Stable isotope coadministration methodology for the estimation of the fraction of imipramine metabolized to desipramine.


:The application of a stable isotope coadministration technique for estimating the fraction (fm) of imipramine (IP) that is converted to desipramine (DMI) is described. Four healthy male subjects received 25 mg of IP-d4 hydrochloride orally with 25 mg of DMI hydrochloride. The plasma concentrations of IP-d4, DMI-d4, and DMI were determined by capillary gas chromatography-mass spectrometry-selected ion monitoring using d8 analogues as internal standards. The fm values, calculated from the ratio of the area under the plasma concentration-time curve of DMI-d4 to that of DMI, varied from 0.54 to 0.85.


J Pharm Sci


Sasaki Y,Shinohara Y,Baba S




Has Abstract


1990-02-01 00:00:00














  • Increasing process understanding by analyzing complex interactions in experimental data.

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    journal_title:Journal of pharmaceutical sciences

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    authors: Naelapää K,Allesø M,Kristensen HG,Bro R,Rantanen J,Bertelsen P

    更新日期:2009-05-01 00:00:00

  • Characterization of the physical stability of a lyophilized IgG1 mAb after accelerated shipping-like stress.

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    journal_title:Journal of pharmaceutical sciences

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    authors: Telikepalli S,Kumru OS,Kim JH,Joshi SB,O'Berry KB,Blake-Haskins AW,Perkins MD,Middaugh CR,Volkin DB

    更新日期:2015-02-01 00:00:00

  • Reversible adsorption of nicotinic acid onto charcoal in vitro.

    abstract::The effects of various factors on the adsorption of nicotinic acid onto and desorption from activated charcoal were investigated in vitro. The affinity of nicotinic acid for charcoal was poor both in acidic and neutral media. Adsorption increased with increasing charcoal:drug ratios and decreasing incubation volume:ch...

    journal_title:Journal of pharmaceutical sciences

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    authors: Roivas L,Neuvonen PJ

    更新日期:1992-09-01 00:00:00

  • Effect of Water on the Chemical Stability of Amorphous Pharmaceuticals: 2. Deamidation of Peptides and Proteins.

    abstract::Role of water in chemical (in)stability is revisited, with focus on deamidation in freeze-dried amorphous proteins and peptides. Two distinct patterns for deamidation versus water have been reported, that is, a consistent increase in rate constant with water, and a "hockey stick"-type behavior. For the latter, deamida...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Ohtake S,Feng S,Shalaev E

    更新日期:2018-01-01 00:00:00

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    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Ballbach RL,Brown DJ,Walters SM

    更新日期:1977-11-01 00:00:00

  • Chemical modifications of therapeutic proteins induced by residual ethylene oxide.

    abstract::Ethylene oxide (EtO) is widely used in sterilization of drug product primary containers and medical devices. The impact of residual EtO on protein therapeutics is of significant interest in the biopharmaceutical industry. The potential for EtO to modify individual amino acids in proteins has been previously reported. ...

    journal_title:Journal of pharmaceutical sciences

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    authors: Chen L,Sloey C,Zhang Z,Bondarenko PV,Kim H,Ren D,Kanapuram S

    更新日期:2015-02-01 00:00:00

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    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Chang ZL,Papendick VE

    更新日期:1976-10-01 00:00:00

  • Stability of the Hsp90 inhibitor 17AAG hydroquinone and prevention of metal-catalyzed oxidation.

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    journal_title:Journal of pharmaceutical sciences

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    authors: Guo W,Siegel D,Ross D

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  • Effect of Freeze Dryer Design on Heat Transfer Variability Investigated Using a 3D Mathematical Model.

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    journal_title:Journal of pharmaceutical sciences

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    authors: Scutellà B,Bourlès E,Plana-Fattori A,Fonseca F,Flick D,Trelea IC,Passot S

    更新日期:2018-08-01 00:00:00

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    journal_title:Journal of pharmaceutical sciences

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    authors: Hickey AJ,Edwards DA

    更新日期:2018-03-01 00:00:00

  • Expression of Carboxylesterase Isozymes and Their Role in the Behavior of a Fexofenadine Prodrug in Rat Skin.

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    journal_title:Journal of pharmaceutical sciences

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    authors: Imai T,Ariyoshi S,Ohura K,Sawada T,Nakada Y

    更新日期:2016-02-01 00:00:00

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    journal_title:Journal of pharmaceutical sciences

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    authors: Amann AH

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  • Improving ultrasound reflectivity and stability of echogenic liposomal dispersions for use as targeted ultrasound contrast agents.

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    journal_title:Journal of pharmaceutical sciences

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  • Quantifying errors in tableting data analysis using the Ryshkewitch equation due to inaccurate true density.

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    journal_title:Journal of pharmaceutical sciences

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    authors: Sun CC

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  • The influence of hepatic transport on the distribution volumes and mean residence time of drug in the body and the accuracy of estimating these parameters by the traditional pharmacokinetic calculations.

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    journal_title:Journal of pharmaceutical sciences

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    authors: Berezhkovskiy LM

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  • Overall monotropic behavior of a metastable phase of biclotymol, 2,2'-methylenebis(4-chloro-3-methyl-isopropylphenol), inferred from experimental and topological construction of the related P-T state diagram.

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    journal_title:Journal of pharmaceutical sciences

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    authors: Céolin R,Tamarit JL,Barrio M,López DO,Nicolaï B,Veglio N,Perrin MA,Espeau P

    更新日期:2008-09-01 00:00:00

  • Bioavailability and efficacy of antisense morpholino oligomers targeted to c-myc and cytochrome P-450 3A2 following oral administration in rats.

