Convenient synthesis of (RS)-4-amino-3-hydroxybutyric acid.

abstract：:Chitosan and egg phosphatidylcholine (ePC) were used as a unique combination to prepare composite films for localized drug delivery. In comparison to other phospholipids analyzed, ePC was found to produce chitosan-based films with minimal swelling and a high degree of stability. The properties of the chitosan-ePC film...

journal_title：Journal of pharmaceutical sciences

authors： Grant J,Blicker M,Piquette-Miller M,Allen C

更新日期：2005-07-01 00:00:00

abstract：:The promoting efficacies of N-acyl derivatives of amino acids on the rectal absorption of sodium ampicillin were investigated using the rat rectal loop technique. N-Acyl derivatives with longer carbon chains in the acyl moiety showed a greater promoting potency. The promoting potencies of N-acyl derivatives of phenylg...

journal_title：Journal of pharmaceutical sciences

authors： Wu WM,Murakami T,Higashi Y,Yata N

更新日期：1987-07-01 00:00:00

abstract：:Pyrimethamine, an antimalarial drug, was found to be able to inhibit both enzymes (DHFR-TS and PTR1) of the leishmanial folate pathway, although this effect in vivo appears only in relatively high concentrations. To reach the parasites inside macrophage cells, where they are sheltered, targeted drugs of pyrimethamine,...

journal_title：Journal of pharmaceutical sciences

authors： De Carvalho PB,Ramos DC,Cotrim PC,Ferreira EI

更新日期：2003-10-01 00:00:00

abstract：:Experimental solubilities are reported for anthracene in binary solvent mixtures containing p-dioxane with n-hexane, cyclohexane, n-heptane, methylcyclohexane, n-octane, cyclooctane, and isooctane at 25 degrees C. Results of these measurements, used in conjunction with the nearly ideal binary solvent (NIBS) model, ena...

journal_title：Journal of pharmaceutical sciences

authors： Procyk AD,Bissell M,Street KW Jr,Acree WE Jr

更新日期：1987-08-01 00:00:00

abstract：:Various neutral, cationic, and anionic chemicals contained in hair care products can be absorbed into hair fiber to modulate physicochemical properties such as color, strength, style, and volume. For environmental safety, there is also an interest in understanding hair absorption to wide chemical pollutants. There hav...

journal_title：Journal of pharmaceutical sciences

authors： Li L,Yang S,Chen T,Han L,Lian G

更新日期：2018-04-01 00:00:00

abstract：:This study explored the ability to conduct primary drying during lyophilization at product temperatures above the glass transition temperature of the maximally freeze-concentrated solution (Tg′) in amorphous formulations for four proteins from three different classes. Drying above Tg′ resulted in significant reduction...

journal_title：Journal of pharmaceutical sciences

authors： Depaz RA,Pansare S,Patel SM

更新日期：2016-01-01 00:00:00

abstract：:From a consideration of the basic processes involved in drug elimination, the fraction of drug cleared by the gut and by the liver were described as functions of availability and hepatic clearance. For a drug given orally, a plot of the fraction of drug cleared by the gut or liver against alpha, a proportionality cons...

journal_title：Journal of pharmaceutical sciences

authors： Minchin RF,Ilett KF

更新日期：1982-04-01 00:00:00

abstract：:Melanotan-II (1) is a cyclic heptapeptide analogue of alpha-melanocyte-stimulating hormone (alpha-MSH) which tans the skin and is currently being evaluated for the prevention of sunlight-induced skin cancers. The dissociation constants of 1 were determined using potentiometric titration and ultraviolet spectrophotomet...

journal_title：Journal of pharmaceutical sciences

authors： Lan EL,Ugwu SO,Blanchard J,Fang X,Hruby VJ,Sharma S

更新日期：1994-08-01 00:00:00

abstract：:Twenty-two neutral, lipid-soluble 99mTc complexes have been synthesized from diamine dithiol (DADT) ligands which vary in alkyl substitution pattern on nitrogen and carbon. The logarithm of the partition coefficients (log PC), as well as the capacity factor k', of the purified complexes increased linearly with molecul...

journal_title：Journal of pharmaceutical sciences

authors： Lever SZ,Sun SY,Scheffel UA,Kaltovich FA,Baidoo KE,Goldfarb H,Wagner HN Jr

更新日期：1994-06-01 00:00:00

abstract：:Literature data relevant to the decision to allow a waiver of in vivo bioequivalence testing for the marketing authorization of immediate-release, solid oral dosage forms containing enalapril maleate are reviewed. Enalapril, a prodrug, is hydrolyzed by carboxylesterases to the active angiotensin-converting enzyme inhi...

