A novel class of cardiotonic agents: synthesis and biological evaluation of pyridazino[4,5-b]indoles with cyclic AMP phosphodiesterases inhibiting properties.

abstract：:Three series of 3,4,5-trisubstituted pyrazolesulfonylurea derivatives were prepared and evaluated as hypoglycemic agents. Preliminary biological testing revealed that the new compounds possess moderate hypoglycemic activity. ...

journal_title：Journal of pharmaceutical sciences

authors： Soliman R,Mokhtar H,Mohamed HF

更新日期：1983-09-01 00:00:00

abstract：:In liver microsomes, selexipag (NS-304; ACT-293987) mainly undergoes hydrolytic removal of the sulfonamide moiety by carboxylesterase 1 (CES1) to yield the pharmacologically active metabolite MRE-269 (ACT-333679). However, it is not known how much CES in the liver and intestine contributes to the hydrolysis of selexip...

journal_title：Journal of pharmaceutical sciences

authors： Imai S,Ichikawa T,Sugiyama C,Nonaka K,Yamada T

更新日期：2019-02-01 00:00:00

abstract：:The purpose of this study was to understand the combined effect of two polymers showing drug-polymer interactions on amorphous stabilization and dissolution enhancement of indomethacin (IND) in amorphous ternary solid dispersions. The mechanism responsible for the enhanced stability and dissolution of IND in amorphous...

journal_title：Journal of pharmaceutical sciences

authors： Prasad D,Chauhan H,Atef E

更新日期：2014-11-01 00:00:00

abstract：:Dissolving microneedle patches offer promise as a simple, minimally invasive method of drug and vaccine delivery to the skin that avoids the need for hypodermic needles. However, it can be difficult to control the amount and localization of drug within microneedles. In this study, we developed novel microneedle design...

journal_title：Journal of pharmaceutical sciences

authors： Chu LY,Choi SO,Prausnitz MR

更新日期：2010-10-01 00:00:00

abstract：:By the use of NMR spectroscopy, the highly colored reaction products formed by ouabain or digitoxin in with 1,3,5-trinitrobenzene or 2,4,6-trinitroanisole in the presence of alkali (as used for the determination of these glycosides) are shown to be Meisenheimer complexes. The complexes are produced by attachment of a ...

journal_title：Journal of pharmaceutical sciences

authors： Burns LB,Stedman RJ,Tuckerman MM

更新日期：1977-05-01 00:00:00

abstract：:Variability in the time to crystallization is a major technical and economic hurdle in using amorphous solids in dosage forms. It is hypothesized that amorphous solids "age", and that the older they are, the more relaxed they are and the higher the probability of crystallization. At present, there is no method that al...

journal_title：Journal of pharmaceutical sciences

authors： Hilden LR,Morris KR

更新日期：2003-07-01 00:00:00

abstract：:Previous studies from this laboratory suggested that a solution model (Flory-Huggins equation) modified by a free volume model (Vrentas equation) could satisfactorily describe water absorption into an amorphous solid composed of a sugar or a polymer. This paper has extended the studies of single solutes to binary mixt...

journal_title：Journal of pharmaceutical sciences

authors： Zhang J,Zografi G

更新日期：2001-09-01 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：:Intravenously administered (i.v.) drug-cyclodextrin (CD) inclusion complexes are generally expected to dissociate rapidly and completely, such that the i.v. pharmacokinetic profile of a drug is unchanged in the presence of CD. The altered pharmacokinetics of a synthetic ozonide in rats has been attributed to an unusua...

journal_title：Journal of pharmaceutical sciences

authors： Leong NJ,Prankerd RJ,Shackleford DM,Mcintosh MP

更新日期：2015-04-01 00:00:00

abstract：:Safety evaluation of self-assembled polymeric micelles is important for biomedical involvement in drug delivery systems in the future. In this study, biodegradable monomethyl poly (ethylene glycol)-poly (ε-caprolactone)-poly (trimethylene carbonate) [MPEG-P(CL-co-TMC)] copolymer was synthesized and characterized by Fo...

journal_title：Journal of pharmaceutical sciences

authors： Yang X,Cao D,Wang N,Sun L,Li L,Nie S,Wu Q,Liu X,Yi C,Gong C

更新日期：2014-01-01 00:00:00

abstract：:A high-performance liquid chromatographic method for the determination of (Z)- and (E)-doxepin hydrochloride isomers was developed. The analysis employs a column packed with spherical silica microparticles (5-6 mum), and a mobile phase of acetonitrile-chloroform-diethylamine (750:250:0.2) permits baseline resolution a...

