Enhanced potency of human calcitonin when fibrillation is avoided.

abstract：:This study evaluates the effect of variation in the ambient moisture on the compaction behavior of microcrystalline cellulose (MCC) powder. The study was conducted by comparing the physico-mechanical properties of, and the near infrared (NIR) spectra collected on, compacts prepared by roller compaction with those coll...

journal_title：Journal of pharmaceutical sciences

authors： Gupta A,Peck GE,Miller RW,Morris KR

更新日期：2005-10-01 00:00:00

abstract：:The disposition of radioactivity following oral administration of 14C-norgestimate was compared to that following administration of the drug in combination with 3H-ethinyl estradiol in humans. Seven normal, healthy female subjects were each administered one capsule orally containing 14C-norgestimate either alone (74.4...

journal_title：Journal of pharmaceutical sciences

authors： Weintraub HS,Abrams LS,Patrick JE,McGuire JL

更新日期：1978-10-01 00:00:00

abstract：:Time and resource constraints necessitate increasingly early decision making to accelerate or stop preclinical drug discovery programs. Early discovery drug candidates may be potent inhibitors of new targets, but all too often exhibit poor pharmaceutical and pharmacokinetic properties that limit the in vivo exposure. ...

journal_title：Journal of pharmaceutical sciences

authors： Chiang PC,South SA,Foster KA,Daniels JS,Wene SP,Albin LA,Thompson DC

更新日期：2010-07-01 00:00:00

abstract：:A GLC method for the determination of procainamide in biological fluids is presented. By using a dipropyl analog of procainamide as an internal standard, both compounds can be chromatographed directly, yielding linear calibration curves and a sensitivity that allows quantitative determination of concentrations as low ...

journal_title：Journal of pharmaceutical sciences

authors： Simons KJ,Levy RH

更新日期：1975-12-01 00:00:00

abstract：:Solubilities in isoctane and water were determined for several C1-phenolic esters of prostaglandin F2 alpha and prostaglandin E2 and acetates having the same phenol moiety. Linear free energy relationships for solubility among the series were observed with slopes of approximately 1. These results suggest that the cont...

journal_title：Journal of pharmaceutical sciences

authors： Anderson BD,Conradi RA

更新日期：1980-04-01 00:00:00

abstract：:A new parameter, the kinetic ratio, is suggested for estimating product potency during storage under ambient warehouse temperatures. Actual warehouse temperature data were integrated using Arrhenius kinetics, and the resulting potency errors, due both to the integration method and to temperature averaging, were evalua...

journal_title：Journal of pharmaceutical sciences

authors： Scher M

更新日期：1980-03-01 00:00:00

abstract：:A method for the determination of sematilide levels in human plasma is described. After the addition of an internal standard, plasma samples are adjusted to pH 8.5 and extracted with a solution of 7.5% isopropanol in methylene chloride. Separation from co-extracted matrix constituents is performed by reversed-phase HP...

journal_title：Journal of pharmaceutical sciences

authors： Dancik S,Koziol T,Nisperos E,Woolf E

更新日期：1991-02-01 00:00:00

abstract：:Vitamin E tocopherol polyethylene glycol succinate (TPGS) is a non-ionic surface active agent, known to enhance the bioavailability of lipophilic compounds via wettability, solubility, and in some cases permeability enhancement. MK-0536 is an anti-retroviral drug with poor wettability and solubility and a high dose. B...

journal_title：Journal of pharmaceutical sciences

authors： Tatavarti A,Kesisoglou F

更新日期：2015-11-01 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：:p-Bromospiperone was prepared from the reaction of spiperone with bromine. It was tested for dopamine receptor binding affinity in vitro and its ability to stimulate prolactin secretion in vivo. The results indicate no significant change of biological activities due to the bromination of spiperone. ...

journal_title：Journal of pharmaceutical sciences

authors： Huang CC,Friedman AM,So R,Simonovic M,Meltzer HY

更新日期：1980-08-01 00:00:00

abstract：:Avoiding unwanted immunogenicity is of key importance in the development of therapeutic drug proteins. Animal models are of less predictive value because most of the drug proteins are recognized as foreign proteins. However, different methods have been developed to obtain immunotolerant animal models. So far, the immu...

