InVitro, Ex Vivo, and In Vivo Evaluation of a Dual pH/Redox Responsive Nanoliposomal Sludge for Transdermal Drug Delivery.

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 rapid, automated method for the determination of phenylbutazone in plasma and urine was developed. The method offers distinct advantages over earlier procedures and is particularly suitable for large-scale bioavailability studies. ...

journal_title：Journal of pharmaceutical sciences

authors： Lukas G,Borman CB,Zak SB

更新日期：1976-01-01 00:00:00

abstract：:Quantitative determination of serum concentrations of carvedilol [(+/-)-1-(carbazol-4-yloxy)-3-[[2-(o-methoxyphenoxy)ethyl) amino]-2-propanol], a combined alpha- and beta-adrenergic receptor antagonist, was obtained using HPLC with spectrofluorometric detection. Carvedilol was extracted from alkalinized serum with eth...

journal_title：Journal of pharmaceutical sciences

authors： Varin F,Cubeddu LX,Powell JR

更新日期：1986-12-01 00:00:00

abstract：:Tryptophan (Trp) oxidation in proteins leads to a number of events, including changes in color, higher order structure (HOS), and biological activity. We describe here a number of new findings through a comprehensive characterization of 6 monoclonal antibodies (mAbs) following selective oxidation of Trp residues by 2,...

journal_title：Journal of pharmaceutical sciences

authors： Barnett GV,Balakrishnan G,Chennamsetty N,Hoffman L,Bongers J,Tao L,Huang Y,Slaney T,Das TK,Leone A,Kar SR

更新日期：2019-06-01 00:00:00

abstract：:Methods for the determination of diphenoxylate hydrochloride and atropine sulfate combinations in solutions and powdered tablet composites are presented. A semiautomated assay for diphenoxylate hydrochloride in individual tablets (content uniformity) also is presented. The USP XIX assays for these products are cumbers...

journal_title：Journal of pharmaceutical sciences

authors： Ballbach RL,Brown DJ,Walters SM

更新日期：1977-11-01 00:00:00

abstract：:The aim was to study a new method of dissolution in vitro, the "Bio-Dis" apparatus, and to compare it with the classical rotating bottle method. Several theophylline controlled-release drug dosage forms were studied. Dissolution testing was performed in increasing pH in standard conditions and after treatment with pea...

journal_title：Journal of pharmaceutical sciences

authors： Esbelin B,Beyssac E,Aiache JM,Shiu GK,Skelly JP

更新日期：1991-10-01 00:00:00

abstract：:The absorption and pharmacokinetics of sulofenur [N-(indan-5-sulfonyl)-N'-(4-chlorophenyl)urea, LY186641] and its major metabolites were examined in mice, rats, monkeys, and dogs. The compound is a diarylsulfonylurea currently being evaluated as an oncolytic agent in phase I and II trials. In all species, sulofenur wa...

journal_title：Journal of pharmaceutical sciences

authors： Ehlhardt WJ,Sullivan HR,Wood PG,Woodland JM,Hamilton M,Hamilton C,Cornpropst D,Grindey GB,Worzalla JF,Bewley JR

更新日期：1993-07-01 00:00:00

abstract：:A wide variety of computational models covering statistical, mechanistic, and machine learning (locked and adaptive) methods are explored for use in biopharmaceutical manufacturing. Limited discussion exists on how to establish the credibility of a computational model for application in biopharmaceutical manufacturing...

journal_title：Journal of pharmaceutical sciences

authors： Bideault G,Scaccia A,Zahel T,Forero RL,Daluwatte C

更新日期：2021-01-22 00:00:00

abstract：:A characterization and optimization of the in vitro transdermal iontophoretic transport of 5-hydroxy-2-(N,N,-di-n-propylamino)tetralin (5-OH-DPAT) is presented. The utility of acetaminophen as a marker of electroosmotic flow was studied as well. The following parameters of iontophoretic transport of 5-OH-DPAT were exa...

journal_title：Journal of pharmaceutical sciences

authors： Ackaert OW,Van Smeden J,De Graan J,Dijkstra D,Danhof M,Bouwstra JA

更新日期：2010-01-01 00:00:00

abstract：:The aim of the present work was to prepare and characterize chitosan-stearic acid conjugate nanomicelles for encapsulation of amphotericin B (AmB) and to evaluate the in vitro nebulization of the formulations. Water soluble chitosan was grafted to stearic acid (SA) chains via 1-ethyl-3-(3-dimethylaminopropyl)carbodiim...

