Bioavailability assessment under quasi- and nonsteady-state conditions III: Application.

abstract：:Two high-performance liquid chromatographic (HPLC) assay procedures were developed for the determination of salicylamide and its metabolites in serum, urine, and saliva. One method involves reverse-phase ion-pair chromatography and UV detection, and is used to determine salicylamide, salicylamide glucuronide, and sali...

journal_title：Journal of pharmaceutical sciences

authors： Morris ME,Levy G

更新日期：1983-06-01 00:00:00

abstract：:The fungal microorganism Cunninghamella echinulata was utilized to para-hydroxylate the synthetic substrate (+/-)-1-isopropylamino-3-phenoxy-propan-2-ol (1). The resulting product, (+/-)-1-(4-hydroxyphenoxy)-3-isopropylamino-propan-2-ol, or (+/-)-prenalterol, (2) was formed in greater than 85% yield. Extracts from inc...

journal_title：Journal of pharmaceutical sciences

authors： Pasutto FM,Singh NN,Jamali F,Coutts RT,Abuzar S

更新日期：1987-02-01 00:00:00

abstract：:A highly sensitive and specific electron-capture GLC assay capable of detecting picogram quantities of metoclopramide, a procaine derivative, in biological fluids was developed. This assay consisted of extracting metoclopramide from an alkalinized aqueous layer into benzene. A portion of the organic phase was derivati...

journal_title：Journal of pharmaceutical sciences

authors： Tam YK,Axelson JE

更新日期：1978-08-01 00:00:00

abstract：:The expression of carboxylesterase (CES) and the transdermal movement of an ester prodrug were studied in rat skin. Ethyl-fexofenadine (ethyl-FXD) was used as a model lipophilic prodrug that is slowly hydrolyzed to its parent drug, FXD (MW 502). Among the CES1 and CES2 isozymes, Hydrolase A is predominant in rat skin ...

journal_title：Journal of pharmaceutical sciences

authors： Imai T,Ariyoshi S,Ohura K,Sawada T,Nakada Y

更新日期：2016-02-01 00:00:00

abstract：:We previously reported nonaqueous silicone elastomer gels (SEGs) for sustained vaginal administration of the CCR5-targeted entry inhibitor maraviroc (MVC). Here, we describe chemically modified SEGs (h-SEGs) in which the hydrophobic cyclomethicone component was partially replaced with relatively hydrophilic silanol-te...

journal_title：Journal of pharmaceutical sciences

authors： Forbes CJ,McCoy CF,Murphy DJ,Woolfson AD,Moore JP,Evans A,Shattock RJ,Malcolm RK

更新日期：2014-05-01 00:00:00

abstract：:Aliphatic polyesters have great utility as temporary prosthetics and surgical aids, and in drug delivery systems. Knowledge of the mechanism and pathways of hydrolysis can form a basis for the design and selection of a controlled-release system. Because of the importance of hydrolysis to the properties of such a syste...

journal_title：Journal of pharmaceutical sciences

authors： Maniar ML,Kalonia DS,Simonelli AP

更新日期：1991-08-01 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：:The release kinetics of a polymeric-controlled release device are determined by its geometry and dimensions. A method to calculate the required size and shape of diffusion-controlled dosage forms to achieve a particular release profile is presented. The diffusion parameters are determined for various drugs (theophylli...

journal_title：Journal of pharmaceutical sciences

authors： Siepmann J,Ainaoui A,Vergnaud JM,Bodmeier R

更新日期：1998-07-01 00:00:00

abstract：:High-throughput lyophilization process was designed and developed for protein formulations using a single-step drying approach at a shelf temperature (Ts) of ≥40°C. Model proteins were evaluated at different protein concentrations in amorphous-only and amorphous-crystalline formulations. Single-step drying resulted in...

journal_title：Journal of pharmaceutical sciences

authors： Pansare SK,Patel SM

更新日期：2019-04-01 00:00:00

abstract：:The pharmacokinetic profiles of cimetropium bromide, after either intravenous injection of 10 mg or oral ingestion of 200 mg, were determined in eight healthy volunteers. After intravenous administration, the plasma levels and urinary excretion indicated that the drug is distributed and eliminated at a rapid rate (ter...