journal_title：Journal of pharmaceutical sciences

authors： Whall TJ,Dokladalova J

更新日期：1979-11-01 00:00:00

abstract：:N-Acetyl-DL-penicillamine (IIIb), a structural analog of N-acetyl-L-cysteine (IIIa), did not protect mice from lethal doses of acetaminophen (I), whereas IIIa offered protection. This lack of efficacy of IIIb probably is due to the decreased nucleophilicity of its sulfhydryl group compared to that of IIIa, the probabl...

journal_title：Journal of pharmaceutical sciences

authors： Zera RT,Nagasawa HT

更新日期：1980-09-01 00:00:00

abstract：:4,5-Dimethoxykynuramine was synthesized in a three-step sequence originating with veratrole. Indirect evidence indicates that the drug was converted in vivo to the hypotensive agent 6,7-dimethoxy-4-quinolinol by the action of monoamine oxidase. ...

journal_title：Journal of pharmaceutical sciences

authors： Schwan TJ,Honkomp LJ,Snyder HR Jr,Watson EJ

更新日期：1978-03-01 00:00:00

abstract：:The absorption of propicillin from the rat stomach and small intestine in situ was examined as a function of recirculating solution pH. The in vitro interphase transport from an aqueous buffer of various pH values to the octanol phase was also studied for several penicillins by the use of a two-phase rolling cell. The...

journal_title：Journal of pharmaceutical sciences

authors： Tsuji A,Miyamoto E,Hashimoto N,Yamana T

更新日期：1978-12-01 00:00:00

abstract：:Phosphate is specifically adsorbed by aluminum hydroxycarbonate by anion ligand exchange. IR analysis indicated that phosphate exchanged with specifically adsorbed carbonate. Adsorption is favored by low pH and is inversely related to particle size. Adsorption of phosphate decreases the rate of acid neutralization of ...

journal_title：Journal of pharmaceutical sciences

authors： Liu JC,Feldkamp JR,White JL,Hem SL

更新日期：1984-10-01 00:00:00

abstract：:In phenobarbital measurement by GLC with the flash-methylation technique, using trimethylanilinium hydroxide as a methylating reagent, a small amount of water decomposed phenobarbital and interfered with the quantitative analysis. Thus, both the sample and the methylating reagent must be sufficiently dehydrated to att...

journal_title：Journal of pharmaceutical sciences

authors： Kurata K,Takeuchi M,Yoshida K

更新日期：1979-09-01 00:00:00

abstract：:Spray-dried dispersions (SDDs) are an important technology for enhancing the oral bioavailability of poorly water-soluble drugs. To design an effective oral SDD formulation, the key rate-determining step(s) for oral drug absorption must be understood. This work combined in vivo and in vitro tests with in silico modeli...

journal_title：Journal of pharmaceutical sciences

authors： Stewart A,Yates I,Mudie D,Pivette P,Goodwin A,Sarmiento A,Winter M,Morgen M,Vodak D

更新日期：2019-01-01 00:00:00

abstract：:The neuroprotective blood-brain barrier (BBB) keeps many drug candidates below therapeutic levels in the central nervous system. Glutathione PEGylated liposomal doxorubicin (2B3-101) has been developed to safely enhance the delivery of doxorubicin to brain tumors. However, doxorubicin concentration in extracellular br...

journal_title：Journal of pharmaceutical sciences

authors： Birngruber T,Raml R,Gladdines W,Gatschelhofer C,Gander E,Ghosh A,Kroath T,Gaillard PJ,Pieber TR,Sinner F

更新日期：2014-07-01 00:00:00

abstract：:This study explored the ability to conduct primary drying during lyophilization at product temperatures above the glass transition temperature of the maximally freeze-concentrated solution (Tg′) in amorphous formulations for four proteins from three different classes. Drying above Tg′ resulted in significant reduction...

journal_title：Journal of pharmaceutical sciences

authors： Depaz RA,Pansare S,Patel SM

更新日期：2016-01-01 00:00:00

abstract：:This article describes a procedure to facilitate scale-up for the primary drying phase of lyophilization using a combination of empirical testing and numerical modeling. Freeze dry microscopy is used to determine the temperature at which lyophile collapse occurs. A laboratory scale freeze-dryer equipped with manometri...

journal_title：Journal of pharmaceutical sciences

authors： Kramer T,Kremer DM,Pikal MJ,Petre WJ,Shalaev EY,Gatlin LA

更新日期：2009-01-01 00:00:00

abstract：:The highly lipid soluble, free-base form of halofantrine (Hf base; approximately 50 mg/mL in triglyceride lipids), a highly lipophilic (calculated log P approximately 8.5) antimalarial, has recently been shown to undergo significant intestinal lymphatic transport (54% of administered dose) after postprandial administr...

