Insights From an Integrated Physiologically Based Pharmacokinetic Model for Brain Penetration.

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：:A spectrophotofluorometric method is described for the quantitative analysis of coumarin, umbelliferone, and mixtures thereof in whole blood. The two drugs were selectively isolated from blood by solvent extraction. Analysis of the isolated coumarin was based on the measurement of the fluorophore at activation and emi...

journal_title：Journal of pharmaceutical sciences

authors： Tan HS,Ritschel WA,Sanders PR

更新日期：1976-01-01 00:00:00

abstract：:An analysis of the disintegration-dissolution sequence of drug release from a tablet leads to a mathematical expression relating disintegration to the dissolution profile of the tablet and the dissolution rate of the primary drug particles in the tablet. The equation describing the disintegration of an acetaminophen t...

journal_title：Journal of pharmaceutical sciences

authors： Nelson KG,Wang LY

更新日期：1978-01-01 00:00:00

abstract：:The relative sweetness, onset times, and durations of response of D-glucose, D-xylose, D-quinovose, D-galactose, L-arabinose, and D-fucose were determined at four temperatures. The results can be interpreted by simple concepts of intramolecular hydrogen bonding which indicate that the so-called gamma-function of the t...

journal_title：Journal of pharmaceutical sciences

authors： Birch GG,Dziedzic SZ,Shallenberger RS,Lindley MG

更新日期：1981-03-01 00:00:00

abstract：:Accurate prediction of target occupancy facilitates central nervous system drug development. In this review, we discuss the predictability of serotonin transporter (SERT) occupancy in human brain estimated from in vitro Ki values for human SERT and plasma concentrations of unbound drug (Cu,plasma), as well as the impa...

journal_title：Journal of pharmaceutical sciences

authors： Yahata M,Chiba K,Watanabe T,Sugiyama Y

更新日期：2017-09-01 00:00:00

abstract：:L-3-(3-Hydroxy-4-pivaloyloxyphenyl)alanine (1, NB-355) is a novel L-dopa prodrug. After oral administration with carbidopa in rats, 1 demonstrated 2.3 times longer duration (MRT) and 1.4 times larger bioavailability (AUC) on plasma L-dopa concentrations than those of L-dopa itself. Similar results were obtained in dog...

journal_title：Journal of pharmaceutical sciences

authors： Ihara M,Tsuchiya Y,Sawasaki Y,Hisaka A,Takehana H,Tomimoto K,Yano M

更新日期：1989-07-01 00:00:00

abstract：:A procedure for the determination of mianserin, desmethylmianserin, and 8-hydroxymianserin in plasma at therapeutic concentrations by liquid chromatography with electrochemical detection is described. Following a multiple-step extraction from alkaline plasma into methyl-tert-butyl ether, the reconstituted extract was ...

journal_title：Journal of pharmaceutical sciences

authors： Suckow RF,Cooper TB,Quitkin FM,Stewart JW

更新日期：1982-08-01 00:00:00

abstract：:Biopolymer-based hydrogels such as mucus and the basal lamina play a key role in biology, where they control the exchange of material between different compartments. They also pose a barrier that needs to be overcome for successful drug delivery. Characterizing the permeability properties of such hydrogels is mandator...

journal_title：Journal of pharmaceutical sciences

authors： Vladescu I,Lieleg O,Jang S,Ribbeck K

更新日期：2012-01-01 00:00:00

abstract：:Live attenuated influenza vaccine (LAIV) is considered one of the most effective vaccines and can be manufactured quickly and inexpensively to counter seasonal or pandemic influenza. Lyophilization is widely used in vaccine production. However, it requires a longer production cycle and large-scale equipment, thus posi...

journal_title：Journal of pharmaceutical sciences

authors： Sun Y,Shen Z,Zhang C,Yi Y,Zhu K,Xu F,Kong W

更新日期：2019-07-01 00:00:00

abstract：:This study was designed to examine the effect of benzalkonium chloride/ethylenediaminetetraacetic acid (BAK/EDTA) on the ocular bioavailability (Focular) of ketorolac tromethamine after ocular instillation to normal and de-epithelialized corneas of rabbits both in vitro and in vivo. The in vitro Focular of the formula...

