Stereospecific metabolic reduction of ketones.

abstract：:A procedure was developed for the separation and selective quantitative determination of the (S)(+)- and (R)(-)-enantiomers of the racemic anti-inflammatory drug carprofen as their diastereomeric l-(-)-alpha-methylbenzylamides. These derivatives are obtained in equivalent yields by reacint purified 14C-carprofen from ...

journal_title：Journal of pharmaceutical sciences

authors： Kemmerer JM,Rubio FA,McClain RM,Koechlin BA

更新日期：1979-10-01 00:00:00

abstract：:To estimate the feasibility of novel containers for drugs, poly(ethylene oxide)-poly(beta-benzyl L-aspartate) (PEO-PBLA) micelles were prepared by dialysis against water using different solvents. The solvent selected is very important because it drastically affects the stability of polymeric micelles. The critical mic...

journal_title：Journal of pharmaceutical sciences

authors： La SB,Okano T,Kataoka K

更新日期：1996-01-01 00:00:00

abstract：:Electron micrographs of Pseudomonas aeruginosa grown in nutrient broth or broth containing subinhibitory concentrations of benzalkonium chloride indicate that benzalkonium chloride at 50 and 100 mug/ml strips off the outer cell membrane. Cells grown in the presence of edetate disodium, 50-100 mug/ml had convoluted sur...

journal_title：Journal of pharmaceutical sciences

authors： Richards RM,Cavill RH

更新日期：1976-01-01 00:00:00

abstract：:Simulated intestinal media (SIM) containing bile salt (BS) and phospholipids (PL) with and without medium chain lipolytic products (MC-LP) or long chain lipolytic products (LC-LP) were developed to study the solubility of seocalcitol. Both MC-LP and LC-LP were studied in order to investigate the influence of fatty aci...

journal_title：Journal of pharmaceutical sciences

authors： Grove M,Pedersen GP,Nielsen JL,Müllertz A

更新日期：2005-08-01 00:00:00

abstract：:Thiamine hydrochloride (Vitamin B(1), THCl) can exist as a nonstoichiometric hydrate (NSH) and as a hemihydrate (HH). NSH can contain up to approximately 1 molar equivalent of water and be dehydrated to an isomorphic desolvate (ID) with minimal change in lattice structure. Crystallographic and spectroscopic techniques...

journal_title：Journal of pharmaceutical sciences

authors： Chakravarty P,Berendt RT,Munson EJ,Young VG Jr,Govindarajan R,Suryanarayanan R

更新日期：2010-02-01 00:00:00

abstract：:Site I of human serum albumin is an important and complex region for high-affinity binding of drugs. Equilibrium dialysis showed independent binding of dansyl-L-asparagine (DNSA) and n-alkyl p-aminobenzoates (p-ABEs) to regions Ib and Ic, respectively, in the pH range 6.0-9.0. However, individual binding of DNSA incre...

journal_title：Journal of pharmaceutical sciences

authors： Yamasaki K,Maruyama T,Takadate A,Suenaga A,Kragh-Hansen U,Otagiri M

更新日期：2004-12-01 00:00:00

abstract：:Tryptophan (Trp) oxidation in proteins leads to a number of events, including changes in color, higher order structure (HOS), and biological activity. We describe here a number of new findings through a comprehensive characterization of 6 monoclonal antibodies (mAbs) following selective oxidation of Trp residues by 2,...

journal_title：Journal of pharmaceutical sciences

authors： Barnett GV,Balakrishnan G,Chennamsetty N,Hoffman L,Bongers J,Tao L,Huang Y,Slaney T,Das TK,Leone A,Kar SR

更新日期：2019-06-01 00:00:00

abstract：:The assessment of provenance of heparin is becoming a major concern for the pharmaceutical industry and its regulatory bodies. Batch-specific [carbon (δ(13) C), nitrogen (δ(15) N), oxygen (δ(18) O), sulfur (δ(34) S), and hydrogen (δD)] stable isotopic compositions of five different animal-derived heparins were perform...

journal_title：Journal of pharmaceutical sciences

authors： Jasper JP,Zhang F,Poe RB,Linhardt RJ

更新日期：2015-02-01 00:00:00

abstract：:Pyrimethamine, an antimalarial drug, was found to be able to inhibit both enzymes (DHFR-TS and PTR1) of the leishmanial folate pathway, although this effect in vivo appears only in relatively high concentrations. To reach the parasites inside macrophage cells, where they are sheltered, targeted drugs of pyrimethamine,...

