Rate- and Extent-Limiting Factors of Oral Drug Absorption: Theory and Applications.

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

authors： Takahashi DM

更新日期：1980-02-01 00:00:00

abstract：:Metronidazole (MTZ) is a drug of choice for protozoal infections such as luminal amoebiasis. We designed and synthesized N-nicotinoyl-2-{2-(2-methyl-5-nitroimidazol-1-yl)ethyloxy}-D,L-glycine (NMG) as a colon-specific prodrug of MTZ. The synthetic yield of NMG was about 34%. The apparent partition coefficient of MTZ w...

journal_title：Journal of pharmaceutical sciences

authors： Kim D,Hong S,Jung S,Jung Y,Kim YM

更新日期：2009-11-01 00:00:00

abstract：:The physical state of a dosage form, crystalline versus amorphous, is critical in determining its solid-state physical and chemical properties. This minireview describes the physics associated with the preparation and storage of amorphous solids including a review of the common theories of the glass transition and rel...

journal_title：Journal of pharmaceutical sciences

authors： Hilden LR,Morris KR

更新日期：2004-01-01 00:00:00

abstract：:The hydrophobic substituent parameter for a system of meta- and para-disubstituted benzenes, XC6H4Y, defined as pi X/PhY = log PXC6H4Y - log PC6H5Y, where P is the octanol-water partition coefficient and X and Y are variable and fixed substituents, respectively, varies from one system to another, according to the vari...

journal_title：Journal of pharmaceutical sciences

authors： Fujita T

更新日期：1983-03-01 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

authors： Karesh SM,Eckelman WC,Reba RC

更新日期：1977-02-01 00:00:00

abstract：:The objective of this study was to determine reasons behind the low oral (p.o.) bioavailability of glucosamine. By using male Sprague-Dawley rats, the movement of glucosamine through everted gut, the effect of dose and glucose, and inhibition of a glucose transporter (GLUT2) by quercetin were studied. Glucosamine phar...

journal_title：Journal of pharmaceutical sciences

authors： Ibrahim A,Gilzad-kohan MH,Aghazadeh-Habashi A,Jamali F

更新日期：2012-07-01 00:00:00

abstract：:Spectrophotometric assay for cycloserine based on the interaction of the drug with 9-methoxyacridine as a chromogenic agent is described. The highly colored substituted acridine product was identified as 9-(d-4-imino-3-isoxazolidinone)acridine. Color development was affected by time and temperature of heating and by t...

journal_title：Journal of pharmaceutical sciences

authors： Stewart JT,Yoo GS

更新日期：1988-05-01 00:00:00

abstract：:A spectrodensitometric assay was developed for propranolol based on measurement of the absorbance of the drug on silica gel plates irradiated at 822 nm. Quantities as low as 0.10 microgram can be detected, and a linear relationship was obtained between 0.010 and 0.400 microgram. The percent recovery from plasma spiked...

journal_title：Journal of pharmaceutical sciences

authors： Hadzija BW,Mattocks AM

更新日期：1978-09-01 00:00:00

abstract：:An assay is described for the determination of the H2-receptor antagonist, cimetidine, in human plasma and urine. Alkalinized plasma or urine was extracted with methylene chloride, the organic phase was evaporated, and the reconstituted residue was analysed by high-pressure liquid chromatography (HPLC) using a reverse...

journal_title：Journal of pharmaceutical sciences

authors： Mihaly GW,Cockbain S,Jones DB,Hanson RG,Smallwood RA

更新日期：1982-05-01 00:00:00

abstract：:Several Several 10-(1-acetyl-4-arylthiosemicarbazido) phenothiazines and their corresponding cyclized 10-(2-arylimino-3-acetylamino-4-thiazolidonyl)phenothiazines were synthetized and characterized by their sharp melting points and elemental analyses. All compounds inhibited nicotinamide adenine dinucleotide (NAD)-dep...

journal_title：Journal of pharmaceutical sciences

authors： Singh SP,Ali B,Auyong TK,Parmar SS,De Boer B

更新日期：1976-03-01 00:00:00

abstract：:Nasal mucosa excised from dogs or rabbits was mounted as a flat sheet in an in vitro chamber. The permeability was assessed by measuring the unidirectional flux of the radiolabeled tracer compounds, water, sucrose, polyethylene glycol, and cholecystokinin octapeptide. The permeability coefficients calculated from the ...

