Relationship between molecular structure and cytochrome P450-metabolic intermediate complex formation, studied with orphenadrine analogues.

abstract：:Mebendazole (MBZ) is a common benzimidazole anthelmintic that exists in three different polymorphic forms, A, B, and C. Polymorph C is the pharmaceutically preferred form due to its adequated aqueous solubility. No single crystal structure determinations depicting the nature of the crystal packing and molecular confor...

journal_title：Journal of pharmaceutical sciences

authors： Martins FT,Neves PP,Ellena J,Camí GE,Brusau EV,Narda GE

更新日期：2009-07-01 00:00:00

abstract：:In vitro iontophoretic administration of drugs through a microporous polyolefin membrane with hydrophilic urethane polymerfilled pores was done for the ionized drugs dexamethasone sodium phosphate, hydrocortisone sodium phosphate, and prednisolone sodium succinate, and for a nonionizable drug cortisone acetate. Curren...

journal_title：Journal of pharmaceutical sciences

authors： Tu YH,Allen LV Jr

更新日期：1989-03-01 00:00:00

abstract：:A GLC method was developed for the determination of ethylene oxide and its two reaction products, ethylene chlorohydrin and ethylene glycol, in ophthalmic solutions at the levels recently proposed by the Food and Drug Administration. The method requires no extractions, sample preparations, or elaborate trapping and co...

journal_title：Journal of pharmaceutical sciences

authors： Manius GJ

更新日期：1979-12-01 00:00:00

abstract：:The utility of inhaled protein therapeutics to treat lung-resident diseases is limited by protein degradation in the lungs and rapid clearance. This study therefore aimed to evaluate the impact of PEGylation on the lung and systemic exposure of interferon (IFN) α2 after intratracheal administration to rats. An inverse...

journal_title：Journal of pharmaceutical sciences

authors： Mcleod VM,Chan LJ,Ryan GM,Porter CJ,Kaminskas LM

更新日期：2015-04-01 00:00:00

abstract：:The objective of this study was to determine the relative importance of metabolism by cytochrome P450 (CYP) enzymes versus efflux by P-glycoprotein (P-gp) in restricting the intestinal mucosal permeation of cyclic prodrugs (AOA-DADLE, CA-DADLE, OMCA-DADLE) of the opioid peptide DADLE (H-Tyr-D-Ala-Gly-Phe-D-Leu-OH). AO...

journal_title：Journal of pharmaceutical sciences

authors： Ouyang H,Chen W,Andersen TE,Steffansen B,Borchardt RT

更新日期：2009-01-01 00:00:00

abstract：:Elucidation of the most stable form of an active pharmaceutical ingredient (API) is a critical step in the development process. Polymorph screening for an API with a complex polymorphic profile can present a significant challenge. The presented case illustrates an extensively polymorphic compound with an additional pr...

journal_title：Journal of pharmaceutical sciences

authors： Campeta AM,Chekal BP,Abramov YA,Meenan PA,Henson MJ,Shi B,Singer RA,Horspool KR

更新日期：2010-09-01 00:00:00

abstract：:This study compares one of the previously studied formulations with commercial amoxicillin capsules. The results indicate that the percentage of the dose absorbed is similar in both formulations; nevertheless, the amoxicillin capsules present a higher absorption rate. The in vivo--in vitro correlations in terms of res...

journal_title：Journal of pharmaceutical sciences

authors： Llabrés M,Vila JL,Martínez-Pacheco R

更新日期：1982-08-01 00:00:00

abstract：:Phenytoin (DPH) was delivered to the brain by a dihydropyridine in equilibrium pyridinium salt redox system, which was evaluated for anticonvulsant activity. Following iv injection of the lipophilic delivery system of DPH (2) to rats, concentrations of DPH were lower but sustained and, after 30 min, essentially the sa...