journal_title：Journal of pharmaceutical sciences

authors： De Carvalho PB,Ramos DC,Cotrim PC,Ferreira EI

更新日期：2003-10-01 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：:A new indole based chalcone molecule MOMIPP induced methuosis mediated cell death in gliobastoma and other cancer cell lines. But the drug was insoluble in water and had a very short plasma half-life. The purpose of this work was to develop a formulation that can provide sustained levels of MOMIPP in vivo. Initial stu...

journal_title：Journal of pharmaceutical sciences

authors： Oppong F,Li Z,Fakhrabadi EA,Raorane T,Giri PM,Liberatore MW,Sarver JG,Trabbic CJ,Hosier CE,Erhardt PW,Maltese WA,Nesamony J

更新日期：2020-09-01 00:00:00

abstract：:Membrane permeation enhancers have received significant attention in recent years for enabling the oral absorption of poorly permeable drug molecules. In this study, we investigated the ability of His-Ala-Val (HAV) and Ala-Asp-Thr (ADT) peptides derived from the extracellular-1 (EC1) domain of E-cadherin proteins to i...

journal_title：Journal of pharmaceutical sciences

authors： Dening TJ,Siahaan TJ,Hageman MJ

更新日期：2020-12-23 00:00:00

abstract：:The poor aqueous solubility of carbamazepine was dramatically increased via complexation with various chemically modified beta-cyclodextrins and gamma-cyclodextrins. A preparation of carbamazepine and 2-hydroxypropyl-beta-cyclodextrin was found to be stable to steam sterilization and to storage under a variety of cond...

journal_title：Journal of pharmaceutical sciences

authors： Brewster ME,Anderson WR,Estes KS,Bodor N

更新日期：1991-04-01 00:00:00

abstract：:Carvedilol is a new beta-blocking agent with vasodilating activities, which is a racemic mixture of R(+)- and S(-)-enantiomers. Since the two enantiomers differ in pharmacological properties, it is necessary to individually measure their plasma concentrations in order to evaluate the pharmacological effects of racemic...

journal_title：Journal of pharmaceutical sciences

authors： Fujimaki M,Murakoshi Y,Hakusui H

更新日期：1990-07-01 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：:A series of 4-substituted aminoquinoline-3-carboxylates was prepared and evaluated for antimicrobial activity. Four of the compounds (VIII, XIII, XV, and XXIII) exhibited low activity against Staphylococcus aureus. ...

journal_title：Journal of pharmaceutical sciences

authors： Marecki PE,Bambury RE

更新日期：1984-08-01 00:00:00

abstract：:Stent implantation following angioplasty is the standard treatment of coronary artery disease necessitating interventional procedures. The use of stents as a platform for local drug delivery is a popular strategy to achieve local pharmacological treatment to the diseased artery. Drug eluting stents (DES) are now large...

journal_title：Journal of pharmaceutical sciences

authors： Sharkawi T,Cornhill F,Lafont A,Sabaria P,Vert M

更新日期：2007-11-01 00:00:00

abstract：:The recently introduced four-parameter extended Hansen approach was used to study the solubility of p-hydroxybenzoic acid and methyl p-hydroxybenzoate in 32 and 35 individual solvents, respectively. The results are compared with those for benzoic acid in 40 solvents. Seventeen of the thirty-two or 53% of the calculate...

journal_title：Journal of pharmaceutical sciences

authors： Martin A,Wu PL,Beerbower A

更新日期：1984-02-01 00:00:00

abstract：:In recent years, biotechnologically derived peptide and protein-based drugs have developed into mainstream therapeutic agents. Peptide and protein drugs now constitute a substantial portion of the compounds under preclinical and clinical development in the global pharmaceutical industry. Pharmacokinetic and exposure/r...

journal_title：Journal of pharmaceutical sciences

authors： Tang L,Persky AM,Hochhaus G,Meibohm B

更新日期：2004-09-01 00:00:00

abstract：:3-N-(1',8'-Naphthalimido)propionic acid was synthesized and shown to effectively lower both serum cholesterol and triglyceride levels in rats and mice. In hyperlipidemic mice, serum lipid levels were lowered significantly, approaching normal levels of cholesterol and below normal levels of triglyceride. The serum lipi...

