Synthesis and irreversible beta-adrenergic blockade with a bromoacetamido derivative of betaxolol.

abstract：:An electron-capture GLC method was developed for measuring pindolol in human plasma and urine. The unchanged drug was extracted with benzene from alkalinized plasma or urine using propranolol as the internal standard. Both compounds subsequently were back-extracted into 0.1 M HCl and then into benzene. After evaporati...

journal_title：Journal of pharmaceutical sciences

authors： Guerret M,Lavene D,Kiechel JR

更新日期：1980-10-01 00:00:00

abstract：:The aim of this study was to determine the sensitivity of transgenic immune tolerant mice for the type and level of aggregation of recombinant human interferon alpha2b (rhIFNalpha2b). RhIFNalpha2b was aggregated by metal-catalyzed oxidation or by incubation at elevated temperature and various pHs. Native rhIFNalpha2b ...

journal_title：Journal of pharmaceutical sciences

authors： Hermeling S,Schellekens H,Maas C,Gebbink MF,Crommelin DJ,Jiskoot W

更新日期：2006-05-01 00:00:00

abstract：:Human alpha(1)-acid glycoprotein (AGP), a major carrier of many basic drugs in circulation, consists of at least two genetic variants, namely A and F1*S variant. Interestingly, the variants of AGP have different drug-binding properties. The purpose of this study was to identify the amino acid residues that are respons...

journal_title：Journal of pharmaceutical sciences

authors： Nishi K,Ueno M,Murakami Y,Fukunaga N,Akuta T,Kadowaki D,Watanabe H,Suenaga A,Maruyama T,Otagiri M

更新日期：2009-11-01 00:00:00

abstract：:Many pathophysiological circumstances vary during 24 h periods. Many physiologic processes undergo biological rhythms, including the sleep-wake rhythm and metabolism. Disruptive effect in the 24 h variations can manifest as the emergence or exacerbation of pathological conditions. So, chronotherapeutics is gaining inc...

journal_title：Journal of pharmaceutical sciences

authors： Ohdo S,Koyanagi S,Matsunaga N,Hamdan A

更新日期：2011-09-01 00:00:00

abstract：:The storage of drug substance at subzero temperatures mitigates potential risks associated with liquid storage, such as degradation and shipping stress, making it the best solution for long-term storage. However, slower (generally uncontrolled) rates of freezing and thawing of drug substance in conventional large stor...

journal_title：Journal of pharmaceutical sciences

authors： Rayfield WJ,Kandula S,Khan H,Tugcu N

更新日期：2017-08-01 00:00:00

abstract：:The combined clearance of endogenous 6β-hydroxycortisol and 6β-hydroxycortisone is suggested biomarker for in vivo cytochrome P450 3A (CYP3A) activity. We aimed to determine whether the combined clearance of these two markers together with information of biopharmaceutics classification system (BCS) of drugs could be u...

journal_title：Journal of pharmaceutical sciences

authors： Luo X,Zheng L,Cai N,Liu Q,Yang S,He X,Cheng Z

更新日期：2015-10-01 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：:An HPLC method for the simultaneous determination of safrole (S), dihydrosafrole (DHS), and chloromethyldihydrosafrole (CM-DHS) in piperonyl butoxide, with fluorimetric detection and elution gradient, is described. Samples with internal standard (piperonyl isobutyrate) are adsorbed on silica cartridges, then eluted wi...

journal_title：Journal of pharmaceutical sciences

authors： Schreiber-Deturmeny EM,Pauli AM,Pastor JL

更新日期：1993-08-01 00:00:00

abstract：:Jet-milling as the common way for micronization of drugs shows several disadvantages. Drug powder properties are decisive for pulmonary use because, besides a small particle size, a good deagglomeration behavior is required. In this study, several anti-inflammatory drugs [beclomethasone-17,21-dipropionate (BDP), betam...

journal_title：Journal of pharmaceutical sciences

authors： Rasenack N,Steckel H,Müller BW

更新日期：2003-01-01 00:00:00

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 biological activity of a series of 10 silver sulfanilamides is studied in relation to the physical parameters pK alpha, log K, and the aqueous solubility. None of the parameters demonstrate a simple relationship with the activity. A discussion of the significance of log K and the solubility in relation to the acti...

