Serum lipid-lowering properties of 6-chloro-9-[2-(6-methyl-3-pyridyl)ethyl]-1,2,3,4-tetrahydrocarbazole-2-carboxylic acid.

abstract：:Peptidomimetic drugs have favorable bioavailability owing to H(+)/peptide transporter 1 (PEPT1) located in the intestine. Sartans are commonly used and likely coadministered with peptidomimetic drugs in the clinic; however, in vivo interactions between sartans and peptidomimetic drugs have not been systemically unders...

journal_title：Journal of pharmaceutical sciences

authors： Huo X,Liu Q,Wang C,Meng Q,Sun H,Peng J,Ma X,Sun P,Liu K

更新日期：2014-02-01 00:00:00

abstract：:In vitro percutaneous permeation of betamethasone 17-valerate through excised human skin was studied. Pressure-sensitive silicone adhesive containing betamethasone 17-valerate in suspension was used as a vehicle. Steady-state flux through the split-thickness skin was similar to that through the isolated epidermis. How...

journal_title：Journal of pharmaceutical sciences

authors： Kubota K,Sznitowska M,Maibach HI

更新日期：1993-05-01 00:00:00

abstract：:A method to determine drugs having a carbothionamido group using an ammonia gas-sensing electrode is described. To obtain analytical accuracy, the effect of factors that influence the potential is also discussed. Ethionamide or prothionamide was refluxed with 20% HCl to give ammonium chloride, hydrogen sulfide, and a ...

journal_title：Journal of pharmaceutical sciences

authors： Tagami S,Maeda H

更新日期：1983-09-01 00:00:00

abstract：:Anhydrotetracycline (AHTC), one of the major toxic decomposition products of the antibiotic tetracycline, contains several potential binding sites to metal ions. The acidity constants of the ligand were calculated in aqueous medium (I = 0.1 M) at 25 and 37 degrees C. We found pKa1 = 3.23 +/- 0.08, pKa2 = 5.94 +/- 0.09...

journal_title：Journal of pharmaceutical sciences

authors： de Siqueira JM,Carvalho S,Paniago EB,Tosi L,Beraldo H

更新日期：1994-03-01 00:00:00

abstract：:The particle sizing performance of a Next Generation Pharmaceutical Impactor (NGI) was compared to that of an Andersen cascade impactor (ACI). A single lot of Vanceril MDIs containing beclomethasone dipropionate (BDP) was used throughout. MDIs were sampled into NGI and ACI in accordance with USP recommendations, at 30...

journal_title：Journal of pharmaceutical sciences

authors： Kamiya A,Sakagami M,Hindle M,Byron PR

更新日期：2004-07-01 00:00:00

abstract：:The aim of this study is to evaluate the effect of peptide cyclization on the blood-brain barrier (BBB) modulatory activity and plasma stability of His-Ala-Val peptides, which are derived from the extracellular 1 domain of human E-cadherin. The activities to modulate the intercellular junctions by linear HAV4 (Ac-SHAV...

journal_title：Journal of pharmaceutical sciences

authors： Alaofi A,On N,Kiptoo P,Williams TD,Miller DW,Siahaan TJ

更新日期：2016-02-01 00:00:00

abstract：:4,5-Dimethoxykynuramine was synthesized in a three-step sequence originating with veratrole. Indirect evidence indicates that the drug was converted in vivo to the hypotensive agent 6,7-dimethoxy-4-quinolinol by the action of monoamine oxidase. ...

journal_title：Journal of pharmaceutical sciences

authors： Schwan TJ,Honkomp LJ,Snyder HR Jr,Watson EJ

更新日期：1978-03-01 00:00:00

abstract：:Locally recurrent prostate cancer can lead to significant morbidity, metastasis, and even death. The objective of this study was to evaluate the efficacy of an injectable polymeric paste formulation containing paclitaxel against orthotopic prostate tumor in rats. The Dunning R-3327 rat prostate adenocarcinoma is exper...

journal_title：Journal of pharmaceutical sciences

authors： Shikanov S,Shikanov A,Gofrit O,Nyska A,Corn B,Domb AJ

更新日期：2009-03-01 00:00:00

abstract：:Solution preparation is the first unit operation of the manufacturing process for spray-dried solid dispersions. Visual inspection and offline high-performance liquid chromatography analysis are routinely used to assess the solution preparation end point as well as the final solution composition. However, the accuracy...

journal_title：Journal of pharmaceutical sciences

authors： Lee YC,Zhou G,Ikeda C,Chouzouri G,Howell L

更新日期：2019-03-01 00:00:00

abstract：:To elucidate drug lipophilicity effects on the bioavailability (BA) of drugs from skin after administration by dissolving microneedles, nine compounds with different lipophilicity indexes (log p value) were formulated into two-layered dissolving microneedles and administered percutaneously to rat skin: desmopressin (D...

