A novel method for determination of drug solubility in polymeric matrices.

abstract：:The pharmacokinetics of erythromycin and erythromycin 2'-propanoate were studied in healthy male volunteers following single and repeated doses of erythromycin stearate tablets, erythromycin estolate capsules, and a suspension. Estolate dosages gave rise to higher plasma levels of total drug than the stearate. However...

journal_title：Journal of pharmaceutical sciences

authors： Welling PG,Elliott RL,Pitterle ME,Corrick-West HP,Lyons LL

更新日期：1979-02-01 00:00:00

abstract：:The metabolism of tocainide, an experimental antiarrhythmic drug, was studied in humans. Urinary excretion of unchanged drug was 28-55% in 24 hr after oral dosing. Urine hydrolysis with hydrochloric acid or beta-glucuronidase increased tocainide recovery to 55-79%. Saccharo-1,4-lactone inhibited the beta-glucuronidase...

journal_title：Journal of pharmaceutical sciences

authors： Elvin AT,Keenaghan JB,Byrnes EW,Tenthorey PA,McMaster PD,Takman BH,Lalka D,Manion CV,Baer DT,Wolshin EM,Meyer MB,Ronfeld RA

更新日期：1980-01-01 00:00:00

abstract：:The pharmacokinetics of tamsulosin (TAM) was investigated using male Sprague-Dawley rats in which plasma alpha(1)-acid glycoprotein (alpha(1)-AGP) levels were elevated by the subcutaneous injection of 0.2 mL/kg of turpentine oil. alpha(1)-AGP levels increased about eight times after turpentine oil treatment, causing a...

journal_title：Journal of pharmaceutical sciences

authors： Matsushima H,Watanabe T,Higuchi S

更新日期：2000-04-01 00:00:00

abstract：:The objective was to examine the influence of Pluronic block-copolymers on the interaction between the drug efflux transporter, P-glycoprotein and HIV-1 protease inhibitors (PIs). The ATPase assay determined the effect of various Pluronics on PI-stimulated P-gp ATPase activity. Cellular accumulation studies were condu...

journal_title：Journal of pharmaceutical sciences

authors： Shaik N,Pan G,Elmquist WF

更新日期：2008-12-01 00:00:00

abstract：:Two previously reported but unidentified phenylburazone degradation products were isolated from a tablet that was stored at 60 degrees for 203 days. The compounds, alpha-(N-phenylcarbamoyl)-N-caproylhydrazobenzene and alpha-hydroxy-alpha-(N-phenylcarbamoyl)-N-caproylhydrazobenzene, were isolated by chromatography, ide...

journal_title：Journal of pharmaceutical sciences

authors： Matsui F,Robertson DL,Poirier MA,Lovering EG

更新日期：1980-04-01 00:00:00

abstract：:Contraceptive natural steroids, such as progesterone and estradiol, are ineffective when administered orally because of extensive metabolism in the gastrointestinal (GI) tract during absorption and first-pass metabolism. Consequently, highly potent and potentially harmful synthetic steroids are now being used in oral...

journal_title：Journal of pharmaceutical sciences

authors： Hussain AA,Hirai S,Bawarshi R

更新日期：1981-04-01 00:00:00

abstract：:This work establishes a predictive model that explicitly recognizes microstructural parameters in the description of the overall mass uptake and local gradients of moisture into tablets. Model equations were formulated based on local tablet geometry to describe the transient uptake of moisture. An analytical solution ...

journal_title：Journal of pharmaceutical sciences

authors： Klinzing GR,Zavaliangos A

更新日期：2016-08-01 00:00:00

abstract：:Approximately 30% of active pharmaceutical ingredients (APIs) experience agglomeration, granulation, and breakage during agitated drying. Currently, there is no small-scale bench tool to help assess and observe granulation behavior of APIs in the laboratory and subsequently lead to the development of a robust drying m...

journal_title：Journal of pharmaceutical sciences

authors： Zhang S,Lamberto DJ

更新日期：2014-01-01 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：:We extend and modify the Noyes-Whitney equation and the Hixon-Crowell cube root law to include surface roughness effects on the dissolution rate of drugs. The problem is treated theoretically in terms of the fractal reaction dimension, DR, of the effective surface which undergoes dissolution. Effects of changes in DR ...