journal_title：Journal of pharmaceutical sciences

authors： Shek E,Murakami T,Nath C,Pop E,Bodor NS

更新日期：1989-10-01 00:00:00

abstract：:Plasma levels were determined frequently after single doses of perfluorooctyl bromide were administered to beagle dogs at doses of either 30.8 g/kg po or 3.9 g/kg intratracheally. The apparent first-order half-life during the terminal elimination phase was about 1 day after oral medication and about 7 days after intra...

journal_title：Journal of pharmaceutical sciences

authors： Lee FH,Scrime M,Edelson J

更新日期：1978-07-01 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：: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 effects of various factors on the adsorption of nicotinic acid onto and desorption from activated charcoal were investigated in vitro. The affinity of nicotinic acid for charcoal was poor both in acidic and neutral media. Adsorption increased with increasing charcoal:drug ratios and decreasing incubation volume:ch...

journal_title：Journal of pharmaceutical sciences

authors： Roivas L,Neuvonen PJ

更新日期：1992-09-01 00:00:00

abstract：:Fibril formation (aggregation) of human and bovine insulin and six human insulin mutants in hydrochloric acid were investigated by visual inspection, Thioflavin T fluorescence spectroscopy, transmission electron microscopy (TEM), and Fourier transform infrared (FTIR) spectroscopy. The fibrillation tendencies of the wi...

journal_title：Journal of pharmaceutical sciences

authors： Garriques LN,Frokjaer S,Carpenter JF,Brange J

更新日期：2002-12-01 00:00:00

abstract：:A conventional atomistic approach of estimating molecular hydrophobicity (log P) was improved by taking into account the proximity effect of substituent groups as well as the importance of solute-solvent interaction in the partition phenomena. The new method reassigns atomic parameters when the molecule is fully expos...

journal_title：Journal of pharmaceutical sciences

authors： Masuda T,Jikihara T,Nakamura K,Kimura A,Takagi T,Fujiwara H

更新日期：1997-01-01 00:00:00

abstract：:Delayed absorption of nifedipine when administered as a 20 mg immediate release soft gelatin capsule to fasted volunteers has been reported. Physiologically based pharmacokinetic (PBPK) modeling and in vitro dissolution data were used to explore our hypothesis that at high doses of nifedipine it precipitates in the st...

journal_title：Journal of pharmaceutical sciences

authors： Thelen K,Jantratid E,Dressman JB,Lippert J,Willmann S

更新日期：2010-06-01 00:00:00

abstract：:The aims of the present study were to formulate stable onion phases of the biodegradable surfactant PEG-8 Distearate (PEG8DS) and evaluate application of the onion phases in encapsulating sumatriptan succinate, a BCS class III potent antimigraine drug. Drug loaded and placebo onion phases were prepared by shearing lyo...

journal_title：Journal of pharmaceutical sciences

authors： Redkar M,Hassan PA,Aswal V,Devarajan P

更新日期：2007-09-01 00:00:00

abstract：:Solubilities in isoctane and water were determined for several C1-phenolic esters of prostaglandin F2 alpha and prostaglandin E2 and acetates having the same phenol moiety. Linear free energy relationships for solubility among the series were observed with slopes of approximately 1. These results suggest that the cont...

journal_title：Journal of pharmaceutical sciences

authors： Anderson BD,Conradi RA

更新日期：1980-04-01 00:00:00

abstract：:A simple, sensitive GLC assay was developed for fusaric acid, the active metabolite of bupicomide, to follow the disposition of this investigational antihypertensive agent in patients undergoing therapy. Fusaric acid is efficiently extracted from biological samples, derivatized by on-column methylation, and chromatogr...

journal_title：Journal of pharmaceutical sciences

authors： Fung KK,Koda RT,Maronde RF,Cohen JL

更新日期：1976-04-01 00:00:00

abstract：:Curcumin has been investigated as a potential photosensitizer (PS) in antimicrobial photodynamic therapy (aPDT). The phototoxic effect of curcumin is dependent on proper formulations of the compound because of the lipophilic nature of the molecule and the extremely low water solubility at physiological conditions. In ...