journal_title：Journal of pharmaceutical sciences

authors： Khoo SM,Prankerd RJ,Edwards GA,Porter CJ,Charman WN

更新日期：2002-03-01 00:00:00

abstract：:Two types of drug release mechanisms-matrix controlled (Q - t1/2 relationship) and partition controlled (Q - t relationship)-were reported previously. The dependency of the transition between these two processes on the solution solubility of drug is now analyzed. Mathematical expressions are derived to treat the syste...

journal_title：Journal of pharmaceutical sciences

authors： Chien YW,Lambert HJ,Lin TK

更新日期：1975-10-01 00:00:00

abstract：:A quantitative high-pressure liquid chromatographic method, using a reversed-phase column coupled to a fluorescence detector, was developed to determine salicylic acid in bulk aspirin and plain and buffered aspirin tablets. The aspirin was dissolved, filtered, and injected into the chromatograph; the fluorescence of t...

journal_title：Journal of pharmaceutical sciences

authors： Kirchhoefer RD,Juhl WE

更新日期：1980-05-01 00:00:00

abstract：:Oxidation of 7,8-dimethoxy-1,2,3,4-tetrahydroisoquinoline with potassium permanganate in acetone afforded 7,8-dimethoxy-3,4-dihydroisoquinoline as the primary product. Hence, oxidation of the appropriate secondary nonphenolic 7,8-dioxygenated tetrahydroisoquinoline alkaloid is thus a facile method for the generation o...

journal_title：Journal of pharmaceutical sciences

authors： el-Fishawy AM,Slatkin DJ,Knapp JE,Schiff PL Jr

更新日期：1984-11-01 00:00:00

abstract：:Membrane permeation enhancers have received significant attention in recent years for enabling the oral absorption of poorly permeable drug molecules. In this study, we investigated the ability of His-Ala-Val (HAV) and Ala-Asp-Thr (ADT) peptides derived from the extracellular-1 (EC1) domain of E-cadherin proteins to i...

journal_title：Journal of pharmaceutical sciences

authors： Dening TJ,Siahaan TJ,Hageman MJ

更新日期：2020-12-23 00:00:00

abstract：:The reaction of UICEL-A/102, a cellulose II powder recently prepared from Avicel(R) PH-102 by treatment with an aqueous sodium hydroxide solution, with glutaraldehyde in 0.01 N HCl has been investigated to improve its binder properties, without adversely affecting the rapid disintegration characteristic. The results s...

journal_title：Journal of pharmaceutical sciences

authors： de la Luz Reus Medina M,Kumar V

更新日期：2007-02-01 00:00:00

abstract：:It is shown that a suitable dosage interval, tau, can be estimated by a factor times the sum of the mean residence time (MRT) of the central compartment (MRTC) and the MRT of the absorption site (MRTA). This value of tau will provide a ratio, maximum steady-state plasma concentration: minimum steady-state plasma conce...

journal_title：Journal of pharmaceutical sciences

authors： Wagner JG

更新日期：1987-01-01 00:00:00

abstract：:Circular dichroism (CD) spectroscopy is routinely used in the biopharmaceutical industry to study the effects of manufacturing, formulation, and storage conditions on protein conformation and stability, and these results are often included in regulatory filings. In this context, the purpose of CD spectroscopy is often...

journal_title：Journal of pharmaceutical sciences

authors： Li CH,Nguyen X,Narhi L,Chemmalil L,Towers E,Muzammil S,Gabrielson J,Jiang Y

更新日期：2011-11-01 00:00:00

abstract：:Here, we report the structural characterization of several amorphous drugs made using the method of quenching molten droplets suspended in an acoustic levitator. (13) C NMR, X-ray, and neutron diffraction results are discussed for glassy cinnarizine, carbamazepine, miconazole nitrate, probucol, and clotrimazole. The (...

journal_title：Journal of pharmaceutical sciences

authors： Benmore CJ,Weber JK,Tailor AN,Cherry BR,Yarger JL,Mou Q,Weber W,Neuefeind J,Byrn SR

更新日期：2013-04-01 00:00:00

abstract：:To study the effect of substituents on the antitumor activities of analogs of 1-phenyl-3-benzyl-3-methyltriazenes, a series of compounds was designed and synthesized in which the substituent on the 1-phenyl was an electron-withdrawing group and the substituent on the 3-benzyl had a broad range of physicochemical prope...

journal_title：Journal of pharmaceutical sciences

authors： Dunn WJ 3rd,Greenberg MJ

更新日期：1977-10-01 00:00:00