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    journal_title:Journal of pharmaceutical sciences

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    authors: Arora V,Knapp DC,Reddy MT,Weller DD,Iversen PL

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  • Properties and stability of a liquid crystal form of cyclosporine-the first reported naturally occurring peptide that exists as a thermotropic liquid crystal.

    abstract::A new solid-state form of cyclosporine produced by spray-drying exhibited characteristics consistent with a liquid crystal. No sharp diffraction peaks were observed by powder X-ray diffraction; however, analysis by both small-angle X-ray diffraction (SAXR) and microscopic under polarized light (PLM) confirmed the exis...

    journal_title:Journal of pharmaceutical sciences

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    authors: Lechuga-Ballesteros D,Abdul-Fattah A,Stevenson CL,Bennett DB

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  • 3D Printing of Solid Oral Dosage Forms: Numerous Challenges With Unique Opportunities.

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    journal_title:Journal of pharmaceutical sciences

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    authors: Okafor-Muo OL,Hassanin H,Kayyali R,ElShaer A

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  • Solubility advantage of amorphous pharmaceuticals, part 3: Is maximum solubility advantage experimentally attainable and sustainable?

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    journal_title:Journal of pharmaceutical sciences

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    authors: Murdande SB,Pikal MJ,Shanker RM,Bogner RH

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  • Cardiovascular actions of three harmala alkaloids: harmine, harmaline, and harmalol.

    abstract::Each of three harmala alkaloids, harmine, harmaline, and harmalol, decreased heart rate and increased pulse pressure, peak aortic flow, and myocardial contractile force in intact normotensive anesthetized dogs. Harmine reduced systemic arterial blood pressure and total peripheral vascular resistance; harmaline-evoked ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Aarons DH,Rossi GV,Orzechowski RF

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  • Synergistic effect of low-frequency ultrasound and sodium lauryl sulfate on transdermal transport.

    abstract::Application of low-frequency ultrasound has been shown to enhance transdermal transport of drugs (low-frequency sonophoresis). In this paper, we show that the efficacy of low-frequency ultrasound in enhancing transdermal transport can be further increased by its combination with sodium lauryl sulfate (SLS), a well-kno...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Mitragotri S,Ray D,Farrell J,Tang H,Yu B,Kost J,Blankschtein D,Langer R

    更新日期:2000-07-01 00:00:00

  • Alkylation of 6-mercaptopurine (6-MP) with N-alkyl-N-alkoxycarbonylaminomethyl chlorides: S6-(N-alkyl-N-alkoxycarbonyl)aminomethyl-6-MP prodrug structure effect on the dermal delivery of 6-MP.

    abstract::The S6-(N-alkyl-N-alkoxycarbonyl)aminomethyl-6-MP (6-CARB-6-MP) prodrugs 5-20 were synthesized from the reaction of 6-MP with N-alkyl-N-alkyoxycarbonylaminomethyl chlorides (4) in dimethyl sulfoxide in overall yields of 5-62%, depending on the N-alkyl and the alkoxy groups involved. The derivatives were fully characte...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Siver KG,Sloan KB

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  • Effect of repeated skin application on percutaneous absorption of salicylic acid.

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    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Roberts MS,Harlock E

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  • Synthesis and irreversible beta-adrenergic blockade with a bromoacetamido derivative of betaxolol.

    abstract::1-[4-(2-Cyclopropylmethoxyethyl)phenoxy]-3-[1-p-(bromoacetamidophe nyl) -2-methyl-2-propylamine]-2-propranol (8), which is a derivative of the beta 1-adrenergic agent betaxolol, was synthesized. Compound 8 showed less potent beta-adrenergic blocking activity than betaxolol in an in vitro test with guinea pig tracheal ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Amlaiky N,Leclerc G

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  • Regulation of Tight-Junction Integrity by Insulin in an In Vitro Model of Human Blood-Brain Barrier.

    abstract::Although insulin receptor is expressed at the human blood-brain barrier (BBB), the physiological and pathologic roles of insulin signaling in biologic responses at the BBB remain unclear. Here, we investigate insulin signaling at the human BBB using human cerebral microvascular endothelial cell line (hCMEC/D3) as a we...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Ito S,Yanai M,Yamaguchi S,Couraud PO,Ohtsuki S

    更新日期:2017-09-01 00:00:00

  • Compressibility of anhydrous tricalcium phosphate.

    abstract::It is shown that tricalcium phosphate follows a simple Heckel relationship in pressures of usual tablet compression, only if a density of 1.92 g/mL is used. This coincides with the density obtained by wet pycnometry, whereas the crystallographical density is 3.1 g/mL. The interpretation is that some of the pore space ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Hou XP,Carstensen JT

    更新日期:1985-04-01 00:00:00

  • Mechanistic studies of the transdermal iontophoretic delivery of 5-OH-DPAT in vitro.

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    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Ackaert OW,Van Smeden J,De Graan J,Dijkstra D,Danhof M,Bouwstra JA

    更新日期:2010-01-01 00:00:00

  • Developability index: a rapid in silico tool for the screening of antibody aggregation propensity.

    abstract::Determining the aggregation propensity of protein-based biotherapeutics is an important step in the drug development process. Typically, a great deal of data collected over a large period of time is needed to estimate the aggregation propensity of biotherapeutics. Thus, candidates cannot be screened early on for aggre...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Lauer TM,Agrawal NJ,Chennamsetty N,Egodage K,Helk B,Trout BL

    更新日期:2012-01-01 00:00:00