Chemical modifications of therapeutic proteins induced by residual ethylene oxide.

abstract：:The pharmacologically active compound (33% reduction in rabbit intraocular pressure recovery rate assay) 1-ethyl-6-fluoro-1,2,3,4-tetrahydroquinoline (MC4), which showed ocular hypotensive action and had optimum physicochemical properties, was characterized for its ocular absorption and distribution properties to bett...

journal_title：Journal of pharmaceutical sciences

authors： Pamulapati CR,Schoenwald RD

更新日期：2011-12-01 00:00:00

abstract：:Two generalized modes of erosion kinetics, that is, the power law mode and root type mode, respectively, were found to be able to better describe the reported weight loss data compared to the existing linear mode, for commonly used surface-eroding polymer microspheres. Based on the newly identified modes, a set of dru...

journal_title：Journal of pharmaceutical sciences

authors： You S,Yang Z,Wang CH

更新日期：2016-06-01 00:00:00

abstract：:Inhibition of endogenous prostacyclin and thromboxane biosynthesis by aspirin is critically dose-dependent in humans. Gastrointestinal and hepatic hydrolysis may limit systemic availability of aspirin, especially in low doses, perhaps contributing to the biochemical selectivity of aspirin. Existing analytical methods ...

journal_title：Journal of pharmaceutical sciences

authors： Pedersen AK,FitzGerald GA

更新日期：1985-02-01 00:00:00

abstract：:The synthesis of the diethyl analog of neostigmine, its preliminary pharmacology, and its use as an internal standard for the GLC assay of neostigmine are described. Both the diethyl analog and neostigmine undergo thermal demethylation in the injection port. The column selected produced satisfactory resolution and sho...

journal_title：Journal of pharmaceutical sciences

authors： Ward HE Jr,Freeman JJ,Sowell JW,Kosh JW

更新日期：1981-04-01 00:00:00

abstract：:This work compares the conformational stability, backbone flexibility, and aggregation propensity of monomer and dimer fractions of an IgG1 monoclonal antibody (mAb) generated on UVA light exposure for up to 72 h collected by preparative size-exclusion chromatography, compared with unstressed control. UVA light exposu...

journal_title：Journal of pharmaceutical sciences

authors： Bommana R,Chai Q,Schöneich C,Weiss WF 4th,Majumdar R

更新日期：2018-06-01 00:00:00

abstract：:Tritium-labeled progesterone was administered to mature female rats in the proestrous stage by three different routes, gastric intubation, subcutaneous injection, and uterine intraluminal instillation, to study the kinetics involved in the uptake and retention of radioactivity by the uterus and various other tissues. ...

journal_title：Journal of pharmaceutical sciences

authors： Fang SM,Lin CS,Lyon V

更新日期：1977-12-01 00:00:00

abstract：:The synthesis of some substituted 7-hydroxy-5H-1,3,4-oxadiazolo [3,2-a]pyrimidin-5-ones, a class of bicyclics with unexplored pharmacotoxicological properties, is described. Reacting the 2-phenyl derivative with bis(2,4,5-trichlorophenyl)benzylmalonate afforded a linear pyrano-oxadiazolopyrimidinedione. The assigned s...

journal_title：Journal of pharmaceutical sciences

authors： Soliman FS,Shafik RM,Darwish M

更新日期：1982-02-01 00:00:00

abstract：:The ability to produce and isolate relatively pure amounts of relevant degradation products is key to several aspects of drug product development: (a) aid in the unambiguous structural identification of such degradation products, fulfilling regulatory requirements to develop safe formulations (International Conference...

journal_title：Journal of pharmaceutical sciences

authors： Nanda KK,Mozziconacci O,Small J,Allain LR,Helmy R,Wuelfing WP

更新日期：2019-04-01 00:00:00

abstract：:The structural integrity and conformational stability of various IgG1-Fc proteins produced from the yeast Pichia pastoris with different glycosylation site occupancy (di-, mono-, and nonglycosylated) were determined. In addition, the physical stability profiles of three different forms of nonglycosylated Fc molecules ...

journal_title：Journal of pharmaceutical sciences

authors： Alsenaidy MA,Okbazghi SZ,Kim JH,Joshi SB,Middaugh CR,Tolbert TJ,Volkin DB

更新日期：2014-06-01 00:00:00

abstract：:The widespread use of butylated hydroxyanisole (I) and butylated hydroxytoluene (II) as food antioxidants recently has been criticized by the Food and Drug Administration because of their pharmacological and toxicological effects. Interest also has arisen recently in the use of these compounds as anticancer agents. Th...

