A Simplified Model of Moisture Transport in Hydrophilic Porous Media With Applications to Pharmaceutical Tablets.

abstract：:Lysosomes are acidic intracellular organelles that can extensively sequester basic lipophilic drugs due to pH and membrane partitioning, and therefore may significantly influence subcellular drug concentrations. Current in vitro methods for lysosomal drug sequestration evaluation typically lack the ability to accurate...

journal_title：Journal of pharmaceutical sciences

authors： Francis L,Harrell A,Hallifax D,Galetin A

更新日期：2020-09-01 00:00:00

abstract：:The affinity chromatographic technique was used to study the interaction of bovine serum albumin and salicylic acid at 3.3 +/- 1.1 degrees. Beaded agarose gel, on which the albumin was immobilized by covalent linkage, was packed in a column as an affinity adsorbent. Frontal analysis was performed on this column to eva...

journal_title：Journal of pharmaceutical sciences

authors： Nakano NI,Oshio T,Fujimoto Y,Amiya T

更新日期：1978-07-01 00:00:00

abstract：:The synthesis of some 6-substituted 3,5-dioxo- and 3-thioxo-5-oxo-2,3,4,5-tetrahydro-1,2,4-triazines for possible antineoplastic activity is reported. The assigned structures were substantiated by IR, NMR, and mass spectral studies of representative members of the series. Four compounds were tested against P-388 lymph...

journal_title：Journal of pharmaceutical sciences

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

更新日期：1979-02-01 00:00:00

abstract：:Quality-by-design (QbD) is a systematic approach to drug development, which begins with predefined objectives, and uses science and risk management approaches to gain product and process understanding and ultimately process control. The concept of QbD can be extended to analytical methods. QbD mandates the definition ...

journal_title：Journal of pharmaceutical sciences

authors： Vogt FG,Kord AS

更新日期：2011-03-01 00:00:00

abstract：:New butyrate derivatives were synthesized to investigate the residence time of potent butyric acid in vivo. These derivatives were triglycerides in which one, two, or three butyric acid molecules were bound to glycerol or to mono- and dipalmitic esters of glycerol. Pharmacokinetic studies showed that a constant plasma...

journal_title：Journal of pharmaceutical sciences

authors： Planchon P,Pouillart P,Ronco G,Villa P,Pieri F

更新日期：1993-10-01 00:00:00

abstract：:There is a need to evaluate the permeability of human ulcerated tissue and periulcer tissue in order to assess the possible treatment of such a localized pathological lesion with a topical therapy. In vitro percutaneous absorption studies were undertaken to evaluate an animal model that may mimic this clinical situati...

journal_title：Journal of pharmaceutical sciences

authors： Walker M,Hulme TA,Rippon MG,Walmsley RS,Gunnigle S,Lewin M,Winsey S

更新日期：1997-12-01 00:00:00

abstract：:The present studies were undertaken to describe the dynamic nature of the degradation and absorption of insulin in the subcutaneous injection site and to develop agents which would stabilize this dosage form. [125I]Insulin with 0.2-U/kg of unlabeled insulin in 10 microliters of aqueous solution was injected subcutaneo...

journal_title：Journal of pharmaceutical sciences

authors： Hori R,Komada F,Okumura K

更新日期：1983-04-01 00:00:00

abstract：:Quercetin had been shown to be effective in the management of arthritis. However, bioavailability of quercetin is a concern for such treatment. This work aims at the development of intra-articular drug delivery system by controlled release of quercetin (loaded in microspheres) for the management of rheumatoid arthriti...

journal_title：Journal of pharmaceutical sciences

authors： Natarajan V,Krithica N,Madhan B,Sehgal PK

更新日期：2011-01-01 00:00:00

abstract：:Levetiracetam therapy is often associated with high levels of individual variation in the recommended dose required to achieve preferential treatment. Thus, a reliable and dynamic regulation system to accurately tailor dose is necessary. The main objective of this study is to explore and prepare a dose-flexible contro...

journal_title：Journal of pharmaceutical sciences

authors： Cui M,Li Y,Wang S,Chai Y,Lou J,Chen F,Li Q,Pan W,Ding P

更新日期：2019-02-01 00:00:00

abstract：:The absorption, protein binding, blood-to-plasma ratio, renal excretion, and pharmacokinetics of the dopamine-2 agonists (D2-agonists) 4-(2-di-n-propylaminoethyl)-7-hydroxy-2-(3H)-indolone (1), N-(2'-hydroxy-5'-[N,N-di-n-propylaminoethylphenyl])methanesulfonamide (2), and 4-(2-di-n-propylaminoethyl)-2-(3H)-indolone (3...

