Synthesis of 10alpha-methoxy-delta8,9-lysergaldehyde from elymoclavine.

abstract：:The objective of this study was to examine the ocular absorption behavior of an amphiphilic prodrug after instillation onto the cornea of rabbits. A micellar solution of O-palmitoyl tilisolol (PalTL), an amphiphilic prodrug, was prepared. After instillation of tilisolol (TL) and PalTL, the drug concentrations in the t...

journal_title：Journal of pharmaceutical sciences

authors： Kawakami S,Nishida K,Mukai T,Yamamura K,Kobayashi K,Sakaeda T,Nakamura J,Nakashima M,Sasaki H

更新日期：2001-12-01 00:00:00

abstract：:A crude chloroform-soluble fraction of the ethanol extract of the leaves of Bursera klugii showed activity against two test systems, the P-388 lymphocytic leukemia (3PS) and the human epidermoid carcinoma of the nasopharynx (9KB). The PS activity was due to two constituents, sapelins A and B. ...

journal_title：Journal of pharmaceutical sciences

authors： Jolad SD,Wiedhopf RM,Cole JR

更新日期：1977-06-01 00:00:00

abstract：:The pharmacokinetics and safety of TY-11345 [(+/-)-2-[(4-methoxy-6,7,8,9-tetrahydro-5H-cyclohepta[b]pyridin-9- yl)sulfinyl]-1H-benzimidazole sodium salt], a novel gastric proton pump inhibitor, were studied in healthy male volunteers after single (20, 40, and 80 mg) and repeated oral doses (60 mg, once daily for 7 day...

journal_title：Journal of pharmaceutical sciences

authors： Uematsu T,Nakano M,Kosuge K,Nagai A,Sato A,Nakashima M

更新日期：1994-10-01 00:00:00

abstract：:A titration method was developed for the determination of diphenhydramine, quinine, neostigmine, sparteine, strychnine, homatropine, atropine, physostigmine, and procaine in aqueous solution. Tetraphenylborate was used as a titrant with tetrabromophenolphthalein ethyl ester as an indicator in the presence of organic s...

journal_title：Journal of pharmaceutical sciences

authors： Tsubouchi M,Mitsushio H,Yamasaki N,Matsuoka K

更新日期：1981-11-01 00:00:00

abstract：:The purpose of this study was to evaluate the therapeutic efficacy of a new calcium phosphate (CaP)-based formulation in improving the bone mineral deficiency in ovariectomized (OVX) rats. The ions release experiments for CaP preparations (G2: 0.46% Mg, 5.78% Zn, and 2.5% F; G3:3.1% Mg, 0.03% Zn, and 3.01% F; G4: 1.25...

journal_title：Journal of pharmaceutical sciences

authors： Otsuka M,Oshinbe A,Legeros RZ,Tokudome Y,Ito A,Otsuka K,Higuchi WI

更新日期：2008-01-01 00:00:00

abstract：:1-[4-(2-Cyclopropylmethoxyethyl)phenoxy]-3-[1-p-(bromoacetamidophe nyl) -2-methyl-2-propylamine]-2-propranol (8), which is a derivative of the beta 1-adrenergic agent betaxolol, was synthesized. Compound 8 showed less potent beta-adrenergic blocking activity than betaxolol in an in vitro test with guinea pig tracheal ...

journal_title：Journal of pharmaceutical sciences

authors： Amlaiky N,Leclerc G

更新日期：1985-10-01 00:00:00

abstract：:Repetitive administration is routinely used to maintain therapeutic drug levels, but previous studies have documented an accelerated blood clearance of some lipid-based delivery systems under these conditions. To assess the effect of repetitive administration, non-PEGylated lipoplexes (+/-0.5) were administered 4 time...

journal_title：Journal of pharmaceutical sciences

authors： Betker JL,Anchordoquy TJ

更新日期：2017-03-01 00:00:00

abstract：:A wide variety of computational models covering statistical, mechanistic, and machine learning (locked and adaptive) methods are explored for use in biopharmaceutical manufacturing. Limited discussion exists on how to establish the credibility of a computational model for application in biopharmaceutical manufacturing...