journal_title：Journal of pharmaceutical sciences

authors： Brenden N,Madeyski-Bengtson K,Martinsson K,Svärd R,Albery-Larsdotter S,Granath B,Lundgren H,Lövgren A

更新日期：2013-03-01 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：:The purpose of this work was to investigate the self-associating behavior observed in high concentration monoclonal antibody (MAb1) solutions at pH 6.0. Zeta potential measurements over the pH range (4.0-9.0) showed lower net charges present on the molecule at pH 6.0 and 7.0. The point of zero charge or crossover from...

journal_title：Journal of pharmaceutical sciences

authors： Yadav S,Liu J,Shire SJ,Kalonia DS

更新日期：2010-03-01 00:00:00

abstract：:A sensitive, specific, high-performance liquid chromatographic procedure was developed for the measurement of plasma tiflamizole levels. Acidic plasma samples were extracted with three volumes of ether. The ether extracts were combined and evaporated to dryness. The residue was dissolved in acetonitrile, washed with h...

journal_title：Journal of pharmaceutical sciences

authors： Rakestraw DC,Whitney CC Jr

更新日期：1984-12-01 00:00:00

abstract：:The purpose of this study was to examine the external predictability of an in vitro-in vivo correlation (IVIVC) for a metoprolol hydrophilic matrix extended-release formulation, with an acceptable internal predictability, in the presence of a range of formulation/manufacturing changes. In addition, this report evaluat...

journal_title：Journal of pharmaceutical sciences

authors： Mahayni H,Rekhi GS,Uppoor RS,Marroum P,Hussain AS,Augsburger LL,Eddington ND

更新日期：2000-10-01 00:00:00

abstract：:Water evaporation rates were measured from thin samples of a model layered structure of stratum corneum lipids with 32% water. A model with only free fatty acids present gave the lowest evaporation rates, while a model with only oleic acid gave values approximately 50% higher. Using the total lipid spectrum of stratum...

journal_title：Journal of pharmaceutical sciences

authors： Friberg SE,Kayali I

更新日期：1989-08-01 00:00:00

abstract：:The location and conformation of fosinopril sodium (FS) in a lamellar liquid crystal of water, sodium dodecyl sulfate, and decanol was studied by low-angle X-ray diffraction. The result showed the FS molecule to be located within the amphiphilic part of the liquid crystalline structure with the polar parts anchored at...

journal_title：Journal of pharmaceutical sciences

authors： Friberg SE,Moaddel T,Morris KR,Abramowitz R,Amsberry KL

更新日期：1994-05-01 00:00:00

abstract：:A series of molecular complexes, both co-crystals and salts, of a triazole drug-alprazolam-with carboxylic acids, boric acid, boronic acids, and phenols have been analyzed with respect to heterosynthons present in the crystal structures. In all cases, the triazole ring behaves as an efficient hydrogen bond acceptor wi...

journal_title：Journal of pharmaceutical sciences

authors： Varughese S,Azim Y,Desiraju GR

更新日期：2010-09-01 00:00:00

abstract：:Three analogs of thyroliberin (I) were prepared. These compounds, N-m-chloroacetylbenzoyl-phenylalanyl-prolineamide (VIa), N-p-chloroacetylbenzoyl-phenylalanyl-prolineamide (VIb) and N-chloroacetyl-alanyl-phenylalanyl-prolineamide (IX), were designed as potential I antagonist affinity labels. However, no significant a...

journal_title：Journal of pharmaceutical sciences

authors： Goebel RJ,Currie BL,Bowers CY

更新日期：1982-09-01 00:00:00

abstract：:Electron donor-acceptor complexes for a group of quinolines and naphthalenes with 9-(dicyanomethylene)-2,4,7-trinitrofluorene in 1,2-dichloroethane were studied by optical absorption methods. Association constants, molar absorptivities, and charge-transfer transition energies were evaluated for each system, together w...

