Prediction of plasma protein binding displacement and its implications for quantitative assessment of metabolic drug-drug interactions from in vitro data.

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：:A modified NF method for the quantitative determination of pentaerythritol tetranitrate is reported. A solution of powder is made directly from the dosage form in glacial acetic acid and is then reacted with phenoldisulfonic acid TS. The proposed method saves approximately 75% of the time required with the NF method. ...

journal_title：Journal of pharmaceutical sciences

authors： Gupta VD

更新日期：1978-05-01 00:00:00

abstract：:Phenylpropanolamine was determined by measuring its fluorescent fluorescamine derivative. The method is rapid, sensitive, and easily automated. Statistics are presented for an effervescent cold product, and recovery data are presented for other commercially available products. ...

journal_title：Journal of pharmaceutical sciences

authors： Shankle LL

更新日期：1978-11-01 00:00:00

abstract：:Colonic drug delivery is intended for local or systemic therapies. The lack of predictive in vitro or animal model leads to considerable time delays in colonic product development. The objective of this scintigraphic study was to provide "proof of concept" for a novel capsule-type colonic delivery system (Colon-Target...

journal_title：Journal of pharmaceutical sciences

authors： Ishibashi T,Pitcairn GR,Yoshino H,Mizobe M,Wilding IR

更新日期：1998-05-01 00:00:00

abstract：:Taxanes such as paclitaxel (Taxol) and docetaxel (Taxotere) are promising agents for use against ovarian cancer and other malignancies. Recently, SB-T-1011, a semisynthetic taxane, has been prepared from 14-hydroxy-10-deacetylbaccatin III. SB-T-1011 shows similar or greater in vitro cytostatic activity than paclitaxel...

journal_title：Journal of pharmaceutical sciences

authors： Sharma A,Straubinger RM,Ojima I,Bernacki RJ

更新日期：1995-12-01 00:00:00

abstract：:Low-density lipoproteins (LDLs), the physiological vehicles for lipids, are potentially useful drug delivery devices for (hydrophobic) drugs. The physicochemical characteristics of LDL loaded with the adriamycin derivative AD 32 or the N-mustard derivative WB 4291 were compared to that of native and reconstituted LDL ...

journal_title：Journal of pharmaceutical sciences

authors： Westesen K,Gerke A,Koch MH

更新日期：1995-02-01 00:00:00

abstract：:Chloroquine (7-chloro-4-[[4-(diethylamino)-1-methylbutyl]amino]quinoline; CQ) accumulates in the insoluble fraction of rat muscle homogenates with an equilibrium distribution ratio of 7.8 L/kg. This is of a similar magnitude to muscle:plasma ratios observed in vivo. Uptake is approximately linear, even up to concentra...

journal_title：Journal of pharmaceutical sciences

authors： MacIntyre AC,Cutler DJ

更新日期：1986-11-01 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：:Three dimensional terahertz pulsed imaging (TPI) was evaluated as a novel tool for the nondestructive characterization of different solid oral dosage forms. The time-domain reflection signal of coherent pulsed light in the far infrared was used to investigate film-coated tablets, sugar-coated tablets, multilayered con...

journal_title：Journal of pharmaceutical sciences

authors： Zeitler JA,Shen Y,Baker C,Taday PF,Pepper M,Rades T

更新日期：2007-02-01 00:00:00

abstract：:The aim of the present work was to investigate the preparation of PLGA nanoparticles (PNP) and PLGA-Hp55 nanoparticles (PHNP) as potential drug carriers for oral insulin delivery. The nanoparticles were prepared by a modified emulsion solvent diffusion method in water, and their physicochemical characteristics, drug r...

journal_title：Journal of pharmaceutical sciences

authors： Cui FD,Tao AJ,Cun DM,Zhang LQ,Shi K

更新日期：2007-02-01 00:00:00

abstract：:The tissue penetration and distribution of antibiotics is of great importance, since most of the infections occur in the tissue. At the infection site, the free, unbound fraction of the antibiotic is responsible for the antiinfective effect. These free extracellular concentrations can be measured by microdialysis. It ...

journal_title：Journal of pharmaceutical sciences

authors： Nolting A,Costa TD,Vistelle R,Rand KH,Derendorf H

更新日期：1996-04-01 00:00:00

abstract：:An in vitro technique was developed to characterize the intermittent flume patterns associated with the short bursts of metered-dose aerosols. Two orthogonal video images are utilized to describe the complex shape and direction of the flume pattern. This technique facilitates the evaluation of components manufactured ...

journal_title：Journal of pharmaceutical sciences

authors： Miszuk S,Gupta BM,Chen FC,Clawans C,Knapp JZ

更新日期：1980-06-01 00:00:00

abstract：:First-order rate constants (k) were determined for the hydrolysis of ceftazidime in the pH range of 0.5 to 8.5 at 45, 55, and 65 degrees C by a stability-indicating HPLC assay. In the absence of buffer effects, the pH-rate expression was k = kH1f1(aH+) + kH2f2(aH+) + kH3f3(aH+) + kSf3 + kOHf3(aOH-), where KH and KOH a...

journal_title：Journal of pharmaceutical sciences

authors： Zhou M,Notari RE

更新日期：1995-05-01 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：:The metabolism of tocainide, an experimental antiarrhythmic drug, was studied in humans. Urinary excretion of unchanged drug was 28-55% in 24 hr after oral dosing. Urine hydrolysis with hydrochloric acid or beta-glucuronidase increased tocainide recovery to 55-79%. Saccharo-1,4-lactone inhibited the beta-glucuronidase...