journal_title：Journal of pharmaceutical sciences

authors： Ito Y,Yoshimura M,Tanaka T,Takada K

更新日期：2012-03-01 00:00:00

abstract：:Mathematical models were determined relating preservative concentration and D values (decimal reduction times at 25 degrees C; pH 6.9-7.1) against Escherichia coli in aqueous medium. Preservatives investigated were 2-bromo-2-nitro-1,3-propanediol (Bronopol), N-(hydroxymethyl)-N-(1,3-dihydroxymethyl-2, 5-dioxo-4-imidaz...

journal_title：Journal of pharmaceutical sciences

authors： Hurwitz SJ,McCarthy TJ

更新日期：1985-08-01 00:00:00

abstract：:The complex of L-L-boronophenylalanine (L-p-BPA) with fructose has been used for the past 5 years in clinical trials of boron neutron capture therapy to treat both melanoma and glioblastoma multiforme. However, the structure of this complex in water buffered at physiologic pH has not been established. In the (1)H NMR ...

journal_title：Journal of pharmaceutical sciences

authors： Shull BK,Spielvogel DE,Head G,Gopalaswamy R,Sankar S,Devito K

更新日期：2000-02-01 00:00:00

abstract：:Angiogenesis--process of new blood-vessel growth from existing vasculature--is an integral part of both normal developmental processes and numerous pathologies such as cancer, ischemic diseases and chronic inflammation. Angiogenesis plays a crucial role facilitating tumour growth and the metastatic process, and it is ...

journal_title：Journal of pharmaceutical sciences

authors： Mauriz JL,González-Gallego J

更新日期：2008-10-01 00:00:00

abstract：:This work aimed at establishing a framework to screen and understand the product variability deeming from factors that affect the quality features of cream formulations. As per Quality by Design - based approach, cream quality target profile and critical quality attributes were identified, and a risk assessment analys...

journal_title：Journal of pharmaceutical sciences

authors： Simões A,Veiga F,Vitorino C

更新日期：2019-10-01 00:00:00

abstract：:We extend and modify the Noyes-Whitney equation and the Hixon-Crowell cube root law to include surface roughness effects on the dissolution rate of drugs. The problem is treated theoretically in terms of the fractal reaction dimension, DR, of the effective surface which undergoes dissolution. Effects of changes in DR ...

journal_title：Journal of pharmaceutical sciences

authors： Farin D,Avnir D

更新日期：1992-01-01 00:00:00

abstract：:The distribution conditions in oil-water emulsions prepared by emulsifying a 1:1 eutectic mixture of lidocaine and prilocaine with a nonionic surfactant in water were studied by membrane and gel filtration methods. In this system, the local anesthetics are considered to be freely dissolved, surfactant solubilized, and...

journal_title：Journal of pharmaceutical sciences

authors： Nyqvist-Mayer AA,Brodin AF,Frank SG

更新日期：1985-11-01 00:00:00

abstract：:The trichloroacetyl carbamates of 38 corticosteroids and chemically related compounds were prepared, and their NMR spectra in deuterochloroform were obtained. The effects of the introduction of a number of functional groups on the chemical shift of the carbamate proton signals were determined. ...

journal_title：Journal of pharmaceutical sciences

authors： Lanouette M,Legault D,Lodge BA

更新日期：1976-08-01 00:00:00

abstract：:The absorption of the model drug carbenoxolone was reevaluated using an in situ rat intestinal perfusion technique in which disappearance from the intestinal lumen, binding to the perfused jejunal segment, and appearance in the mesenteric (jejunal) vein were measured. The effect of the degree of ionization on these pr...

journal_title：Journal of pharmaceutical sciences

authors： Blanchard J,Tang LM,Earle ME

更新日期：1990-05-01 00:00:00

abstract：:The spherically agglomerated crystals of aminophylline (theophylline-ethylenediamine complex) can be compounded directly into pharmaceutical formulations without further processing, e.g., granulation. Such crystals were prepared by mixing theophylline and ethylenediamine in a partially miscible solvent system, i.e., o...

journal_title：Journal of pharmaceutical sciences

authors： Kawashima Y,Aoki S,Takenaka H,Miyake Y

更新日期：1984-10-01 00:00:00

abstract：:Nephropathic cystinosis is a rare autosomal recessive disease characterised by raised lysosomal levels of cystine in the cells of all the organs. It is treated by the 6-h oral administration of the aminothiol, cysteamine, which has an offensive taste and smell. In an attempt to reduce this frequency and improve the tr...

