Fluorometric determination of trifluoromethyl-substituted 2,3-bis(4-methoxyphenyl)indoles in biological materials.

abstract：:We present a systematic evaluation of the Wajima superpositioning method to estimate the human intravenous (i.v.) pharmacokinetic (PK) profile based on a set of 54 marketed drugs with diverse structure and range of physicochemical properties. We illustrate the use of average of "best methods" for the prediction of cle...

journal_title：Journal of pharmaceutical sciences

authors： Lombardo F,Berellini G,Labonte LR,Liang G,Kim S

更新日期：2016-03-01 00:00:00

abstract：:Some fused pyridazino[4,5-b]indoles (7) were synthesized. These new compounds present a planar topography and some resemblance to carbazeram, imadozan, and other pyridazino agents with cardiotonic activity. These compounds also possess a complementary effect as inhibitors of platelet aggregation. 6-(3,5-Dimethylpyrazo...

journal_title：Journal of pharmaceutical sciences

authors： Monge A,Aldana I,Losa MJ,Font M,Castiella E,Frechilla D,Cenarruzabeitia E,Martinez de Irujo JJ,Lopez-Unzu J,Alberdi E

更新日期：1993-05-01 00:00:00

abstract：:AZD1175 and AZD2207 are 2 highly lipophilic compounds with a significant risk of not achieving therapeutic plasma concentrations due to solubility-limited absorption. The compounds have the same molecular weight and minimal structural differences. The aim of the present work was to investigate whether salts could be a...

journal_title：Journal of pharmaceutical sciences

authors： Tannergren C,Karlsson E,Sigfridsson K,Lindfors L,Ku A,Polentarutti B,Carlert S

更新日期：2016-11-01 00:00:00

abstract：:In recent years, controlled release coatings, comprised of drug-polymer composites, have been integrated with medical devices, improving device functionality and performance. However, relationships between material properties, manufacturing environment, composite (micro)structure, and subsequent release kinetics are n...

journal_title：Journal of pharmaceutical sciences

authors： Saylor DM,Kim CS,Patwardhan DV,Warren JA

更新日期：2009-01-01 00:00:00

abstract：:The synthesis, local anesthetic and antiarrhythmic properties, and CNS toxicity of 14 2-(3-alkylaminoalkylamido)-pyrroles are described. Most of the compounds exhibited local anesthetic activity by the guinea pig wheal test, with seven showing comparable or greater activity than lidocaine. Most compounds also exhibite...

journal_title：Journal of pharmaceutical sciences

authors： Sowell JW Sr,Block AJ,Derrick ME,Freeman JJ,Kosh JW,Mubarak PF,Tenthorey PA

更新日期：1981-05-01 00:00:00

abstract：:The ratio between ocular and systemic drug concentrations describes the relative safety of ophthalmic dosage forms of the same drug in terms of its systemic side effects. In this study, we evaluated the effects of epinephrine pretreatment and solution pH on the aqueous humor:plasma and iris-ciliary body:plasma ratios ...

journal_title：Journal of pharmaceutical sciences

authors： Kyyrönen K,Urtti A

更新日期：1990-08-01 00:00:00

abstract：:Some N,N'-bis(3-substituted benzylideneaminopropyl) piperazines were synthesized and characterized by their sharp melting points and elemental analyses. These substituted piperazines possessed anti-inflammatory activity, and the protection afforded by these compounds against carrageenan-induced edema ranged from 23 to...

journal_title：Journal of pharmaceutical sciences

authors： Chaturvedi AK,Sastry BV,Chaudhari A,Parmar SS

更新日期：1976-03-01 00:00:00

abstract：:Bisphosphonates are widely used for the treatment of bone diseases, including hypercalcemia and osteoporosis. However, the bioavailability (BA) of orally administered bisphosphonates is low, at approximately 0.9%-1.8%. In addition, the oral administration of bisphosphonates is associated with mucosal damage, including...

journal_title：Journal of pharmaceutical sciences

authors： Katsumi H,Takashima M,Sano J,Nishiyama K,Kitamura N,Sakane T,Hibi T,Yamamoto A

更新日期：2011-09-01 00:00:00

abstract：:The objective of the present research was to investigate the stability of an amorphous drug, Delta(9)-tetrahydrocannabinol (THC) in polymer-based transmucosal systems. THC was incorporated in polyethylene oxide and hydroxypropylcellulose matrices by a hot-melt fabrication procedure, utilizing various processing aids. ...

journal_title：Journal of pharmaceutical sciences

authors： Munjal M,Stodghill SP,Elsohly MA,Repka MA

更新日期：2006-08-01 00:00:00

abstract：:A physical model approach to the topical delivery of a vidarabine ester prodrug was investigated. It involved modeling, theoretical simulations, experimental method development for factoring and quantifying parameters, and, finally, employment of the deduced parameters to determine the steady-state species fluxes and ...