journal_title：Journal of pharmaceutical sciences

authors： Hall IH,Chapman JM Jr,Voorstad PJ,Cocolas GH

更新日期：1984-07-01 00:00:00

abstract：:Insulin-degrading enzyme (IDE) has been implicated in the intracellular degradation of insulin in insulin target cells. Knowledge of the existence of this enzyme in the intestine will be beneficial to the achievement of clinical oral efficacy of insulin. A comparative study was conducted with rat intestine, human colo...

journal_title：Journal of pharmaceutical sciences

authors： Chang LL,Stout LE,Wong WD,Buls JG,Rothenberger DA,Shier WT,Sorenson RL,Bai JP

更新日期：1997-01-01 00:00:00

abstract：:A difference spectrophotometric analytical method was developed for the selective determination of p-hydroxybenzoic acid in the presence of its alkyl esters without prior separation. Based on the spectral shift to a shorter wavelength accompanyint carboxyl dissociation, the procedure measures as little as 2% of this a...

journal_title：Journal of pharmaceutical sciences

authors： Fink DW,Fink HC,Tolan JW,Blodinger J

更新日期：1978-06-01 00:00:00

abstract：:The objectives of this work are to explore the pi-pi complexation of amitriptyline with pi electron-deficient aromatic rings and demonstrate the feasibility of pi-pi complexation for overdosed drug detoxification. Water-soluble oligochitosan was chemically modified with dinitrobenzenesulfonyl groups to induce selectiv...

journal_title：Journal of pharmaceutical sciences

authors： Lee DW,Flint J,Morey T,Dennis D,Partch R,Baney R

更新日期：2005-02-01 00:00:00

abstract：:Accelerated stability studies (37 degrees, 47 degrees, and 57 degrees) were conducted on buffered aqueous solutions (pH 7.4, 8.4, and 9.4) of hydrocortisone in the presence of various molar ratios of D-fructose. First-order degradation was observed. Significant improvement in hydrocortisone stability was seen in those...

journal_title：Journal of pharmaceutical sciences

authors： Bansal NP,Holleran EM,Jarowski CI

更新日期：1983-09-01 00:00:00

abstract：:The major objective of this study was to investigate and characterize the solution properties of cromolyn sodium (in D(2)O or D(2)O/H(2)O phosphate buffer at pH 7.5) using nuclear magnetic resonance (NMR) spectroscopy. The self-association of cromolyn molecules was examined primarily via one-dimensional (1)H and (13)C...

journal_title：Journal of pharmaceutical sciences

authors： Ding X,Stringfellow TC,Robinson JR

更新日期：2004-05-01 00:00:00

abstract：:In this study, the cytotoxicity of doxorubicin (DOX) loaded stearic acid grafted chitosan oligosaccharide (CSO-SA) micelles and its core modified drug delivery systems were investigated in vitro. The in vitro drug release experiments using cellular culture medium, Roswell Park Memorial Institute 1640 (RPMI-1640) mediu...

journal_title：Journal of pharmaceutical sciences

authors： Ye YQ,Chen FY,Wu QA,Hu FQ,Du YZ,Yuan H,Yu HY

更新日期：2009-02-01 00:00:00

abstract：:Application of ultrasound enhances transdermal transport of drugs (sonophoresis). The enhancement may result from enhanced diffusion due to ultrasound-induced skin alteration and/or from forced convection. To understand the relative roles played by these two mechanisms in low-frequency sonophoresis (LFS, 20 kHz), a th...

journal_title：Journal of pharmaceutical sciences

authors： Tang H,Mitragotri S,Blankschtein D,Langer R

更新日期：2001-05-01 00:00:00

abstract：:A colorimetric procedure for benzocaine and a number of its dosage forms was developed; it offers improvement in ease, speed, and sensitivity over the official method. The method is based on the formation of a red Schiff base between benzocaine and p-dimethylaminocinnamaldehyde in a nonaqueous acidic medium. At the ma...

journal_title：Journal of pharmaceutical sciences

authors： Tan HS,Bruemmer GA,Shelton D

更新日期：1977-07-01 00:00:00

abstract：:One of the challenges with predictive modeling is how to quantify the reliability of the models' predictions on new objects. In this work we give an introduction to conformal prediction, a framework that sits on top of traditional machine learning algorithms and which outputs valid confidence estimates to predictions ...

journal_title：Journal of pharmaceutical sciences

authors： Alvarsson J,Arvidsson McShane S,Norinder U,Spjuth O

更新日期：2021-01-01 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