The Degradation Chemistry of GSK2879552: Salt Selection and Microenvironmental pH Modulation to Stabilize a Cyclopropyl Amine.

abstract：:Nonionic block copolymers are surfactants synthesized using propylene oxide and ethylene oxide, and they can be designed so that individual copolymers have unique vaccine adjuvant properties. We have designed and produced nonionic block copolymers based on high molecular weight (MW), 9-15 kDA, cores of poly(oxypropyle...

journal_title：Journal of pharmaceutical sciences

authors： Newman MJ,Todd CW,Balusubramanian M

更新日期：1998-11-01 00:00:00

abstract：:Phenytoin-loaded alkyd nanoemulsions were prepared spontaneously using the phase inversion method from a mixture of novel biosourced alkyds and Tween 80 surfactant. Exposure of human adult keratinocytes (HaCaT cells) for 48 h to alkyd nanoemulsions producing phenytoin concentrations of 3.125-200 μg/mL resulted in rela...

journal_title：Journal of pharmaceutical sciences

authors： Teo SY,Yew MY,Lee SY,Rathbone MJ,Gan SN,Coombes AGA

更新日期：2017-01-01 00:00:00

abstract：:Carboxy group-terminated synthetic polymers--branched poly(ethylene glycol), poly(acryloylmorpholine), and poly(vinylpyrrolidone)--were made amphiphilic by derivatization with phosphatidyl ethanolamine via the terminal carboxy group and then incorporated into lecithin-cholesterol liposomes prepared by the detergent di...

journal_title：Journal of pharmaceutical sciences

authors： Torchilin VP,Trubetskoy VS,Whiteman KR,Caliceti P,Ferruti P,Veronese FM

更新日期：1995-09-01 00:00:00

abstract：:Chlortetracycline was successfully separated from its degradation products and from other tetracyclines on a paper chromatogram previously impregnated with a mixture of edetate disodium and urea solution in pH 5.0 McIlvaine buffer. Chlortetracycline separation from its degradation products and from both tetracycline a...

journal_title：Journal of pharmaceutical sciences

authors： Youssef MK,Attia IA,Safwat S

更新日期：1978-04-01 00:00:00

abstract：:A method is described for screening compounds that inhibit crystallization in solution to enable more accurate measurement of amorphous drug solubility. Three polymers [polyvinylpyrrolidone, hydroxypropyl methylcellulose, and hydroxypropyl methylcellulose acetate succinate (HPMCAS)] were screened for their ability to ...

journal_title：Journal of pharmaceutical sciences

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

更新日期：2011-10-01 00:00:00

abstract：:Prostaglandin F2 alpha was administered intraamniotically to 132 mid-first trimester gravidas to determine the dose-24-hour abortifacient response relationship. Single doses between 15-50 mg and multiple doses between 15-25 mg were administered to 3 groups each, the latter regimen at 6-hour intervals. Trials were de...

journal_title：Journal of pharmaceutical sciences

authors： Brenner WE,Hendricks CH,Fishburne JI Jr,Staurovsky L,Braaksma J,Taft R

更新日期：1973-08-01 00:00:00

abstract：:The major route of degradation of tetrazepam (1) is oxidation to 7-chloro-5-(3-keto-cyclohexen-1-yl)-1,3-dihydro-1-methyl-2H-1, 4-benzodiazepin-2-one (3) via the stable 7-chloro-5-(3-hydroperoxy-cyclohexen-1-yl)-1,3-dihydro-1-methyl-2H -1, 4 benzodiazepin-2-one (2). Minor degradation products are 7-chloro-5-(1,2-epoxy...

journal_title：Journal of pharmaceutical sciences

authors： Boccardi G,Deleuze C,Gachon M,Palmisano G,Vergnaud JP

更新日期：1992-02-01 00:00:00

abstract：:The objective of this study was to establish the optimal blood concentrations of the potent P-glycoprotein (P-gp) inhibitor GF120918 (Elacridar) required to achieve maximal knockout of this efflux transporter in the blood-brain barrier (BBB) of mice, rats, and guinea pigs. Genetic mdr1a/b(-/-) knockout mice and "chemi...

journal_title：Journal of pharmaceutical sciences

authors： Cutler L,Howes C,Deeks NJ,Buck TL,Jeffrey P

更新日期：2006-09-01 00:00:00

abstract：:Water vapor absorption isotherms for amorphous solids with the same chemical composition but differing in molecular weight (i.e., PVP-90, PVP-30, and PVP-12), and for glucose, trehalose, and two molecular weight grades of dextran were obtained at 30 degrees C and analyzed using the Brunauer-Emmett-Teller (BET) equatio...

