abstract：:Many pathophysiological circumstances vary during 24 h periods. Many physiologic processes undergo biological rhythms, including the sleep-wake rhythm and metabolism. Disruptive effect in the 24 h variations can manifest as the emergence or exacerbation of pathological conditions. So, chronotherapeutics is gaining inc...

journal_title：Journal of pharmaceutical sciences

authors： Ohdo S,Koyanagi S,Matsunaga N,Hamdan A

更新日期：2011-09-01 00:00:00

abstract：:Bisphosphonates are widely used for the treatment of bone diseases, including hypercalcemia and osteoporosis. However, the bioavailability (BA) of orally administered bisphosphonates is low, at approximately 0.9%-1.8%. In addition, the oral administration of bisphosphonates is associated with mucosal damage, including...

journal_title：Journal of pharmaceutical sciences

authors： Katsumi H,Takashima M,Sano J,Nishiyama K,Kitamura N,Sakane T,Hibi T,Yamamoto A

更新日期：2011-09-01 00:00:00

abstract：:The present work shows that the heated carbamazepine (CBZ) powder form III can be described as purely triclinic form I or a mixture of triclinic form I and monoclinic form III, depending on the resolution of the X-ray diffraction equipment used. Visual identification of the minor phase is possible when high-resolution...

journal_title：Journal of pharmaceutical sciences

authors： Antonio SG,Benini FR,Ferreira FF,Rosa PC,Paiva-santos Cde O

更新日期：2011-07-01 00:00:00

abstract：:This study is to enhance the dissolution rate of a poorly water-soluble drug, quercetin, by fabricating nanocrystals using high-pressure homogenization. The particle size, crystallinity, dissolution, and antioxidant effects of fabricated quercetin nanocrystals have been investigated. Characterization of the original q...

journal_title：Journal of pharmaceutical sciences

authors： Sahoo NG,Kakran M,Shaal LA,Li L,Müller RH,Pal M,Tan LP

更新日期：2011-06-01 00:00:00

abstract：:The purpose of this study was to investigate the phase-sensitive delivery systems (D,L-polylactide in triacetin) for controlled delivery of insulin at basal level. The effect of varying concentration of zinc, polymer, and insulin on the in vitro release of insulin was evaluated. Stability of released insulin was inves...

journal_title：Journal of pharmaceutical sciences

authors： Al-Tahami K,Oak M,Singh J

更新日期：2011-06-01 00:00:00

abstract：:Poor dissolution performance is one of the challenges encountered in dosage form design of amorphous solid dispersions (ASDs). This study was aimed to investigate the effect of solid-liquid interactions of an encapsulated ASD on drug release. Drug release profiles of a molecularly interacting amorphous celecoxib solid...

journal_title：Journal of pharmaceutical sciences

authors： Puri V,Dantuluri AK,Bansal AK

更新日期：2011-06-01 00:00:00

abstract：:The absorption-enhancing effects of polyamidoamine (PAMAM) dendrimers with various generations (G0-G3) and concentrations [0.1%-1.0% (w/v)] on the pulmonary absorption of peptide and protein drugs were studied in rats. Insulin and calcitonin were chosen as models of peptide and protein drugs, and their pulmonary absor...

journal_title：Journal of pharmaceutical sciences

authors： Dong Z,Hamid KA,Gao Y,Lin Y,Katsumi H,Sakane T,Yamamoto A

更新日期：2011-05-01 00:00:00

abstract：:The antifungal activity of amphotericin B (AmB) incorporated in three cholesteryl carbonate esters (CCEs), sodium cholesteryl carbonate, cholesteryl palmityl carbonate, and dicholesteryl carbonate, was examined to assess their potential for use in a dry powder aerosol. Formulations containing dissolved AmB were stable...

