Synthesis of alkylaminoalkylamides of substituted 2-aminopyrroles as potential local anesthetic and antiarrhythmic agents. II: beta-Amines.

abstract：:The intracellular delivery of small interfering RNA (siRNA) is a therapeutic strategy to transiently block gene expression. Two silencing RNA strategies utilize either synthetic double stranded RNA or plasmid DNA encoding a short hairpin RNA (shRNA). In the present study, we have quantitatively compared the potency of...

journal_title：Journal of pharmaceutical sciences

authors： McAnuff MA,Rettig GR,Rice KG

更新日期：2007-11-01 00:00:00

abstract：:Certain disulfide analogues of cystamine were prepared and evaluated for the ability to inhibit gamma-glutamylcysteine synthetase (GCS), the rate-limiting enzyme in glutathione synthesis. The compound SAPH-3 disulfide (2a) was found to be the most effective inactivator of GCS reported to date. Studies of structural an...

journal_title：Journal of pharmaceutical sciences

authors： Schor NF,Cheng B,Siuda JF

更新日期：1991-04-01 00:00:00

abstract：:The effect of caffeine on the absorption of ergotamine from the rat small intestine was studied. The results of a series of experiments showed that caffeine significantly enhanced absorption of ergotamine from solutions of pH 5.0 when both substances were in solution and when an intact blood supply was either absent (...

journal_title：Journal of pharmaceutical sciences

authors： Anderson JR,Drehsen G,Pitman IH

更新日期：1981-06-01 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：:Ascorbic acid (100 mg/ml) and sodium bisulfite (0.5 and 20 mg/ml) prevented more than 10% oxidation of apomorphine hydrochloride in water maintained at room temperature over 1-3 days. Refrigeration at 5 degrees prevented oxidation of apomorphine hydrochloride in aqueous solutions for 1 week. Neither ascorbic acid nor ...

journal_title：Journal of pharmaceutical sciences

authors： Wilcox RE,Humphrey DW,Riffee WH,Smith RV

更新日期：1980-08-01 00:00:00

abstract：:The purpose of this study was to understand the combined effect of two polymers showing drug-polymer interactions on amorphous stabilization and dissolution enhancement of indomethacin (IND) in amorphous ternary solid dispersions. The mechanism responsible for the enhanced stability and dissolution of IND in amorphous...

journal_title：Journal of pharmaceutical sciences

authors： Prasad D,Chauhan H,Atef E

更新日期：2014-11-01 00:00:00

abstract：:Systemic administration of drugs is ineffective in the treatment of central nervous system disorders because of the blood-brain barrier. Nasal administration has been suggested as an alternative administration route as drugs absorbed in the olfactory epithelium bypass the blood-brain barrier and reach the brain within...

journal_title：Journal of pharmaceutical sciences

authors： Wu IY,Nikolaisen TE,Škalko-Basnet N,di Cagno MP

更新日期：2019-08-01 00:00:00

abstract：:The influence of hepatic uptake and efflux, which includes passive diffusion and transporter-mediated component, on drug distribution volumes [steady-state volume of distribution (V(ss)) and terminal volume of distribution (V(β))], mean residence time (MRT), clearance, and terminal half-life is considered using a simp...

journal_title：Journal of pharmaceutical sciences

authors： Berezhkovskiy LM

更新日期：2011-11-01 00:00:00

abstract：:Postabsorptive factors which can affect systemic drug exposure are assumed to be dependent on the active pharmaceutical ingredient (API), and thus independent of formulation. In contrast, preabsorptive factors, for example, hypochlorhydria, might affect systemic exposure in both an API and a formulation-dependent way....

journal_title：Journal of pharmaceutical sciences

authors： Cristofoletti R,Patel N,Dressman JB

更新日期：2017-02-01 00:00:00

abstract：:Recent murine studies found that rifapentine, dosed daily, at least halved tuberculosis treatment times compared with standard rifampicin and isoniazid-containing regimens. However, in humans, an inhalable form of rifapentine may be necessary to considerably shorten treatment duration because of the physiological barr...

