Kinetic analysis of enantiomers of threo-methylphenidate and its metabolite in two healthy subjects after oral administration as determined by a gas chromatographic-mass spectrometric method.


:A gas chromatographic-mass spectrometric method was developed for the stereoselective quantification of threo-methylphenidate (MPD) and its metabolite, ritalinic acid (RA), in plasma or urine. The plasma concentrations of (+)-MPD after oral administration of two 10-mg conventional tablets containing racemic MPD.HCl or of 20-mg of racemic MPD.HCl crystals to two healthy subjects were much higher than those of the (-)-isomer. The plasma concentrations of the metabolite, (-)-RA, were higher than that of the (+)-isomer during the first 4 h after administration of racemic MPD.HCl in both tablet and crystal forms. Although in urine both (+)- and (-)-RA were largely excreted in 48 h (37 and 40% of the dose, respectively), the percentage excretion of (-)-RA during the first 3-4 h was approximately twice that of the (+)-isomer. These results suggest that one reason for the difference in the plasma levels between (+)- and (-)-MPD may be due to differences in their rates of metabolism. Pharmacokinetic parameters of (+)-MPD after administration of 10 mg of (+)-MPD.HCl crystals were almost the same as those after administration of racemic MPD.HCl crystals. The AUC infinity 0 of (-)-MPD after administration of 10 mg of (-)-MPD.HCl crystals was smaller than that after administration of racemic MPD.HCl crystals.


J Pharm Sci


Aoyama T,Kotaki H,Honda Y,Nakagawa F




Has Abstract


1990-06-01 00:00:00














  • Kinetics and mechanism of oxidation of promazine and promethazine by ferric perchlorate.

    abstract::The equilibrium constants, kinetics, and mechanism of promazine and promethazine oxidation by ferric perchlorate were investigated at different temperatures and acidities using a stopped-flow spectrophotometric technique. The overall reaction can be represented as follows: (formula: see text) where P+ represents the r...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Gasco MR,Carlotti ME

    更新日期:1978-02-01 00:00:00

  • Dissolving Microneedles Integrated With Liquid Crystals Facilitate Transdermal Delivery of Sinomenine Hydrochloride.

    abstract::The purpose of this study was to investigate the feasibility of delivering sinomenine hydrochloride (SH) transdermally using composite dissolving microneedles (DM) which integrated with liquid crystals (H2). The fabricated SH-loaded composite DM was evaluated for their appearance, mechanical strength, irritation, and ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Gui Z,Wu X,Wang S,Cao Y,Wan J,Shan Q,Yang Z,Zhang J,Gui S

    更新日期:2017-12-01 00:00:00

  • Identification of the major degradation products of 4-methoxy-2-(3-phenyl-2-propynyl)phenol formed by exposure to air and light.

    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

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    authors: Schiavi M,Serafini S,Italia A,Villa M,Fronza G,Selva A

    更新日期:1992-08-01 00:00:00

  • Improved delivery through biological membranes XD: Percutaneous absorption and metabolism of methylsulfinylmethyl 2-acetoxybenzoate and related aspirin prodrugs.

    abstract::Oxidative-reductive interconversion of the methylthiomethyl ester of aspirin and the corresponding sulfoxide and sulfone derivatives can be detected in rat liver homogenate, in addition to the extremely facile hydrolysis of these esters. The methylthiomethyl and methylsulfinylmethyl 2-acetoxybenzoates penetrate freshl...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Loftsson T,Bodor N

    更新日期:1981-07-01 00:00:00

  • Degradation kinetics of phentolamine hydrochloride in solution.

    abstract::The degradation kinetics of phentolamine hydrochloride in aqueous solution over a pH range of 1.2 to 7.2 and its stability in propylene glycol- or polyethylene glycol 400-based solutions were investigated. The observed rate constants were shown to follow apparent first-order kinetics in all cases. The pKa determinatio...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Wang DP,Tu YH,Allen LV Jr

    更新日期:1988-11-01 00:00:00

  • Kinetic ratio as a parameter for product stability calculations.

    abstract::A new parameter, the kinetic ratio, is suggested for estimating product potency during storage under ambient warehouse temperatures. Actual warehouse temperature data were integrated using Arrhenius kinetics, and the resulting potency errors, due both to the integration method and to temperature averaging, were evalua...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Scher M

    更新日期:1980-03-01 00:00:00

  • Combined use of pharmacokinetic modeling and a steady-state delivery approach allows early assessment of IkappaB kinase-2 (IKK-2) target safety and efficacy.

    abstract::NF-kappaB activation is clearly linked to the pathogenesis of multiple inflammatory diseases including arthritis. The prominent role of IkappaB kinase-2 (IKK-2) in regulating NF-kappaB signaling in response to proinflammatory stimuli has made IKK-2 a primary anti-inflammation therapeutic target. PHA-408, a potent and ...

    journal_title:Journal of pharmaceutical sciences

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    authors: Chiang PC,Kishore NN,Thompson DC

    更新日期:2010-03-01 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

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    authors: Hou XP,Carstensen JT

    更新日期:1985-04-01 00:00:00

  • Enantiotropically-related polymorphs of {4-(4-chloro-3-fluorophenyl)-2-[4-(methyloxy)phenyl]-1,3-thiazol-5-yl} acetic acid: crystal structures and multinuclear solid-state NMR.

    abstract::Single crystal X-ray diffraction (SCXRD), powder X-ray diffraction (PXRD), and solid-state NMR (SSNMR) techniques are used to analyze the structures of two nonsolvated polymorphs of {4-(4-chloro-3-fluorophenyl)-2-[4-(methyloxy)phenyl]-1,3-thiazol-5-yl} acetic acid. These polymorphs are enantiotropically-related with a...

    journal_title:Journal of pharmaceutical sciences

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    authors: Vogt FG,Katrincic LM,Long ST,Mueller RL,Carlton RA,Sun YT,Johnson MN,Copley RC,Light ME

    更新日期:2008-11-01 00:00:00

  • Potential antineoplastics I: substituted 3,5-dioxo-and 3-thioxo-5-oxo-2,3,4,5-tetrahydro-1,2,4-triazines.