journal_title：Journal of pharmaceutical sciences

authors： Chuealee R,Wiedmann TS,Srichana T

更新日期：2011-05-01 00:00:00

abstract：:Literature data relevant to the decision to allow a waiver of in vivo bioequivalence (BE) testing for the approval of immediate release (IR) solid oral dosage forms containing metronidazole are reviewed. Metronidazole can be assigned to Biopharmaceutics Classification System Class I. Most BE studies that were identifi...

journal_title：Journal of pharmaceutical sciences

authors： Rediguieri CF,Porta V,G Nunes DS,Nunes TM,Junginger HE,Kopp S,Midha KK,Shah VP,Stavchansky S,Dressman JB,Barends DM

更新日期：2011-05-01 00:00:00

abstract：:Oil-frozen water-in-oil-in-water (W₁/O/W₂) double emulsions (DE) containing ethanol up to 40% (w/v) in the external aqueous W₂ phase exhibited external coalescence upon thawing of the oil phase, releasing up to 85% of the encapsulated protein of the internal aqueous phase. These emulsions were studied in vitro as pote...

journal_title：Journal of pharmaceutical sciences

authors： Jaimes-Lizcano YA,Lawson LB,Papadopoulos KD

更新日期：2011-04-01 00:00:00

abstract：:The purpose of this study was to investigate corneal mucoadhesion, pharmacokinetics in lacrimal fluid and aqueous humor, the immune suppression induced by corneal transplantation of mycophenolate mofetil (MMF) nanosuspensions (NS), and the use of a chitosan-modified MMF nanosuspension (C-NS) as an ophthalmic delivery ...

journal_title：Journal of pharmaceutical sciences

authors： Wu XG,Xin M,Yang LN,Shi WY

更新日期：2011-04-01 00:00:00

abstract：:In 2005, the World Health Organization (WHO) proposed that provided an active pharmaceutical ingredient could meet certain criteria, bioequivalence could be evaluated with a set of laboratory tests, obviating the need for expensive and time-consuming pharmacokinetic studies in humans. The aim of this work was to deter...

journal_title：Journal of pharmaceutical sciences

authors： Strauch S,Jantratid E,Stahl M,Rägo L,Dressman JB

更新日期：2011-03-01 00:00:00

abstract：:Quality-by-design (QbD) is a systematic approach to drug development, which begins with predefined objectives, and uses science and risk management approaches to gain product and process understanding and ultimately process control. The concept of QbD can be extended to analytical methods. QbD mandates the definition ...

journal_title：Journal of pharmaceutical sciences

authors： Vogt FG,Kord AS

更新日期：2011-03-01 00:00:00

abstract：:Effects of the commercial drug zanamivir (Relenza) covalently attached to poly-l-glutamine on the infectivity of influenza A viruses are examined using the plaque reduction assay and binding affinity to viral neuraminidase (NA). These multivalent drug conjugates exhibit (i) up to a 20,000-fold improvement in anti-infl...

journal_title：Journal of pharmaceutical sciences

authors： Weight AK,Haldar J,Alvarez de Cienfuegos L,Gubareva LV,Tumpey TM,Chen J,Klibanov AM

更新日期：2011-03-01 00:00:00

abstract：:15-Lipoxygenase (15-LOX) is one of the key enzymes responsible for the formation of oxidized low-density lipoprotein, a major causal factor for atherosclerosis. Δ(9)-Tetrahydrocannabinol (Δ(9)-THC), a major component of marijuana, has suggested to suppress atherosclerosis. Although Δ(9)-THC seems to be attractive for ...

journal_title：Journal of pharmaceutical sciences

authors： Takeda S,Jiang R,Aramaki H,Imoto M,Toda A,Eyanagi R,Amamoto T,Yamamoto I,Watanabe K

更新日期：2011-03-01 00:00:00

abstract：:Flecainide acetate forms acetic acid solvates with 0.5 and 2 acetic acid molecules. Powder X-ray diffraction, differential thermal analysis/thermogravimetric, infrared, and potentiometric titration were used to determine the composition of solvates. Flecainide acetate hemisolvate with acetic acid decomposes to form a ...