journal_title：Journal of pharmaceutical sciences

authors： Webb NE,Thompson CC

更新日期：1978-02-01 00:00:00

abstract：:The stereochemistries of geometric isomers of 4-(2-bromo-1,2-diphenylvinyl)phenol, 4-(2-bromo-1,2-diphenylvinyl)anisole, and 2-[p-(2-bromo-1,2-diphenylvinyl)phenoxy]triethylamine were determined by conversion of the phenolic analog to the ethers and subsequent comparison of physical properties with those of 2-[p-(2-ch...

journal_title：Journal of pharmaceutical sciences

authors： Richardson A Jr,Benson HD,Hite G

更新日期：1976-10-01 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：:To design safe, efficient synthetic gene therapy vectors, it is desirable to understand the intracellular mechanisms that facilitate their delivery from the cell surface to the nucleus. Elements of the cytoskeleton and molecular motor proteins are known to play a pivotal role in most intracellular active transport pro...

journal_title：Journal of pharmaceutical sciences

authors： Drake DM,Pack DW

更新日期：2008-04-01 00:00:00

abstract：:Three families of alloxan derivatives, 5-arylthiobarbituric, 5-aryliminobarbituric, and 5-aryldialuric acids, were prepared as prospective radioiodine-transporting radiopharmaceuticals for the delineation of pancreatic insulinomas. Members of each class were screened for effects on blood sugar levels in a rat glucose ...

journal_title：Journal of pharmaceutical sciences

authors： Adams WE,Heindel ND,Tutwiler G,Fawthrop H

更新日期：1984-03-01 00:00:00

abstract：:Three dissolution apparatus, the rotating basket, the rotating paddle, and the rotating filter--stationary basket, were evaluated for their suitability as production control tools and their relation to blood level studies in dogs. The rotating basket and rotating paddle assemblies were easier to use and less variable ...

journal_title：Journal of pharmaceutical sciences

authors： Hardwidge EA,Sarapu AC,Laughlin WC

更新日期：1978-12-01 00:00:00

abstract：:The absorption-enhancing effects of polyamidoamine (PAMAM) dendrimers with various generations (G0-G3) and concentrations [0.1%-1.0% (w/v)] on the pulmonary absorption of peptide and protein drugs were studied in rats. Insulin and calcitonin were chosen as models of peptide and protein drugs, and their pulmonary absor...

journal_title：Journal of pharmaceutical sciences

authors： Dong Z,Hamid KA,Gao Y,Lin Y,Katsumi H,Sakane T,Yamamoto A

更新日期：2011-05-01 00:00:00

abstract：:Carbamazepine (CBZ) is a leading molecule in the management of epilepsy. Surveys have revealed that a sufficient lack of therapeutically efficient CBZ transbuccal formulation exists. Therefore, this investigation was directed toward designing multiparticulate composite construct (MCC) for the transbuccal delivery of C...

journal_title：Journal of pharmaceutical sciences

authors： Adeleke OA,Choonara YE,Du Toit LC,Pillay V

更新日期：2014-04-01 00:00:00

abstract：:A program is described that permits iterative least-squares nonlinear regression fitting of polyexponential curves using the Hewlett Packard HP 41 CV programmable calculator. The program enables the analysis of pharmacokinetic drug level profiles with a high degree of precision. Up to 15 data pairs can be used, and in...

journal_title：Journal of pharmaceutical sciences

authors： Thornhill DP,Schwerzel E

更新日期：1985-05-01 00:00:00

abstract：:Sol-to-gel systems of ciprofloxacin hydrochloride were prepared utilizing the phase transition properties of hydroxy propyl methyl cellulose K 15 M grade (HPMC) and carbopol 934. The sol-to-gel systems were sterilized by gamma radiation and/or filtration. The sol-to-gel systems were evaluated for rheological character...

journal_title：Journal of pharmaceutical sciences

authors： Charoo NA,Kohli K,Ali A

更新日期：2003-02-01 00:00:00

abstract：:Although many biotech products are successfully stored in the frozen state, there are cases of degradation of biologicals during freeze storage. These examples are discussed in the Perspective to emphasize the fact that stability of frozen biologicals should not be taken for granted. Frozen-state degradation (predomin...

journal_title：Journal of pharmaceutical sciences

authors： Authelin JR,Rodrigues MA,Tchessalov S,Singh SK,McCoy T,Wang S,Shalaev E

更新日期：2020-01-01 00:00:00