journal_title：Journal of pharmaceutical sciences

authors： El-Rashidy R,Niazi S

更新日期：1980-12-01 00:00:00

abstract：:Corneal permeability data taken from the literature were analyzed for possible quantitative relationships with physicochemical properties. Although a parabolic relationship was obtained with good correlation between lipophilicity, as expressed by the 1-octanol-water partition coefficients, log Poctanol (or the distrib...

journal_title：Journal of pharmaceutical sciences

authors： Yoshida F,Topliss JG

更新日期：1996-08-01 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 aim of this study was to characterize the in vitro hepatic uptake kinetics of sodium fluorescein (NaFluo) and identify the transporters involved. NaFluo exhibited saturable uptake kinetics in suspended rat and human hepatocytes as reflected by K(m) values of 22.5 and 14.1 µM, and V(max) values of 98.3 and 5.8 pmol...

journal_title：Journal of pharmaceutical sciences

authors： De Bruyn T,Fattah S,Stieger B,Augustijns P,Annaert P

更新日期：2011-11-01 00:00:00

abstract：:Nonsteroidal anti-inflammatory drugs (NSAIDs) are among the most frequently used drugs in the world, primarily for symptoms associated with osteoarthritis and other chronic musculoskeletal conditions. However, adverse effects caused by oral administration, such as local or systemic disturbance in the gastrointestinal ...

journal_title：Journal of pharmaceutical sciences

authors： Cheng Y,Man N,Xu T,Fu R,Wang X,Wang X,Wen L

更新日期：2007-03-01 00:00:00

abstract：:Maintaining a native-like structure of protein pharmaceuticals during lyophilization is an important aspect of formulation. Infrared spectroscopy can be used to evaluate the effectiveness of formulations in protecting the secondary structural integrity of proteins in the dried solid. This necessitates making quantitat...

journal_title：Journal of pharmaceutical sciences

authors： Kendrick BS,Dong A,Allison SD,Manning MC,Carpenter JF

更新日期：1996-02-01 00:00:00

abstract：:3,6-Diformyl- and 3,6-dipropanoylmorphine and 6-formyl- and 6-propanoylmorphine were prepared to obtain longer acting, heroin-like compounds. The 6-acylated compounds were more potent than heroin subcutaneously and were orally effective, and their duration of action was at least two to three times greater than that of...

journal_title：Journal of pharmaceutical sciences

authors： May EL,Jacobson AE

更新日期：1977-02-01 00:00:00

abstract：:Dose individualization is essential in epilepsy treatment, especially in antiepileptic drugs that present high interindividual variability such as lamotrigine. We aimed an observational study to develop a population pharmacokinetic model for quantitative evaluation of the factors that influence lamotrigine pharmacokin...

journal_title：Journal of pharmaceutical sciences

authors： Chávez-Castillo CE,Medellín-Garibay SE,Milán-Segovia RDC,Rodríguez-Leyva I,Romano-Moreno S

更新日期：2020-09-01 00:00:00

abstract：:Bioadhesive polymers that bind to the gastric mucin or epithelial cell surface are useful in drug delivery for the purposes of (a) retaining a dosage from in the GI tract and (b) increasing the intimacy and duration of contact of drug with the absorbing membrane. Polycarbophil has previously been shown to have bioadhe...

journal_title：Journal of pharmaceutical sciences

authors： Longer MA,Ch'ng HS,Robinson JR

更新日期：1985-04-01 00:00:00

abstract：:This paper describes the synthesis and characterization of cationic copolymers with different macromolecular architecture and drug delivery properties of the corresponding dexamethasone sodium phosphate (DSP)-loaded systems. Copolyelectrolytes comprising poly[2-(acryloyloxy)ethyl] trimethylammonium chloride (PAETMAC) ...

journal_title：Journal of pharmaceutical sciences

authors： Georgieva D,Kostova B,Ivanova S,Rachev D,Tzankova V,Kondeva-Burdina M,Christova D

更新日期：2014-08-01 00:00:00

abstract：:The concentrations of antipyrine in plasma and saliva were equivalent in normal volunteers and in patients with acute viral hepatitis following oral doses of antipyrine. Estimates of clearance, volume of distribution, and half-life made from either plasma or saliva samples were not statistically different in these sub...

journal_title：Journal of pharmaceutical sciences

authors： Meffin PJ,Williams RL,Blaschke TF,Rowland M

更新日期：1977-01-01 00:00:00

abstract：:The intense blue color formed in the official assay of menadione injection by treatment of the sample with 2,4-dinitrophenylhydrazine and ammonia is shown by data from visible light spectra and mass spectra and by comparison of the pKa value with that of the corresponding reaction product of acetone to be due to proto...