journal_title：Journal of pharmaceutical sciences

authors： Veldre K,Actiņs A,Eglite Z

更新日期：2011-02-01 00:00:00

abstract：:Tumor necrosis factor-related apoptosis-inducing ligand (TRAIL) has received considerable attention as a potential anticancer agent. However, recombinant Apo2L/TRAIL has several limitations, which include a weak pharmacokinetic profile, namely, a short biological half-life and rapid renal clearance, and an inability t...

journal_title：Journal of pharmaceutical sciences

authors： Kim TH,Jiang HH,Youn YS,Park CW,Lim SM,Jin CH,Tak KK,Lee HS,Lee KC

更新日期：2011-02-01 00:00:00

abstract：:Apomorphine, a dopamine receptor agonist for treating Parkinson's disease, has very poor oral bioavailability (<2%) due to the first-pass effect. The aim of this work was to investigate whether the oral bioavailability and brain regional distribution of apomorphine could be improved by utilizing solid lipid nanopartic...

journal_title：Journal of pharmaceutical sciences

authors： Tsai MJ,Huang YB,Wu PC,Fu YS,Kao YR,Fang JY,Tsai YH

更新日期：2011-02-01 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：:In spite of the recent advances in technology to optimize the absorption, distribution, metabolism and elimination (ADME) properties of new and promising medicinal products to reduce clinical failures, the investigation of drug disposition in the pediatric and elderly populations continues to be under evaluated. With ...

journal_title：Journal of pharmaceutical sciences

authors： Chien JY,Ho RJ

更新日期：2011-01-01 00:00:00

abstract：:The aim of the present work was to prepare and characterize chitosan-stearic acid conjugate nanomicelles for encapsulation of amphotericin B (AmB) and to evaluate the in vitro nebulization of the formulations. Water soluble chitosan was grafted to stearic acid (SA) chains via 1-ethyl-3-(3-dimethylaminopropyl)carbodiim...

journal_title：Journal of pharmaceutical sciences

authors： Gilani K,Moazeni E,Ramezanli T,Amini M,Fazeli MR,Jamalifar H

更新日期：2011-01-01 00:00:00

abstract：:A revised classification system for oral drugs was developed using the biopharmaceutics classification system (BCS) as a starting point. The revised system is designed to have a greater focus on drug developability. Intestinal solubility, the compensatory nature of solubility and permeability in the small intestine an...

journal_title：Journal of pharmaceutical sciences

authors： Butler JM,Dressman JB

更新日期：2010-12-01 00:00:00

abstract：:A semi-automated protein binding assay using equilibrium dialysis (ED) and a novel mixed-matrix methodology has been developed. This method decreases mass spectrometer run time and reduces the likelihood of experimental artifacts. In this cassette-based approach, a single matrix is prepared following dialysis by mixin...

journal_title：Journal of pharmaceutical sciences

authors： Plise EG,Tran D,Salphati L

更新日期：2010-12-01 00:00:00

abstract：:The aim of this article was to prepare a topical powder for the treatment of fungal infections, such as Candida intertrigo and tinea pedis. Thus, an econazole nitrate (ECO) formulation with improved drug dissolution and proper moisture adsorption was designed. ECO was melt with the mesoporous silicate MCM-41 (drug/MCM...

journal_title：Journal of pharmaceutical sciences

authors： Ambrogi V,Perioli L,Pagano C,Marmottini F,Moretti M,Mizzi F,Rossi C

更新日期：2010-11-01 00:00:00

abstract：:This work investigated the impact of primary drying conditions on the microstructure and protein stability of bovine serum albumin (BSA) containing lyophilized cakes. Two primary drying conditions were employed (termed 'conservative', slower drying rate and 'aggressive', higher drying rate) at two protein loadings (5 ...

