Synthesis, physicochemical parameters, and in vitro evaluation of N1-p-chlorophenyl-N5-alkylbiguanides.

abstract：:The crystal and molecular structures of 6-methylmercaptopurine trihydrate and of azathioprine dihydrate were determined by the use of three-dimensional, X-ray, diffractometer data and were refined by least squares. Both molecules crystallize in the N(9)-H tautomer form, in contrast to the N(7)-H tautomer form found in...

journal_title：Journal of pharmaceutical sciences

authors： Cook WJ,Bugg CE

更新日期：1975-02-01 00:00:00

abstract：:The crystal structure of zolpidem hemitartrate hemihydrate (I, Form E) has been solved from high-resolution laboratory powder diffraction data. It crystallizes in the orthorhombic P2(1)2(1)2(1) space group with a = 22.4664(6) A, b = 26.0420(7) A, and c = 7.4391(1) A. Protonation of zolpidem molecules could not be unam...

journal_title：Journal of pharmaceutical sciences

authors： Halasz I,Dinnebier RE

更新日期：2010-02-01 00:00:00

abstract：:Mechanical shock may cause cavitation in vials containing liquid formulations of therapeutic proteins and generate protein aggregates and other particulates. To test whether common formulation components such as protein molecules, air bubbles, or polysorbate 20 (PS20) micelles might nucleate cavitation, a high-speed v...

journal_title：Journal of pharmaceutical sciences

authors： Wu H,Chisholm CF,Puryear M,Movafaghi S,Smith SD,Pokhilchuk Y,Lengsfeld CS,Randolph TW

更新日期：2020-03-01 00:00:00

abstract：:The hepatic distribution, biliary excretion, and mass balance of liposomal amphotericin B (L-AmB) were investigated in recirculated isolated perfused rat liver. The results were compared with those from the conventional AmB formulation, amphotericin B deoxycholate (D-AmB). L-AmB was introduced as a bolus into the perf...

journal_title：Journal of pharmaceutical sciences

authors： Hong Y,Ramzan I,McLachlan AJ

更新日期：2005-01-01 00:00:00

abstract：:This study describes the adaptation of conventional titrimetric and spectrophotometric techniques to a microscale for the determination of drug ionization constants (pKa) and partition coefficients (log P). The apparatus for determining pKa and compound purity (or equivalent weight) consists of a three-port conical gl...

journal_title：Journal of pharmaceutical sciences

authors： Morgan ME,Lui K,Anderson BD

更新日期：1998-02-01 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：:The effect of dietary polyphenols on the intestinal glucuronidation and absorption of a model phenolic drug, alpha-naphthol (alpha-NA), was studied in isolated rat small intestine. (-)-Epicatechin significantly inhibited the glucuronidation of alpha-NA. Chrysin, (-)-epigallocatechin galleate (EGCG), and quercetin decr...

journal_title：Journal of pharmaceutical sciences

authors： Mizuma T,Awazu S

更新日期：2004-09-01 00:00:00

abstract：:An Amended Solvation Energy Relationship (ASER) was recently reported to successfully predict the aqueous solubilities of a set of 664 organic compounds. The average absolute error and root mean square error are 0.43 and 0.62 log units, respectively. When the General Solubility Equation (GSE) is applied to the same se...

journal_title：Journal of pharmaceutical sciences

authors： Yang G,Ran Y,Yalkowsky SH

更新日期：2002-02-01 00:00:00

abstract：UNLABELLED:Given a good correlation between onsets of crystallization and mobility above T(g), one might be able to predict crystallization onsets at a temperature of interest far below T(g) from this correlation and measurement of mobility at a temperature below T(g). Such predictions require that: (a) correlation bet...

journal_title：Journal of pharmaceutical sciences

authors： Bhugra C,Shmeis R,Krill SL,Pikal MJ

更新日期：2008-01-01 00:00:00

abstract：:The cobalt 60 radiolytic degradation products have been identified in the following corticosteroids: cortisone, cortisone acetate, hydrocortisone, hydrocortisone acetate, hydrocortisone sodium succinate, isoflupredone acetate, methylprednisolone, methylprednisolone acetate, prednisolone, prednisolone acetate, and pred...

