Physicochemical property modification strategies based on enzyme substrate specificities II: alpha-chymotrypsin hydrolysis of aspirin derivatives.

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：:A rapid, precise, and accurate high-performance liquid chromatographic procedure is presented for the stimultaneous determination of amitriptyline hydrochloride and chlordiazepoxide in two-component tablet formulations. The impurities and decomposition products of both components were separated, making the determinati...

journal_title：Journal of pharmaceutical sciences

authors： Burke D,Sokoloff H

更新日期：1980-02-01 00:00:00

abstract：:A reinvestigation of the constituents of the Osage orange (maclura pomifera) yielded, in addition to the previously reported triterpenses (lupeol, butyrospermol, and lupan-3beta,20-diol), the pigments osajin and pomiferin, and a previously unreported constituent. The structure of this new compound was investigated. On...

journal_title：Journal of pharmaceutical sciences

authors： Gearien JE,Klein M

更新日期：1975-01-01 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：:HPLC analysis confirmed a difference in the chemical composition of commercial versus NF reference standard potassium guaiacolsulfonate. After separation by fractional crystallization, the two constituents comprising the former sample were identified by 1H-NMR as potassium guaiacol-4- and -5-sulfonate, respectively. T...

journal_title：Journal of pharmaceutical sciences

authors： Tangtatsawasdi P,Krikorian SE

更新日期：1984-09-01 00:00:00

abstract：:(+-)-Carbovir [(+-)-9-[4 alpha-(hydroxymethyl)-cyclopent-2-ene-1 alpha-yl]guanine; NSC 614846] is a novel carbocyclic nucleoside analogue which has been shown to be a potent and selective inhibitor of HIV in vitro. As part of an effort to develop a parenteral formulation for subsequent clinical and toxicological evalu...

journal_title：Journal of pharmaceutical sciences

authors： Anderson BD,Chiang CY

更新日期：1990-09-01 00:00:00

abstract：:We report the preparation and structural characterization of a family of primary alcohol solvates of a small-molecule hydrochloride salt. The structures of the solvates are probed by powder and single crystal X-ray diffraction, and the compounds were additionally characterized by polarized light microscopy, thermograv...

journal_title：Journal of pharmaceutical sciences

authors： Vasudevan KV,Peterson ML

更新日期：2018-06-01 00:00:00

abstract：:Mycophenolate mofetil (MPM), a new immunosuppressant, is the morpholinoethyl ester of mycophenolic acid (MPA). The distribution in blood and pharmacokinetics of MPA after administration of MPM were examined. The plasma to erythrocyte concentration ratio was low (0.10-0.15). MPA existed in rat plasma as the highly boun...

journal_title：Journal of pharmaceutical sciences

authors： Sugioka N,Koyama H,Ohta T,Kishimoto H,Yasumura T,Takada K

更新日期：1996-03-01 00:00:00

abstract：:Pharmaceutical aerosols are used to treat many pulmonary diseases. The use of low-density powders has proven useful to support efficient drug delivery. Measurements must account for the low-density, spherical particle features contributing to aerodynamic behavior. Ideally, the aerodynamic particle size distribution (A...

journal_title：Journal of pharmaceutical sciences

authors： Hickey AJ,Edwards DA

更新日期：2018-03-01 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：:An exsorption technique which can assess the transport of a drug from blood to the intestinal lumen was used to study the effects of glucose and to determine the presence of segmental differences in drug transport across the rat small intestinal membrane following intravenous drug administration. The drugs used in the...

journal_title：Journal of pharmaceutical sciences

authors： Johno I,Kitazawa S

更新日期：1985-03-01 00:00:00

abstract：:The development of order during the aging of aluminum hydroxide gel prepared by the reaction of aluminum chloride and ammonium hydroxide to a final pH of 7.0 can be monitored by differential thermal analysis. The loss fo acid reactivity upon aging is accompanied by an increase in the temperature and intensity of the d...