journal_title：Journal of pharmaceutical sciences

authors： Swagzdis JE,Wittendorf RW,DeMarinis RM,Mico BA

更新日期：1986-10-01 00:00:00

abstract：:A high-speed liquid chromatographic system is described, which can be used for the simultaneous identification of the anabolic steroid methandrostenolone and its impurities and the quantitation of each of these compounds. Separation is effected by adsorption chromatography on a slurry-packed microparticulate silica ge...

journal_title：Journal of pharmaceutical sciences

authors： Butterfield AG,Lodge BA,Pound NJ,Sears RW

更新日期：1975-03-01 00:00:00

abstract：:Cisplatin (CDDP) is an effective anticancer agent for many solid tumors but has significant systemic toxicity limiting its use in many patients. We have designed a loco-regional delivery system to increase platinum levels in the lymphatics, where early metastasis is most likely to occur, while reducing systemic toxici...

journal_title：Journal of pharmaceutical sciences

authors： Cai S,Xie Y,Davies NM,Cohen MS,Forrest ML

更新日期：2010-06-01 00:00:00

abstract：:To explore the possibility of cyclodextrin click clusters (CCCs) as a new cyclodextrin-based excipient, we prepared three different CCCs; heptakis{6-(4-hydroxymethyl-1H-[1,2,3]triazol-1-yl)-6-deoxy}-β-cyclodextrin (HT-β-CD), heptakis{6-(4-hydroxymethyl-1H-[1,2,3]triazol-1-yl)-6-deoxy}{2,3-di-O-methyl}-β-cyclodextrin (...

journal_title：Journal of pharmaceutical sciences

authors： Le HT,Jeon HM,Lim CW,Kim TW

更新日期：2014-10-01 00:00:00

abstract：:The acidic, neutral, and alkaline degradations of six therapeutically useful cephalosporins (cephalothin, cephaloridine, cephaloglycin, cephalexin, cephradine, and cefazolin), 7-amino-cephalosporanic acid, 7-aminodeacetoxycephalosporanic acid, and some 7-substituted derivatives were followed by high-pressure liquid ch...

journal_title：Journal of pharmaceutical sciences

authors： Yamana T,Tsuji A

更新日期：1976-11-01 00:00:00

abstract：:Although PEGylation of biologics is currently the gold standard for half-life extension, the technology has a number of limitations, most importantly the non-biodegradability of PEG and the extremely high viscosity at high concentrations. HESylation is a promising alternative based on coupling to the biodegradable pol...

journal_title：Journal of pharmaceutical sciences

authors： Liebner R,Meyer M,Hey T,Winter G,Besheer A

更新日期：2015-02-01 00:00:00

abstract：:The objective of this study was to determine the relative importance of metabolism by cytochrome P450 (CYP) enzymes versus efflux by P-glycoprotein (P-gp) in restricting the intestinal mucosal permeation of cyclic prodrugs (AOA-DADLE, CA-DADLE, OMCA-DADLE) of the opioid peptide DADLE (H-Tyr-D-Ala-Gly-Phe-D-Leu-OH). AO...

journal_title：Journal of pharmaceutical sciences

authors： Ouyang H,Chen W,Andersen TE,Steffansen B,Borchardt RT

更新日期：2009-01-01 00:00:00

abstract：:The objective of this work was to delineate the contribution of thermodynamic activities of ionized and unionized species on buccal drug permeation. The flux and permeability of a model acidic (nimesulide) and basic (bupivacaine) drug were determined across porcine buccal mucosa at different pH conditions. Thermodynam...

journal_title：Journal of pharmaceutical sciences

authors： Kokate A,Li X,Singh P,Jasti BR

更新日期：2008-10-01 00:00:00

abstract：:Diazepam (1), a hypnotic and anxiolytic drug in worldwide use, formed an intermediate product in a mixture of ethanol and sodium hydroxide ([NaOH] > or = 1 M). The intermediate product slowly decomposed to form 2-(methylamino)-5-chlorobenzophenone imine (2) and 2-(methylamino)-5-chlorobenzophenone (3). The amount of 2...

journal_title：Journal of pharmaceutical sciences

authors： Yang SK,Tang R,Yang TJ,Pu QL,Bao Z

更新日期：1996-07-01 00:00:00

abstract：:The aim of the study was to determine and compare the degree of swelling and the swelling kinetics of poly(ethylene oxide) (PEO) hydrophilic matrix tablets without any additives for matrixes with different molecular weight polydispersities. A wide range of "mixed" polydisperse PEO tablets were obtained by mixing two P...

journal_title：Journal of pharmaceutical sciences

authors： Körner A,Larsson A,Andersson A,Piculell L

更新日期：2010-03-01 00:00:00

abstract：:A three-way crossover bioavailability study was performed using nine adult male volunteers with three different commercial prednisone tablets. Plasma samples were assayed for prednisolone, the active metabolite of prednisone, by a radioimmunoassay method. Statistical analysis showed significant differences in the rate...