journal_title：Journal of pharmaceutical sciences

authors： Imbimbo BP,Daniotti S,Vidi A,Foschi D,Saporiti F,Ferrante L

更新日期：1986-07-01 00:00:00

abstract：:Postabsorptive factors which can affect systemic drug exposure are assumed to be dependent on the active pharmaceutical ingredient (API), and thus independent of formulation. In contrast, preabsorptive factors, for example, hypochlorhydria, might affect systemic exposure in both an API and a formulation-dependent way....

journal_title：Journal of pharmaceutical sciences

authors： Cristofoletti R,Patel N,Dressman JB

更新日期：2017-02-01 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 p-aminobenzyl analogues (8a and 8b, respectively) of the cardioselective beta-adrenergic receptor antagonists practolol and atenolol were prepared from the corresponding phenoxymethyloxiranes in 30 and 13% yields, respectively. The dissociation constants for the beta-adrenergic receptor were measured in membrane p...

journal_title：Journal of pharmaceutical sciences

authors： Jones GS Jr,Bylund DB,Hanson RN

更新日期：1992-04-01 00:00:00

abstract：:Cationic antimicrobial peptides are good candidates for new diagnostics and antimicrobial agents. They can rapidly kill a broad range of microbes and have additional activities that have impact on the quality and effectiveness of innate responses and inflammation. Furthermore, the challenge of bacterial resistance to ...

journal_title：Journal of pharmaceutical sciences

authors： Brouwer CP,Wulferink M,Welling MM

更新日期：2008-05-01 00:00:00

abstract：:Biopolymer-based hydrogels such as mucus and the basal lamina play a key role in biology, where they control the exchange of material between different compartments. They also pose a barrier that needs to be overcome for successful drug delivery. Characterizing the permeability properties of such hydrogels is mandator...

journal_title：Journal of pharmaceutical sciences

authors： Vladescu I,Lieleg O,Jang S,Ribbeck K

更新日期：2012-01-01 00:00:00

abstract：:The hydrolysis of acetylcholine and acetylcholine mustard by acetylcholinesterase was compared over a substrate concentration range of 1-10 mM. Reactions were allowed to proceed for 2 min at 25 degrees. Results of these experiments reveal that the substrates have similar affinities for the enzyme, whereas the maximum ...

journal_title：Journal of pharmaceutical sciences

authors： Hudgins PM,Stubbins JF

更新日期：1975-08-01 00:00:00

abstract：:Boron analogues of carbamoylcholine and thiocholine and esters of these analogues were prepared. These compounds were fairly stable toward hydrolysis and demonstrated moderate anti-inflammatory and hypolipidemic activities in mice. The hypolipidemic activity of the compounds at a dose of 8 mg/kg/day was equivalent in ...

journal_title：Journal of pharmaceutical sciences

authors： Sood A,Sood CK,Spielvogel BF,Hall IH,Wong OT

更新日期：1992-05-01 00:00:00

abstract：:2',7'-Bis(2-carboxyethyl)-5(6)-carboxyfluorescein (BCECF) is a fluorescent probe used to examine multidrug resistance-associated protein (MRP) transporter activity in cells. BCECF is introduced into the cell as the nonfluorescent membrane permeable acetoxymethyl ester, BCECF-AM, where it is hydrolyzed to the membrane ...

journal_title：Journal of pharmaceutical sciences

authors： Bachmeier CJ,Trickler WJ,Miller DW

更新日期：2004-04-01 00:00:00

abstract：:A solution of selegiline hydrochloride reference standard, which contained no detectable impurities at the time of its preparation, was found by HPLC to contain a trace of a compound at the locus of methamphetamine when analyzed after 1 year. Heating selegiline solutions at pH 7 and 105 degrees C produced methamphetam...

journal_title：Journal of pharmaceutical sciences

authors： Chafetz L,Desai MP,Sukonik L

更新日期：1994-09-01 00:00:00

abstract：:The interaction of L-tryptophan with alpha-cyclodextrin was investigated in a 0.1 M phosphate buffer at pH 7.4 with a LKB 2277 microcalorimeter, using flow mixed mode at 25 degrees C. The thermodynamic parameters for inclusion complex formation obtained are as follows; DeltaG(0) = - 7.03 kJ/mol (K = 17.0), DeltaH(0) =...