journal_title：Journal of pharmaceutical sciences

authors： Bult A,Bajema BL,Boelema GJ,Saene JJ,Doornbos DA

更新日期：1984-01-01 00:00:00

abstract：:Targeted echogenic liposome dispersions for ultrasonic enhancement of vasoactive and pathological components of endothelium and atherosclerosis have recently been developed. The component lipids required for acoustic and targeting properties include phosphatidylcholine, phosphatidylethanolamine phosphatidylglycerol (P...

journal_title：Journal of pharmaceutical sciences

authors： Huang SL,Hamilton AJ,Nagaraj A,Tiukinhoy SD,Klegerman ME,McPherson DD,Macdonald RC

更新日期：2001-12-01 00:00:00

abstract：:3D cultures of primary human hepatocytes (PHH) are emerging as a more in vivo-like culture system than previously available hepatic models. This work describes the characterisation of drug metabolism in 3D PHH spheroids. Spheroids were formed from three different donors of PHH and the expression and activities of impo...

journal_title：Journal of pharmaceutical sciences

authors： Kanebratt KP,Janefeldt A,Vilén L,Vildhede A,Samuelsson K,Milton L,Björkbom A,Persson M,Leandersson C,Andersson TB,Hilgendorf C

更新日期：2021-01-01 00:00:00

abstract：:Acitretin, a retinoid for the treatment of severe psoriasis, exhibits extremely low aqueous solubility and high photosensitivity. This study investigated the effects of the complexation of acitretin with the respective hydroxypropyl-beta-cyclodextrin (HPBCD) and randomly substituted methyl-beta-cyclodextrin (RMBCD) on...

journal_title：Journal of pharmaceutical sciences

authors： Liu X,Lin HS,Thenmozhiyal JC,Chan SY,Ho PC

更新日期：2003-12-01 00:00:00

abstract：:A GLC method for the determination of valproic acid and ethosuximide in plasma was developed. The procedure involved a single solvent extraction of drugs from acidified plasma samples, followed by a GLC injection of the unconcentrated organic phase. This rapid, sensitive, specific, and reproducible method has been use...

journal_title：Journal of pharmaceutical sciences

authors： Riva R,Albani F,Baruzzi A

更新日期：1982-01-01 00:00:00

abstract：:Chloroquine (7-chloro-4-[[4-(diethylamino)-1-methylbutyl]amino]quinoline; CQ) accumulates in the insoluble fraction of rat muscle homogenates with an equilibrium distribution ratio of 7.8 L/kg. This is of a similar magnitude to muscle:plasma ratios observed in vivo. Uptake is approximately linear, even up to concentra...

journal_title：Journal of pharmaceutical sciences

authors： MacIntyre AC,Cutler DJ

更新日期：1986-11-01 00:00:00

abstract：:Both nonequilibrium and equilibrium models were proposed to explain the optimal biological response to a set of congeners with respect to the oil-water partition coefficient (P). A detailed analysis of the kinetic model proposed by Hansch demonstrates the bilinear form of the model, with the initial slope of the logar...

journal_title：Journal of pharmaceutical sciences

authors： Cooper ER,Berner B,Bruce RD

更新日期：1981-01-01 00:00:00

abstract：:The aim of this study is to prepare novel pH-sensitive beads to obtain a gastric mucosa protective formulation and to ensure drug delivery into the intestine. Diclofenac sodium was used as a model drug. Bead formation was achieved by ionotropic gelation method using three-component gel system containing sodium alginat...

journal_title：Journal of pharmaceutical sciences

authors： Fenyvesi Z,Auner A,Schmalz D,Pásztor E,Csóka G,Gyires K,Marton S,Klebovich I,Antal I

更新日期：2009-11-01 00:00:00

abstract：:Both developing (Days --1-+12 relative to inoculation) and established (Days +18-+29) stages of Mycobacterium butyricum adjuvant-induced polyarthritis in rats were treated orally with cryogenine (100 mg/kg/day), a prototype anti-inflammatory (phenylbutazone, 100 mg/kg/day), or a prototype immunosuppressive (cyclophosp...