journal_title：Journal of pharmaceutical sciences

authors： Kane MP,Tsuji K

更新日期：1983-01-01 00:00:00

abstract：:In this work, a novel risk-based methodology for lot release is proposed. Its objective is to assess the risk that a lot declared to have passed truly meets product specifications. The methodology consists of 3 parts: adaptive sample size determination, estimation of the probability that the product was within specifi...

journal_title：Journal of pharmaceutical sciences

authors： Mockus L,Reklaitis G,Morris K,LeBlond D

更新日期：2020-02-01 00:00:00

abstract：:The objective of this study was to investigate the permeation-enhancing effect of thiolated polycarbophil (PCP) on peptide drugs. Mediated by a carbodiimide, increasing amounts of cysteine (Cys) were covalently bound to sodium neutralized PCP (NaPCP). The extent of covalently attached Cys was determined by quantifying...

journal_title：Journal of pharmaceutical sciences

authors： Clausen AE,Bernkop-Schnürch A

更新日期：2000-10-01 00:00:00

abstract：:3-N-(1',8'-Naphthalimido)propionic acid was synthesized and shown to effectively lower both serum cholesterol and triglyceride levels in rats and mice. In hyperlipidemic mice, serum lipid levels were lowered significantly, approaching normal levels of cholesterol and below normal levels of triglyceride. The serum lipi...

journal_title：Journal of pharmaceutical sciences

authors： Hall IH,Chapman JM Jr,Voorstad PJ,Cocolas GH

更新日期：1984-07-01 00:00:00

abstract：:The plasma concentrations and urinary excretions of bisoprolol enantiomers in four Japanese male healthy volunteers after a single oral administration of 20 mg of racemic bisoprolol were evaluated. The AUC(infinity) and elimination half-life of (S)-(-)-bisoprolol were slightly larger than those of (R)-(+)-bisoprolol i...

journal_title：Journal of pharmaceutical sciences

authors： Horikiri Y,Suzuki T,Mizobe M

更新日期：1998-03-01 00:00:00

abstract：:The purpose of this study was to examine the effects of extracts and flavone derivatives from the rhizome of Kaempferia parviflora on P-glycoprotein (P-gp)-mediated transport in LLC-GA5-COL150, a transfectant cell line of a porcine kidney epithelial cell line LLC-PK1 with human MDR1 cDNA. Ethanol extract obtained from...

journal_title：Journal of pharmaceutical sciences

authors： Patanasethanont D,Nagai J,Yumoto R,Murakami T,Sutthanut K,Sripanidkulchai BO,Yenjai C,Takano M

更新日期：2007-01-01 00:00:00

abstract：:Using quantitative structure-retention relationships (QSRR) methodologies the Kovats gas chromatographic retention indices for both apolar (DB-1) and polar (DB-Wax) columns for 48 compounds from Ylang-Ylang essential oil were empirically predicted from calculated and experimental data on molecular structure. Topologic...

journal_title：Journal of pharmaceutical sciences

authors： Olivero J,Gracia T,Payares P,Vivas R,Díaz D,Daza E,Geerlings P

更新日期：1997-05-01 00:00:00

abstract：:Amorphous nifedipine (NFD), which has a smooth surface immediately after preparation, was shown to have structures resembling clusters of curling and branching fibers approximately 1 μm wide by atomic force microscopy (AFM) after storage at 25°C. The size of the cluster-like structures increased with storage over time...

journal_title：Journal of pharmaceutical sciences

authors： Miyazaki T,Aso Y,Kawanishi T

更新日期：2011-10-01 00:00:00

abstract：:The objective of this study was to determine reasons behind the low oral (p.o.) bioavailability of glucosamine. By using male Sprague-Dawley rats, the movement of glucosamine through everted gut, the effect of dose and glucose, and inhibition of a glucose transporter (GLUT2) by quercetin were studied. Glucosamine phar...

journal_title：Journal of pharmaceutical sciences

authors： Ibrahim A,Gilzad-kohan MH,Aghazadeh-Habashi A,Jamali F

更新日期：2012-07-01 00:00:00

abstract：:Amphiphilic cyclodextrins (CDs) are biocompatible derivatives of natural CDs and are able to form nanoparticles or polyplexes spontaneously. In this study, nanoparticles prepared from nonionic (6OCaproβCD) or cationic amphiphilic CD (PC βCDC6) were used comparatively to develop nanoparticles intended for breast cancer...

