In vitro and in vivo-release of nitroglycerin from a new transdermal therapeutic system.

abstract：:A sensitive activity assay for high volume evaluation of human renin inhibitory peptides (RIPs) in rat sera (range 2-80 ng/ml) was developed based on the low affinity of RIPs to rat renin and their high affinity to human renin. The utility of this activity assay was tested by measuring concentrations of a human RIP, U...

journal_title：Pharmaceutical research

authors： Ruwart MJ,Sharma SK,Harris DW,Lakings DB,Rush BD,Wilkinson KF,Cornette JC,Evans DB,Friis JM,Cook KJ

更新日期：1990-04-01 00:00:00

abstract：:Although much effort has been devoted to opioid research since the identification of enkephalins, understanding of the physiological importance and mechanisms of action of endogenous opioids lags behind understanding of opiate alkaloids such as morphine. In recent years, several novel approaches have been refined with...

journal_title：Pharmaceutical research

authors： Rapaka RS,Porreca F

更新日期：1991-01-01 00:00:00

abstract：:A novel method of dipeptide synthesis is described that can be carried out in aqueous solution and does not require complicated protecting and deprotecting procedures. An analgesic neuropeptide named kyotorphin, H-Tyr-Arg-OH, was synthesized from unprotected tyrosine and arginine in a new enzymatic reaction catalyzed ...

journal_title：Pharmaceutical research

authors： Kitabatake S,Tsurutani R,Nakajima H,Tomita K,Yoshihara Y,Ueda H,Takagi H,Imahori K

更新日期：1987-04-01 00:00:00

abstract：:We studied the effects of two verapamil analogs, anipamil and ronipamil, in traumatic shock. Noble-Collip drum trauma produced a shock state characterized by an eight-fold increase in plasma cathepsin D activity, a 13-fold increase in the rate of plasma myocardial depressant factor (MDF) accumulation, and a survival t...

journal_title：Pharmaceutical research

authors： Hock CE,Daitch JS,Lefer AM

更新日期：1985-05-01 00:00:00

abstract：PURPOSE:Cell penetrating peptides (CPPs) were widely used as motifs for drug delivery to tumor. In former study, an RGD reverse sequence dGR was used to develop active-targeting liposome R8dGR-Lip, which showed well penetrating ability and treatment efficiency on glioma model. However, recurrence after tumor resection ...

journal_title：Pharmaceutical research

authors： Qiu Y,Yu Q,Liu Y,Tang J,Wang X,Lu Z,Xu Z,He Q

更新日期：2018-04-26 00:00:00

abstract：:Cholinesterases are ubiquitous carboxylesterase type B enzymes capable of hydrolyzing the neurotransmitter acetylcholine which are transiently expressed in multiple germline, embryonic, and tumor cells. The acute poisoning effects of various organophosphorous compounds are generally attributed to their irreversible co...

journal_title：Pharmaceutical research

authors： Soreq H,Zakut H

更新日期：1990-01-01 00:00:00

abstract：PURPOSE:To evaluate different dissolution testing methods and subsequently develop a simple to perform but reproducible and discriminating dissolution technique for inhalative powders. METHODS:From a dry powder a fraction of aerosolized particles with an aerodynamic particle size below 5 μm was collected on regenerate...

journal_title：Pharmaceutical research

authors： May S,Jensen B,Wolkenhauer M,Schneider M,Lehr CM

更新日期：2012-08-01 00:00:00

abstract：:The dermal route is an attractive route for vaccine delivery due to the easy skin accessibility and a dense network of immune cells in the skin. The development of microneedles is crucial to take advantage of the skin immunization and simultaneously to overcome problems related to vaccination by conventional needles (...

journal_title：Pharmaceutical research

authors： Leone M,Mönkäre J,Bouwstra JA,Kersten G

更新日期：2017-11-01 00:00:00

abstract：PURPOSE:We examined the ability of a protein transduction domain (PTD), YARA, to penetrate in the skin and carry a conjugated peptide, P20. The results with YARA were compared to those of a well-known PTD (TAT) and a control, nontransducing peptide (YKAc). The combined action of PTDs and lipid penetration enhancers was...

journal_title：Pharmaceutical research

authors： Lopes LB,Brophy CM,Furnish E,Flynn CR,Sparks O,Komalavilas P,Joshi L,Panitch A,Bentley MV

更新日期：2005-05-01 00:00:00

abstract：PURPOSE:Polyethylenimine (PEI) is a highly effective gene delivery vector, but because it is an off-the shelf material, its properties may not be optimal. To investigate the effects of the protonation properties of the polymer, we generated PEI derivatives by acetylating varying fractions of the primary and secondary a...

