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

abstract：:The objective of this study was to propose novel surface-modified nanostructured lipid carriers with partially deacetylated water-soluble chitosan (NLC-PDSC) as an efficient ocular delivery system to improve its transcorneal penetration and precorneal retention. PDSC with a deacetylation degree of around 50% was synth...

journal_title：Journal of pharmaceutical sciences

authors： Tian B,Luo Q,Song S,Liu D,Pan H,Zhang W,He L,Ma S,Yang X,Pan W

更新日期：2012-03-01 00:00:00

abstract：:Two novel series of steroidal derivatives containing various thiourea and substituted thiazoline moieties attached to the 2- or 4-position of estrone were synthesized and examined for in vitro effect on bovine pancreatic ribonuclease activity. All compounds studied exhibited a catabolic activity. The steroidal thiazol...

journal_title：Journal of pharmaceutical sciences

authors： Ibrahim ES,Omar AM,Habib NS,Aboulwafa OM,El-Sewedy SM,Bourdais J

更新日期：1983-10-01 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：:The purpose of the present study was to develop a physiologically based pharmacokinetic model for dextromethorphan (DEX) and its metabolites in extensive and poor metabolizers. The model was used to study the influence of dissolution rates on the sensitivity of maximum plasma concentration and area under the concentra...

journal_title：Journal of pharmaceutical sciences

authors： Bolger MB,Macwan JS,Sarfraz M,Almukainzi M,Löbenberg R

更新日期：2019-01-01 00:00:00

abstract：:The objective of this article was to monitor phase transformation in thiamine hydrochloride, from a nonstoichiometric hydrate (NSH) to a hemihydrate (HH), in stored tablets, prepared both by direct compression and wet granulation, and to relate the storage-induced phase transformation with changes in tablet microstruc...

journal_title：Journal of pharmaceutical sciences

authors： Chakravarty P,Suryanarayanan R,Govindarajan R

更新日期：2012-04-01 00:00:00

abstract：:6-Amino-2-mercapto-5-methylpyrimidine-4-carboxylic acid proved to be a potent hypolipidemic agent in rodents at the low dose of 20 mg/kg/d. The agent effectively reduced the liver enzyme activities required for the synthesis of triglycerides and cholesterol. Lower lipid levels in tissue were observed in mice but not i...

journal_title：Journal of pharmaceutical sciences

authors： Hall IH,Cocolas GH,Murthy AR,Rhyne KA,Knowles M

更新日期：1985-07-01 00:00:00

abstract：:The assessment of provenance of heparin is becoming a major concern for the pharmaceutical industry and its regulatory bodies. Batch-specific [carbon (δ(13) C), nitrogen (δ(15) N), oxygen (δ(18) O), sulfur (δ(34) S), and hydrogen (δD)] stable isotopic compositions of five different animal-derived heparins were perform...

journal_title：Journal of pharmaceutical sciences

authors： Jasper JP,Zhang F,Poe RB,Linhardt RJ

更新日期：2015-02-01 00:00:00

abstract：:Two nonporous and three porous amorphous silicas were used as dispersion media to convert corticoid solutions into free-flowing powders. The corticoids (prednisone, prednisolone, and hydrocortisone) were dissolved in N,N-dimethylacetamide-polyethylene glycol 400 (7:3 v/v) and their 10% (w/v) solutions were mixed with ...

journal_title：Journal of pharmaceutical sciences

authors： Liao CC,Jarowski CI

更新日期：1984-03-01 00:00:00

abstract：:Statistical assessment of bioavailability and bioequivalence of drug products is generally carried out with a univariate analysis by independently comparing each relevant parameter [such as, area under the drug concentration curve (AUC) and peak drug concentration (Cmax)] of the test and reference products. The assump...

journal_title：Journal of pharmaceutical sciences

authors： Hsu HC,Lu HL,Chan KK

更新日期：1995-06-01 00:00:00

abstract：:This study aimed to investigate the surface energy factors behind improved aerosolization performance of spray-dried colistin powder formulations compared with those produced by jet milling. Inhalable colistin powder formulations were produced by jet milling or spray drying (with or without l-leucine). Scanning electr...

journal_title：Journal of pharmaceutical sciences

authors： Jong T,Li J,Morton DA,Zhou QT,Larson I

更新日期：2016-03-01 00:00:00

abstract：:Homologous series of L-methionine alkyl ester hydrochlorides and tosylates were synthesized and evaluated for in vitro growth inhibitory activity in Meth A sarcoma. Cytotoxicity, as determined by [3H]thymidine incorporation, was found to be directly proportional to alkyl chain length and surface tension lowering activ...

journal_title：Journal of pharmaceutical sciences

authors： Clement MA,Chapman JM,Roberts J

更新日期：1989-06-01 00:00:00

abstract：:The kinetics and pathways for degradation of (+/-)-4'-ethyl-2-methyl-3-(1-pyrrolidinyl)propiophenone hydrochloride (HY-770; 1), a newly developed muscle-relaxing agent, and its analogues were studied in aqueous solution at 50 degrees C, ionic strength 0.5 M, and pH 8.0-12.0. Compound 1 and its four analogues followed ...

journal_title：Journal of pharmaceutical sciences

authors： Nagata O,Terasaki T,Yada E,Sato H,Tamai I,Tsuji A

更新日期：1989-01-01 00:00:00

abstract：:This whitepaper highlights current challenges and opportunities associated with continuous synthesis, workup, and crystallization of active pharmaceutical ingredients (drug substances). We describe the technologies and requirements at each stage and emphasize the different considerations for developing continuous proc...