journal_title：Journal of pharmaceutical sciences

authors： Varan G,Öncül S,Ercan A,Benito JM,Ortiz Mellet C,Bilensoy E

更新日期：2016-10-01 00:00:00

abstract：:Electron micrographs of Pseudomonas aeruginosa grown in nutrient broth or broth containing subinhibitory concentrations of benzalkonium chloride indicate that benzalkonium chloride at 50 and 100 mug/ml strips off the outer cell membrane. Cells grown in the presence of edetate disodium, 50-100 mug/ml had convoluted sur...

journal_title：Journal of pharmaceutical sciences

authors： Richards RM,Cavill RH

更新日期：1976-01-01 00:00:00

abstract：:The pharmacokinetics of sulfisoxazole and sulfanilamide were studied in control rats and in rats treated for 5 days with a daily 100 mg/kg ip dose of phenobarbital. These drugs represent the organic anionic and nonionized drugs, respectively, whose nonmicrosomal enzymatic metabolisms were unstimulated by phenobarbital...

journal_title：Journal of pharmaceutical sciences

authors： Nagwekar JB,Kundu S

更新日期：1982-04-01 00:00:00

abstract：:An immune response for a nasal ovalbumin (OVA) powder formulation with an applied nasal delivery platform technology, consisting of a powdery nasal carrier and a device, was evaluated in monkeys with similar upper respiratory tracts and immune systems to those of humans, in order to assess the applicability to a vacci...

journal_title：Journal of pharmaceutical sciences

authors： Torikai Y,Sasaki Y,Sasaki K,Kyuno A,Haruta S,Tanimoto A

更新日期：2020-12-03 00:00:00

abstract：:Most of the global healthcare issues facing us--from expanding access to care, to providing medical and dental care in the aftermath of disasters--are far too complex for any single sector to successfully solve. Industry, the healthcare profession, government, academia and non-governmental organizations (NGOs) are all...

journal_title：Journal of pharmaceutical sciences

authors： Bergman SM

更新日期：2008-12-01 00:00:00

abstract：:The objective of the present study was to investigate the iontophoretic transport behavior across multiple membranes of different barrier properties. Spectra/Por(R) (SP) and Ionac membranes were the synthetic membranes and sclera was the biomembrane in this model study. The barrier properties of SP membranes were dete...

journal_title：Journal of pharmaceutical sciences

authors： Molokhia SA,Zhang Y,Higuchi WI,Li SK

更新日期：2008-01-01 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：: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：:Two polymorphs of celastrol were discovered and fully characterized by X-ray powder diffraction, thermogravimetry analysis, and differential scanning calorimetry. The single-crystal structures of form I and the isostructural solvate of form II were disclosed by single-crystal X-ray diffraction. The apparent solubility...

journal_title：Journal of pharmaceutical sciences

authors： Zha J,Zhang Q,Li M,Wang JR,Mei X

更新日期：2018-11-01 00:00:00

abstract：:Mixture response-surface methodology can be used as a technique to predict solubility in mixed solvent systems. The present report shows that if the intent is to predict solubility in nonideal solutions, mixture response-surface methodology is a better technique than one which assumes a particular mechanism to hold tr...

journal_title：Journal of pharmaceutical sciences

authors： Ochsner AB,Belloto RJ Jr,Sokoloski TD

更新日期：1985-02-01 00:00:00

abstract：:The aim of this study to administer hydrocortisone (HC) percutaneously in the form of polymeric nanoparticles (NPs) to alleviate its transcutaneous absorption, and to derive additional wound-healing benefits of chitosan. HC-loaded NPs had varied particle sizes, zeta potentials, and entrapment efficiencies, when drug-t...

journal_title：Journal of pharmaceutical sciences

authors： Hussain Z,Katas H,Amin MC,Kumulosasi E,Sahudin S

更新日期：2013-03-01 00:00:00

abstract：:The insidious nature of Zika virus (ZIKV) infections can have a devastating consequence for fetal development. Recent reports have highlighted that chloroquine (CQ) is capable of inhibiting ZIKV endocytosis in brain cells. We applied pharmacokinetic modeling to develop a predictive model for CQ exposure to identify an...

journal_title：Journal of pharmaceutical sciences

authors： Olafuyi O,Badhan RKS

更新日期：2019-01-01 00:00:00