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    journal_title:Journal of pharmaceutical sciences

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    authors: Ibrahim el-SA,Shams el-Dine SA,Soliman FS,Labouta IM

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  • Vehicle effects in percutaneous absorption: in vitro study of influence of solvent power and microscopic viscosity of vehicle on benzocaine release from suspension hydrogels.

    abstract::The release through silicone rubber membranes of benzocaine suspended in carbomer hydrogels containing different concentrations of low molecular weight polysols (ethylene glycol, propylene glycol, glycerol, and sorbitol) was studied to establish general principles and procedures for control of the effects on percutane...

    journal_title:Journal of pharmaceutical sciences

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    authors: Di Colo G,Carelli V,Giannaccini B,Serafini MF,Bottari F

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  • High Sensitivity Detection of a Solubility Limiting Surface Transformation of Drug Particles by DNP SENS.

    abstract::We investigate the presence of a surface species for the active pharmaceutical ingredient (API) AZD9496 with dynamic nuclear polarization surface enhanced nuclear spectroscopy (DNP SENS). We show that using DNP we can elucidate the presence of an amorphous form of the API at the surface of crystalline particles of the...

    journal_title:Journal of pharmaceutical sciences

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    authors: Viger-Gravel J,Pinon AC,Björgvinsdóttir S,Skantze U,Svensk Ankarberg A,Von Corswant C,Schantz S,Emsley L

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  • X-ray diffraction and infrared spectroscopy of N,N-dimethylformamide and dimethyl sulfoxide solvatomorphs of betulonic acid.

    abstract::X-ray diffraction and infrared spectroscopy measurements for the N,N-dimethylformamide (DMF) and dimethyl sulfoxide (DMSO) solvatomorphs of betulonic acid (BA) were investigated. BA [3-oxolup-20(29)-en-28-oic acid, C(30)H(46)O(3)] exhibits a wide spectrum of biological activities and is considered to be a promising na...

    journal_title:Journal of pharmaceutical sciences

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    authors: Boryczka S,Jastrzebska M,Bębenek E,Kusz J,Zubko M,Kadela M,Michalik E

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  • Investigation of PEG crystallization in frozen PEG-sucrose-water solutions: II. Characterization of the equilibrium behavior during freeze-thawing.

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    journal_title:Journal of pharmaceutical sciences

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  • Enabling tablet product development of 5-fluorocytosine through integrated crystal and particle engineering.

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    journal_title:Journal of pharmaceutical sciences

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    authors: Perumalla SR,Sun CC

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  • Formation of insoluble particulates in a spray-dried F(ab')(2) fragment.

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    journal_title:Journal of pharmaceutical sciences

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    authors: Lassner P,Adler M,Lee G

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    journal_title:Journal of pharmaceutical sciences

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    authors: Baxter JG,Brass C,Schentag JJ,Slaughter RL

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  • Cactus alkaloids XXXIII: beta-phenethylamines from the Guatemalan cactus Pilosocereus maxonii.

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    journal_title:Journal of pharmaceutical sciences

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    authors: Pummangura S,Nichols DE,McLaughlin JL

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  • A novel approach to preparing water soluble prodrug forms of cisplatin analogues bearing chelating diamines.

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    journal_title:Journal of pharmaceutical sciences

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    authors: Köckerbauer R,Bednarski PJ

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    journal_title:Journal of pharmaceutical sciences

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    authors: Thompson TA,Borman CH,Goodblatt RS,Roth WJ 3rd

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  • Application of salivary concentration data to pharmacokinetic studies with antipyrine.

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    journal_title:Journal of pharmaceutical sciences

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    authors: Meffin PJ,Williams RL,Blaschke TF,Rowland M

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  • Agglomerative crystallization of ABT-510 in a partially miscible solvent system.

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    authors: Sheikh AY,Pal A,Viswanath S,Tolle JC

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  • Δ9-tetrahydrocannabinol and its major metabolite Δ9-tetrahydrocannabinol-11-oic acid as 15-lipoxygenase inhibitors.

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    journal_title:Journal of pharmaceutical sciences

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    authors: Takeda S,Jiang R,Aramaki H,Imoto M,Toda A,Eyanagi R,Amamoto T,Yamamoto I,Watanabe K

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    journal_title:Journal of pharmaceutical sciences

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    journal_title:Journal of pharmaceutical sciences

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    authors: Turner CE,Hsu MH,Knapp JE,Schiff PL Jr,Slatkin DJ

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    journal_title:Journal of pharmaceutical sciences

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    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Wang YC

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  • Tocainide conjugation in humans: novel biotransformation pathway for a primary amine.

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    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Elvin AT,Keenaghan JB,Byrnes EW,Tenthorey PA,McMaster PD,Takman BH,Lalka D,Manion CV,Baer DT,Wolshin EM,Meyer MB,Ronfeld RA

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    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Bhat PG,Flanagan DR,Donovan MD

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