journal_title：Journal of pharmaceutical sciences

authors： Zhang J,Zografi G

更新日期：2000-08-01 00:00:00

abstract：:A hydraulic calcium phosphate cement made of beta-tricalcium phosphate [beta-Ca3(PO4)2], monocalcium phosphate monohydrate [Ca(H2PO4)2-H2O], and water was used as a delivery system for the antibiotic gentamicin sulfate (GS). GS, added as powder or as aqueous solution, was very beneficial to the physicochemical propert...

journal_title：Journal of pharmaceutical sciences

authors： Bohner M,Lemaître J,Van Landuyt P,Zambelli PY,Merkle HP,Gander B

更新日期：1997-05-01 00:00:00

abstract：:A series of even numbered fatty acid esters (C2-C18) of p-[N,N-bis(2-chloroethyl)amino]phenol were synthesized and evaluated as to acute toxicity as well as effectiveness against L-1210 mouse leukemia. The acetate through the decanoate derivatives demonstrated toxicity between 2 and 3 times that of phenol mustard in H...

journal_title：Journal of pharmaceutical sciences

authors： Wynn JE,Caldwell ML,Robinson JR,Beamer RL,Bauguess CT

更新日期：1982-07-01 00:00:00

abstract：:This study aims to investigate the drug-drug interactions (DDIs) between orally administered atorvastatin (ATV) and rifampicin (RIF) in rats. The isotope-IV method was used for the analysis of the increased systemic exposure (AUCpo) of ATV, in which a small amount of deuterium-labeled ATV (ATV-d5) was intravenously in...

journal_title：Journal of pharmaceutical sciences

authors： Yamashita S,Hasegawa T,Tachihara M,Minami K,Higashino H,Togashi K,Mutaguchi K,Kataoka M

更新日期：2017-09-01 00:00:00

abstract：:The role of particle size and surface modification on biodistribution of nanocarriers is widely reported. We report for the first time the role of nanoparticle shape on biodistribution. Our study demonstrates that irregular shaped polymer lipid nanoparticles (LIPOMER) evade kupffer cells and localize in the spleen. We...

journal_title：Journal of pharmaceutical sciences

authors： Devarajan PV,Jindal AB,Patil RR,Mulla F,Gaikwad RV,Samad A

更新日期：2010-06-01 00:00:00

abstract：:Ascorbic acid (100 mg/ml) and sodium bisulfite (0.5 and 20 mg/ml) prevented more than 10% oxidation of apomorphine hydrochloride in water maintained at room temperature over 1-3 days. Refrigeration at 5 degrees prevented oxidation of apomorphine hydrochloride in aqueous solutions for 1 week. Neither ascorbic acid nor ...

journal_title：Journal of pharmaceutical sciences

authors： Wilcox RE,Humphrey DW,Riffee WH,Smith RV

更新日期：1980-08-01 00:00:00

abstract：:The estimates of infinity values obtained using Prony's method are shown to be subject to significant error arising from small errors in the assigned sample times. The error of the estimate may be reduced by increasing the time interval between samples. ...

journal_title：Journal of pharmaceutical sciences

authors： Newburger J,Stavchansky S,Pearlman RS

更新日期：1980-10-01 00:00:00

abstract：:A pharmacokinetic study was performed in plasma and cerebrospinal fluid (CSF) of patients suffering from brain tumors to describe the disposition of methotrexate. An open three-compartment model was developed to fit together the data obtained in plasma and CSF. The pharmacokinetic parameters obtained by the model agre...

journal_title：Journal of pharmaceutical sciences

authors： Chatelut E,Roche H,Plusquellec Y,Peyrille F,De Biasi J,Pujol A,Canal P,Houin G

更新日期：1991-08-01 00:00:00

abstract：:Targeted echogenic liposome dispersions for ultrasonic enhancement of vasoactive and pathological components of endothelium and atherosclerosis have recently been developed. The component lipids required for acoustic and targeting properties include phosphatidylcholine, phosphatidylethanolamine phosphatidylglycerol (P...

journal_title：Journal of pharmaceutical sciences

authors： Huang SL,Hamilton AJ,Nagaraj A,Tiukinhoy SD,Klegerman ME,McPherson DD,Macdonald RC

更新日期：2001-12-01 00:00:00

abstract：:The blood-brain barrier permeation has been investigated by using a topological substructural molecular design approach (TOPS-MODE). A linear regression model was developed to predict the in vivo blood-brain partitioning coefficient on a data set of 119 compounds, treated as the logarithm of the blood-brain concentrat...

journal_title：Journal of pharmaceutical sciences

authors： Cabrera MA,Bermejo M,Pérez M,Ramos R

更新日期：2004-07-01 00:00:00

abstract：:This work investigated the feasibility of developing benznidazole (BZL) tablets, allowing fast, reproducible, and complete drug dissolution, by compressing BZL-Polyethylene Glycol (PEG) 6000 physical mixtures (PMs) and solid dispersions (SDs). SDs were prepared by the solvent evaporation method at different drug:polym...

