Preformulation-Assisted Design and Characterization of Modified Release Gastroretentive Floating Extrudates Towards Improved Bioavailability and Minimized Side Effects of Baclofen.

abstract：:The thermodynamic relationship between FI and FII of ethyl 4-aminobenzoate (benzocaine) has been investigated. Slurry conversion experiments show that the transition temperature below which FI is stable is located between 302 K-303 K (29 °C-30 °C). The polymorphs FI and FII have been characterised by infrared spectros...

journal_title：Journal of pharmaceutical sciences

authors： Cheuk D,Svärd M,Rasmuson ÅC

更新日期：2020-11-01 00:00:00

abstract：:High pressure liquid chromatography using reversed-phase and/or ion-pair techniques was used to optimize resolution of aspirin-containing muscle relaxant mixtures as well as other therapeutic agents commonly found in muscle relaxant-analgesic mixtures. The compounds were chromatographed on an octadecylsilane column us...

journal_title：Journal of pharmaceutical sciences

authors： Stewart JT,Honigberg IL,Coldren JW

更新日期：1979-01-01 00:00:00

abstract：:Uptake of the fluorescent probe, 1-anilino-8-naphthalene-sulfonate (I) into isolated rat liver cells was studied using both fluorescence and filtration methods. The time course of the fluorescence enhancement of I after addition to the isolated liver cells was analyzed in terms of rapid, medium, and slow phases. The s...

journal_title：Journal of pharmaceutical sciences

authors： Sugiyama Y,Kimura S,Lin JH,Izukura M,Awazu S,Hanano M

更新日期：1983-08-01 00:00:00

abstract：:To characterize and evaluate human serum albumin-encapsulated nanoparticles for drug delivery of a tyrosine kinase inhibitor combined with induction of photothermal ablation combination therapy of renal cell carcinoma (RCC), nanoparticles of varying preparations and concentrations were characterized via zeta potential...

journal_title：Journal of pharmaceutical sciences

authors： Callaghan C,Peralta D,Liu J,Mandava SH,Maddox M,Dash S,Tarr MA,Lee BR

更新日期：2016-01-01 00:00:00

abstract：:The correlation of log P (in octanol--water) with the nonempirical, topologically dependent, calculated molecular connectivity index (1chiv) delineates substituted hydroxyureas into two families of linearly related groups of compounds. The first group, composed of the 3-substituted ethyl, n-propyl, and n-butyl analogs...

journal_title：Journal of pharmaceutical sciences

authors： Parker GR

更新日期：1978-04-01 00:00:00

abstract：:3-Fluoro-, 3-chloro-, and 3-bromocyclophosphamide were prepared from the reaction of trifluoromethylhypofluorite, sodium hypochlorite, and bromine with the anticancer drug cyclophosphamide. Treatment of cis- and trans-4-phenylcyclophosphamide and 5,6-benzocyclophosphamide with sodium hypochlorite afforded cis- and tra...

journal_title：Journal of pharmaceutical sciences

authors： Zon G,Ludeman SM,Ozkan G,Chandrasegaran S,Hammer CF,Dickerson R,Mizuta K,Egan W

更新日期：1983-06-01 00:00:00

abstract：:Personalized medicine aims to determine the most adequate treatment and dose regimen to obtain the maximum efficacy and minimum side effect by taking into account patients' characteristics. For numerous reasons, one being ethical and methodological hurdles in including specific populations in clinical trials, innovati...

journal_title：Journal of pharmaceutical sciences

authors： Marsousi N,Desmeules JA,Rudaz S,Daali Y

更新日期：2017-09-01 00:00:00

abstract：:The relative sweetness, onset times, and durations of response of D-glucose, D-xylose, D-quinovose, D-galactose, L-arabinose, and D-fucose were determined at four temperatures. The results can be interpreted by simple concepts of intramolecular hydrogen bonding which indicate that the so-called gamma-function of the t...

journal_title：Journal of pharmaceutical sciences

authors： Birch GG,Dziedzic SZ,Shallenberger RS,Lindley MG

更新日期：1981-03-01 00:00:00

abstract：:A dermal penetration enhancer has been found which improves the dermal delivery of a wide variety of drugs and at the same time has a history of low toxicity for human dermal application. N,N-Diethyl-m-toluamide (I) has been shown to improve the delivery of many drugs through hairless mouse skin in an in vitro diffusi...