journal_title：Journal of pharmaceutical sciences

authors： Nishijo J,Tsuchitani M

更新日期：2001-02-01 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：:A high-speed liquid chromatographic system is described, which can be used for the simultaneous identification of the anabolic steroid methandrostenolone and its impurities and the quantitation of each of these compounds. Separation is effected by adsorption chromatography on a slurry-packed microparticulate silica ge...

journal_title：Journal of pharmaceutical sciences

authors： Butterfield AG,Lodge BA,Pound NJ,Sears RW

更新日期：1975-03-01 00:00:00

abstract：:Despite being a major breakthrough in multiple myeloma therapy, carfilzomib (CFZ, a second-generation proteasome inhibitor drug) has been largely ineffective against solid cancer, possibly due to its pharmacokinetic drawbacks including metabolic instability. Recently, quinic acid (QA, a low-affinity ligand of selectin...

journal_title：Journal of pharmaceutical sciences

authors： Jun Y,Xu J,Kim H,Park JE,Jeong YS,Min JS,Yoon N,Choi JY,Yoo J,Bae SK,Chung SJ,Yeo Y,Lee W

更新日期：2020-04-01 00:00:00

abstract：:Carbamazepine is the first-line anti-epileptic drug for focal seizures and generalized tonic-clonic seizures. Although sustained-release formulations exist, an initial burst of drug release is still present and this results in side effects. Zero-order release formulations reduce fluctuations in serum drug concentratio...

journal_title：Journal of pharmaceutical sciences

authors： Lim SH,Chia SM,Kang L,Yap KY

更新日期：2016-07-01 00:00:00

abstract：:Modifications of antibacterial activity have been demonstrated using combinations of two antibacterials from trimethoprim, sulfonamides (sulfadiazine, sulfamerazine, and silver sulfadiazine), silver nitrate, and dibromopropamidine isethionate, either formulated in a cream base or dissolved in peptone water. The creams...

journal_title：Journal of pharmaceutical sciences

authors： Richards RM,Taylor RB,Xing DK

更新日期：1991-09-01 00:00:00

abstract：:The chromatographic retention behavior of dextromethorphan hydrobromide on an octadecylsilane column was investigated as a function of the pairing ion and the mobile phase composition. Dramatic increases in the capacity factor were observed with pairing ions containing more than eight carbons and with decreasing organ...

journal_title：Journal of pharmaceutical sciences

authors： Kubiak EJ,Munson JW

更新日期：1980-12-01 00:00:00

abstract：:Allopurinol exhibits good bioavailability (78-90%) after administration of oral dosage forms to humans and rabbits; however, it is not absorbed rectally from any of the dosage forms to any significant extent. Oral administration of allopurinol in a polyethylene glycol suspension, to which allopurinol may be reversibly...

journal_title：Journal of pharmaceutical sciences

authors： Patel VS,Kramer WG

更新日期：1986-03-01 00:00:00

abstract：:Although several mathematical models have been reported for the estimation of human plasma concentration profiles of drug substances after dermal application, the successful cases that can predict human pharmacokinetic profiles are limited. Therefore, the aim of this study is to investigate the prediction of human pla...

journal_title：Journal of pharmaceutical sciences

authors： Yamamoto S,Karashima M,Arai Y,Tohyama K,Amano N

更新日期：2017-09-01 00:00:00

abstract：:The molecular modeling program SYBYL was used to simulate the adsorption of various barbiturates by an activated charcoal surface. The compounds barbituric acid (BA), barbital (B), phenobarbital (PB), mephobarbital (M), and primidone (Pr) were modeled, and their structures were energetically minimized. These structure...

journal_title：Journal of pharmaceutical sciences

authors： Wurster DE,Kolling WM,Knosp BM

更新日期：1994-12-01 00:00:00

abstract：:The synthesis, hydrolysis rate, and bioavailability of 1-(p-acetaminophenoxy)-1-ethoxyethane, an acetaminophen prodrug, are described. The prodrug is less soluble than acetaminophen and stable at neutral pH. However, in an acidic environment, the compound cleaves rapidly, generating acetaminophen. When both the prodru...

journal_title：Journal of pharmaceutical sciences

authors： Hussain A,Kulkarni P,Perrier D

更新日期：1978-04-01 00:00:00