journal_title：Journal of pharmaceutical sciences

authors： Chan JG,Duke CC,Ong HX,Chan JC,Tyne AS,Chan HK,Britton WJ,Young PM,Traini D

更新日期：2014-05-01 00:00:00

abstract：:This study examined the safety, pharmacodynamic and pharmacokinetic similarity of the human recombinant filgrastim products ior®LeukoCIM and Neupogen® following a 28-day repeated subcutaneous dose administration in male and female Sprague-Dawley rats with a 14-day recovery period. Safety profiling was based on clinica...

journal_title：Journal of pharmaceutical sciences

authors： Licollari A,Riddle K,Taylor SR,Ledon N,Bolger GT

更新日期：2017-06-01 00:00:00

abstract：:The purpose of this work was to investigate the self-associating behavior observed in high concentration monoclonal antibody (MAb1) solutions at pH 6.0. Zeta potential measurements over the pH range (4.0-9.0) showed lower net charges present on the molecule at pH 6.0 and 7.0. The point of zero charge or crossover from...

journal_title：Journal of pharmaceutical sciences

authors： Yadav S,Liu J,Shire SJ,Kalonia DS

更新日期：2010-03-01 00:00:00

abstract：:In this study, powder surface imaging was utilized in evaluation of particle size-related segregation behavior of granules during vibration and tableting processes. Altogether, eight granule batches were manufactured using a fluidized bed granulator. The particle size distribution of each batch was measured with sieve...

journal_title：Journal of pharmaceutical sciences

authors： Lakio S,Hatara J,Tervakangas H,Sandler N

更新日期：2012-06-01 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：:Knowledge of slip or cleavage planes can facilitate the fundamental understanding of mechanical properties of organic crystals important to pharmaceutical operations, such as tableting and milling. Slip/cleavage planes were frequently assigned based on attachment energy calculation. These crystallographic planes can a...

journal_title：Journal of pharmaceutical sciences

authors： Sun CC,Kiang YH

更新日期：2008-08-01 00:00:00

abstract：:An F(ab')2 fragment of an IgG has been spray-dried on a bench-top machine to examine the presence of insoluble particulates in the redissolved powder product. Preliminary experiments showed that treatment of the F(ab')2 in aqueous solution in a water bath at 65°C for 1 h produced fragmentation and also insoluble parti...

journal_title：Journal of pharmaceutical sciences

authors： Lassner P,Adler M,Lee G

更新日期：2014-04-01 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：:Simultaneously Manufactured Nano-In-Micro (SIMANIM) particles for the pulmonary delivery of antibodies have been prepared by the spray-drying of a double-emulsion containing human IgG (as a model antibody), lactose, poly(lactide-co-glycolide) (PLGA) and dipalmitoylphosphatidylcholine (DPPC). The one-step drying proces...

journal_title：Journal of pharmaceutical sciences

authors： Kaye RS,Purewal TS,Alpar HO

更新日期：2009-11-01 00:00:00

abstract：:Quercetin had been shown to be effective in the management of arthritis. However, bioavailability of quercetin is a concern for such treatment. This work aims at the development of intra-articular drug delivery system by controlled release of quercetin (loaded in microspheres) for the management of rheumatoid arthriti...

journal_title：Journal of pharmaceutical sciences

authors： Natarajan V,Krithica N,Madhan B,Sehgal PK

更新日期：2011-01-01 00:00:00

abstract：:Corneal penetration studies were conducted in unanesthetized albino rabbits using various organic compounds representing both polar and nonpolar species. Very low molecular weight compounds demonstrate rapid uptake into the aqueous humor despite the lipid-like barrier imposed by the corneal epithelium. Evidence that t...

journal_title：Journal of pharmaceutical sciences

authors： Grass GM,Robinson JR

更新日期：1988-01-01 00:00:00

abstract：:The sensitivity of pharmacokinetic deconvolution algorithms with respect to simulated experimental error has been studied. Approximations of cumulative absorption profiles reconstructed from simulated data sets with normally distributed random error were compared with corresponding known input functions. The coinciden...