journal_title：Journal of pharmaceutical sciences

authors： Windheuser JJ,Haslam JL,Caldwell L,Shaffer RD

更新日期：1982-11-01 00:00:00

abstract：:A model based on heat transport control was developed to describe the uptake of water on a deliquescent solid in an atmosphere of pure water vapor. The model assumes the presence of a saturated liquid film on the surface of the solid. The decrease in the vapor pressure of water over the surface, brought about by the c...

journal_title：Journal of pharmaceutical sciences

authors： Van Campen L,Amidon GL,Zografi G

更新日期：1983-12-01 00:00:00

abstract：:Understanding the effect of surfactant properties is critical when designing vesicular delivery systems. This review evaluates previous studies to explain the influence of surfactant properties on the behavior of lipid vesicular systems, specifically their size, charge, stability, entrapment efficiency, pharmacokineti...

journal_title：Journal of pharmaceutical sciences

authors： Bnyan R,Khan I,Ehtezazi T,Saleem I,Gordon S,O'Neill F,Roberts M

更新日期：2018-05-01 00:00:00

abstract：:This study examined the safety, pharmacodynamic and pharmacokinetic similarity of the human recombinant filgrastim products ior®LeukoCIM and Neupogen® following a 28-day repeated subcutaneous dose administration in male and female Sprague-Dawley rats with a 14-day recovery period. Safety profiling was based on clinica...

journal_title：Journal of pharmaceutical sciences

authors： Licollari A,Riddle K,Taylor SR,Ledon N,Bolger GT

更新日期：2017-06-01 00:00:00

abstract：:Thirty-four vasodilators were screened in several in vitro biochemical assays related to smooth muscle excitation-contraction coupling, binding to beta 1-,beta 2-, and alpha-adrenergic receptors, inhibition of phosphodiesterase activity, and antagonism of calcium accumulation. Isoproterenol and perhexiline only exhibi...

journal_title：Journal of pharmaceutical sciences

authors： Greenslade FC,Scott CK,Newquist KL,Krider KM,Chasin M

更新日期：1982-01-01 00:00:00

abstract：:Peptide-based therapies have the potential to induce antibody formation if the molecules differ from a native human peptide. Several reports have disclosed the occurrence of antibody generation in a patient treated with exenatide. The immune response can be problematic from a clinical stand point, particularly if the ...

journal_title：Journal of pharmaceutical sciences

authors： Lim SM,Eom HN,Jiang HH,Sohn M,Lee KC

更新日期：2015-01-01 00:00:00

abstract：:The synthesis, characterization, and therapeutic evaluation of a series of partially esterified derivatives of pentetic (diethylenetriaminepentaacetic) acid are reported. These compounds were prepared in an attempt to promote increased decorporation of insoluble colloidal forms of plutonium, which are removed by pente...

journal_title：Journal of pharmaceutical sciences

authors： Guilmette RA,Parks JE,Lindenbaum A

更新日期：1979-02-01 00:00:00

abstract：:The pharmaceutical industry has large investments in compound library enrichment, high throughput biological screening, and biopharmaceutical (ADME) screening. As the number of compounds submitted for in vitro ADME screens increases, data analysis, interpretation, and reporting will become rate limiting in providing A...

journal_title：Journal of pharmaceutical sciences

authors： Stoner CL,Gifford E,Stankovic C,Lepsy CS,Brodfuehrer J,Prasad JV,Surendran N

更新日期：2004-05-01 00:00:00

abstract：:Thiamine hydrochloride (Vitamin B(1), THCl) can exist as a nonstoichiometric hydrate (NSH) and as a hemihydrate (HH). NSH can contain up to approximately 1 molar equivalent of water and be dehydrated to an isomorphic desolvate (ID) with minimal change in lattice structure. Crystallographic and spectroscopic techniques...

journal_title：Journal of pharmaceutical sciences

authors： Chakravarty P,Berendt RT,Munson EJ,Young VG Jr,Govindarajan R,Suryanarayanan R

更新日期：2010-02-01 00:00:00

abstract：:The use of various synthetic lipids and polymers to deliver DNA for gene therapy applications has been the subject of intense examination for the last 15 years. Our understanding of the processes involved in the delivery of DNA, although still limited, can be described in terms of specific physical and chemical barrie...

journal_title：Journal of pharmaceutical sciences

authors： Wiethoff CM,Middaugh CR

更新日期：2003-02-01 00:00:00

abstract：:The pharmacokinetics and safety of TY-11345 [(+/-)-2-[(4-methoxy-6,7,8,9-tetrahydro-5H-cyclohepta[b]pyridin-9- yl)sulfinyl]-1H-benzimidazole sodium salt], a novel gastric proton pump inhibitor, were studied in healthy male volunteers after single (20, 40, and 80 mg) and repeated oral doses (60 mg, once daily for 7 day...