journal_title：Journal of pharmaceutical sciences

authors： Sullivan TJ,Sakmar E,Albert KS,Blair DC,Wagner JG

更新日期：1975-10-01 00:00:00

abstract：:Specifically tailored amino acid-based formulations were previously shown to have a high potential to avoid stress-mediated degradation of complex molecules such as monoclonal antibodies and viral vectors. By using adenovirus 5 (Ad5) as a model, we studied whether such formulations may also efficiently protect viral v...

journal_title：Journal of pharmaceutical sciences

authors： Reinauer EB,Grosso SS,Henz SR,Rabas JA,Rodenstein C,Altrichter J,Scholz M,Kemter KF

更新日期：2020-01-01 00:00:00

abstract：:Drying is a common pharmaceutical process, whose potential to modify the final drug and/or dosage form properties is often underestimated. In the present study, pellets consisting of the matrix former calcium stearate (CaSt) incorporating the active pharmaceutical ingredient ibuprofen were prepared via wet extrusion a...

journal_title：Journal of pharmaceutical sciences

authors： Schrank S,Kann B,Windbergs M,Glasser BJ,Zimmer A,Khinast J,Roblegg E

更新日期：2013-11-01 00:00:00

abstract：:Cholesterol promotes basal and verapamil-induced ATPase activity of P-glycoprotein (P-gp). We investigated whether these effects are related to each other and to the impact of the sterol on bilayer fluidity and verapamil membrane affinity. P-gp was reconstituted in egg-phosphatidylcholine (PhC) liposomes with or witho...

journal_title：Journal of pharmaceutical sciences

authors： Belli S,Elsener PM,Wunderli-Allenspach H,Krämer SD

更新日期：2009-05-01 00:00:00

abstract：:A computational approach which concomitantly determines the capacity-limited rate constants of parent drug elimination and metabolite formation is presented. The approach applies both the presently derived total excretory recovery versus dose relationships of the metabolite and the AUC versus dose relationships of the...

journal_title：Journal of pharmaceutical sciences

authors： Chow AT,Jusko WJ

更新日期：1990-10-01 00:00:00

abstract：:Release characteristics of two ethylated beta-cyclodextrins [heptakis(2,6-di-O-ethyl)-beta-cyclodextrin (diethyl-beta-cyclodextrin) and heptakis(2,3,6-tri-O-ethyl)-beta-cyclodextrin (triethyl-beta-cyclodextrin)] as sustained-release drug carriers were evaluated using diltiazem hydrochloride, a water-soluble calcium an...

journal_title：Journal of pharmaceutical sciences

authors： Horiuchi Y,Hirayama F,Uekama K

更新日期：1990-02-01 00:00:00

abstract：:Biopharmaceuticals represent an important and growing class of medicines. Immunogenic responses to biopharmaceuticals in patients can sometimes result in reduced safety and efficacy. Although multiple factors are known to influence immunogenicity, our understanding of the complex underlying mechanisms remains imperfec...

journal_title：Journal of pharmaceutical sciences

authors： Bee JS,Goletz TJ,Ragheb JA

更新日期：2012-10-01 00:00:00

abstract：:A theory of charge, fluid-mass, and solute (including macromolecular) transport through porous media is applied to describe transport phenomena across the external layer of mammalian skin. Linear relationships are derived between transport fluxes and applied fields. These relationships introduce six effective transder...

journal_title：Journal of pharmaceutical sciences

authors： Edwards DA,Langer R

更新日期：1994-09-01 00:00:00

abstract：:Protein immunogenicity is intensively researched by academics, biopharmaceutical companies, and authorities as it can compromise the safety and efficacy of a biopharmaceutical drug. So far, the exact protein aggregate properties inducing immune responses are not known. Possible protein-related factors could be size, c...

journal_title：Journal of pharmaceutical sciences

authors： Werner BP,Winter G

更新日期：2018-11-01 00:00:00

abstract：:Selected synthetic luteinizing hormone releasing hormone preparations were assayed, and their potencies were determined relative to one sample utilizing primary cultures of enzymatically dispersed rat anterior pituitary cells. Preliminary cell culture experiments indicated that luteinizing hormone releasing hormone ha...

journal_title：Journal of pharmaceutical sciences

authors： Dermody WC,Pastushok CA,Sakowski R,Vaitkus JW,Reel JR

更新日期：1977-03-01 00:00:00

abstract：:Metronidazole and four derivatives were studied in vitro to investigate the differences in the extent of their binding to plasma proteins. Modification at the terminal portion of the alkyl side chain resulted in wide differences in the extent of binding. Molecular orbital calculations were performed by the CNDO and MI...

journal_title：Journal of pharmaceutical sciences

authors： Sanvordeker DR,Chien YW,Lin TK,Lambert HJ

更新日期：1975-11-01 00:00:00