journal_title：Pharmaceutical research

authors： Forrest ML,Meister GE,Koerber JT,Pack DW

更新日期：2004-02-01 00:00:00

abstract：PURPOSE:To provide a systematic biophysical approach towards a better understanding of impact of conjugation chemistry on higher order structure and physical stability of an antibody drug conjugate (ADC). METHODS:ADC was prepared using thiol-maleimide chemistry. Physical stabilities of ADC and its parent IgG1 mAb were...

journal_title：Pharmaceutical research

authors： Guo J,Kumar S,Prashad A,Starkey J,Singh SK

更新日期：2014-07-01 00:00:00

abstract：:A biopharmaceutics drug classification scheme for correlating in vitro drug product dissolution and in vivo bioavailability is proposed based on recognizing that drug dissolution and gastrointestinal permeability are the fundamental parameters controlling rate and extent of drug absorption. This analysis uses a transp...

journal_title：Pharmaceutical research

authors： Amidon GL,Lennernäs H,Shah VP,Crison JR

更新日期：1995-03-01 00:00:00

abstract：PURPOSE:The objective of the current study was to investigate whether blood-brain barrier (BBB) permeability studies in vitro could be accelerated by running several compounds together in the same experiment. METHODS:To address this question, we compared the transport of six compounds run separately with the results o...

journal_title：Pharmaceutical research

authors： Berezowski V,Landry C,Lundquist S,Dehouck L,Cecchelli R,Dehouck MP,Fenart L

更新日期：2004-05-01 00:00:00

abstract：PURPOSE:The type and relative importance of saturated and unsaturated phospholipid components of surfactant within the epithelial lining fluid (ELF) of the inner and outer surfaces of the lung is not known. METHODS:Seven healthy dogs were anesthetized and a bronchoalveolar lavage (BAL) was performed, immediately follo...

journal_title：Pharmaceutical research

authors： Mills PC,Chen Y,Hills YC,Hills BA

更新日期：2005-11-01 00:00:00

abstract：PURPOSE:The purpose of this study was to establish a useful methodology, possibly providing information on the stoichiometry of pharmaceutical drug salts obtained from salt screening by using a multiwell plate and a Raman microscope. METHODS:Tamoxifen salt screening was conducted with monobasic and polybasic acids on ...

journal_title：Pharmaceutical research

authors： Kojima T,Onoue S,Murase N,Katoh F,Mano T,Matsuda Y

更新日期：2006-04-01 00:00:00

abstract：PURPOSE:The aim was to investigate anticancer drug-loaded poly(carbonate-ester) nanospheres as potential drug delivery systems for cancer therapy. METHODS:Functional poly(carbonate-ester) copolymers (HPCP-SD) were synthesized by the incorporation of sulfadiazine as the tumor-targeting groups to hydroxyl groups of poly...

journal_title：Pharmaceutical research

authors： Yan GP,Zong RF,Li L,Fu T,Liu F,Yu XH

更新日期：2010-12-01 00:00:00

abstract：PURPOSE:To investigate the mechanisms involved in transport of sulfasalazine in Caco-2 cells. METHODS:Permeability coefficients of sulfasalazine and its analogs across Caco-2 cell monolayers were measured as a function of direction of transport, energy and concentration dependence, and in the presence of inhibitors of...

journal_title：Pharmaceutical research

authors： Liang E,Proudfoot J,Yazdanian M

更新日期：2000-10-01 00:00:00

abstract：PURPOSE:A double-mutant E224A/E262A full-length botulinum neurotoxin (BoNT) Type A with structural similarity to native BoNT/A but lacking the endopeptidase activity provides an ideal surrogate for testing pharmacokinetics and immunochemical characteristics of BoNT. METHODS:We determined lethality (LD50) of deactivate...

journal_title：Pharmaceutical research

authors： Ravichandran E,Janardhanan P,Patel K,Riding S,Cai S,Singh BR

更新日期：2016-03-01 00:00:00

abstract：PURPOSE:Modulation of 5-HT3 receptor in the central nervous system (CNS) is a promising approach for treatment of neuropathic pain. The goal was to evaluate the role of P-glycoprotein (Pgp) in limiting exposure of different parts of the CNS to ondansetron (5-HT3 receptor antagonist) using wild-type and genetic knockout...

journal_title：Pharmaceutical research

authors： Chiang M,Back HM,Lee JB,Oh S,Guo T,Girgis S,Park C,Haroutounian S,Kagan L

更新日期：2020-09-28 00:00:00

abstract：:The binding of 1-anilino-8-naphthalenesulfonate (ANS) to bovine serum albumin (BSA), human serum albumin (HSA), and human plasma has been studied by potentiometric titration utilizing a laboratory constructed ion selective electrode (ISE) of ANS. Three classes of ANS binding sites were found on BSA, HSA, and plasma at...

journal_title：Pharmaceutical research

authors： Valsami GN,Macheras PE,Koupparis MA

更新日期：1991-07-01 00:00:00

abstract：PURPOSE:Type I collagen accumulates during liver fibrosis primarily because α-complex protein-2 (αCP(2)), encoded by the poly(rC) binding protein 2 (PCBP2) gene, binds to the 3' end of the collagen mRNA and increases its half-life. This study aimed to reverse the pro-fibrogenic effect of alcohol on hepatic stellate cel...