journal_title：Journal of pharmaceutical sciences

authors： Süverkrüp R,Bonnacker I,Raubach HJ

更新日期：1989-11-01 00:00:00

abstract：:Abbott-232 is a chemically stable, highly water soluble non-hygroscopic compound selected for development as a potent uroselective alpha(1A) agonist. An anhydrate, a monohydrate, and an amorphous phase were isolated. The anhydrate was chosen for formulation development based on solid-state characterization. Excipients...

journal_title：Journal of pharmaceutical sciences

authors： Wardrop J,Law D,Qiu Y,Engh K,Faitsch L,Ling C

更新日期：2006-11-01 00:00:00

abstract：:During the manufacturing process of biopharmaceuticals, peristaltic pumps are employed at different stages for transferring and dosing of the final product. Commonly used silicone tubings are known for particle shedding from the inner tubing surface due to friction in the pump head. These nanometer sized silicone rubb...

journal_title：Journal of pharmaceutical sciences

authors： Deiringer N,Haase C,Wieland K,Zahler S,Haisch C,Friess W

更新日期：2020-12-09 00:00:00

abstract：:A theory of charge, fluid-mass, and solute (including macromolecular) transport through porous media is applied to describe transport phenomena across the external layer of mammalian skin. Linear relationships are derived between transport fluxes and applied fields. These relationships introduce six effective transder...

journal_title：Journal of pharmaceutical sciences

authors： Edwards DA,Langer R

更新日期：1994-09-01 00:00:00

abstract：:Acitretin, a retinoid for the treatment of severe psoriasis, exhibits extremely low aqueous solubility and high photosensitivity. This study investigated the effects of the complexation of acitretin with the respective hydroxypropyl-beta-cyclodextrin (HPBCD) and randomly substituted methyl-beta-cyclodextrin (RMBCD) on...

journal_title：Journal of pharmaceutical sciences

authors： Liu X,Lin HS,Thenmozhiyal JC,Chan SY,Ho PC

更新日期：2003-12-01 00:00:00

abstract：:The plasma concentrations and urinary excretions of bisoprolol enantiomers in four Japanese male healthy volunteers after a single oral administration of 20 mg of racemic bisoprolol were evaluated. The AUC(infinity) and elimination half-life of (S)-(-)-bisoprolol were slightly larger than those of (R)-(+)-bisoprolol i...

journal_title：Journal of pharmaceutical sciences

authors： Horikiri Y,Suzuki T,Mizobe M

更新日期：1998-03-01 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：:This work reports the measurement of the partition rate of a model drug, ibuprofen (IBU), from aqueous solutions into octanol in the absence and presence of common pharmaceutical excipients including glucose, lactose, maltoheptaose, hydroxypropyl methylcellulose, polyvinylpyrrolidone, polyvinylpyrrolidone-vinyl acetat...

journal_title：Journal of pharmaceutical sciences

authors： Xu H,Wang W,Shi Y,Gao P

更新日期：2019-01-01 00:00:00

abstract：:Maintaining good content uniformity (CU) is a significant challenge for low-dose oral tablets in particular when using direct compression (DC). Using 6 model active pharmaceutical ingredients, we show that a platform DC tablet formulation suitable for developing low-dose API with excellent CU can be developed. This pl...

journal_title：Journal of pharmaceutical sciences

authors： Sun WJ,Aburub A,Sun CC

更新日期：2017-07-01 00:00:00

abstract：:The use of various synthetic lipids and polymers to deliver DNA for gene therapy applications has been the subject of intense examination for the last 15 years. Our understanding of the processes involved in the delivery of DNA, although still limited, can be described in terms of specific physical and chemical barrie...

journal_title：Journal of pharmaceutical sciences

authors： Wiethoff CM,Middaugh CR

更新日期：2003-02-01 00:00:00