journal_title：Journal of pharmaceutical sciences

authors： Gilani K,Moazeni E,Ramezanli T,Amini M,Fazeli MR,Jamalifar H

更新日期：2011-01-01 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：:N-linked glycosylation is an important post translational modification that occurs on Asparagine 297 residue or a homologous position on the Fc portion of monoclonal antibodies (mAbs). mAb Fc glycans play important roles in antibody structure, stability, and function including effector function and pharmacokinetics. T...

journal_title：Journal of pharmaceutical sciences

authors： Voruganti S,Xu J,Li X,Balakrishnan G,Singh SM,Kar SR,Das TK

更新日期：2021-02-01 00:00:00

abstract：:Deiodination of diatrizoic acid, an anionic radiopaque, was found to be catalyzed by Cu(II). Through a detailed study of o-iodobenzoic acid, a model compound, the copper-catalyzed SN1 mechanism was established based on observations of common ion, salt, and pH effects. Meta- and para-iodobenzoic acids were unreactive. ...

journal_title：Journal of pharmaceutical sciences

authors： Wang YC

更新日期：1980-06-01 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

abstract：:Deflocculated suspensions of coarse powders tend to cake as the individual particles settle out and form compact, cohesive sediments. Limited flocculation results in looser sediments because the settled-out flocs incorporate large amounts of the liquid suspending medium. Controlled flocculation of bismuth subnitrate s...

journal_title：Journal of pharmaceutical sciences

authors： Schott H

更新日期：1976-06-01 00:00:00

abstract：:Metronidazole (MTZ) is a drug of choice for protozoal infections such as luminal amoebiasis. We designed and synthesized N-nicotinoyl-2-{2-(2-methyl-5-nitroimidazol-1-yl)ethyloxy}-D,L-glycine (NMG) as a colon-specific prodrug of MTZ. The synthetic yield of NMG was about 34%. The apparent partition coefficient of MTZ w...

journal_title：Journal of pharmaceutical sciences

authors： Kim D,Hong S,Jung S,Jung Y,Kim YM

更新日期：2009-11-01 00:00:00

abstract：:Biopharmaceuticals represent an important and growing class of medicines. Immunogenic responses to biopharmaceuticals in patients can sometimes result in reduced safety and efficacy. Although multiple factors are known to influence immunogenicity, our understanding of the complex underlying mechanisms remains imperfec...

journal_title：Journal of pharmaceutical sciences

authors： Bee JS,Goletz TJ,Ragheb JA

更新日期：2012-10-01 00:00:00

abstract：:Three aspirin derivatives, aspirin phenylalanine ethyl ester, aspirin phenylalanine amide, and aspirin phenyllactic ethyl ester, were investigated with respect to their hydrolysis by alpha-chymotrypsin. Of the three compounds, aspirin phenylalanine ethyl ester was the best substrate, with kcat = 25 sec-1 and Km = 1.3 ...

journal_title：Journal of pharmaceutical sciences

authors： Banerjee PK,Amidon GL

更新日期：1981-12-01 00:00:00

abstract：:The physical state of a dosage form, crystalline versus amorphous, is critical in determining its solid-state physical and chemical properties. This minireview describes the physics associated with the preparation and storage of amorphous solids including a review of the common theories of the glass transition and rel...

journal_title：Journal of pharmaceutical sciences

authors： Hilden LR,Morris KR

更新日期：2004-01-01 00:00:00

abstract：:The capacity factors of several penicillins and cephalosporins, as well as those of 7-aminocephalosporanic acid, 6-aminopenicillanic acid, and 7-aminodeacetoxycephalosporanic acid, were determined at pH 2.5-7.5 with different methanol concentrations in the mobile phase. The influence of ionic strength on activity fact...

journal_title：Journal of pharmaceutical sciences

authors： Salto F,Prieto JG,Alemany MT

更新日期：1980-05-01 00:00:00

abstract：:In our previous research, cocaine applied intranasally in rats diffused or was transported directly from the nasal cavity to the brain. However, the direct nose-brain cocaine transport only contributes to an initial increase in the relative cocaine brain exposure. In this study, we have determined the nose-brain trans...