journal_title：Journal of pharmaceutical sciences

authors： Yu CD,Fox JL,Ho NF,Higuchi WI

更新日期：1979-11-01 00:00:00

abstract：:This work was to investigate the effects of particle size and paddle speed on the particle diffusional layer thickness h(app) in a USP dissolution apparatus II. After the determination of the powder dissolution rates of five size fractions of fenofibrate, including <20, 20-32, 32-45, 63-75, and 90-106 microm, the pres...

journal_title：Journal of pharmaceutical sciences

authors： Sheng JJ,Sirois PJ,Dressman JB,Amidon GL

更新日期：2008-11-01 00:00:00

abstract：:The objective of the present study was to investigate the iontophoretic transport behavior across multiple membranes of different barrier properties. Spectra/Por(R) (SP) and Ionac membranes were the synthetic membranes and sclera was the biomembrane in this model study. The barrier properties of SP membranes were dete...

journal_title：Journal of pharmaceutical sciences

authors： Molokhia SA,Zhang Y,Higuchi WI,Li SK

更新日期：2008-01-01 00:00:00

abstract：:Baclofen immediate release mode of administration exhibit sharp plasma peaking that results in the emergence of side effects like hypotension. This research employs preformulation studies to design an optimum dosage form for baclofen to enhance therapeutic outcomes. These studies include partition coefficient and ex-v...

journal_title：Journal of pharmaceutical sciences

authors： Ibrahim M,Naguib YW,Sarhan HA,Abdelkader H

更新日期：2020-10-15 00:00:00

abstract：:Isothermal crystallization of amorphous nifedipine, phenobarbital, and flopropione was studied at temperatures above and below their glass transition temperatures (T(g)). A sharp decrease in the crystallization rate with decreasing temperature was observed for phenobarbital and flopropione, such that no crystallizatio...

journal_title：Journal of pharmaceutical sciences

authors： Aso Y,Yoshioka S,Kojima S

更新日期：2000-03-01 00:00:00

abstract：:Acetylcarnitine, a naturally occurring compound found in high concentration in heart and skeletal muscle of vertebrates, bears structural resemblance to acetylcholine, and studies have shown that it has slight cholinergic properties. Acetylcarnitine was subjected to conformational analysis by extended Hückel theory (E...

journal_title：Journal of pharmaceutical sciences

authors： Reed KW,Murray WJ,Roche EB

更新日期：1980-09-01 00:00:00

abstract：:The degradation of batanopride hydrochloride, an investigational antiemetic drug, was studied in aqueous buffer solutions (pH 2-10; ionic strength, 0.5; 56 degrees C) in an attempt to improve drug stability for parenteral administration. Degradation occurs by two different mechanisms depending on the pH of the solutio...

journal_title：Journal of pharmaceutical sciences

authors： Nassar MN,House CA,Agharkar SN

更新日期：1992-11-01 00:00:00

abstract：:3-Fluoro-, 3-chloro-, and 3-bromocyclophosphamide were prepared from the reaction of trifluoromethylhypofluorite, sodium hypochlorite, and bromine with the anticancer drug cyclophosphamide. Treatment of cis- and trans-4-phenylcyclophosphamide and 5,6-benzocyclophosphamide with sodium hypochlorite afforded cis- and tra...

journal_title：Journal of pharmaceutical sciences

authors： Zon G,Ludeman SM,Ozkan G,Chandrasegaran S,Hammer CF,Dickerson R,Mizuta K,Egan W

更新日期：1983-06-01 00:00:00

abstract：:Stability of the 1,3,5-triazine derivative (1), a corticotropin-releasing factor inhibitor, was studied in acidic solutions and in solid formulations. Degradant structures were elucidated using liquid chromatography/mass spectrometry (LC/MS) and nuclear magnetic resonance (NMR). Compound 1 was found to undergo hydroly...

journal_title：Journal of pharmaceutical sciences

authors： Badawy S,Hussain M,Zhao F,Ye Q,Huang Y,Palaniswamy V

更新日期：2009-08-01 00:00:00

abstract：:The oral dose metabolism of dilazep dihydrochloride [tetrahydro-1H-1,4-diazepine-1,4(5H)-dipropanol 3,4,5-trimethoxybenzoate] was examined in six hypertensive patients receiving a single oral dose of 600 mg of dilazep (3-3.8 mg/kg BW). Blood was collected at 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, and 24 h after administratio...

journal_title：Journal of pharmaceutical sciences

authors： Sambhi MP,Kannan R,Thananopavarn C,Ookhtens M,Gudenzi M

更新日期：1989-04-01 00:00:00

abstract：:The promoting efficacies of N-acyl derivatives of amino acids on the rectal absorption of sodium ampicillin were investigated using the rat rectal loop technique. N-Acyl derivatives with longer carbon chains in the acyl moiety showed a greater promoting potency. The promoting potencies of N-acyl derivatives of phenylg...

