The relationship between rat intestinal permeability and hydrophilic probe size.

abstract：PURPOSE:Chitosan and its derivatives possess several unique properties relevant in the field of pharmaceutics and medicinal chemistry. This study aimed to evaluate the pharmaceutical performance of an innovative chitosan derivative, methyl acrylate chitosan bearing p-nitrobenzaldehyde (MA*CS*pNBA) Schiff base. METHODS...

journal_title：Pharmaceutical research

authors： Ali SS,Kenawy ER,Sonbol FI,Sun J,Al-Etewy M,Ali A,Huizi L,El-Zawawy NA

更新日期：2018-11-07 00:00:00

abstract：:Various diesters of 9-[(1,3-dihydroxy-2-propoxy)-methyl]guanine (DHPG) were screened in order to identify a derivative with improved oral absorption. The solubilities and dissolution rates decreased with increasing chain length and branching of the ester group. However, the dipropionate ester showed an anomalously fas...

journal_title：Pharmaceutical research

authors： Benjamin EJ,Firestone BA,Bergstrom R,Fass M,Massey I,Tsina I,Lin YY

更新日期：1987-04-01 00:00:00

abstract：PURPOSE:To elucidate the catalytic mechanism of the esterase-like activity of serum albumin (SA), the reactivity of SA from six species was investigated using p-nitrophenyl esters as model substrates. METHODS:The effect of pH and the energetic and thermodynamic profiles of SA were determined for all species for p-nitr...

journal_title：Pharmaceutical research

authors： Sakurai Y,Ma SF,Watanabe H,Yamaotsu N,Hirono S,Kurono Y,Kragh-Hansen U,Otagiri M

更新日期：2004-02-01 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:One of the drawbacks of polycationic and cationic liposomal gene transfer is its sensitivity to serum. Gene therapy requires the transfectant-DNA complex to be resistant to serum as well as blood. Since Ca2+ has proved to be an efficient cofactor of polycationic gene transfer, we decided to investigate its effe...

journal_title：Pharmaceutical research

authors： Haberland A,Knaus T,Zaitsev SV,Buchberger B,Lun A,Haller H,Böttger M

更新日期：2000-02-01 00:00:00

abstract：PURPOSE:TXA9, a novel cardiac glycoside, has a potent anti-proliferative effect against A549 human lung cancer cells, however, possesses a poor water-solubility and a rapid metabolic rate in vivo which limited the further development of TXA9. To overcome the shortcomings of TXA9, four polymer prodrugs of TXA9 were desi...

journal_title：Pharmaceutical research

authors： Li Y,Ye C,Cai C,Zhao M,Han N,Liu Z,Zhai J,Yin J

更新日期：2020-03-12 00:00:00

abstract：:The interaction of dicumarol and phenothiazine neuroleptics binding to alpha 1-acid glycoprotein (AGP) was investigated by circular dichroism (CD) and equilibrium dialysis. The induced CD spectra of the dicumarol-AGP complex were affected differently by the different substituents of the phenothiazine molecule. The sig...

journal_title：Pharmaceutical research

authors： Miyoshi T,Yamamichi R,Maruyama T,Otagiri M

更新日期：1992-07-01 00:00:00

abstract：PURPOSE:To engineer optimized near-infrared (NIR) active thermosensitive liposomes to potentially achieve image-guided delivery of chemotherapeutic agents. METHODS:Thermosensitive liposomes were surface-coated with either polyethylene glycol or dextran. Differential scanning calorimetry and calcein release studies wer...

journal_title：Pharmaceutical research

authors： Turner DC,Moshkelani D,Shemesh CS,Luc D,Zhang H

更新日期：2012-08-01 00:00:00

abstract：:Under the heading "Methods-Synthesis of the Bioreducible Modified-PAE (mPAE)", on page 3, line 14-17, there is an error. The quantity unit of PAE and 2-iminothiolane hydrochloride needs to be corrected to mg instead of g. ...

journal_title：Pharmaceutical research

authors： Gandhi NS,Godeshala S,Koomoa-Lange DT,Miryala B,Rege K,Chougule MB

更新日期：2018-09-05 00:00:00

abstract：PURPOSE:The purpose of the study is to characterize glycine crystallization during freezing of aqueous solutions as a function of the glycine salt form (i.e., neutral glycine, glycine hydrochloride, and sodium glycinate), pH, and ionic strength. METHODS:Crystallization was studied by thermal analysis, microscopy, x-ra...