journal_title：Journal of pharmaceutical sciences

authors： Elvin AT,Keenaghan JB,Byrnes EW,Tenthorey PA,McMaster PD,Takman BH,Lalka D,Manion CV,Baer DT,Wolshin EM,Meyer MB,Ronfeld RA

更新日期：1980-01-01 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：:To preserve the positive effect of collagen on tissue regeneration and to locally deliver low molecular weight compounds for an extended time period, a composite for parenteral application was devised based on a collagen sponge with gentamicin-loaded PLGA microparticles incorporated. Antibiotic liberation from the par...

journal_title：Journal of pharmaceutical sciences

authors： Schlapp M,Friess W

更新日期：2003-11-01 00:00:00

abstract：:The aim of this study was to evaluate a new experimental protocol utilizing isolated frog intestinal sacs for the assessment of intestinal drug permeability in humans. Segments of approximately 5.0 cm in length were used for these experiments. The intestinal sacs were filled with a solution of the appropriate drug in ...

journal_title：Journal of pharmaceutical sciences

authors： Trapani G,Franco M,Trapani A,Lopedota A,Latrofa A,Gallucci E,Micelli S,Liso G

更新日期：2004-12-01 00:00:00

abstract：:We characterized a glucose-sensitive, controlled-release insulin delivery system. Insulin release rates increased when glucose was perfused in the release media surrounding the matrix. The system was composed of solid, particulate insulin, incorporated into an ethylene-vinyl acetate copolymer (EVAc) matrix. Feedback c...

journal_title：Journal of pharmaceutical sciences

authors： Brown LR,Edelman ER,Fischel-Ghodsian F,Langer R

更新日期：1996-12-01 00:00:00

abstract：:An interlaboratory comparison of two extraction methods and one thermal desorption test method for the quantification of ethylene oxide (EO) by gas chromatography in two common medical device materials, high density polyethylene (HDPE) and plasticized polyvinyl chloride (PVC), was conducted by 15 laboratories. The thr...

journal_title：Journal of pharmaceutical sciences

authors： Lao NT,Lu HT,Rego A,Kosakowski RH,Burgess DJ,Hume RD

更新日期：1995-05-01 00:00:00

abstract：:Deiodination of diatrizoic acid, an anionic radiopaque, was found to be catalyzed by Cu(II). Through a detailed study of o-iodobenzoic acid, a model compound, the copper-catalyzed SN1 mechanism was established based on observations of common ion, salt, and pH effects. Meta- and para-iodobenzoic acids were unreactive. ...

journal_title：Journal of pharmaceutical sciences

authors： Wang YC

更新日期：1980-06-01 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：:Insoluble (visible) aggregates of a homodimer fusion glycoprotein, consisting of the first extracellular domain of a human protein, fused to the hinge, C(H)2, and C(H)3 domains of a human immunoglobulin G(1) (IgG(1)), were observed during early formulation development. The soluble fraction of the fusion protein was co...

journal_title：Journal of pharmaceutical sciences

authors： Souillac PO

更新日期：2005-09-01 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：:Methods were developed for the determination of octanoic acid and N-acetyl-DL-tryptophan, which are used as stabilizers in the human blood-derived therapeutic products normal serum albumin and plasma protein fraction. The method for octanoic acid uses GC; quantitation is achieved using heptanoic acid as the internal s...

journal_title：Journal of pharmaceutical sciences

authors： Yu MW,Finlayson JS

更新日期：1984-01-01 00:00:00

abstract：:The ICH Q1B guidance and additional clarifying manuscripts provide the essential information needed to conduct photostability testing for pharmaceutical drug products in the context of manufacturing, packaging, and storage. As the previous 2 papers in this series highlight for drug products administered by injection (...

journal_title：Journal of pharmaceutical sciences

authors： Allain L,Baertschi SW,Clapham D,Foti C,Lantaff WM,Reed RA,Templeton AC,Tønnesen HH

更新日期：2016-05-01 00:00:00

abstract：:Gepirone hydrochloride, an investigational anxiolytic drug, was found to have at least three polymorphic forms which melted at 180 degrees C (I), 212 degrees C (II), and 200 degrees C (III). Thermal analytical studies showed that forms I and II were an enantiotropic pair, as were forms I and III. Form III was monotrop...

journal_title：Journal of pharmaceutical sciences

authors： Behme RJ,Brooke D,Farney RF,Kensler TT

更新日期：1985-10-01 00:00:00

abstract：:The anticonvulsant and CNS-depressant activities of 16 commercially available antiepileptics were subjected to regression analysis. For the maximal electroshock seizure test and pentylenetetrazol seizure threshold test, good correlations were obtained only after diazepam, clonazepam, and carbamazepam were deleted; for...

journal_title：Journal of pharmaceutical sciences

authors： Lien EJ,Liao RC,Shinouda HG

更新日期：1979-04-01 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：:Substance P (SP) was degraded by synaptic membranes of rat spinal cord. Cleavage products were separated by reversed phase high performance liquid chromatography and identified by amino acid composition analyses. Major products of SP were phenylalanine, SP(1-4), SP(1-6), SP(1-7), SP(10-11), and SP(8-9). Both the degra...

journal_title：Journal of pharmaceutical sciences

authors： Sakurada C,Watanabe C,Sakurada S,Tan-No K,Sakurada T

更新日期：1999-11-01 00:00:00