journal_title：Journal of pharmaceutical sciences

authors： Hersey SJ,Jackson RT

更新日期：1987-12-01 00:00:00

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

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

更新日期：2021-01-05 00:00:00

abstract：:Literature data relevant to the decision to allow a waiver of in vivo bioequivalence testing for the marketing authorization of immediate-release, solid oral dosage forms containing enalapril maleate are reviewed. Enalapril, a prodrug, is hydrolyzed by carboxylesterases to the active angiotensin-converting enzyme inhi...

journal_title：Journal of pharmaceutical sciences

authors： Verbeeck RK,Kanfer I,Löbenberg R,Abrahamsson B,Cristofoletti R,Groot DW,Langguth P,Polli JE,Parr A,Shah VP,Mehta M,Dressman JB

更新日期：2017-08-01 00:00:00

abstract：:It is understood that a potential issue for drugs with poor aqueous solubility is low oral absorption. If oral exposure issues arise when working with a low solubility drug candidate, the common action is to rely on enabling formulations to solve the issue. However, this approach becomes troublesome in the pre-clinica...

journal_title：Journal of pharmaceutical sciences

authors： Chiang PC,Sutherlin D,Pang J,Salphati L

更新日期：2016-06-01 00:00:00

abstract：:The comparative pharmacokinetics of free MTP-PE (muramyl tripeptide phosphatidyl ethanolamine) and MTP-PE entrapped in negatively charged multilamellar liposomes (liposomal MPT-PE) was evaluated in rats at a bolus intravenous (i.v.) dose of 0.2 mg/kg and in dogs at a bolus i.v. dose of 0.1 mg/kg. Additional studies we...

journal_title：Journal of pharmaceutical sciences

authors： Gay B,Cardot JM,Schnell C,van Hoogevest P,Gygax D

更新日期：1993-10-01 00:00:00

abstract：:An immune response for a nasal ovalbumin (OVA) powder formulation with an applied nasal delivery platform technology, consisting of a powdery nasal carrier and a device, was evaluated in monkeys with similar upper respiratory tracts and immune systems to those of humans, in order to assess the applicability to a vacci...

journal_title：Journal of pharmaceutical sciences

authors： Torikai Y,Sasaki Y,Sasaki K,Kyuno A,Haruta S,Tanimoto A

更新日期：2020-12-03 00:00:00

abstract：:The physical stability of an immunoglobulin G4 monoclonal antibody (mAb) upon dilution into intravenous (i.v.) bags containing 0.9% saline was examined. Soluble aggregates and subvisible particles were observed by size-exclusion high-performance liquid chromatography (SE-HPLC) and light obscuration when formulated wit...

journal_title：Journal of pharmaceutical sciences

authors： Kumru OS,Liu J,Ji JA,Cheng W,Wang YJ,Wang T,Joshi SB,Middaugh CR,Volkin DB

更新日期：2012-10-01 00:00:00

abstract：:Simple assays for extraction and determination of the concentrations of the antibiotics oxytetracycline, oxolinic acid, and flumequine in a drug dosage form for farmed fish are described. HPLC with UV detection was used in the analyses. The recovery of all three drugs was approximately 100%, and the precision varied f...

journal_title：Journal of pharmaceutical sciences

authors： Rogstad A,Weng B

更新日期：1993-05-01 00:00:00

abstract：:A rapid and sensitive spectrophotometric method has been developed to quantitate the peroxides present in sorbitan monooleate and monostearate. The method relies on the peroxide conversion of iodide to iodine. The method has also been found to work for polysorbate 60. ...

journal_title：Journal of pharmaceutical sciences

authors： Magill A,Becker AR

更新日期：1984-11-01 00:00:00

abstract：:The binding of Cu2+ and Ni2+ to bovine, dog, and human serum albumin has been studied by the 35Cl NMR probe technique. The number of primary copper sites were estimated to be 1.3 for human serum albumin, 3.1 for bovine serum albumin, and 6.6 for dog serum albumin. A similar number of primary nickel sites was determine...

journal_title：Journal of pharmaceutical sciences

authors： Mohanakrishnan P,Chignell CF,Cox RH

更新日期：1985-01-01 00:00:00

abstract：:Boron analogues of carbamoylcholine and thiocholine and esters of these analogues were prepared. These compounds were fairly stable toward hydrolysis and demonstrated moderate anti-inflammatory and hypolipidemic activities in mice. The hypolipidemic activity of the compounds at a dose of 8 mg/kg/day was equivalent in ...