journal_title：Journal of pharmaceutical sciences

authors： Wu WM,Murakami T,Higashi Y,Yata N

更新日期：1987-07-01 00:00:00

abstract：:17-Chloroacetylajmaline and 17-acetylajmaline are reported to have in vivo antiarrhythmic activity and are metabolized by hydrolysis. Since the hydrolysis product, ajmaline, may be the actual antiarrhythmic agent, the hydrolysis of these derivatives by various tissues of the guinea pig, rat, and mouse was determined i...

journal_title：Journal of pharmaceutical sciences

authors： Salmona M,Lakszner K,Fanelli R,Saronio C,Bianchi R,Mussini E

更新日期：1975-09-01 00:00:00

abstract：:In this paper we describe the synthesis and characterization of magnetic microcapsules, intended for use in vivo, and which contain polyethyleneimine nucleophilic targets capable of trapping electrophilic carcinogens. The microcapsules, 15-50 microns in diameter, consist of a semipermeable cross-linked nylon membrane ...

journal_title：Journal of pharmaceutical sciences

authors： Povey AC,Bartsch H,Nixon JR,O'Neill IK

更新日期：1986-09-01 00:00:00

abstract：:The objective of this study was to investigate the permeation-enhancing effect of thiolated polycarbophil (PCP) on peptide drugs. Mediated by a carbodiimide, increasing amounts of cysteine (Cys) were covalently bound to sodium neutralized PCP (NaPCP). The extent of covalently attached Cys was determined by quantifying...

journal_title：Journal of pharmaceutical sciences

authors： Clausen AE,Bernkop-Schnürch A

更新日期：2000-10-01 00:00:00

abstract：UNLABELLED:Given a good correlation between onsets of crystallization and mobility above T(g), one might be able to predict crystallization onsets at a temperature of interest far below T(g) from this correlation and measurement of mobility at a temperature below T(g). Such predictions require that: (a) correlation bet...

journal_title：Journal of pharmaceutical sciences

authors： Bhugra C,Shmeis R,Krill SL,Pikal MJ

更新日期：2008-01-01 00:00:00

abstract：:A method is presented for encapsulating high molecular weight biological materials such as viral antigen, concanavalin A, and other proteins with cellulose acetate phthalate. The method is simple, inexpensive, and rapid; the process takes approximately 15 min. Capsules generated by this method are produced as microsph...

journal_title：Journal of pharmaceutical sciences

authors： Maharaj I,Nairn JG,Campbell JB

更新日期：1984-01-01 00:00:00

abstract：:Methadyl acetate was metabolized by microsomal preparations of rat liver to yield nor-methadyl acetate and 6-(dimethylamino)-4,4-diphenyl-3-heptanol. The identification and separation of these three compounds was established by TLC, using iodoplatinate spray as a visualizing agent. ...

journal_title：Journal of pharmaceutical sciences

authors： Kochhar MM,Hamrick ME,Bavda LT

更新日期：1976-01-01 00:00:00

abstract：:The absorption of triazolam from pelleted drug-diet mixtures by mice under steady-state conditions was determined for doses up to 150 mg/kg/day by measuring alpha-hydroxytriazolam, the principal urinary metabolite of triazolam in the mouse, in urine samples collected over a 24-hour period. Following beta-glucuronide g...

journal_title：Journal of pharmaceutical sciences

authors： Adams WJ,Bombardt PA,Code RA

更新日期：1983-10-01 00:00:00

abstract：:In this article, we show that crystalline lactulose can be amorphized directly in the solid state by mechanical milling. Moreover, compared to similar materials, the amorphization kinetics of lactulose is found to be very rapid and the amorphous state thus obtained appears to be very stable against recrystallization o...

journal_title：Journal of pharmaceutical sciences

authors： Ngono F,Willart JF,Cuello G,Jimenez-Ruiz M,Affouard F

更新日期：2019-02-01 00:00:00

abstract：:To evaluate the regional delivery of conventional aerosol medications, a new whole-lung computational fluid dynamics modeling approach was applied for metered dose inhaler (MDI) and dry powder inhaler (DPI) aerosols delivered to healthy and constricted airways. The computational fluid dynamics approach included comple...

journal_title：Journal of pharmaceutical sciences

authors： Walenga RL,Longest PW

更新日期：2016-01-01 00:00:00

abstract：:Three novel series of 4-oxoquinazoline derivatives were prepared and evaluated as potential antimicrobial agents. Evaluation of the antimicrobial activity of a variety of 4-substituted-1-thiosemicarbazides, 3,4-disubstituted thiazolines, and 3-substituted-5-thiazolidones reveals that the majority possess significant i...

journal_title：Journal of pharmaceutical sciences

authors： Habib NS,Khalil MA

更新日期：1984-07-01 00:00:00