Desethylaprophen: a metabolite of aprophen with antimuscarinic activities.

abstract：:Literature data relevant to the decision to waive in vivo bioequivalence testing for the approval of generic immediate release solid oral dosage forms of proguanil hydrochloride are reviewed. To elucidate the Biopharmaceutics Classification System (BCS) classification, experimental solubility and dissolution studies w...

journal_title：Journal of pharmaceutical sciences

authors： Plöger GF,Abrahamsson B,Cristofoletti R,Groot DW,Langguth P,Mehta MU,Parr A,Polli JE,Shah VP,Tajiri T,Dressman JB

更新日期：2018-07-01 00:00:00

abstract：:The oral dose metabolism of dilazep dihydrochloride [tetrahydro-1H-1,4-diazepine-1,4(5H)-dipropanol 3,4,5-trimethoxybenzoate] was examined in six hypertensive patients receiving a single oral dose of 600 mg of dilazep (3-3.8 mg/kg BW). Blood was collected at 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, and 24 h after administratio...

journal_title：Journal of pharmaceutical sciences

authors： Sambhi MP,Kannan R,Thananopavarn C,Ookhtens M,Gudenzi M

更新日期：1989-04-01 00:00:00

abstract：:Robust higher order structure (HOS) characterization capability and strategy are critical throughout biopharmaceutical development from initial candidate selection and formulation screening to process optimization and manufacturing. This case study describes the utility of several orthogonal HOS methods as investigati...

journal_title：Journal of pharmaceutical sciences

authors： Budyak IL,Doyle BL,Weiss WF 4th

更新日期：2015-04-01 00:00:00

abstract：:The capacity factors of several penicillins and cephalosporins, as well as those of 7-aminocephalosporanic acid, 6-aminopenicillanic acid, and 7-aminodeacetoxycephalosporanic acid, were determined at pH 2.5-7.5 with different methanol concentrations in the mobile phase. The influence of ionic strength on activity fact...

journal_title：Journal of pharmaceutical sciences

authors： Salto F,Prieto JG,Alemany MT

更新日期：1980-05-01 00:00:00

abstract：:This study aimed to investigate the surface energy factors behind improved aerosolization performance of spray-dried colistin powder formulations compared with those produced by jet milling. Inhalable colistin powder formulations were produced by jet milling or spray drying (with or without l-leucine). Scanning electr...

journal_title：Journal of pharmaceutical sciences

authors： Jong T,Li J,Morton DA,Zhou QT,Larson I

更新日期：2016-03-01 00:00:00

abstract：:Drug transporters expressed in liver and kidney play a critical role in the elimination of a wide range of drugs and xenobiotics and inhibition of these transporters may therefore cause clinically significant drug-drug interactions (DDIs). Currently, in vitro transporter inhibition data are used to assess the risk tha...

journal_title：Journal of pharmaceutical sciences

authors： Chu X,Chan GH,Evers R

更新日期：2017-09-01 00:00:00

abstract：:A tetrazole ring is often used in drug discovery as a replacement for the carboxylic acid group. Previous work indicates that compounds containing a tetrazole moiety show asymmetric permeability in Caco-2 cells characteristic of an efflux transporter substrate. The aim of this study is to determine which transporters ...

journal_title：Journal of pharmaceutical sciences

authors： Young AM,Audus KL,Proudfoot J,Yazdanian M

更新日期：2006-04-01 00:00:00

abstract：:The axial and radial tensile strengths were compared to the hardness of compressed tablets containing various concentrations of lubricants. Since radial tensile strength measurement considers the thickness of a tablet, and only tensile stress and axial tensile strength express the strength in the direction in which ca...

journal_title：Journal of pharmaceutical sciences

authors： Jarosz PJ,Parrott EL

更新日期：1982-06-01 00:00:00

abstract：:Owing to proliferation of antibiotic-resistant bacteria, the use of antibiotics for livestock growth promotion is banned in many countries and alternatives to in-feed antibiotics are needed. Cinnamon essential oil exhibits strong in vitro antibacterial activity; however, direct addition of essential oils to animal fee...