journal_title：Journal of pharmaceutical sciences

authors： Sood A,Sood CK,Spielvogel BF,Hall IH,Wong OT

更新日期：1992-05-01 00:00:00

abstract：:Treatment of systemic diseases by means of the inhalation route is hampered by uncertainties of the drug dose applied by inhalation. In this study, the hypothesis was tested that by standardization of the breathing maneuver used for inhalation, the interindividual variability of the dose deposited intrathoracically ca...

journal_title：Journal of pharmaceutical sciences

authors： Brand P,Friemel I,Meyer T,Schulz H,Heyder J,Häubetainger K

更新日期：2000-06-01 00:00:00

abstract：:The degradation kinetics of metronidazole in aqueous solutions of pH 3.1 to 9.9 under accelerated storage conditions were studied. The stability of metronidazole in solutions containing propylene glycol or polyethylene glycol 400 was also investigated. The reaction order for metronidazole in these aqueous and solvent ...

journal_title：Journal of pharmaceutical sciences

authors： Wang DP,Yeh MK

更新日期：1993-01-01 00:00:00

abstract：:The physiological pH changes and peristalsis activities in gastrointestinal (GI) tract have big impact on the dissolution of oral drug products, when those oral drug products include APIs with pH-dependent solubility. It is well documented that predicting the bioperformance of those oral drug products can be challengi...

journal_title：Journal of pharmaceutical sciences

authors： Tsume Y,Patel S,Wang M,Hermans A,Kesisoglou F

更新日期：2020-11-01 00:00:00

abstract：:The full parameterization for the stratum corneum biphasic microtransport model presented previously in this Journal [95:620-648 (2006)] is developed through a combination of fundamental transport theory and calibration with existing data. Of the five microscopic transport properties, four (D(cor), K(cor/w), D(lip), K...

journal_title：Journal of pharmaceutical sciences

authors： Wang TF,Kasting GB,Nitsche JM

更新日期：2007-11-01 00:00:00

abstract：:The development of an ocular dosage form containing xanthan gum and capable of interacting with mucin in the precorneal area is a challenge. The polymer concentration that can be applied is restricted because of the limited patient acceptability of highly viscous preparations. The precorneal mucin concentration is low...

journal_title：Journal of pharmaceutical sciences

authors： Ceulemans J,Vinckier I,Ludwig A

更新日期：2002-04-01 00:00:00

abstract：:In a continuing search for new biologically active agents derived from indolizine, 3-(2-aminoethyl)-2-methylindolizine, 3-(2-aminoethyl)-2-methyl-5,6,7,8-tetrahydroindolizine, and some mono- and di-N-substituted derivatives were prepared. Initial pharmacological screening showed that these compounds possess anti-5-hyd...

journal_title：Journal of pharmaceutical sciences

authors： Antonini I,Claudi F,Gulini U,Micossi L,Venturi F

更新日期：1979-03-01 00:00:00

abstract：:A simple enzyme immunoassay for the determination of captopril was developed. A specific antibody for captopril was produced in rabbits that were immunized with a hapten-bovine immunoglobulin G conjugate, which was prepared by using 4-(maleimidomethyl)cyclohexane carboxylic acid as a spacer group. The limit of detecti...

journal_title：Journal of pharmaceutical sciences

authors： Kinoshita H,Nakamaru R,Tanaka S,Tohira Y,Sawada M

更新日期：1986-07-01 00:00:00

abstract：:This work was to investigate the effects of particle size and paddle speed on the particle diffusional layer thickness h(app) in a USP dissolution apparatus II. After the determination of the powder dissolution rates of five size fractions of fenofibrate, including <20, 20-32, 32-45, 63-75, and 90-106 microm, the pres...

journal_title：Journal of pharmaceutical sciences

authors： Sheng JJ,Sirois PJ,Dressman JB,Amidon GL

更新日期：2008-11-01 00:00:00

abstract：:Phenylpropanolamine was determined by measuring its fluorescent fluorescamine derivative. The method is rapid, sensitive, and easily automated. Statistics are presented for an effervescent cold product, and recovery data are presented for other commercially available products. ...

journal_title：Journal of pharmaceutical sciences

authors： Shankle LL

更新日期：1978-11-01 00:00:00