journal_title：Journal of pharmaceutical sciences

authors： Madhu C,Rix PJ,Shackleton MJ,Nguyen TG,Tang-Liu DD

更新日期：1996-04-01 00:00:00

abstract：:Low-density lipoproteins (LDLs), the physiological vehicles for lipids, are potentially useful drug delivery devices for (hydrophobic) drugs. The physicochemical characteristics of LDL loaded with the adriamycin derivative AD 32 or the N-mustard derivative WB 4291 were compared to that of native and reconstituted LDL ...

journal_title：Journal of pharmaceutical sciences

authors： Westesen K,Gerke A,Koch MH

更新日期：1995-02-01 00:00:00

abstract：:Release of drug from a single-layer film containing dispersed drug follows a diffusion-controlled matrix model, where the quantity released per unit area is proportional to the square root of time. The kinetics may be made linear with time (zero order) by laminating a second film without drug to the releasing side of ...

journal_title：Journal of pharmaceutical sciences

authors： Borodkin S,Tucker FE

更新日期：1975-08-01 00:00:00

abstract：:A wide variety of computational models covering statistical, mechanistic, and machine learning (locked and adaptive) methods are explored for use in biopharmaceutical manufacturing. Limited discussion exists on how to establish the credibility of a computational model for application in biopharmaceutical manufacturing...

journal_title：Journal of pharmaceutical sciences

authors： Bideault G,Scaccia A,Zahel T,Forero RL,Daluwatte C

更新日期：2021-01-22 00:00:00

abstract：:The metabolic disposition of 14C-labeled carprofen [(+/-)-6-chloro-alpha-methylcarbazole-2-acetic acid] was investigated in rats, dogs, and humans. Carprofen is eliminated predominantly by biotransformation in these three species. In dogs and rats, the direct conjugation of carprofen to form an ester glucuronide and o...

journal_title：Journal of pharmaceutical sciences

authors： Rubio F,Seawall S,Pocelinko R,DeBarbieri B,Benz W,Berger L,Morgan L,Pao J,Williams TH,Koechlin B

更新日期：1980-11-01 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 pharmacokinetics and tissue distribution of methotrexate (MTX) were investigated following intra-articular injection of either MTX solution or controlled release MTX loaded microspheres in healthy rabbit joints. MTX solution or MTX loaded microspheres (size 30-100 mum) (10 mg MTX) was injected into the right knee ...

journal_title：Journal of pharmaceutical sciences

authors： Liang LS,Wong W,Burt HM

更新日期：2005-06-01 00:00:00

abstract：:The aim of this study was to utilize high-speed video imaging for understanding the disintegrability of compacts and disintegrant action upon wetting. High-speed video imaging was used to visualize the disintegration of compacts and effect of wetting on free disintegrant particles. Acquired images were processed using...

journal_title：Journal of pharmaceutical sciences

authors： Desai PM,Liew CV,Heng PW

更新日期：2012-06-01 00:00:00

abstract：:It is shown that a suitable dosage interval, tau, can be estimated by a factor times the sum of the mean residence time (MRT) of the central compartment (MRTC) and the MRT of the absorption site (MRTA). This value of tau will provide a ratio, maximum steady-state plasma concentration: minimum steady-state plasma conce...

journal_title：Journal of pharmaceutical sciences

authors： Wagner JG

更新日期：1987-01-01 00:00:00

abstract：:Aggregation of therapeutic monoclonal antibodies has a potential risk of immunogenicity, requiring minimization of aggregate formation. We have developed a fitting formula for antibody aggregation at 40°C based on physicochemical parameters, including colloidal and conformational stabilities. An IgG1 monoclonal antibo...

journal_title：Journal of pharmaceutical sciences

authors： Oyama H,Koga H,Tadokoro T,Maenaka K,Shiota A,Yokoyama M,Noda M,Torisu T,Uchiyama S

更新日期：2020-01-01 00:00:00

abstract：:Chagas disease due to chronic infection with Trypanosoma cruzi is a neglected cause of heart disease, affecting approximately 6-10 million individuals in Latin America and elsewhere. T. cruzi Tc24, a calcium-binding protein in the flagellar pocket of the parasite, is a candidate antigen for an injectable therapeutic v...

journal_title：Journal of pharmaceutical sciences

authors： Biter AB,Weltje S,Hudspeth EM,Seid CA,McAtee CP,Chen WH,Pollet JB,Strych U,Hotez PJ,Bottazzi ME

更新日期：2018-05-01 00:00:00

abstract：:The aim of this study was to characterize the metabolic pathways of 2-methoxyestradiol (2ME2), an investigational anticancer drug. In vitro metabolism studies were performed by incubation of 2ME2 with human liver microsomes under various conditions and metabolite identification was performed using liquid chromatograph...

