Development of a method for study of the tendency of drug products to adhere to the esophagus.

abstract：:Pinacidil [(+/-)-2-cyano-1-(4-pyridyl)-3-(1,2,2-trimethylpropyl)guanidine monohydrate] is a novel, direct-acting vasodilator antihypertensive agent. The cyano 14C-labeled drug is rapidly and completely absorbed after an oral 12.5-mg dose in solution. The blood:plasma concentration ratios (0.8-0.9) indicate transient p...

journal_title：Journal of pharmaceutical sciences

authors： DeLong AF,Oldham SW,DeSante KA,Nell G,Henry DP

更新日期：1988-02-01 00:00:00

abstract：:Previously, we reported that repeated oral treatment with etoposide (ETP) increased ileal membrane localization of P-glycoprotein (P-gp) and that this was possibly mediated by increased expression of the ezrin/radixin/moesin (ERM)/phosphorylated ERM (p-ERM) via activation of RhoA/ROCK. These changes caused decreases i...

journal_title：Journal of pharmaceutical sciences

authors： Kobori T,Harada S,Nakamoto K,Tokuyama S

更新日期：2013-05-01 00:00:00

abstract：:In an attempt to explain the mechanism of protein stabilization conferred by detergents, we investigated the effect of Tween 80 on aggregation of bovine serum albumin (BSA) using circular dichroism (CD) and native gel electrophoresis. CD thermal scans showed that BSA denatures at about 54 degrees C in 20 mM Tris, pH 7...

journal_title：Journal of pharmaceutical sciences

authors： Arakawa T,Kita Y

更新日期：2000-05-01 00:00:00

abstract：:We have shown that adsorbability of local anesthetics onto activated carbon, expressed by the partition coefficients at infinite dilution, correlated well with the pharmacological activity. However, there is no parameter that can singly express the tendency to be adsorbed. Adsorbability is a loosely defined term and i...

journal_title：Journal of pharmaceutical sciences

authors： Abe I,Kamaya H,Ueda I

更新日期：1990-04-01 00:00:00

abstract：:A high-pressure liquid chromatographic procedure for the accurate determination of disopyramide and its chief metabolite in plasma is presented. The method is suitable for monitoring patients receiving disopyramide therapy. A reversed-phase cyanopropylsilane column is utilized with a mobile phase of 50% acetonitrile a...

journal_title：Journal of pharmaceutical sciences

authors： Nygard G,Shelver WH,Khalil SK

更新日期：1979-10-01 00:00:00

abstract：:The blood-brain barrier permeation has been investigated by using a topological substructural molecular design approach (TOPS-MODE). A linear regression model was developed to predict the in vivo blood-brain partitioning coefficient on a data set of 119 compounds, treated as the logarithm of the blood-brain concentrat...

journal_title：Journal of pharmaceutical sciences

authors： Cabrera MA,Bermejo M,Pérez M,Ramos R

更新日期：2004-07-01 00:00:00

abstract：:The pharmaceutical preparation, chromatography, and biological distribution of a series of new chemical analogs of palmitic acid and diethylenetriaminepentaacetic acid, ethylenediaminetetraacetic acid, or diethylenetriamine are described. The biological distribution in rabbits 30 min after intravenous administration o...

journal_title：Journal of pharmaceutical sciences

authors： Karesh SM,Eckelman WC,Reba RC

更新日期：1977-02-01 00:00:00

abstract：:A method for the measurement, in human plasma, of all tertiary and secondary tricyclic antidepressants prescribed in the United States is described. The method uses electron beam ionization GLC-mass spectrometry, employing a computer-controlled multiple-ion detector. This method, mass fragmentography, is used with int...

journal_title：Journal of pharmaceutical sciences

authors： Biggs JT,Holland WH,Chang S,Hipps PP,Sherman WR

更新日期：1976-02-01 00:00:00

abstract：:Polysorbate 80, a surfactant often assumed to be inert, was found to bind a number of biochemically important ions (K+, Na+, NH4+, Ca2+) and transport them through a model membrane (CH2Cl2). The rates and fluxes of potassium ions were found to depend on the initial concentration of potassium ion, the polysorbate 80 co...