journal_title：Journal of pharmaceutical sciences

authors： Chow HH,Anavy N,Villalobos A

更新日期：2001-11-01 00:00:00

abstract：:Interaction between nonsteroidal anti-inflammatory drugs (NSAIDs) and other drugs occurs relatively frequently because of the wide use of NSAIDs. Such interactions with drugs of narrow therapeutic index used in serious disease states may lead to toxicity. Gentamicin toxicity is based on its concentration in serum, and...

journal_title：Journal of pharmaceutical sciences

authors： Shivprakash,Gandhi TP,Patel RB,Sheikh MA,Jhala A,Santani DD

更新日期：1994-04-01 00:00:00

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：:In this study, the effects of structurally related organic impurities on the molecular dynamics of amorphous sulfamethazine were evaluated using thermal analysis. Sulfanilamide (SNA), sulfamerazine (SMR), and sulfadimethoxine were used as virtual impurities of sulfamethazine. The amorphous state was prepared in situ i...

journal_title：Journal of pharmaceutical sciences

authors： Hamada Y,Ono M,Ohara M,Yonemochi E

更新日期：2017-04-01 00:00:00

abstract：:Intestinal transport of the type III phosphodiesterase inhibitor cilostazol was characterized to evaluate the influence of secretory transporter. Intestinal absorption of cilostazol measured by the in situ closed loop method, showed regional differences, with high permeability in the upper part of the small intestine....

journal_title：Journal of pharmaceutical sciences

authors： Toyobuku H,Tamai I,Ueno K,Tsuji A

更新日期：2003-11-01 00:00:00

abstract：:Drugs possessing the ability to bind to melanin-rich tissue, such as the eye, are linked with higher ocular exposure, and therefore have the potential to affect the efficacy and safety profiles of therapeutics. A high-throughput melanin chromatographic affinity assay has been developed and validated, which has allowed...

journal_title：Journal of pharmaceutical sciences

authors： Reilly J,Williams SL,Forster CJ,Kansara V,End P,Serrano-Wu MH

更新日期：2015-12-01 00:00:00

abstract：:Systematic structural modifications were performed on the natural sesquiterpene lactone tenulin to define those groupings essential to, or significant in, its in vivo antitumor activity. Accordingly, the following tenulin analogs were prepared: dihydrotenulin, 2,3-epoxytenulin, isotenulin, dihydroisotenulin, 2,3-epoxy...

journal_title：Journal of pharmaceutical sciences

authors： Waddell TG,Austin AM,Cochran JW,Gerhart KG,Hall IH,Lee KH

更新日期：1979-06-01 00:00:00

abstract：:Sugars and polyols have been used routinely with lyophilized proteins and peptides as bulking agents, cryoprotectants, and lyoprotectants. However, reducing sugars may present a problem as excipients since they are potentially reactive with proteins. In this stability study of recombinant human relaxin (Rix) with vari...

journal_title：Journal of pharmaceutical sciences

authors： Li S,Patapoff TW,Overcashier D,Hsu C,Nguyen TH,Borchardt RT

更新日期：1996-08-01 00:00:00

abstract：:The in vitro binding of warfarin by human serum albumin was studied at various temperatures and at pH 7.4 by a frontal gel filtration technique. The results can be best described in terms of a two class-of-binding site model, in which the numbers of primary and secondary sites are constrained to the average values for...

journal_title：Journal of pharmaceutical sciences

authors： Oester YT,Keresztes-Nagy S,Mais RF,Becktel J,Zaroslinski JF

更新日期：1976-11-01 00:00:00

abstract：:The geometry and structural features of the inclusion complexes of beta-cyclodextrin (beta-CD) with the chiral antiamnesic drugs (+/-)-1-benzyl-4-hydroxymethylpyrrolidin-2-one (WEB-1868). (+/-)-1-benzenesulfonyl-5-ethoxypyrrolidin-2-one (RU-35929), and (+/-)-1-(3-pyridinlysulfonyl)-5-ethoxypyrrolidin-2-one (RU-47010) ...

journal_title：Journal of pharmaceutical sciences

authors： Amato ME,Djedaïni F,Pappalardo GC,Perly B,Scarlata G

更新日期：1992-12-01 00:00:00