journal_title：Journal of pharmaceutical sciences

authors： Ma YH,Wang Q,Gong J,Wu XY

更新日期：2016-03-01 00:00:00

abstract：:In recent years, controlled release coatings, comprised of drug-polymer composites, have been integrated with medical devices, improving device functionality and performance. However, relationships between material properties, manufacturing environment, composite (micro)structure, and subsequent release kinetics are n...

journal_title：Journal of pharmaceutical sciences

authors： Saylor DM,Kim CS,Patwardhan DV,Warren JA

更新日期：2009-01-01 00:00:00

abstract：:A conventional atomistic approach of estimating molecular hydrophobicity (log P) was improved by taking into account the proximity effect of substituent groups as well as the importance of solute-solvent interaction in the partition phenomena. The new method reassigns atomic parameters when the molecule is fully expos...

journal_title：Journal of pharmaceutical sciences

authors： Masuda T,Jikihara T,Nakamura K,Kimura A,Takagi T,Fujiwara H

更新日期：1997-01-01 00:00:00

abstract：:A stability-indicating analytical method is described for the simultaneous determination of nitrate, and if present, its reductive degradation product, nitrite, in toothpastes. Nitrate and nitrite were extracted from the toothpaste using distilled water and separated from other water-soluble excipients by two RP-8 col...

journal_title：Journal of pharmaceutical sciences

authors： Lulla H,Chen SS,Sena FJ

更新日期：1984-07-01 00:00:00

abstract：:The skin penetration of 10 nonsteroidal antiinflammatory drugs (NSAIDs) was investigated after application in the lipophilic vehicle light mineral oil. The skin permeabilities and maximum fluxes, which were calculated from the concentration decreases of the applied solutions in the steady state phases, were correlated...

journal_title：Journal of pharmaceutical sciences

authors： Wenkers BP,Lippold BC

更新日期：1999-12-01 00:00:00

abstract：:The affinity chromatographic technique was used to study the interaction of bovine serum albumin and salicylic acid at 3.3 +/- 1.1 degrees. Beaded agarose gel, on which the albumin was immobilized by covalent linkage, was packed in a column as an affinity adsorbent. Frontal analysis was performed on this column to eva...

journal_title：Journal of pharmaceutical sciences

authors： Nakano NI,Oshio T,Fujimoto Y,Amiya T

更新日期：1978-07-01 00:00:00

abstract：:Gas pycnometry is applied to determine the density of solid materials. The analysis of lyophilisates is particularly challenging because of their porous structure. In this study, the density of raw materials and freeze-dried products was determined using different pycnometric methodologies and gases [helium (He), nitr...

journal_title：Journal of pharmaceutical sciences

authors： Stange U,Scherf-Clavel M,Gieseler H

更新日期：2013-11-01 00:00:00

abstract：:A GLC determination of cyclobenzaprine in human plasma and urine is described. After extraction from alkalinized samples with heptane-isopentyl alcohol (97:3), the drug and internal standard were back-extracted into 0.1 N HCl and then reextracted into ether. Use of a lower homolog of the drug as an internal standard w...

journal_title：Journal of pharmaceutical sciences

authors： Hucker HB,Stauffer SC

更新日期：1976-08-01 00:00:00

abstract：:Dissolution testing is routinely conducted in the pharmaceutical industry to provide in vitro drug release information for quality control purposes. The most common dissolution testing system for solid dosage forms is the United States Pharmacopeia (USP) Dissolution Testing Apparatus 2. This apparatus is very sensitiv...

journal_title：Journal of pharmaceutical sciences

authors： Wang Y,Armenante PM

更新日期：2012-02-01 00:00:00

abstract：:The use of second generation cationic liposomes to deliver cytotoxic drugs to solid tumors is a rational and promising therapeutic approach, given the natural affinity of cationic carrier molecules for the tumor microvasculature. Cationic liposomal therapeutics are effective in the treatment of cancers that are resist...

journal_title：Journal of pharmaceutical sciences

authors： Campbell RB,Ying B,Kuesters GM,Hemphill R

更新日期：2009-02-01 00:00:00

abstract：:The increased incidence of human immunodeficiency virus infection in women has identified an urgent need to develop a female-controlled method to prevent acquisition of human immunodeficiency virus and other sexually transmitted diseases. Women would apply the product intravaginally before intercourse. Development of ...