journal_title：Journal of pharmaceutical sciences

authors： Burns LB,Stedman RJ,Tuckerman MM

更新日期：1978-02-01 00:00:00

abstract：:Responses from the second Product Quality Research Institute (PQRI) Blend Uniformity Working Group (BUWG) survey of industry have been reanalyzed to identify potential links between formulation and processing variables and the measured uniformity of blends and unit dosage forms. As expected, the variability of the ble...

journal_title：Journal of pharmaceutical sciences

authors： Hancock BC,Garcia-Munoz S

更新日期：2013-03-01 00:00:00

abstract：:The use of enzymes as therapeutics is very promising because of their catalytic activity and specificity. However, intracellular delivery of active enzymes is challenging due to their low stability and large size. The production of protein-enzyme nanoparticles was investigated with the goal of developing a protein car...

journal_title：Journal of pharmaceutical sciences

authors： Estrada LH,Chu S,Champion JA

更新日期：2014-06-01 00:00:00

abstract：:NF-kappaB activation is clearly linked to the pathogenesis of multiple inflammatory diseases including arthritis. The prominent role of IkappaB kinase-2 (IKK-2) in regulating NF-kappaB signaling in response to proinflammatory stimuli has made IKK-2 a primary anti-inflammation therapeutic target. PHA-408, a potent and ...

journal_title：Journal of pharmaceutical sciences

authors： Chiang PC,Kishore NN,Thompson DC

更新日期：2010-03-01 00:00:00

abstract：:Alkyl esters of ketorolac were synthesized as potential prodrugs for transdermal delivery and evaluated to determine the relationship between their skin permeation characteristics and their physicochemical properties. Solubility of the prodrugs in various vehicles was determined at room temperature while lipophilicity...

journal_title：Journal of pharmaceutical sciences

authors： Doh HJ,Cho WJ,Yong CS,Choi HG,Kim JS,Lee CH,Kim DD

更新日期：2003-05-01 00:00:00

abstract：:The rapid hydrolysis of epoprostenol to 6-keto-prostaglandin F1 alpha is hydronium ion-catalyzed even at pH 10 or higher. In the presence of 1.0% hexadecyltrimethylammonium chloride, the rate was reduced significantly (1580-fold at pH 2 and 283-fold at a physiological pH). This decrease in the hydrolysis rate is attri...

journal_title：Journal of pharmaceutical sciences

authors： Cho MJ

更新日期：1982-04-01 00:00:00

abstract：:Controlled-release delivery of 6-beta-naltrexol (NTXOL), the major active metabolite of naltrexone, via a transdermal patch is desirable for treatment of alcoholism. Unfortunately, NTXOL does not diffuse across skin at a therapeutic rate. Therefore, the focus of this study was to evaluate microneedle (MN) skin permeat...

journal_title：Journal of pharmaceutical sciences

authors： Banks SL,Pinninti RR,Gill HS,Paudel KS,Crooks PA,Brogden NK,Prausnitz MR,Stinchcomb AL

更新日期：2010-07-01 00:00:00

abstract：:Gelrite, a heteropolysaccharide that forms a gel in the presence of cations, was tested in humans for its efficacy as an ophthalmic vehicle by a nonivasive fluorometric technique. Fluorescein was used as the tracer, and its concentration in the anterior chamber was used as the principal measure of bioavailability. The...

journal_title：Journal of pharmaceutical sciences

authors： Maurice DM,Srinivas SP

更新日期：1992-07-01 00:00:00

abstract：:It is shown that tricalcium phosphate follows a simple Heckel relationship in pressures of usual tablet compression, only if a density of 1.92 g/mL is used. This coincides with the density obtained by wet pycnometry, whereas the crystallographical density is 3.1 g/mL. The interpretation is that some of the pore space ...

journal_title：Journal of pharmaceutical sciences

authors： Hou XP,Carstensen JT

更新日期：1985-04-01 00:00:00

abstract：:The purpose of this paper was to investigate the relaxation behavior of amorphous hesperetin (HRN), using dielectric spectroscopy, and assessment of its crystallization kinetics above glass transition temperature (Tg ). Amorphous HRN exhibited both local (β-) and global (α-) relaxations. β-Relaxation was observed belo...

journal_title：Journal of pharmaceutical sciences

authors： Shete G,Khomane KS,Bansal AK

更新日期：2014-01-01 00:00:00