journal_title：Journal of pharmaceutical sciences

authors： Leonardi D,Salomon CJ

更新日期：2013-03-01 00:00:00

abstract：:Chitosan microspheres were evaluated for sustained-release of recombinant human interleukin-2 (rIL-2) in this study. In addition, the effects of different formulation factors, such as chitosan and protein concentrations, the volume of sodium sulfate solution, addition technique of rIL-2, and presence of glutaraldehyde...

journal_title：Journal of pharmaceutical sciences

authors： Ozbaş-Turan S,Akbuğa J,Aral C

更新日期：2002-05-01 00:00:00

abstract：:A stability-specific high-pressure liquid chromatographic (HPLC) method was developed to assay intact chlorambucil (I) in the presence of its hydrolytic decomposition products. The HPLC method was used to follow the degradation kinetics of I over pH 1.0-10.0 in the presence of various buffers with and without added ch...

journal_title：Journal of pharmaceutical sciences

authors： Chatterji DC,Yeager RL,Gallelli JF

更新日期：1982-01-01 00:00:00

abstract：:A single method for the quantitative determinations of three active ingredients, phenylephrine hydrochloride, phenylpropanolamine hydrochloride, and brompheniramine maleate, and one inactive ingredient (sodium benzoate) in a commercial product for colds is reported. The method is based on paired ion high-pressure liqu...

journal_title：Journal of pharmaceutical sciences

authors： Ghanekar AG,Das Gupta V

更新日期：1978-06-01 00:00:00

abstract：:A GLC assay to quantitate the methaqualone metabolite 2-methyl-3-(2-hydroxymethylphenyl)-4(3H)-quinazolinone was developed. Standard curves were linear, and recovery of the metabolite from tissue homogenates averaged 89%. In vitro metabolism of methaqualone by the 10,000Xg supernatant fraction of rat liver homogenate ...

journal_title：Journal of pharmaceutical sciences

authors： Hindmarsh KW,Hamon NW,LeGatt DF,Wallace SM

更新日期：1978-11-01 00:00:00

abstract：:To relate the reported positive effect of food on the oral bioavailability of abiraterone to the intraluminal behavior of abiraterone acetate, an in vivo experiment was performed, in which duodenal fluids and plasma samples were collected from healthy volunteers after the administration of abiraterone acetate in faste...

journal_title：Journal of pharmaceutical sciences

authors： Geboers S,Stappaerts J,Mols R,Snoeys J,Tack J,Annaert P,Augustijns P

更新日期：2016-09-01 00:00:00

abstract：:Responses from the second Product Quality Research Institute (PQRI) Blend Uniformity Working Group (BUWG) survey of industry have been reanalyzed to identify potential links between formulation and processing variables and the measured uniformity of blends and unit dosage forms. As expected, the variability of the ble...

journal_title：Journal of pharmaceutical sciences

authors： Hancock BC,Garcia-Munoz S

更新日期：2013-03-01 00:00:00

abstract：:One manifestation of cystic fibrosis (CF) is the presence of a viscid mucus secretion in the lungs. The clearance of this mucus is significantly slower than in "normals" due to uncoordinated beating of the cilia and the increased viscosity of the mucus. In these studies, the permeabilities of p-aminosalicylic acid, is...

journal_title：Journal of pharmaceutical sciences

authors： Bhat PG,Flanagan DR,Donovan MD

更新日期：1996-06-01 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 poor aqueous solubility of carbamazepine was dramatically increased via complexation with various chemically modified beta-cyclodextrins and gamma-cyclodextrins. A preparation of carbamazepine and 2-hydroxypropyl-beta-cyclodextrin was found to be stable to steam sterilization and to storage under a variety of cond...

journal_title：Journal of pharmaceutical sciences

authors： Brewster ME,Anderson WR,Estes KS,Bodor N

更新日期：1991-04-01 00:00:00

abstract：:The pathogenic bacterium Staphylococcus aureus can penetrate host cells. However, intracellular S. aureus is not considered during antimicrobial agent selection in clinical chemotherapy because of the lack of information about drug transportability into cells in vivo. We focused on agents used to treat methicillin-res...

journal_title：Journal of pharmaceutical sciences

authors： Kobuchi S,Kita Y,Hiramatsu Y,Sasaki K,Uno T,Ito Y,Sakaeda T

更新日期：2021-02-01 00:00:00

abstract：:The extent of formation of solasodiene from solasodine upon treatment with hydrochloric acid under various conditions was determined. The diene formed was assayed by using the characteristic extinction at 236 nm. Diene formation was effected by the acid concentration and the boiling point of the solvent used. Optimal ...

journal_title：Journal of pharmaceutical sciences

authors： Segal R,Breuer A,Milo-Goldzweig I

更新日期：1978-08-01 00:00:00