journal_title：Journal of pharmaceutical sciences

authors： Uematsu T,Nakano M,Kosuge K,Nagai A,Sato A,Nakashima M

更新日期：1994-10-01 00:00:00

abstract：:A heparin derivative sufficiently lipophilic to be bound to plastics, forming blood-compatible supports, or to be used as an anticoagulant by transdermal or oral routes would be of great pharmaceutical interest. For such applications, the functional groups within heparin's antithrombin III binding site, responsible fo...

journal_title：Journal of pharmaceutical sciences

authors： Liu J,Pervin A,Gallo CM,Desai UR,Van Gorp CL,Linhardt RJ

更新日期：1994-07-01 00:00:00

abstract：:There is a growing interest in developing inhibitors of the neonatal Fc-receptor, FcRn, for use in the treatment for humoral autoimmune conditions. We have developed a new physiologically based pharmacokinetic model that is capable of characterizing the pharmacokinetics and pharmacodynamics of anti-FcRn monoclonal ant...

journal_title：Journal of pharmaceutical sciences

authors： Li T,Balthasar JP

更新日期：2019-01-01 00:00:00

abstract：:A method for the measurement of a potential diuretic-antihypertensive agent, (+/-)-[[6,7-dichloro-2-(4-fluorophenyl)-2-methyl-1-oxo-5-indanyl] oxy]acetic acid, in biological fluids is described. The procedure involves the addition of a related internal standard to the specimens followed by extraction of the acids into...

journal_title：Journal of pharmaceutical sciences

authors： Weidner LL,Zacchei AG

更新日期：1984-02-01 00:00:00

abstract：:An emerging technology subtype that has been adopted by formulators to address low-solubility issues is the supersaturating drug delivery system; this system is based on the "spring" and "parachute" design elements, which have been applied to lipid-based formulations, S(M)EDDS, solid dispersions, nano-based systems, a...

journal_title：Journal of pharmaceutical sciences

authors： Augustijns P,Brewster ME

更新日期：2012-01-01 00:00:00

abstract：:Bacmecillinam is an amdinocillin prodrug designed to be easily hydrolyzed in biological materials, so special procedures were developed for the collection of blood specimens. Whole blood was collected in tubes containing bacampicillin as an adsorption inhibitor and kept at -70 degrees; the extracting solvent, hexane-m...

journal_title：Journal of pharmaceutical sciences

authors： Westerlund D,Pettersson B,Carlqvist J

更新日期：1982-10-01 00:00:00

abstract：:The present study was carried out to investigate the blood-to-retina transport of nicotine across the inner blood-retinal barrier (BRB). Using the in vivo vascular injection method, the blood-to-retina influx clearance of nicotine across the BRB was determined as 131 μL/(min?g retina), which is much higher than that o...

journal_title：Journal of pharmaceutical sciences

authors： Tega Y,Kubo Y,Yuzurihara C,Akanuma S,Hosoya K

更新日期：2015-09-01 00:00:00

abstract：:In liver microsomes, selexipag (NS-304; ACT-293987) mainly undergoes hydrolytic removal of the sulfonamide moiety by carboxylesterase 1 (CES1) to yield the pharmacologically active metabolite MRE-269 (ACT-333679). However, it is not known how much CES in the liver and intestine contributes to the hydrolysis of selexip...

journal_title：Journal of pharmaceutical sciences

authors： Imai S,Ichikawa T,Sugiyama C,Nonaka K,Yamada T

更新日期：2019-02-01 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：:Solubilization of nonpolar drugs constitutes one of the most important tasks in parenteral formulations design. This study investigates and assesses the solubility enhancement of Fluasterone by various techniques including cosolvency, micellization, and complexation. Of the solubilizing agents used, the modified beta-...

journal_title：Journal of pharmaceutical sciences

authors： Zhao L,Li P,Yalkowsky SH

更新日期：1999-10-01 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：:The granule strength (crushing load) of lactose granulated with 1-9% povidone was measured initially and at intervals during a 1-year period. The granule strengths of dibasic calcium phosphate dihydrate granulated with various concentrations of starch and povidone were measured. The axial and radial tensile strengths ...

journal_title：Journal of pharmaceutical sciences

authors： Jarosz PJ,Parrott EL

更新日期：1983-05-01 00:00:00