journal_title：Journal of pharmaceutical sciences

authors： Bideault G,Scaccia A,Zahel T,Forero RL,Daluwatte C

更新日期：2021-01-22 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：: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：:In vitro studies on the photodecomposition of uric acid in the presence of the monosodium salt of riboflavin 5'-phosphate in buffers at various pH values, in methanol, and in human plasma are reported. The decomposition rate increased with increasing pH and was independent of solvent or buffer species. The mechanism a...

journal_title：Journal of pharmaceutical sciences

authors： Newburger J,Combs AB,Hsu TF

更新日期：1977-11-01 00:00:00

abstract：:A diffusion model for the percutaneous absorption of a solute through the skin is developed for the specific case of a constant donor concentration with a finite removal rate from the receptor due to either perfusion rate or sampling. The model has been developed to include a viable epidermal resistance and a donor-st...

journal_title：Journal of pharmaceutical sciences

authors： Anissimov YG,Roberts MS

更新日期：1999-11-01 00:00:00

abstract：:Electrolytes often break emulsions to which they were added as active ingredients, adjuvants, or impurities. The stability of oil-in-water emulsions containing octoxynol 9 NF as the emulsifier and various added electrolytes was investigated by measuring droplet size, turbidity, and oil separation on storage at various...

journal_title：Journal of pharmaceutical sciences

authors： Schott H,Royce AE

更新日期：1983-12-01 00:00:00

abstract：:DNA co-condensates were formed by reacting [125I]DNA with an admixture of a high-mannose glycopeptide (Man9-CWK(18)) and either of two poly(ethylene glycol) peptides (PEG-VS-CWK(18) or PEG-SS-CWK(18)) followed by cross-linking with 6-50 mol equiv of glutaraldehyde. [125I]DNA co-condensates were administered intravenou...

journal_title：Journal of pharmaceutical sciences

authors： Yang Y,Park Y,Man S,Liu Y,Rice KG

更新日期：2001-12-01 00:00:00

abstract：:A physiologic pharmacokinetic model describing percutaneous absorption of topically applied compounds in the isolated perfused porcine skin flap (IPPSF) is presented. As an extension of a previously reported hybrid physiologically relevant compartmental model of uptake of intra-arterially administered drug in the IPPS...

journal_title：Journal of pharmaceutical sciences

authors： Williams PL,Carver MP,Riviere JE

更新日期：1990-04-01 00:00:00

abstract：:Volunteers were injected im with 100 mg of tripelennamine (pyribenzamine).HCl dissolved in saline. Timed urine was collected. Tripelennamine and its metabolites were identified by GC/MS. Amounts of free tripelennamine excreted in the 0-2-, 2-4-, 4-8-, 8-12-, and 12-24-h urine samples were found to be 0.30, 0.56, 0.17,...

journal_title：Journal of pharmaceutical sciences

authors： Yeh SY

更新日期：1991-09-01 00:00:00

abstract：:Polymeric nanoparticles (NPs) are interesting drug carriers for dermal application and drug targeting to certain skin structures. NP interactions with diseased skin and the associated benefits and risks have been hardly explored. Today, we study the behavior of polymeric NPs for selective drug delivery to inflamed ski...

journal_title：Journal of pharmaceutical sciences

authors： Abdel-Mottaleb MM,Moulari B,Beduneau A,Pellequer Y,Lamprecht A

更新日期：2012-11-01 00:00:00

abstract：:Liposomes containing sodium ioxitalamate were prepared by sonication. Suitable amounts of purified soybean phosphatidylcholine and cholesterol were used at various molar ratios. Stearylamine or dicetylphosphate were added to this lipid composition when charged liposomes were required. After sonication and removal of u...

journal_title：Journal of pharmaceutical sciences

authors： Benita S,Poly PA,Puisieux F,Delattre J

更新日期：1984-12-01 00:00:00

abstract：:The degradation kinetics and mechanism of a potent new cephalosporin, cefotaxime sodium, in aqueous solution were investigated at pH 0-10 at 25 degrees and an ionic strength of 0.5. The degradation rates were determined by high-pressure liquid chromatography and were observed to follow pseudo first-order kinetics with...

journal_title：Journal of pharmaceutical sciences

authors： Berge SM,Henderson NL,Frank MJ

更新日期：1983-01-01 00:00:00

abstract：:Insight into the stratum corneum (SC) permeation pathway for hydrophilic compounds is gained by comparing experimental measurements of permeability and lag time (tlag) with the predictions of a finite element (FE) model. A database of permeability and lag time measurements (n=27) of hydrophilic compounds was compiled ...