journal_title：Journal of pharmaceutical sciences

authors： Thoman CJ

更新日期：1986-10-01 00:00:00

abstract：:Injectable microcapsules containing 75% (w/w) cyclazocine, a narcotic antagonist, were prepared with dl-poly(lactic acid) as the coating material. Capsule fractions falling between 105 and 295 mum released about 90% of their cyclazocine in 8 days of rotating-bottle extraction at 37 degrees in pH 7.4 phosphate buffer. ...

journal_title：Journal of pharmaceutical sciences

authors： Mason N,Thies C,Cicero TJ

更新日期：1976-06-01 00:00:00

abstract：:The release kinetics of a polymeric-controlled release device are determined by its geometry and dimensions. A method to calculate the required size and shape of diffusion-controlled dosage forms to achieve a particular release profile is presented. The diffusion parameters are determined for various drugs (theophylli...

journal_title：Journal of pharmaceutical sciences

authors： Siepmann J,Ainaoui A,Vergnaud JM,Bodmeier R

更新日期：1998-07-01 00:00:00

abstract：:The physiological pH changes and peristalsis activities in gastrointestinal (GI) tract have big impact on the dissolution of oral drug products, when those oral drug products include APIs with pH-dependent solubility. It is well documented that predicting the bioperformance of those oral drug products can be challengi...

journal_title：Journal of pharmaceutical sciences

authors： Tsume Y,Patel S,Wang M,Hermans A,Kesisoglou F

更新日期：2020-11-01 00:00:00

abstract：:Biodegradable, dextran-based ion-exchange microspheres (IE-MS) have been used for localized delivery of anticancer drugs and chemosensitizers. Because of their hydrophilic nature, the IE-MS release their payload quickly. The purpose of this work was to develop an IE-MS system that could provide a broad range of releas...

journal_title：Journal of pharmaceutical sciences

authors： Liu Z,Wu XY,Ballinger JR,Bendayan R

更新日期：2000-06-01 00:00:00

abstract：:Solid solutions of felodipine with EUDRAGIT E and EUDRAGIT E/NE were shown to dramatically increase the dissolution rate of felodipine in biorelevant media. Of the two polymer systems, extrudates containing 5% EUDRAGIT NE showed a faster dissolution rate and less recrystallization (no precipitation within 2 h). Althou...

journal_title：Journal of pharmaceutical sciences

authors： Nollenberger K,Gryczke A,Meier Ch,Dressman J,Schmidt MU,Brühne S

更新日期：2009-04-01 00:00:00

abstract：:The purpose of the study is to understand the effect of altitude on the performance of selected pressurized metered dose inhalers (pMDIs) and dry powder inhalers (DPIs). A testing apparatus that created consistent breath profiles through the Alberta Idealized Throat was designed to test five pMDIs and two DPIs at alti...

journal_title：Journal of pharmaceutical sciences

authors： Titosky JTF,Morin CMD,Suderman JD,Olfert JS,Finlay WH,Vehring R

更新日期：2014-07-01 00:00:00

abstract：:Plasma binding of chlordiazepoxide, diazepam, loraxepam, and oxazepam was determined by equilibrium dialysis in 20 male, healthy volunteers, 25-86 years old. A wide range of binding was observed, with the free fraction varying twofold for lorazepam, fourfold for chlordiazepoxide and diazepam, and over 20-fold for oxa...

journal_title：Journal of pharmaceutical sciences

authors： Johnson RF,Schenker S,Roberts RK,Desmond PV,Wilkinson GR

更新日期：1979-10-01 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：:Nonionic block copolymers are surfactants synthesized using propylene oxide and ethylene oxide, and they can be designed so that individual copolymers have unique vaccine adjuvant properties. We have designed and produced nonionic block copolymers based on high molecular weight (MW), 9-15 kDA, cores of poly(oxypropyle...