journal_title：Journal of pharmaceutical sciences

authors： Buchan B,Kay G,Matthews KH,Cairns D

更新日期：2012-10-01 00:00:00

abstract：:To gain further insight into the effect of molecular mobility on the crystallization rate of amorphous drugs, the mean relaxation times of amorphous nifedipine and phenobarbital were calculated based on the Adam-Gibbs-Vogel (AGV) equation, using the parameters D, T(0), and T(f), derived from the heating rate dependenc...

journal_title：Journal of pharmaceutical sciences

authors： Aso Y,Yoshioka S,Kojima S

更新日期：2001-06-01 00:00:00

abstract：:Even though gelatin is the most widely used polymeric excipient in pharmaceutical products, scant attention has been paid to its interaction with small organic molecules. The present work deals with the interaction of gelatin and four monosulfonated or monocarboxylated azo dyes having hydrocarbon moieties of different...

journal_title：Journal of pharmaceutical sciences

authors： Gautam J,Schott H

更新日期：1994-07-01 00:00:00

abstract：:A simple, sensitive GLC assay was developed for fusaric acid, the active metabolite of bupicomide, to follow the disposition of this investigational antihypertensive agent in patients undergoing therapy. Fusaric acid is efficiently extracted from biological samples, derivatized by on-column methylation, and chromatogr...

journal_title：Journal of pharmaceutical sciences

authors： Fung KK,Koda RT,Maronde RF,Cohen JL

更新日期：1976-04-01 00:00:00

abstract：:The solubility of a series of compounds was determined in a wide polarity spectrum of normal aliphatic alcohols over a limited temperature range. The solutes chosen were the methyl through n-butyl p-hydroxybenzoates, several of these being useful preservatives. Solubility profiles were determined for these compounds, ...

journal_title：Journal of pharmaceutical sciences

authors： Alexander KS,Mauger JW,Petersen H Jr,Paruta AN

更新日期：1977-01-01 00:00:00

abstract：:Heckel analysis, tablet tensile strength, and indentation hardness were determined for a series of sieved and roller compacted microcrystalline cellulose mixtures under both unlubricated and lubricated conditions with magnesium stearate. These results have been used to evaluate the loss of reworkability following roll...

journal_title：Journal of pharmaceutical sciences

authors： He X,Secreast PJ,Amidon GE

更新日期：2007-05-01 00:00:00

abstract：:The hydrolytic degradation of pirbuterol was investigated under saturated oxygen conditions over a wide range of pH values and at different temperatures. Two of the five observed breakdown products were positively identified. The first-order decomposition rate appeared to depend on the rate constants of the four disso...

journal_title：Journal of pharmaceutical sciences

authors： Bansal PC,Monkhouse DC

更新日期：1977-06-01 00:00:00

abstract：:The influences of 1-ethyl-, 1-butyl-, 1-hexyl-, and 1-octyl-2-pyrrolidone in their saline solutions on the transport of beta-estradiol, corticosterone, and hydrocortisone across hairless mouse skin under in vitro conditions have been investigated by the physical model approach. The experimental data were interpreted w...

journal_title：Journal of pharmaceutical sciences

authors： Yoneto K,Ghanem AH,Higuchi WI,Peck KD,Li SK

更新日期：1995-03-01 00:00:00

abstract：:Brain cancers are among the most lethal tumors due to their rapid development and poor prognosis. Despite the existing potential of novel therapeutic strategies for the treatment of brain cancer, the major remaining challenge associated with clinical translation is the lack of effective and safe delivery strategies to...

journal_title：Journal of pharmaceutical sciences

authors： Guo J,Schlich M,Cryan JF,O'Driscoll CM

更新日期：2017-12-01 00:00:00

abstract：:The wettability of the (001), (100), and (011) crystallographic facets of macroscopic aspirin crystals has been experimentally investigated using a sessile drop contact angle (theta) method. theta for a nonpolar liquid was very similar for all three facets, though significant theta differences were observed for three ...

journal_title：Journal of pharmaceutical sciences

authors： Heng JY,Bismarck A,Lee AF,Wilson K,Williams DR

更新日期：2007-08-01 00:00:00

abstract：:The synthesis of some 6-substituted 3,5-dioxo- and 3-thioxo-5-oxo-2,3,4,5-tetrahydro-1,2,4-triazines for possible antineoplastic activity is reported. The assigned structures were substantiated by IR, NMR, and mass spectral studies of representative members of the series. Four compounds were tested against P-388 lymph...

journal_title：Journal of pharmaceutical sciences

authors： Ibrahim el-SA,Shams el-Dine SA,Soliman FS,Labouta IM

更新日期：1979-02-01 00:00:00