journal_title：Journal of pharmaceutical sciences

authors： Verbeeck RK,Kanfer I,Löbenberg R,Abrahamsson B,Cristofoletti R,Groot DW,Langguth P,Polli JE,Parr A,Shah VP,Mehta M,Dressman JB

更新日期：2017-08-01 00:00:00

abstract：:The effects of the granule size and density on the drying rate kinetics of tablet granulations were studied using lactose and sulfathiazole granules prepared with acacia mucilage and providone solution. The drying rate kinetics consisted of three distinct phases of drying when the drying rate was platted against remai...

journal_title：Journal of pharmaceutical sciences

authors： Opankunle WO,Bhutani BR,Bhatia VN

更新日期：1975-06-01 00:00:00

abstract：:Magnetic resonance imaging (MRI) with chemical shift resolution is a recent extension of MRI and it provides information about species resolved molecular transport on the macroscopic scale in complex systems. In this contribution, we show that by using this novel method, one can predict the behavior of drug and food m...

journal_title：Journal of pharmaceutical sciences

authors： Lafitte G,Thuresson K,Söderman O

更新日期：2007-02-01 00:00:00

abstract：:The knowledge of physicochemical properties of organic compounds becomes increasingly important in pharmaceutical sciences, chemical engineering, and other fields. In this study, we developed UPPER (Unified Physicochemical Property Estimation Relationships), a comprehensive model for the estimation of 20 physicochemic...

journal_title：Journal of pharmaceutical sciences

authors： Lian B,Yalkowsky SH

更新日期：2014-09-01 00:00:00

abstract：:The physicochemical properties of ricobendazole (RBZ) were characterized using conventional methods. Solubility in some pharmaceutical solvents, pH-solubility, ionization properties, and lipophilicity are described. The solubility of RBZ in water is 62 mug/mL and very poor in common pharmaceutical solvents, for exampl...

journal_title：Journal of pharmaceutical sciences

authors： Wu Z,Razzak M,Tucker IG,Medlicott NJ

更新日期：2005-05-01 00:00:00

abstract：:The influence of various test meals and coadministered water volumes on erythromycin stearate bioavailability from orally dosed film-coated tablets was studied in healthy human subjects. Serum erythromycin levels were uniformly reduced by all test meals, with the reduction in mean peak serum levels varying from 47 to ...

journal_title：Journal of pharmaceutical sciences

authors： Welling PG,Huang H,Hewitt PF,Lyons LL

更新日期：1978-06-01 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：:A series of 2-(alpha-hydroxyacetyl)pyridine thiosemicarbazones was synthesized as potential antimalarial and antibacterial agents. Their synthesis was achieved by the condensation of N4-mono- or N4,N4-disubstituted thiosemicarbazides with 2-(alpha-hydroxyacetyl)pyridine. The latter was prepared by selective bromine ox...

journal_title：Journal of pharmaceutical sciences

authors： Klayman DL,Lin AJ,Hoch JM,Scovill JP,Lambros C,Dobek AS

更新日期：1984-12-01 00:00:00

abstract：:A procedure was developed for the separation and selective quantitative determination of the (S)(+)- and (R)(-)-enantiomers of the racemic anti-inflammatory drug carprofen as their diastereomeric l-(-)-alpha-methylbenzylamides. These derivatives are obtained in equivalent yields by reacint purified 14C-carprofen from ...

journal_title：Journal of pharmaceutical sciences

authors： Kemmerer JM,Rubio FA,McClain RM,Koechlin BA

更新日期：1979-10-01 00:00:00

abstract：:Topical lidocaine has been recently marketed as a new treatment for post-herpetic neuralgia. The aim of our study was to characterize the absorption profile of and systemic exposure to lidocaine from patch and gel formulations in normal volunteers, patients with post-herpetic neuralgia, and patients with acute herpes ...

journal_title：Journal of pharmaceutical sciences

authors： Campbell BJ,Rowbotham M,Davies PS,Jacob P 3rd,Benowitz NL

更新日期：2002-05-01 00:00:00

abstract：:The objective of this study was to investigate product performance of freeze dried l-arginine/sucrose-based formulations under variation of excipient weight ratios, l-arginine counter ions and formulation pH as a matrix to stabilize a therapeutic monoclonal antibody (MAb) during freeze drying and shelf life. Protein a...

journal_title：Journal of pharmaceutical sciences

authors： Stärtzel P,Gieseler H,Gieseler M,Abdul-Fattah AM,Adler M,Mahler HC,Goldbach P