journal_title：Journal of pharmaceutical sciences

authors： Lakhani NJ,Sparreboom A,Xu X,Veenstra TD,Venitz J,Dahut WL,Figg WD

更新日期：2007-07-01 00:00:00

abstract：:The problem of optimizing ocular bioavailability of topically applied ophthalmic drugs is discussed. A formula for drug concentration in the tear film is derived using well-known pharmacokinetic relationships and a first-order drug decay model for the tear film. The time integral of the tear film concentration is then...

journal_title：Journal of pharmaceutical sciences

authors： Keister JC,Cooper ER,Missel PJ,Lang JC,Hager DF

更新日期：1991-01-01 00:00:00

abstract：:An alumina (Al(2)O(3))-steroid-ethanol model is used for forced degradation testing of corticosteroids to predict chemical stability and degradation products in pressurized metered-dose inhaler (pMDI) solution formulations. The model involves an ethanolic solution of a test steroid with Al(2)O(3), stressed at elevated...

journal_title：Journal of pharmaceutical sciences

authors： Wu ZZ,Thatcher ML,Lundberg JK,Ogawa MK,Jacoby CB,Battiste JL,Ledoux KA

更新日期：2012-06-01 00:00:00

abstract：:Drugs possessing the ability to bind to melanin-rich tissue, such as the eye, are linked with higher ocular exposure, and therefore have the potential to affect the efficacy and safety profiles of therapeutics. A high-throughput melanin chromatographic affinity assay has been developed and validated, which has allowed...

journal_title：Journal of pharmaceutical sciences

authors： Reilly J,Williams SL,Forster CJ,Kansara V,End P,Serrano-Wu MH

更新日期：2015-12-01 00:00:00

abstract：:The effect of dimethyl sulfoxide, dimethyl formamide, and dimethyl acetamide on the basal stratum corneum of excised nude mouse skin was investigated. All of these dipolar aprotic solvents caused a swelling of the basal stratum corneum cells and a disruption of the normal keratin pattern. This behavior suggests that d...

journal_title：Journal of pharmaceutical sciences

authors： Sharata HH,Burnette RR

更新日期：1988-01-01 00:00:00

abstract：:Ion cluster technique in conjunction with gas chromatography-mass spectrometry (GC-MS) was used for the identification and quantitation of major metabolites of cocaine (1a) in rat and humans. In a typical experiment, a female rat weighing 250 gm was intraperitoneally administered a 20-mg/kg mixture of 1a, NCD3-cocaine...

journal_title：Journal of pharmaceutical sciences

authors： Jindal SP,Lutz T

更新日期：1989-12-01 00:00:00

abstract：:To reduce the inherent variability in serum uric acid levels of animals allowed ad libitum exposure to food containing potassium oxonate and uric acid, male Sprague-Dawley rats were trained to eat their daily food allotment in a 1.25-hr period each morning. After training the rats were fed a food mixture containing 5%...

journal_title：Journal of pharmaceutical sciences

authors： Newburger J,Hsu TF,Combs AB

更新日期：1979-05-01 00:00:00

abstract：:The spherically agglomerated crystals of aminophylline (theophylline-ethylenediamine complex) can be compounded directly into pharmaceutical formulations without further processing, e.g., granulation. Such crystals were prepared by mixing theophylline and ethylenediamine in a partially miscible solvent system, i.e., o...

journal_title：Journal of pharmaceutical sciences

authors： Kawashima Y,Aoki S,Takenaka H,Miyake Y

更新日期：1984-10-01 00:00:00

abstract：:Phospholipids have been extensively evaluated as an anchor for both PEGylation and receptor-targeting in liposomal formulations. However, cholesterol, another important component in biomembranes, has not been fully investigated as an alternative anchor. In this study, the potential role of cholesterol for anchoring PE...

journal_title：Journal of pharmaceutical sciences

authors： Zhao XB,Muthusamy N,Byrd JC,Lee RJ

更新日期：2007-09-01 00:00:00

abstract：:Dendrimers have emerged as a promising drug delivery system due to their well defined size, tailorability, and multifunctional nature. However, their application in brain delivery is relatively a new area of research. The present study was aimed at evaluating the uptake and permeation of polyether-copolyester (PEPE) d...

journal_title：Journal of pharmaceutical sciences

authors： Dhanikula RS,Hammady T,Hildgen P

更新日期：2009-10-01 00:00:00