journal_title：Pharmaceutical research

authors： Akers MJ,Milton N,Byrn SR,Nail SL

更新日期：1995-10-01 00:00:00

abstract：PURPOSE:To develop a semi-physiological-based model describing simultaneously the time course of immature and mature B-lymphocytes after topotecan (TPT) administration to tumor-bearing rats. METHODS:Twenty-four tumor-bearing BDIX male rats received a single 6 mg/kg intra-peritoneal dose of TPT or saline. Mature and im...

journal_title：Pharmaceutical research

authors： Vélez de Mendizábal N,Martínez-Forero I,Garrido MJ,Bandrés E,García-Foncillas J,Segura C,Trocóniz IF

更新日期：2010-03-01 00:00:00

abstract：:Nasal sprays containing different concentrations of the somatostatin analogue octreotide and sodium tauro-24,25-dihydrofusidate (STDHF) as an absorption promoter were evaluated in two consecutive pharmacokinetic studies in healthy volunteers to characterize their bioavailability and local tolerability. The concentrati...

journal_title：Pharmaceutical research

authors： Kissel T,Drewe J,Bantle S,Rummelt A,Beglinger C

更新日期：1992-01-01 00:00:00

abstract：PURPOSE:The use of "Trojan Horse" nanocarriers for antibiotics to enhance the activity of antibiotics against susceptible and resistant bacteria is investigated. METHODS:Antibiotic carriers (CD-MAN and CD-GLU) are prepared from β-cyclodextrin grafted with sugar molecules (D-mannose and D-glucose, respectively) via azi...

journal_title：Pharmaceutical research

authors： Li M,Neoh KG,Xu L,Yuan L,Leong DT,Kang ET,Chua KL,Hsu LY

更新日期：2016-05-01 00:00:00

abstract：PURPOSE:To investigate influence of ion induced mesophasic transformation on pharmaceutical performance of in situ gelling system consisting of glyceryl monooleate. METHODS:The prepared system showed mesophasic transformation during its conversion from sol to gel upon controlled hydration. The process of mesophasic tr...

journal_title：Pharmaceutical research

authors： Patil SS,Venugopal E,Bhat S,Mahadik KR,Paradkar AR

更新日期：2013-07-01 00:00:00

abstract：PURPOSE:The heats of reaction between the enantiomers and racemates of ibuprofen and naproxen and human serum albumin (HSA) are to be measured with and without the addition of octanoic acid. The effects of octanoic acid on the free energies of interaction between the drugs and HSA is to be determined and compared to th...

journal_title：Pharmaceutical research

authors： Cheruvallath VK,Riley CM,Narayanan SR,Lindenbaum S,Perrin JH

更新日期：1996-01-01 00:00:00

abstract：PURPOSE:The purpose of this work was to investigate the mechanisms of cocrystal formation during cogrinding and storage of solid reactants, and to establish the effects of water by cogrinding with hydrated form of reactants and varying RH conditions during storage. METHODS:The hydrogen bonded 1:1 carbamazepine-sacchar...

journal_title：Pharmaceutical research

authors： Jayasankar A,Somwangthanaroj A,Shao ZJ,Rodríguez-Hornedo N

更新日期：2006-10-01 00:00:00

abstract：PURPOSE:Comparison of the dissociation kinetics of rapid-acting insulins lispro, aspart, glulisine and human insulin under physiologically relevant conditions. METHODS:Dissociation kinetics after dilution were monitored directly in terms of the average molecular mass using combined static and dynamic light scattering....

journal_title：Pharmaceutical research

authors： Gast K,Schüler A,Wolff M,Thalhammer A,Berchtold H,Nagel N,Lenherr G,Hauck G,Seckler R

更新日期：2017-11-01 00:00:00

abstract：:The bioavailability of a new sustained-release potassium chloride (KCl) tablet, designed for once-a-day dosing, was compared to a KCl elixir using urinary excretion data. The study utilized 25 male volunteers dosed in a crossover design in a dietary/activity-controlled environment. The regimens consisted of a total of...

journal_title：Pharmaceutical research

authors： Betlach CJ,Arnold JD,Frost RW,Leese PT,Gonzalez MA

更新日期：1987-10-01 00:00:00

abstract：:The mechanical properties of dry and wet polymeric films prepared from various aqueous polymeric dispersions were evaluated by a puncture test. They were studied with respect to type of polymer dispersion [cellulosic: Aquacoat and Surelease; acrylic: Eudragit NE, L, RS, and RL 30 D], plasticizer type (water-soluble or...