journal_title：Journal of pharmaceutical sciences

authors： Aboul-Enein N,Sam J

更新日期：1976-09-01 00:00:00

abstract：:Release of drug from a single-layer film containing dispersed drug follows a diffusion-controlled matrix model, where the quantity released per unit area is proportional to the square root of time. The kinetics may be made linear with time (zero order) by laminating a second film without drug to the releasing side of ...

journal_title：Journal of pharmaceutical sciences

authors： Borodkin S,Tucker FE

更新日期：1975-08-01 00:00:00

abstract：:The estimates of infinity values obtained using Prony's method are shown to be subject to significant error arising from small errors in the assigned sample times. The error of the estimate may be reduced by increasing the time interval between samples. ...

journal_title：Journal of pharmaceutical sciences

authors： Newburger J,Stavchansky S,Pearlman RS

更新日期：1980-10-01 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：:Corneal permeability data taken from the literature were analyzed for possible quantitative relationships with physicochemical properties. Although a parabolic relationship was obtained with good correlation between lipophilicity, as expressed by the 1-octanol-water partition coefficients, log Poctanol (or the distrib...

journal_title：Journal of pharmaceutical sciences

authors： Yoshida F,Topliss JG

更新日期：1996-08-01 00:00:00

abstract：:Near infrared (NIR) spectroscopy was used for quantitatively monitoring polymorph conversion of an active pharmaceutical ingredient (API) in wet granulation. The API under pharmaceutical development has two different polymorphs. Polymorph A is the stable form for drug development and polymorph B is the undesired form ...

journal_title：Journal of pharmaceutical sciences

authors： Li W,Worosila GD,Wang W,Mascaro T

更新日期：2005-12-01 00:00:00

abstract：:A sensitive (10 ng/mL) and specific high-performance liquid chromatographic (HPLC) assay, with electrochemical (EC) detection, for the geometric isomers of 3-hydroxy-N-(2-phenyl-2-(2-thienyl)ethenyl-5-(trifluoromethyl)benzo(b) thiophene-2-carboxamide in dog and human plasma has been developed. Both isomers strongly ab...

journal_title：Journal of pharmaceutical sciences

authors： Matuszewski BK,Kanovsky SM,Constanzer ML,Yeh KC,Bayne WF

更新日期：1988-10-01 00:00:00

abstract：:High-throughput lyophilization process was designed and developed for protein formulations using a single-step drying approach at a shelf temperature (Ts) of ≥40°C. Model proteins were evaluated at different protein concentrations in amorphous-only and amorphous-crystalline formulations. Single-step drying resulted in...

journal_title：Journal of pharmaceutical sciences

authors： Pansare SK,Patel SM

更新日期：2019-04-01 00:00:00

abstract：:In pharmaceutical development alternative drug delivery modalities are being increasingly employed. One example is an implant, which achieves gradual drug release in patients over a period of many months or years. Due to the complexity of these long-acting formulations, advanced physical characterization methods are d...

journal_title：Journal of pharmaceutical sciences

authors： Skomski D,Liu Z,Su Y,John CT,Doty A,Forster SP,Teller R,Barrett SE,Xu W

更新日期：2020-09-01 00:00:00

abstract：:Solution pH and ionic strength (I) have complex effects on protein stability. We developed an experimental approach based on exploitation of the zwitterionic characteristic of amino acid molecules to probe the relative contribution from each. A variety of types of amino acid solutions were adopted to investigate the e...

journal_title：Journal of pharmaceutical sciences

authors： Zhou R,Nashine V,Palm T,Gandhi R,Adams M

更新日期：2014-10-01 00:00:00

abstract：:Vehicle effects may be caused by thermodynamic effects and by specific (penetration enhancing) effects. To investigate the effects of various lipophilic vehicles on drug penetration, an in vivo permeability study was conducted with methyl nicotinate as the model drug. The drug was dissolved in the respective vehicles ...

journal_title：Journal of pharmaceutical sciences

authors： Leopold CS,Lippold BC

更新日期：1995-02-01 00:00:00

abstract：:Carbamazepine is the first-line anti-epileptic drug for focal seizures and generalized tonic-clonic seizures. Although sustained-release formulations exist, an initial burst of drug release is still present and this results in side effects. Zero-order release formulations reduce fluctuations in serum drug concentratio...