journal_title：Journal of pharmaceutical sciences

authors： Parker A,Rigby-Singleton S,Perkins M,Bates D,Le Roux D,Roberts CJ,Madden-Smith C,Lewis L,Teagarden DL,Johnson RE,Ahmed SS

更新日期：2010-11-01 00:00:00

abstract：:Our objective was to characterize, by DSC and XRD, the equilibrium thermal behavior of frozen aqueous solutions containing polyethylene glycol (PEG) and sucrose. Aqueous solutions of (i) PEG (2.5-50% w/w), (ii) sucrose (10% w/v) with different concentrations of PEG (1-20% w/v), and (iii) PEG (2% or 10% w/v) with diffe...

journal_title：Journal of pharmaceutical sciences

authors： Bhatnagar BS,Martin SM,Teagarden DL,Shalaev EY,Suryanarayanan R

更新日期：2010-11-01 00:00:00

abstract：:Local variations in compaction behaviour were investigated, for specimens of different shapes and thickness, comparing predictions from finite element (FE) modelling and results from a recently developed method using small-angle X-ray scattering (SAXS). Good agreement was generally obtained between these methods, in t...

journal_title：Journal of pharmaceutical sciences

authors： Laity PR,Han L,Elliott J,Cameron RE

更新日期：2010-10-01 00:00:00

abstract：:Dissolving microneedle patches offer promise as a simple, minimally invasive method of drug and vaccine delivery to the skin that avoids the need for hypodermic needles. However, it can be difficult to control the amount and localization of drug within microneedles. In this study, we developed novel microneedle design...

journal_title：Journal of pharmaceutical sciences

authors： Chu LY,Choi SO,Prausnitz MR

更新日期：2010-10-01 00:00:00

abstract：:The aim of this work is to determine if a stability testing protocol based on the correlations between crystallization onset and relaxation time above the glass transition temperature (T(g)) can be used to predict the crystallization onsets in amorphous pharmaceutical systems well below their T(g). This procedure assu...

journal_title：Journal of pharmaceutical sciences

authors： Caron V,Bhugra C,Pikal MJ

更新日期：2010-09-01 00:00:00

abstract：:Elucidation of the most stable form of an active pharmaceutical ingredient (API) is a critical step in the development process. Polymorph screening for an API with a complex polymorphic profile can present a significant challenge. The presented case illustrates an extensively polymorphic compound with an additional pr...

journal_title：Journal of pharmaceutical sciences

authors： Campeta AM,Chekal BP,Abramov YA,Meenan PA,Henson MJ,Shi B,Singer RA,Horspool KR

更新日期：2010-09-01 00:00:00

abstract：:A series of molecular complexes, both co-crystals and salts, of a triazole drug-alprazolam-with carboxylic acids, boric acid, boronic acids, and phenols have been analyzed with respect to heterosynthons present in the crystal structures. In all cases, the triazole ring behaves as an efficient hydrogen bond acceptor wi...

journal_title：Journal of pharmaceutical sciences

authors： Varughese S,Azim Y,Desiraju GR

更新日期：2010-09-01 00:00:00

abstract：:Multidrug resistance (MDR) mediated by the overexpression of the drug efflux protein P-glycoprotein is one of the major obstacles to successful cancer chemotherapy. The development of safe and effective MDR-reversing agents is an important approach to addressing this problem clinically. In this study, we evaluated the...

journal_title：Journal of pharmaceutical sciences

authors： Liu R,Zhang Y,Chen Y,Qi J,Ren S,Xushi MY,Yang C,Zhu H,Xiong D

更新日期：2010-07-01 00:00:00

abstract：:The aim of this work was to evaluate the low molecular weight chitosans (LMWCs) as enhancers of transdermal administration of baicalin, an useful drug for the treatment of atopic dermatitis, viral hepatitis, and HIV infection. Permeation experiments were performed in vitro through mouse skin by using Franz cells. Impr...

