposed by the hydroxide ion; the reaction was found out to involve a proton transfer from the ethylsulfonylethyl side chain. At around pH 4.5, the degradation of the uncharged tinidazole was due to the solvent. In more acidic conditions, the reaction mechanism could not be fully resolved. The alkaline hydrolysis of metronidazole was studied on the basis of literature data. A general reaction mechanism was proposed, but an unequivocal explanation for the inflection point in the pH rate profile at pH 6 could not be found. The implications of the proposed reaction mechanism for the hydrolytic behavior of ornidazole were discussed.
journal_name
J Pharm Scijournal_title
Journal of pharmaceutical sciencesauthors
Salo JP,Yli-Kauhaluoma J,Salomies Hdoi
10.1002/jps.10349subject
Has Abstractpub_date
2003-04-01 00:00:00pages
739-46issue
4eissn
0022-3549issn
1520-6017pii
S0022-3549(16)31207-2journal_volume
92pub_type
杂志文章abstract：:There is a need to identify suitable blends of solvents to dissolve drugs. Empirical approaches, such as trial-and-error and response surface, require several solubility measurements. In this study the UNIFAC method was used to predict solubility in highly nonideal multicomponent systems in which only the solute entha...
journal_title：Journal of pharmaceutical sciences
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abstract：:Emodin, a natural anthraquinone polyphenol, has been reported to possess promising in vitro antioxidation, anticancer and anti-inflammatory activities. Whether the in vitro bioactivities can predict in vivo effects remained an unanswered question without understanding emodin pharmacokinetics in animals. To fill this b...
journal_title：Journal of pharmaceutical sciences
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doi：10.1002/jps.2600700818
更新日期：1981-08-01 00:00:00
abstract：:Recent oxidation events on monoclonal antibody candidates prompted us to investigate the mechanism of oxidation of Met, Trp, and His residues and to search for suitable stabilizers. By using parathyroid hormone (1-34), PTH, as a model protein and various oxidants, aided by liquid chromatography, peptide mapping, and m...
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更新日期：2011-10-01 00:00:00
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journal_title：Journal of pharmaceutical sciences
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doi：10.1002/jps.2600670643
更新日期：1978-06-01 00:00:00
abstract：:The rapid hydrolysis of epoprostenol to 6-keto-prostaglandin F1 alpha is hydronium ion-catalyzed even at pH 10 or higher. In the presence of 1.0% hexadecyltrimethylammonium chloride, the rate was reduced significantly (1580-fold at pH 2 and 283-fold at a physiological pH). This decrease in the hydrolysis rate is attri...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600710420
更新日期：1982-04-01 00:00:00
abstract：:Two multisample laboratory powder diffractometers have been evaluated for the purpose of pattern indexing in the context of physical form screening. Both diffractometers utilise foil transmission geometry, primary monochromated radiation, and a position-sensitive detector. Data collected from six compounds (sotalol hy...
journal_title：Journal of pharmaceutical sciences
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doi：10.1002/jps.10459
更新日期：2003-09-01 00:00:00
abstract：:A GLC assay to quantitate the methaqualone metabolite 2-methyl-3-(2-hydroxymethylphenyl)-4(3H)-quinazolinone was developed. Standard curves were linear, and recovery of the metabolite from tissue homogenates averaged 89%. In vitro metabolism of methaqualone by the 10,000Xg supernatant fraction of rat liver homogenate ...
journal_title：Journal of pharmaceutical sciences
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doi：10.1002/jps.2600671114
更新日期：1978-11-01 00:00:00
abstract：:The objectives of this work are to explore the pi-pi complexation of amitriptyline with pi electron-deficient aromatic rings and demonstrate the feasibility of pi-pi complexation for overdosed drug detoxification. Water-soluble oligochitosan was chemically modified with dinitrobenzenesulfonyl groups to induce selectiv...
journal_title：Journal of pharmaceutical sciences
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doi：10.1002/jps.20256
更新日期：2005-02-01 00:00:00
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journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600650629
更新日期：1976-06-01 00:00:00
abstract：:An important part of pharmacokinetic research is fitting models to observed data and estimating the parameters in the model. In general, parameter estimation in pharmacokinetics is a subset of the general problem of nonlinear regression or parameter estimation in nonlinear regression models. The same criteria, algorit...
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doi：10.1002/jps.2600760716
更新日期：1987-07-01 00:00:00
abstract：:Tuberculosis (TB) is a serious infectious disease that affects more than new 10 million patients each year. Many of these cases are resistant to first-line drugs so second-line ones, like fluoroquinolones, need to be incorporated into the therapeutic. Ofloxacin (OF) is a fluoroquinolone which demonstrates high antibio...
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journal_title：Journal of pharmaceutical sciences
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doi：
更新日期：1999-10-01 00:00:00
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journal_title：Journal of pharmaceutical sciences
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doi：10.1021/js950456s
更新日期：1996-08-01 00:00:00
abstract：:Sucrose is a common cryoprotectant and lyoprotectant to stabilize labile biopharmaceuticals during freeze-drying and storage. Sucrose-based formulations require low primary drying temperatures to avoid collapse and monoclonal antibody (mAb) containing products need to be stored refrigerated. The objective of this stud...
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journal_title：Journal of pharmaceutical sciences
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doi：10.1002/jps.24412
更新日期：2015-05-01 00:00:00
abstract：:Alkyl 2-imidazolyl disulfide compounds are novel antitumor agents, one of which is currently being evaluated in Phase I clinical trials. These molecules contain an unsymmetrical disulfide fragment, the lipophilic and electronic contributions of which are still not defined in the literature. Lipophilicity, ionization, ...
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更新日期：2005-04-01 00:00:00
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更新日期：2019-08-01 00:00:00
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journal_title：Journal of pharmaceutical sciences
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doi：10.1002/jps.20863
更新日期：2007-09-01 00:00:00
abstract：:Carboxy group-terminated synthetic polymers--branched poly(ethylene glycol), poly(acryloylmorpholine), and poly(vinylpyrrolidone)--were made amphiphilic by derivatization with phosphatidyl ethanolamine via the terminal carboxy group and then incorporated into lecithin-cholesterol liposomes prepared by the detergent di...
journal_title：Journal of pharmaceutical sciences
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更新日期：1995-09-01 00:00:00