journal_title：Journal of pharmaceutical sciences

authors： Lim SH,Chia SM,Kang L,Yap KY

更新日期：2016-07-01 00:00:00

abstract：:Targeted echogenic liposome dispersions for ultrasonic enhancement of vasoactive and pathological components of endothelium and atherosclerosis have recently been developed. The component lipids required for acoustic and targeting properties include phosphatidylcholine, phosphatidylethanolamine phosphatidylglycerol (P...

journal_title：Journal of pharmaceutical sciences

authors： Huang SL,Hamilton AJ,Nagaraj A,Tiukinhoy SD,Klegerman ME,McPherson DD,Macdonald RC

更新日期：2001-12-01 00:00:00

abstract：:The aim of this study was to characterize the metabolic pathways of 2-methoxyestradiol (2ME2), an investigational anticancer drug. In vitro metabolism studies were performed by incubation of 2ME2 with human liver microsomes under various conditions and metabolite identification was performed using liquid chromatograph...

journal_title：Journal of pharmaceutical sciences

authors： Lakhani NJ,Sparreboom A,Xu X,Veenstra TD,Venitz J,Dahut WL,Figg WD

更新日期：2007-07-01 00:00:00

abstract：:The aim of this study was to utilize high-speed video imaging for understanding the disintegrability of compacts and disintegrant action upon wetting. High-speed video imaging was used to visualize the disintegration of compacts and effect of wetting on free disintegrant particles. Acquired images were processed using...

journal_title：Journal of pharmaceutical sciences

authors： Desai PM,Liew CV,Heng PW

更新日期：2012-06-01 00:00:00

abstract：:The absorption and pharmacokinetics of sulofenur [N-(indan-5-sulfonyl)-N'-(4-chlorophenyl)urea, LY186641] and its major metabolites were examined in mice, rats, monkeys, and dogs. The compound is a diarylsulfonylurea currently being evaluated as an oncolytic agent in phase I and II trials. In all species, sulofenur wa...

journal_title：Journal of pharmaceutical sciences

authors： Ehlhardt WJ,Sullivan HR,Wood PG,Woodland JM,Hamilton M,Hamilton C,Cornpropst D,Grindey GB,Worzalla JF,Bewley JR

更新日期：1993-07-01 00:00:00

abstract：:In this study a 3D printed capsule designed to break from the physiological pressures in the antropyloric region was evaluated for its ability to deliver the synthetic octapeptide octreotide in beagle dogs when co-formulated with the permeation enhancer sodium caprate. The pressure sensitive capsules were compared to ...

journal_title：Journal of pharmaceutical sciences

authors： Berg S,Krause J,Björkbom A,Walter K,Harun S,Granfeldt A,Janzén D,Nunes SF,Antonsson M,Van Zuydam N,Skrtic S,Hugerth A,Weitschies W,Davies N,Abrahamsson B,Bergström CAS

更新日期：2021-01-01 00:00:00

abstract：:Three analogs of thyroliberin (I) were prepared. These compounds, N-m-chloroacetylbenzoyl-phenylalanyl-prolineamide (VIa), N-p-chloroacetylbenzoyl-phenylalanyl-prolineamide (VIb) and N-chloroacetyl-alanyl-phenylalanyl-prolineamide (IX), were designed as potential I antagonist affinity labels. However, no significant a...

journal_title：Journal of pharmaceutical sciences

authors： Goebel RJ,Currie BL,Bowers CY

更新日期：1982-09-01 00:00:00

abstract：:The application of direct zero-order UV spectrophotometric and graphical or derivative background correction methods to selected pharmaceutical preparations shows their relative advantages in different situations. The assay of the active components in a changeable matrix is a problem with formulations having a limited...

journal_title：Journal of pharmaceutical sciences

authors： Traveset J,Such V,Gonzalo R,Gelpi E

更新日期：1980-06-01 00:00:00