journal_title：Journal of pharmaceutical sciences

authors： Watson WC,Malone MH

更新日期：1977-09-01 00:00:00

abstract：:The chemical shifts of the methyl groups of 2,4-dimethylbenzo[g]quinoline are defined with respect to concentration, showing that the methyl resonances are reversed from their expected positions in concentrations normally used in NMR spectroscopy. The phenomenon is explained in terms of the probably "fixation" of bond...

journal_title：Journal of pharmaceutical sciences

authors： Born JL,Harsin CE

更新日期：1977-08-01 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

abstract：:Subcutaneous injection allows for self-administration of monoclonal antibodies using prefilled syringes, autoinjectors, and on-body injector devices. However, subcutaneous injections are typically limited to 1 mL due to concerns of injection pain from volume, viscosity, and formulation characteristics. Back pressure c...

journal_title：Journal of pharmaceutical sciences

authors： Doughty DV,Clawson CZ,Lambert W,Subramony JA

更新日期：2016-07-01 00:00:00

abstract：:Oral Almotriptan maleate (ALM) is used in the treatment of migraine; however, due to its extreme aqueous solubility, shows poor penetration and lesser concentration in the brain thus requiring frequent oral dosing. Being flexible and lipophilic in nature, nanostructured lipid carriers (NLCs) represent a promising tool...

journal_title：Journal of pharmaceutical sciences

authors： Salem LH,El-Feky GS,Fahmy RH,El Gazayerly ON,Abdelbary A

更新日期：2020-07-01 00:00:00

abstract：:The distribution of zidovudine (AZT) between plasma, brain extracellular fluid (ECF), and cerebrospinal fluid (CSF) was investigated in a crossover design study (n = 5) in unanesthetized rabbits. Drug was administered by intravenous (iv) and intracerebroventricular (icv) infusions at the same infusion rate (1.5 mg/h.k...

journal_title：Journal of pharmaceutical sciences

authors： Wang Y,Sawchuk RJ

更新日期：1995-07-01 00:00:00

abstract：:An HPLC methodology is described which enables the quantitation of thiothixene (N,N-dimethyl-9-[3-(4-methyl-1-piperazinyl)-propylidene]thioxanthe ne-2- sulfonamide) in bulk drug, finished product, and dissolution samples using a single analytical column (SiAl: a mixture of silica and alumina). The Z (cis) and the less...

journal_title：Journal of pharmaceutical sciences

authors： Severin G

更新日期：1987-03-01 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：:Systemic administration of drugs is ineffective in the treatment of central nervous system disorders because of the blood-brain barrier. Nasal administration has been suggested as an alternative administration route as drugs absorbed in the olfactory epithelium bypass the blood-brain barrier and reach the brain within...

journal_title：Journal of pharmaceutical sciences

authors： Wu IY,Nikolaisen TE,Škalko-Basnet N,di Cagno MP

更新日期：2019-08-01 00:00:00

abstract：:Numerous studies have demonstrated that the administration of nonsteroidal anti-inflammatory drugs (NSAIDs) increases small intestinal permeability, and this has been suggested to be a prerequisite to enteropathy. It is believed that the inhibitory effect of chiral NSAIDs on the synthesis of prostaglandins and hence t...

journal_title：Journal of pharmaceutical sciences

authors： Davies NM,Wright MR,Russell AS,Jamali F

更新日期：1996-11-01 00:00:00

abstract：:Methods are presented for the separation of tetracycline, tetracycline analogs, and their potential impurities by reversed-phase ion-pair chromatography. The mobile phase consisted of a phosphate buffer with tripropylamine or N,N-dimethyloctylamine as counterions and acetonitrile as the organic modifier. The chromatog...

journal_title：Journal of pharmaceutical sciences

authors： Hermansson J,Andersson M

更新日期：1982-02-01 00:00:00

abstract：:Health authorities require that suitable stability of the drug substance be shown in relevant materials of construction. ICH Q1A(R2) explicitly states that "stability studies should be conducted on drug substance packaged in a container closure system that is the same as or simulates the packaging proposed for storage...

journal_title：Journal of pharmaceutical sciences

authors： Klair N,Kim MT,Lee A,Xiao NJ,Patel AR

更新日期：2020-10-07 00:00:00