journal_title：Journal of pharmaceutical sciences

authors： Baxendale IR,Braatz RD,Hodnett BK,Jensen KF,Johnson MD,Sharratt P,Sherlock JP,Florence AJ

更新日期：2015-03-01 00:00:00

abstract：:A kinetic dialysis technique together with a radiolabeled chenodeoxycholate (CDC) was used to determine the existence of a relationship between the monomer concentration of CDC and the total CDC concentration in different CDC solutions containing 1 or 5 mM sulfobutylether (SBE)-β-cyclodextrin. On the basis of the natu...

journal_title：Journal of pharmaceutical sciences

authors： Liu CL,Chang CL,Jhou SY,Higuchi WI

更新日期：2012-08-01 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：:Three families of alloxan derivatives, 5-arylthiobarbituric, 5-aryliminobarbituric, and 5-aryldialuric acids, were prepared as prospective radioiodine-transporting radiopharmaceuticals for the delineation of pancreatic insulinomas. Members of each class were screened for effects on blood sugar levels in a rat glucose ...

journal_title：Journal of pharmaceutical sciences

authors： Adams WE,Heindel ND,Tutwiler G,Fawthrop H

更新日期：1984-03-01 00:00:00

abstract：:Nasal drug delivery is an interesting route of administration for dihydroergotamine in migraine therapy. The currently available formulation contains dihydroergotamine at 4 mg/mL. For a nasal dose of 2 mg, a volume of 0.5 mL has to be administered, which sometimes leads to spillage of the formulation. The aim of the p...

journal_title：Journal of pharmaceutical sciences

authors： Marttin E,Romeijn SG,Verhoef JC,Merkus FW

更新日期：1997-07-01 00:00:00

abstract：:The central compartment of an n-compartment mammillary model was concatenated with a gradient compartment (i.e., venous sampling compartment) and with a conventional effect compartment to model arterial-venous drug concentration gradients and the arterial drug concentration vs effect relationship, respectively. To mod...

journal_title：Journal of pharmaceutical sciences

authors： Jacobs JR,Nath PA

更新日期：1995-03-01 00:00:00

abstract：:Aqueous solutions of several ionizable substances were stored in plastic infusion bags and the sorption of the substances monitored with time. The substances used were p-nitrophenol, p-toluidine, warfarin sodium [3-(alpha-acetonylbenzyl)-4-hydroxycoumarin sodium salt] and trifluoperazine hydrochloride (10-[3-(4-methyl...

journal_title：Journal of pharmaceutical sciences

authors： Kowaluk EA,Roberts MS,Polack AE

更新日期：1986-06-01 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：:A model for estimating in vivo skin permeability coefficients for finite doses is presented. The ratio of the maximum value of the excretion rate to the steady-state flux is a function of the thickness of the applied vehicle and the vehicle-skin partition coefficient. The decay rate of the excretion is a function of s...

journal_title：Journal of pharmaceutical sciences

authors： Cooper ER,Berner B

更新日期：1985-10-01 00:00:00

abstract：:We investigated the effects of excipients in solutions of keratinocyte growth factor 2 (KGF-2) on protein aggregation during agitation as well as on interfacial shear rheology at the air-water interface. Samples were incubated with or without agitation, and in the presence or absence of the excipients heparin, sucrose...

journal_title：Journal of pharmaceutical sciences

authors： Liu L,Qi W,Schwartz DK,Randolph TW,Carpenter JF

更新日期：2013-08-01 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：: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：:The pharmacokinetics of drug delivery from transdermal controlled-release devices consisting of (a) a membrane plus a reservoir or (b) a monolithic slab are examined. For the period when the devices act as if the drug reservoir were infinite, simple relationships for the steady-state slope and time lag are derived and...

journal_title：Journal of pharmaceutical sciences

authors： Berner B

更新日期：1985-07-01 00:00:00

abstract：:The present study aimed to develop optimized quercetin (QT)-loaded self-nanoemulsifying drug delivery system (SNEDDS) that offers protective effect against liver damage. Solubility study of QT in different oils, surfactants, and cosurfactants was performed. Ternary phase mixtures of the selected components were constr...

journal_title：Journal of pharmaceutical sciences

authors： Ahmed OA,Badr-Eldin SM,Tawfik MK,Ahmed TA,El-Say KM,Badr JM

更新日期：2014-02-01 00:00:00

abstract：:New methods are being applied to distinguish silicone oil droplets from subvisible particles in therapeutic protein formulations. The need to standardize these methods and compare them to established methods is critical to increase the understanding of the risks from protein aggregation and other subvisible particulat...

journal_title：Journal of pharmaceutical sciences

authors： Vandesteeg N,Kilbert C

更新日期：2013-06-01 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：:In an attempt to explain the triamterene stone diathesis, we studied the excretion and solubility of triamterene, 1, and its metabolite, the sulfate ester of the hydroxy derivative of triamterene, 3. The urinary excretion pattern and metabolism in stone formers was the same as in other chronic users of triamterene or ...

journal_title：Journal of pharmaceutical sciences

authors： Sörgel F,Ettinger B,Benet LZ

更新日期：1986-02-01 00:00:00

abstract：:The viscosity and surface tension of systems containing small amounts of salicylic acid in aqueous solutions of cetrimide were determined. An abrupt increase in viscosity was observed, and the molar ratio of salicylic acid to certrimide at which this viscosity increase occurred was 1:2. The surface tension of these sy...

journal_title：Journal of pharmaceutical sciences

authors： Wan LS

更新日期：1977-12-01 00:00:00