journal_title：Journal of pharmaceutical sciences

authors： Zhou X,Liu D,Liu H,Yang Q,Yao K,Wang X,Wang L,Yang X

更新日期：2010-07-01 00:00:00

abstract：:Controlled-release delivery of 6-beta-naltrexol (NTXOL), the major active metabolite of naltrexone, via a transdermal patch is desirable for treatment of alcoholism. Unfortunately, NTXOL does not diffuse across skin at a therapeutic rate. Therefore, the focus of this study was to evaluate microneedle (MN) skin permeat...

journal_title：Journal of pharmaceutical sciences

authors： Banks SL,Pinninti RR,Gill HS,Paudel KS,Crooks PA,Brogden NK,Prausnitz MR,Stinchcomb AL

更新日期：2010-07-01 00:00:00

abstract：:Time and resource constraints necessitate increasingly early decision making to accelerate or stop preclinical drug discovery programs. Early discovery drug candidates may be potent inhibitors of new targets, but all too often exhibit poor pharmaceutical and pharmacokinetic properties that limit the in vivo exposure. ...

journal_title：Journal of pharmaceutical sciences

authors： Chiang PC,South SA,Foster KA,Daniels JS,Wene SP,Albin LA,Thompson DC

更新日期：2010-07-01 00:00:00

abstract：:The effects of various types of substituted and nonsubstituted cyclodextrins (CDs) on the physical and colloidal stability of three different proteins were studied to further ascertain the mechanism by which cyclodextrins stabilize proteins. The three proteins examined in this study are the Clostridium difficile Toxoi...

journal_title：Journal of pharmaceutical sciences

authors： Samra HS,He F,Bhambhani A,Pipkin JD,Zimmerer R,Joshi SB,Middaugh CR

更新日期：2010-06-01 00:00:00

abstract：:Cisplatin (CDDP) is an effective anticancer agent for many solid tumors but has significant systemic toxicity limiting its use in many patients. We have designed a loco-regional delivery system to increase platinum levels in the lymphatics, where early metastasis is most likely to occur, while reducing systemic toxici...

journal_title：Journal of pharmaceutical sciences

authors： Cai S,Xie Y,Davies NM,Cohen MS,Forrest ML

更新日期：2010-06-01 00:00:00

abstract：:Delayed absorption of nifedipine when administered as a 20 mg immediate release soft gelatin capsule to fasted volunteers has been reported. Physiologically based pharmacokinetic (PBPK) modeling and in vitro dissolution data were used to explore our hypothesis that at high doses of nifedipine it precipitates in the st...

journal_title：Journal of pharmaceutical sciences

authors： Thelen K,Jantratid E,Dressman JB,Lippert J,Willmann S

更新日期：2010-06-01 00:00:00

abstract：:The role of particle size and surface modification on biodistribution of nanocarriers is widely reported. We report for the first time the role of nanoparticle shape on biodistribution. Our study demonstrates that irregular shaped polymer lipid nanoparticles (LIPOMER) evade kupffer cells and localize in the spleen. We...

journal_title：Journal of pharmaceutical sciences

authors： Devarajan PV,Jindal AB,Patil RR,Mulla F,Gaikwad RV,Samad A

更新日期：2010-06-01 00:00:00

abstract：:Many pharmaceuticals are formulated as powders to aid drug delivery. A major problem is how to produce powders having high purity, controlled morphology, and retained bioactivity. We demonstrate the use of supercritical carbon dioxide as an antisolvent for meeting this need for two model drug systems, quercetin, a spa...

journal_title：Journal of pharmaceutical sciences

authors： Jacobson GB,Shinde R,McCullough RL,Cheng NJ,Creasman A,Beyene A,Hickerson RP,Quan C,Turner C,Kaspar RL,Contag CH,Zare RN

更新日期：2010-06-01 00:00:00