更新日期：2015-07-01 00:00:00

abstract：:As reported in the previous commentary (Ishii-Watabe et al., J Pharm Sci 2017), the Japanese biopharmaceutical research group is promoting collaborative multilaboratory studies to evaluate and standardize new methodologies for biopharmaceutical characterization and quality control. We have conducted the studies and he...

journal_title：Journal of pharmaceutical sciences

authors： Ishii-Watabe A,Shibata H,Suetomo H,Ikeda Y,Telikepalli S,Kiyoshi M,Hayashi Y,Muto T,Tanaka Y,Ueda S,Iwura T,Saitoh S,Aoyama M,Harazono A,Hyuga M,Goda Y,Torisu T,Uchiyama S

更新日期：2020-05-01 00:00:00

abstract：:(13)C labeling was used to enhance the sensitivity of (13)C solid-state NMR to study the effect of tabletting on the polymorphism of a steroidal drug. The steroidal drug Org OD 14 was (13)C labeled and formulated into tablets containing only 0.5-2.5% active ingredient. The tablets were subsequently studied by solid-st...

journal_title：Journal of pharmaceutical sciences

authors： Booy KJ,Wiegerinck P,Vader J,Kaspersen F,Lambregts D,Vromans H,Kellenbach E

更新日期：2005-02-01 00:00:00

abstract：:Although several mathematical models have been reported for the estimation of human plasma concentration profiles of drug substances after dermal application, the successful cases that can predict human pharmacokinetic profiles are limited. Therefore, the aim of this study is to investigate the prediction of human pla...

journal_title：Journal of pharmaceutical sciences

authors： Yamamoto S,Karashima M,Arai Y,Tohyama K,Amano N

更新日期：2017-09-01 00:00:00

abstract：:Variability in the time to crystallization is a major technical and economic hurdle in using amorphous solids in dosage forms. It is hypothesized that amorphous solids "age", and that the older they are, the more relaxed they are and the higher the probability of crystallization. At present, there is no method that al...

journal_title：Journal of pharmaceutical sciences

authors： Hilden LR,Morris KR

更新日期：2003-07-01 00:00:00

abstract：:Most anticancer drugs are intended to function in the nuclei of cancer cells. If an anticancer drug could be delivered to mitochondria, the source of cellular energy, this organelle would be destroyed, resulting in the arrest of the energy supply and the killing of the cancer cells. To achieve such an innovative strat...

journal_title：Journal of pharmaceutical sciences

authors： Yamada Y,Munechika R,Kawamura E,Sakurai Y,Sato Y,Harashima H

更新日期：2017-09-01 00:00:00

abstract：:Dabrafenib is a small-molecule inhibitor of BRAF kinase activity that is currently being developed for the treatment of BRAF V600 mutation-positive melanoma. This clinical, open-label, two-cohort (n = 14 per cohort), randomized study was designed to evaluate the effect of drug substance particle size, and food on the ...

journal_title：Journal of pharmaceutical sciences

authors： Ouellet D,Grossmann KF,Limentani G,Nebot N,Lan K,Knowles L,Gordon MS,Sharma S,Infante JR,Lorusso PM,Pande G,Krachey EC,Blackman SC,Carson SW

更新日期：2013-09-01 00:00:00

abstract：:A series of N1-p-chlorophenyl-N5-alkylbiguanides were synthesized as potential inhibitors of dental plaque. Partition coefficients and pKa values were determined by standard methods. Biological activity was evaluated against Streptococcus mutans, a pure strain of plaque-forming bacteria. All compounds were compared to...

journal_title：Journal of pharmaceutical sciences

authors： Warner VD,Lynch DM,Ajemian RS

更新日期：1976-07-01 00:00:00

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：:Repetitive administration is routinely used to maintain therapeutic drug levels, but previous studies have documented an accelerated blood clearance of some lipid-based delivery systems under these conditions. To assess the effect of repetitive administration, non-PEGylated lipoplexes (+/-0.5) were administered 4 time...

journal_title：Journal of pharmaceutical sciences

authors： Betker JL,Anchordoquy TJ

更新日期：2017-03-01 00:00:00

abstract：:The use of pharmacological responses such as pupil diameter for dosage individualization, bioavailability, and pharmacokinetic analyses is becoming more widespread. Attempts to use pupil diameter to assess morphine bioavailability illuminate the fact that multiple responses, nonlinearities, and the condition of the su...

journal_title：Journal of pharmaceutical sciences

authors： Kramer PA

更新日期：1977-04-01 00:00:00