journal_title：Journal of pharmaceutical sciences

authors： Hegge AB,Nielsen TT,Larsen KL,Bruzell E,Tønnesen HH

更新日期：2012-04-01 00:00:00

abstract：:An automated two-phase method for the simultaneous fluorometric determination of the spironolactone metabolites canrenone (II) and canrenoic acid (III) in serum is described. The determination is performed by two dichloroethane extractions of the same serum sample at different pH values. The fluorescence developed in ...

journal_title：Journal of pharmaceutical sciences

authors： Neubert P,Koch K

更新日期：1977-08-01 00:00:00

abstract：:A number of arylidene derivatives of alicyclic ketones and some corresponding oximes, oxime esters, and related compounds were prepared as candidate cytotoxic agents. All of the compounds were evaluated against murine L1210 lymphoid leukemia cells. In general, cytotoxicity was greatest with the alpha,beta-unsaturated ...

journal_title：Journal of pharmaceutical sciences

authors： Dimmock JR,Sidhu KK,Chen M,Li J,Quail JW,Allen TM,Kao GY

更新日期：1994-06-01 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：:A thermodynamic analysis of the energy transformations occurring within pharmaceutical tablets during the unloading phase of compaction was performed on Avicel, calcium phosphate, acetaminophen, and calcium oxalate. This analysis was based on viscoelastic stress data collected using an instrumented rotary press and wa...

journal_title：Journal of pharmaceutical sciences

authors： Hoag SW,Rippie EG

更新日期：1994-06-01 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 simulation study was done to determine if 72 h is the most informative sampling duration for bioequivalence (BE) determination in parallel-designed BE studies with drugs that have half-lives of at least 30 h. The impact of absorption and elimination half-lives on informative sampling was evaluated. Two-treatment par...

journal_title：Journal of pharmaceutical sciences

authors： El-Tahtawy A,Harrison F,Zirkelbach JF,Jackson AJ

更新日期：2012-11-01 00:00:00

abstract：:Twenty-two neutral, lipid-soluble 99mTc complexes have been synthesized from diamine dithiol (DADT) ligands which vary in alkyl substitution pattern on nitrogen and carbon. The logarithm of the partition coefficients (log PC), as well as the capacity factor k', of the purified complexes increased linearly with molecul...

journal_title：Journal of pharmaceutical sciences

authors： Lever SZ,Sun SY,Scheffel UA,Kaltovich FA,Baidoo KE,Goldfarb H,Wagner HN Jr

更新日期：1994-06-01 00:00:00

abstract：:Particulate matter present in drug products intended for parenteral administration to patients is typically monitored and controlled in the finished drug product to minimize potential risks to patients. In contrast to particulates found in drug products, the current study evaluated particulates representative of mater...

journal_title：Journal of pharmaceutical sciences

authors： Pollo M,Mehta A,Torres K,Thorne D,Zimmermann D,Kolhe P

更新日期：2019-07-01 00:00:00

abstract：:This study was designed to examine the effect of benzalkonium chloride/ethylenediaminetetraacetic acid (BAK/EDTA) on the ocular bioavailability (Focular) of ketorolac tromethamine after ocular instillation to normal and de-epithelialized corneas of rabbits both in vitro and in vivo. The in vitro Focular of the formula...

journal_title：Journal of pharmaceutical sciences

authors： Madhu C,Rix PJ,Shackleton MJ,Nguyen TG,Tang-Liu DD

更新日期：1996-04-01 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 reports, for the first time, development of tyrosine kinase inhibitor-loaded, thermosensitive liposomes (TKI/TSLs) and their efficacy for treatment of renal cell carcinoma when triggered by focused ultrasound (FUS). Uptake of these nanoparticles into renal cancer cells was visualized with confocal and fluor...

journal_title：Journal of pharmaceutical sciences

authors： Abshire C,Murad HY,Arora JS,Liu J,Mandava SH,John VT,Khismatullin DB,Lee BR

更新日期：2017-05-01 00:00:00