journal_title：Journal of pharmaceutical sciences

authors： Farin D,Avnir D

更新日期：1992-01-01 00:00:00

abstract：:An aqueous solution of trimedoxime bromide, atropine, and benactyzine hydrochloride was formulated to have maximum stability as an antidote in organophosphorus poisoning. The stability of the mixture in glass and plastic cartridges was determined. Glass cartridges were more desirable than plastic; there was less vapor...

journal_title：Journal of pharmaceutical sciences

authors： Zvirblis P,Ellin RI

更新日期：1982-03-01 00:00:00

abstract：:The absorption of the model drug carbenoxolone was reevaluated using an in situ rat intestinal perfusion technique in which disappearance from the intestinal lumen, binding to the perfused jejunal segment, and appearance in the mesenteric (jejunal) vein were measured. The effect of the degree of ionization on these pr...

journal_title：Journal of pharmaceutical sciences

authors： Blanchard J,Tang LM,Earle ME

更新日期：1990-05-01 00:00:00

abstract：:There is a growing clinical interest in developing and commercializing pharmaceutical-grade cannabinoid products, containing primarily tetrahydrocannabinol (THC) and cannabidiol (CBD). The oral bioavailability of THC and CBD is very low due to extensive "first-pass" metabolism. A novel oral THC and CBD formulation, PT...

journal_title：Journal of pharmaceutical sciences

authors： Atsmon J,Cherniakov I,Izgelov D,Hoffman A,Domb AJ,Deutsch L,Deutsch F,Heffetz D,Sacks H

更新日期：2018-05-01 00:00:00

abstract：:An Amended Solvation Energy Relationship (ASER) was recently reported to successfully predict the aqueous solubilities of a set of 664 organic compounds. The average absolute error and root mean square error are 0.43 and 0.62 log units, respectively. When the General Solubility Equation (GSE) is applied to the same se...

journal_title：Journal of pharmaceutical sciences

authors： Yang G,Ran Y,Yalkowsky SH

更新日期：2002-02-01 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：:A new solid-state form of cyclosporine produced by spray-drying exhibited characteristics consistent with a liquid crystal. No sharp diffraction peaks were observed by powder X-ray diffraction; however, analysis by both small-angle X-ray diffraction (SAXR) and microscopic under polarized light (PLM) confirmed the exis...

journal_title：Journal of pharmaceutical sciences

authors： Lechuga-Ballesteros D,Abdul-Fattah A,Stevenson CL,Bennett DB

更新日期：2003-09-01 00:00:00

abstract：:Absorption rates of monobasic beta-lactam antibiotics were measured as a function of lumen solution pH between 4 and 9 by utilizing the rat intestinal recirculating method in situ. Between pH 6.5 and 9, the absorption rate constants of ionized antibiotics were almost identical; but, at pH 4, the unionized species were...

journal_title：Journal of pharmaceutical sciences

authors： Tsuji A,Miyamoto E,Kubo O,Yamana T

更新日期：1979-07-01 00:00:00

abstract：:In this study the relationships between previously reported connectivity indices described by Kier and Hall and steric contributions to the rate constants for several series of reactions are examined. Rate data were examined for four different series of reactions, which were chosen to represent a range of different re...

journal_title：Journal of pharmaceutical sciences

authors： Schug JC,Viers JW,Seeman JI

更新日期：1984-10-01 00:00:00

abstract：:The aim of this study to administer hydrocortisone (HC) percutaneously in the form of polymeric nanoparticles (NPs) to alleviate its transcutaneous absorption, and to derive additional wound-healing benefits of chitosan. HC-loaded NPs had varied particle sizes, zeta potentials, and entrapment efficiencies, when drug-t...

journal_title：Journal of pharmaceutical sciences

authors： Hussain Z,Katas H,Amin MC,Kumulosasi E,Sahudin S

更新日期：2013-03-01 00:00:00

abstract：:Two polymorphs of celastrol were discovered and fully characterized by X-ray powder diffraction, thermogravimetry analysis, and differential scanning calorimetry. The single-crystal structures of form I and the isostructural solvate of form II were disclosed by single-crystal X-ray diffraction. The apparent solubility...