journal_title：Journal of pharmaceutical sciences

authors： Barbero AM,Frasch HF

更新日期：2006-10-01 00:00:00

abstract：:Caco-2 cell monolayers are widely used systems for predicting human intestinal absorption. This study was carried out to develop a quantitative structure-property relationship (QSPR) model of Caco-2 permeability using a novel genetic algorithm-based partial least squares (GA-PLS) method. The Caco-2 permeability data f...

journal_title：Journal of pharmaceutical sciences

authors： Yamashita F,Wanchana S,Hashida M

更新日期：2002-10-01 00:00:00

abstract：:The degradation kinetics of phentolamine hydrochloride in aqueous solution over a pH range of 1.2 to 7.2 and its stability in propylene glycol- or polyethylene glycol 400-based solutions were investigated. The observed rate constants were shown to follow apparent first-order kinetics in all cases. The pKa determinatio...

journal_title：Journal of pharmaceutical sciences

authors： Wang DP,Tu YH,Allen LV Jr

更新日期：1988-11-01 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：:We previously reported nonaqueous silicone elastomer gels (SEGs) for sustained vaginal administration of the CCR5-targeted entry inhibitor maraviroc (MVC). Here, we describe chemically modified SEGs (h-SEGs) in which the hydrophobic cyclomethicone component was partially replaced with relatively hydrophilic silanol-te...

journal_title：Journal of pharmaceutical sciences

authors： Forbes CJ,McCoy CF,Murphy DJ,Woolfson AD,Moore JP,Evans A,Shattock RJ,Malcolm RK

更新日期：2014-05-01 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：:Although displacement from plasma protein binding (dPB) is usually of little clinical significance, it should be taken into account when interpreting changes in total plasma concentrations of drugs subject to metabolically based drug-drug interactions (mDDI). The aim of this study was to develop an approach to predict...

journal_title：Journal of pharmaceutical sciences

authors： Christensen H,Baker M,Tucker GT,Rostami-Hodjegan A

更新日期：2006-12-01 00:00:00

abstract：:Water/n-octanol partition coefficients (log P) for 33 1,2-dithiole-3-thiones and for 18 1,2-dithiol-3-ones were determined by RP-HPLC measurement of the concentration of the solute in aqueous solution after equilibrium. Depending on the nature of the substituents (alkyl or aryl) and their position(s) (4,5, or both) on...

journal_title：Journal of pharmaceutical sciences

authors： Bona M,Boudeville P,Zekri O,Christen MO,Burgot JL

更新日期：1995-09-01 00:00:00

abstract：:The permeability coefficient, Kp, of pure unbranched alkanoic acids (C2-C7) applied to isolated porcine skin, reached a maximum in the solubility parameter (delta 2) range of 9.7-10 cal1 /2/cm3/2. When these and other penetrants were delivered from a solvent vehicle, the following linear relationships could be demonst...

journal_title：Journal of pharmaceutical sciences

authors： Liron Z,Cohen S

更新日期：1984-04-01 00:00:00

abstract：:In adult patients, nilotinib is indicated for chronic myeloid leukemia at an approved oral dose of 300 or 400 mg BID. Physiologically based pharmacokinetic (PBPK) model was developed to describe and supplement limited PK data in the pediatric population ranging from 2 to less than 6 years of age and ultimately inform ...

journal_title：Journal of pharmaceutical sciences

authors： Heimbach T,Lin W,Hourcade-Potelleret F,Tian X,Combes FP,Horvath N,He H

更新日期：2019-06-01 00:00:00

abstract：:(13)C labeling was used to enhance the sensitivity of (13)C solid-state NMR to study the effect of tabletting on the polymorphism of a steroidal drug. The steroidal drug Org OD 14 was (13)C labeled and formulated into tablets containing only 0.5-2.5% active ingredient. The tablets were subsequently studied by solid-st...

journal_title：Journal of pharmaceutical sciences

authors： Booy KJ,Wiegerinck P,Vader J,Kaspersen F,Lambregts D,Vromans H,Kellenbach E

更新日期：2005-02-01 00:00:00