journal_title：Pharmaceutical research

authors： Bodmeier R,Paeratakul O

更新日期：1994-06-01 00:00:00

abstract：PURPOSE:To examine whether the glass transition temperature (Tg) of freeze-dried formulations containing polymer excipients can be accurately predicted by molecular dynamics simulation using software currently available on the market. Molecular dynamics simulations were carried out for isomaltodecaose, a fragment of de...

journal_title：Pharmaceutical research

authors： Yoshioka S,Aso Y,Kojima S

更新日期：2003-06-01 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:With the aim of developing multivalent vaccines for single-injection, we examined the feasibility of combining antigens in biodegradable microspheres. Such vaccines are expected to improve vaccination coverage by reducing the number of vaccination sessions required to generate immunity. METHODS:Mono- and multi...

journal_title：Pharmaceutical research

authors： Boehm G,Peyre M,Sesardic D,Huskisson RJ,Mawas F,Douglas A,Xing D,Merkle HP,Gander B,Johansen P

更新日期：2002-09-01 00:00:00

abstract：:One of the barriers to transdermal delivery of peptides is the metabolic activity of the epidermis. To define this metabolic activity, aminopeptidase activity and Leu-enkephalin metabolism were measured in the epidermis obtained from neonatal mouse skin and in cultured mouse keratinocytes. Aminopeptidase activity was ...

journal_title：Pharmaceutical research

authors： Shah PK,Borchardt RT

更新日期：1991-01-01 00:00:00

abstract：:A method to provide near-constant sustained release of high molecular weight, water-soluble proteins from polyanhydride microspheres is described. The polyanhydrides used were poly(fatty acid dimer) (PFAD), poly(sebacic acid) (PSA), and their copolymers [P(FAD-SA)]. P(FAD-SA) microspheres containing proteins of differ...

journal_title：Pharmaceutical research

authors： Tabata Y,Gutta S,Langer R

更新日期：1993-04-01 00:00:00

abstract：:Animal models are used commonly in various stages of drug discovery and development to aid in the prospective assessment of drug-drug interaction (DDI) potential and the understanding of the underlying mechanism for DDI of a drug candidate. In vivo assessments in an appropriate animal model can be very valuable, when ...

journal_title：Pharmaceutical research

authors： Tang C,Prueksaritanont T

更新日期：2010-09-01 00:00:00

abstract：PURPOSE:Typical methods to study pMDI sprays employ particle sizing or visible light diagnostics, which suffer in regions of high spray density. X-ray techniques can be applied to pharmaceutical sprays to obtain information unattainable by conventional particle sizing and light-based techniques. METHODS:We present a t...

journal_title：Pharmaceutical research

authors： Mason-Smith N,Duke DJ,Kastengren AL,Stewart PJ,Traini D,Young PM,Chen Y,Lewis DA,Soria J,Edgington-Mitchell D,Honnery D

更新日期：2016-05-01 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:A thermodynamic analysis of the binding to rat cortex adenosine A1 receptor of N6-substituted (full agonists) and N6-substituted-deoxyribose (partial agonists) adenosine derivatives was performed. The intrinsic activity of the compounds was evaluated by measurements of the inhibition of forskolin stimulated 3',...

journal_title：Pharmaceutical research

authors： Dalpiaz A,Scatturin A,Pavan B,Varani K,IJzerman AP,Andrea Borea P

更新日期：1999-07-01 00:00:00

abstract：PURPOSE:To develop a safe and effective non-viral vector for gene delivery and transfection in macrophages for potential anti-inflammatory therapy. METHODS:Solid nanoparticles-in-emulsion (NiE) multi-compartmental delivery system was designed using plasmid DNA-encapsulated type B gelatin nanoparticles suspended in the...

journal_title：Pharmaceutical research

authors： Attarwala H,Amiji M

更新日期：2012-06-01 00:00:00

abstract：:Effects of protease inhibitors and absorption enhancers on the absorption of salmon calcitonin (sCT) were evaluated after intratracheal coadministration to rats using the plasma Ca level as an index. Remarkable absorption enhancement could be attained with unsaturated fatty acids such as oleic acid and polyoxyethylene...

journal_title：Pharmaceutical research

authors： Kobayashi S,Kondo S,Juni K

更新日期：1994-09-01 00:00:00