journal_title：Journal of pharmaceutical sciences

authors： Zha J,Zhang Q,Li M,Wang JR,Mei X

更新日期：2018-11-01 00:00:00

abstract：:A series of unrelated steroids were tested for antimineralocorticoid activity by Kagawa's test in male rats and by modified test in female rats. Adrenalectomized male rats given 12 mcg desoxycorticosterone (DOC) and 2.5 ml normal saline received 1 mg of the test steroid, and their urine was analyzed for sodium and po...

journal_title：Journal of pharmaceutical sciences

authors： Solymoss B,Krajny M,Varga S

更新日期：1970-05-01 00:00:00

abstract：:The aim of this study was to investigate the bioavailability enhancement of the biopharmaceutics classification system class II compound ezetimibe loaded in ordered mesoporous silica (OMS) in dogs. The OMS was characterized as highly ordered mesoporous material with a narrow pore size distribution. Ezetimibe was loade...

journal_title：Journal of pharmaceutical sciences

authors： Kiekens F,Eelen S,Verheyden L,Daems T,Martens J,Van Den Mooter G

更新日期：2012-03-01 00:00:00

abstract：:The aim of this work was to optimize the absorption of parathyroid hormone 1-34 (PTH) from the lungs by determining factors favoring its transport from the air spaces into the bloodstream. We simultaneously conducted pharmacokinetic and regional lung deposition studies in vivo in the rat following intratracheal admini...

journal_title：Journal of pharmaceutical sciences

authors： Codrons V,Vanderbist F,Ucakar B,Préat V,Vanbever R

更新日期：2004-05-01 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：:A rapid and simple high-performance liquid chromatographic (HPLC) method for the analysis of dichlorophen in raw material and in dichlorophen-toluene soft gelatin capsules for veterinary use was developed using a reverse-phase technique. This HPLC system was shown to isolate dichlorophen from its major impurity (the t...

journal_title：Journal of pharmaceutical sciences

authors： Shah KA,Samuels SA,Michaels MK,Warren JW

更新日期：1984-06-01 00:00:00

abstract：:The use of various synthetic lipids and polymers to deliver DNA for gene therapy applications has been the subject of intense examination for the last 15 years. Our understanding of the processes involved in the delivery of DNA, although still limited, can be described in terms of specific physical and chemical barrie...

journal_title：Journal of pharmaceutical sciences

authors： Wiethoff CM,Middaugh CR

更新日期：2003-02-01 00:00:00

abstract：:Midazolam (MDZ) is a benzodiazepine commonly administered in preanesthesia of children by oral or by sublingual routes. To mask its bitter taste and enhance its aqueous solubility, we already developed a 0.2% (w/v) MDZ oral solution containing γ-cyclodextrin (γ-CD), which proves to be better accepted by children in pe...

journal_title：Journal of pharmaceutical sciences

authors： Mathiron D,Marçon F,Dubaele JM,Cailleu D,Pilard S,Djedaïni-Pilard F

更新日期：2013-07-01 00:00:00

abstract：:Spray freeze-drying is an evolving technology that combines the benefits of spray-drying and conventional lyophilization techniques to produce drug substance and drug product as free-flowing powders. The high surface-to-volume ratio associated to the submillimeter spray-frozen particles contributes to shorter drying a...

journal_title：Journal of pharmaceutical sciences

authors： Sebastião IB,Bhatnagar B,Tchessalov S,Ohtake S,Plitzko M,Luy B,Alexeenko A

更新日期：2019-06-01 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：:The crystal and molecular structures of 6-methylmercaptopurine trihydrate and of azathioprine dihydrate were determined by the use of three-dimensional, X-ray, diffractometer data and were refined by least squares. Both molecules crystallize in the N(9)-H tautomer form, in contrast to the N(7)-H tautomer form found in...

journal_title：Journal of pharmaceutical sciences

authors： Cook WJ,Bugg CE

更新日期：1975-02-01 00:00:00