journal_title：Journal of pharmaceutical sciences

authors： Sassi AB,McCullough KD,Cost MR,Hillier SL,Rohan LC

更新日期：2004-08-01 00:00:00

abstract：:The phase diagram for the binary system nafcillin sodium-water, was determined using differential scanning calorimetry (DSC) and polarized light microscopy. In the temperature range of -20-30 degrees, three crystalline forms and an amphiphilic liquid crystalline phase were detected. The stable crystalline form of nafc...

journal_title：Journal of pharmaceutical sciences

authors： Bogardus JB

更新日期：1982-01-01 00:00:00

abstract：:A multichannel continuous-flow apparatus for dissolution rate measurements is described. Typical data are presented to demonstrate its utility for studies with bulk drug powders as well as with tablets and capsules without any change of setup. Procedures are given for the preparation of powder samples for dissolution ...

journal_title：Journal of pharmaceutical sciences

authors： Cakiryildiz C,Mehta PJ,Rahmen W,Schoenleber D

更新日期：1975-10-01 00:00:00

abstract：:A theory of charge, fluid-mass, and solute (including macromolecular) transport through porous media is applied to describe transport phenomena across the external layer of mammalian skin. Linear relationships are derived between transport fluxes and applied fields. These relationships introduce six effective transder...

journal_title：Journal of pharmaceutical sciences

authors： Edwards DA,Langer R

更新日期：1994-09-01 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：:The pre-equilibrium capillary zone electrophoretic (pre-eq CZE) method to determine association constants of active anionic forms of antithyroid drugs: 6-n-propyl-2-thiouracil (PTU), 6-methyl-2-thiouracil (MTU), 2-thiouracil (TU) with bovine serum albumin (BSA) under physiological pH 7.4 has been developed for the fir...

journal_title：Journal of pharmaceutical sciences

authors： Chernov'yants MS,Dolinkin AO,Chernyshev AV,Khohlov EV,Golovanova EG

更新日期：2010-03-01 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：:The advisability of a progressive curtailment of organic solvent film coating offers an incentive to develop latex systems. Here, the use of aqueous colloidal dispersions of cellulose acetate, plasticized with water-soluble additives, is proposed as an alternative way to obtain cellulose acetate membranes either by ca...

journal_title：Journal of pharmaceutical sciences

authors： Bindschaedler C,Gurny R,Doelker E

更新日期：1987-06-01 00:00:00

abstract：:An important part of pharmacokinetic research is fitting models to observed data and estimating the parameters in the model. In general, parameter estimation in pharmacokinetics is a subset of the general problem of nonlinear regression or parameter estimation in nonlinear regression models. The same criteria, algorit...

journal_title：Journal of pharmaceutical sciences

authors： Metzler CM

更新日期：1987-07-01 00:00:00

abstract：:The relationship between the concentration of a drug and its pharmacologic effect is of central interest in pharmacodynamics. Various compartmental and noncompartmental methods have been proposed for elucidating this relationship when the plasma drug concentration and effects are both measured. Although the relationsh...

journal_title：Journal of pharmaceutical sciences

authors： Modi NB,Veng-Pedersen P

更新日期：1994-03-01 00:00:00

abstract：:The tissue:plasma partition coefficients (Kp ) are good indicators of the extent of tissue distribution. Therefore, advanced tissue composition-based models were used to predict the Kp values of drugs under in vivo conditions on the basis of in vitro and physiological input data. These models, however, focus on animal...

journal_title：Journal of pharmaceutical sciences

authors： Poulin P

更新日期：2015-06-01 00:00:00

abstract：:The antifungal drug, 5-fluorocytosine (FC), is marketed as a capsule (250 or 500 mg strength) instead of the preferred tablet dosage form. Through systematic characterization of solid-state properties, including mechanical properties, we identify tabletability and poor physical stability of FC as the problems that lik...

journal_title：Journal of pharmaceutical sciences

authors： Perumalla SR,Sun CC

更新日期：2014-04-01 00:00:00