journal_title：Pharmaceutical research

authors： Shukla RS,Qin B,Wan YJ,Cheng K

更新日期：2011-12-01 00:00:00

abstract：PURPOSE:To assess the effects of co-delivering osteoinductive DNA and/or small interfering RNA in directing the osteogenic differentiation of human adipose-derived stem cells (hADSCs) using a combinatorial, non-viral gene delivery approach. METHODS:hADSCs were transfected using combinations of the following genes: BMP...

journal_title：Pharmaceutical research

authors： Ramasubramanian A,Shiigi S,Lee GK,Yang F

更新日期：2011-06-01 00:00:00

abstract：PURPOSE:The fate of inhaled salmon calcitonin (sCT) at the respiratory epithelial barrier was studied with particular emphasis on enzymatic degradation by trypsin, chymotrypsin, and neutrophil elastase. METHODS:Degradation of sCT was assessed by HPLC in cell homogenate, supernatant and intact monolayers of human respi...

journal_title：Pharmaceutical research

authors： Baginski L,Tewes F,Buckley ST,Healy AM,Bakowsky U,Ehrhardt C

更新日期：2012-01-01 00:00:00

abstract：:Significant efforts are made to characterize molecular liabilities and degradation of the drug substance (DS) and drug product (DP) during various product life-cycle stages. The in vivo fate of a therapeutic protein is usually only considered in terms of pharmacokinetics (PKs) and pharmacodynamics (PDs). However, the ...

journal_title：Pharmaceutical research

authors： Schuster J,Koulov A,Mahler HC,Detampel P,Huwyler J,Singh S,Mathaes R

更新日期：2020-01-03 00:00:00

abstract：PURPOSE:Paclitaxel is active and widely used to treat multiple types of solid tumors. The commercially available paclitaxel formulation uses Cremophor/ethanol (C/E) as the solubilizers. Other formulations including nanoparticles have been introduced. This study evaluated the effects of nanoparticle formulation of pacli...

journal_title：Pharmaceutical research

authors： Yeh TK,Lu Z,Wientjes MG,Au JL

更新日期：2005-06-01 00:00:00

abstract：PURPOSE:To compare the adjuvanticity of polymeric particles (new-generation adjuvant) and alum (the traditional and FDA-approved adjuvant) for H5N1 influenza split vaccine, and to investigate respective action mode. METHODS:Vaccine formulations were prepared by incubating lyophilized poly(lactic acid) (PLA) microparti...

journal_title：Pharmaceutical research

authors： Zhang W,Wang L,Liu Y,Chen X,Li J,Yang T,An W,Ma X,Pan R,Ma G

更新日期：2014-04-01 00:00:00

abstract：PURPOSE:Cisplatin, is recognized as a first line therapeutic for the treatment of non-small cell lung cancer (NSCLC). Cisplatin resistance is identified as the most detrimental complication during treatment and has been associated with upregulation of several genes, such as the anti-apoptotic gene survivin. In this stu...

journal_title：Pharmaceutical research

authors： Mattheolabakis G,Ling D,Ahmad G,Amiji M

更新日期：2016-12-01 00:00:00

abstract：:The dose dependency of carbamazepine pharmacokinetics was characterized in rats, a common test animal for antiepileptic drug efficacy. With a randomized Latin square schedule, 5, 10, and 20 mg/kg doses of carbamazepine were injected intravenously into six Sprague-Dawley rats followed by the administration of a 5 or 10...

journal_title：Pharmaceutical research

authors： Remmel RP,Sinz MW,Cloyd JC

更新日期：1990-05-01 00:00:00

abstract：PURPOSE:This work investigated the effect of relative humidity (RH) on bipolar electrostatic charge profiles of dry powder inhaler aerosols using the Bipolar Charge Analyzer (BOLAR). METHODS:Two commercial products, Pulmicort® (400 μg, budesonide) and Bricanyl® (500 μg, terbutaline sulfate) Turbuhaler®, were used as m...

journal_title：Pharmaceutical research

authors： Yu J,Wong J,Ukkonen A,Kannosto J,Chan HK

更新日期：2017-08-01 00:00:00

abstract：PURPOSE:We evaluated the effect of luminal bacterial metabolism on intestinal absorption of azetirelin in rats. In vitro characteristics of bacterial metabolism of azetirelin were also investigated with the goal of overcoming the low stability of the peptidic drug against luminal microorganisms. METHODS:Plasma azetire...

journal_title：Pharmaceutical research

authors： Sasaki I,Tamura T,Shibakawa T,Fujita T,Murakami M,Yamamoto A,Muranishi S

更新日期：1997-08-01 00:00:00