journal_title：Journal of pharmaceutical sciences

authors： Newman MJ,Todd CW,Balusubramanian M

更新日期：1998-11-01 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：: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：:Transcutaneous immunization is the administration of a vaccine on the skin to generate efficient systemic and mucosal immune responses against an antigen. In the present study, reconstituted hepatitis B surface antigen vesicles (HBsAg-REVs) integrated with monophosphoryl lipid A were prepared by the delipidation-recon...

journal_title：Journal of pharmaceutical sciences

authors： Kaurav M,Kumar R,Jain A,Pandey RS

更新日期：2019-11-01 00:00:00

abstract：:Since the FDA approval of Spritam, there has been a growing interest in the application of 3D printing in pharmaceutical science. 3D printing is a method of manufacturing involving the layer-by-layer deposition of materials to create a final product according to a digital model. There are various techniques used to ac...

journal_title：Journal of pharmaceutical sciences

authors： Okafor-Muo OL,Hassanin H,Kayyali R,ElShaer A

更新日期：2020-12-01 00:00:00

abstract：:A rapid and sensitive GLC method was developed for the quantitative determination of methenamine in tablets. The method was shown to possess several advantages over the official NF assay. After dissolution of the whole tablet in absolute ethanol and addition of an internal standard (pentylenetetrazol), an aliquot was ...

journal_title：Journal of pharmaceutical sciences

authors： Strom JG Jr,Jun HW

更新日期：1977-04-01 00:00:00

abstract：:Adequate protein solubility is an important prerequisite for development, manufacture, and administration of biotherapeutic drug candidates, especially for high-concentration protein formulations. A previously established method for determining the relative apparent solubility (thermodynamic activity) of proteins usin...

journal_title：Journal of pharmaceutical sciences

authors： Toprani VM,Joshi SB,Kueltzo LA,Schwartz RM,Middaugh CR,Volkin DB

更新日期：2016-08-01 00:00:00

abstract：:Die filling is a critical process step during tablet production as it defines the tablet weight. Achieving die fill consistency during production of mini-tablets, tablets with diameters ≤6 mm, is considerably more challenging. Although die filling in rotary presses had been studied in relation to the feed paddle desig...

journal_title：Journal of pharmaceutical sciences

authors： Goh HP,Sia Heng PW,Liew CV

更新日期：2019-03-01 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：:Injectable controlled-release formulations are of increasing interest for the treatment of chronic diseases. This study aims to develop and characterize a polymeric matrix for intramuscular or subcutaneous injection, consisting of two biocompatible polymers, particularly suitable for formulating poorly soluble drugs. ...

journal_title：Journal of pharmaceutical sciences

authors： Meeus J,Chen X,Scurr DJ,Ciarnelli V,Amssoms K,Roberts CJ,Davies MC,van Den Mooter G

更新日期：2012-09-01 00:00:00

abstract：:The melting behavior of paracetamol and polyethylene glycol (PEG) 4000, both individually and as binary systems, has been studied using differential scanning calorimetry. The appearance of the PEG peaks was shown to be highly dependent on scanning rate, with evidence for the existence of once-folded and extended chain...

journal_title：Journal of pharmaceutical sciences

authors： Lloyd GR,Craig DQ,Smith A

更新日期：1997-09-01 00:00:00

abstract：:A representative series of hydroxy-5 beta-cholanyl-24-amines were tested both in vitro and in vivo with respect to their activity against the intestinal bacteria responsible for bile acid metabolism. For the in vitro studies, radiolabeled [14C]cholic acid was incubated with human stools both in aerobic and anaerobic c...

journal_title：Journal of pharmaceutical sciences

authors： Roda A,Bellini AM,Mencini E,Minutello A,Fini A,Guarneri M

更新日期：1992-03-01 00:00:00

abstract：:Nonsteroidal anti-inflammatory drugs (NSAIDs) are among the most frequently used drugs in the world, primarily for symptoms associated with osteoarthritis and other chronic musculoskeletal conditions. However, adverse effects caused by oral administration, such as local or systemic disturbance in the gastrointestinal ...

journal_title：Journal of pharmaceutical sciences

authors： Cheng Y,Man N,Xu T,Fu R,Wang X,Wang X,Wen L

更新日期：2007-03-01 00:00:00