abstract：:The present study describes the development of an orally disintegrating tablet containing a non-water-soluble drug delivery system. A model system was applied to evaluate the effect of different-sized particles on tablet characteristics. Cellets were incorporated into tablets prepared by freeze-drying from a 100 mg/mL...

journal_title：Journal of pharmaceutical sciences

authors： Stange U,Führling C,Gieseler H

更新日期：2013-06-01 00:00:00

abstract：:We have developed a hydrogel patch, which could promote antigen penetration through stratum corneum (SC), and have demonstrated its safety and efficacy in animals and humans. For the availability improvement of our system, it is important to develop a device, which enhances antigen penetration through SC more efficien...

journal_title：Journal of pharmaceutical sciences

authors： Matsuo K,Ishii Y,Kawai Y,Saiba Y,Quan YS,Kamiyama F,Hirobe S,Okada N,Nakagawa S

更新日期：2013-06-01 00:00:00

abstract：:New methods are being applied to distinguish silicone oil droplets from subvisible particles in therapeutic protein formulations. The need to standardize these methods and compare them to established methods is critical to increase the understanding of the risks from protein aggregation and other subvisible particulat...

journal_title：Journal of pharmaceutical sciences

authors： Vandesteeg N,Kilbert C

更新日期：2013-06-01 00:00:00

abstract：:In drug release systems using hydrogels as carriers, the presence of the polymer network will reduce the drug release rate, which can extend the release period. For a controlled-release process of drug, usually the ideal situation is to get a zero-order drug release rate. In this paper, the mathematical model of hydro...

journal_title：Journal of pharmaceutical sciences

authors： Xu Y,Jia Y,Wang Z,Wang Z

更新日期：2013-05-01 00:00:00

abstract：:Previously, we reported that repeated oral treatment with etoposide (ETP) increased ileal membrane localization of P-glycoprotein (P-gp) and that this was possibly mediated by increased expression of the ezrin/radixin/moesin (ERM)/phosphorylated ERM (p-ERM) via activation of RhoA/ROCK. These changes caused decreases i...

journal_title：Journal of pharmaceutical sciences

authors： Kobori T,Harada S,Nakamoto K,Tokuyama S

更新日期：2013-05-01 00:00:00

abstract：:The thiazide diuretic chlorothiazide is poorly metabolized, and is predominantly excreted via the kidneys. We have previously shown that chlorothiazide is transported by ATP-binding cassette transporter G2, suggesting a potential role for this transporter in apical efflux of chlorothiazide in the kidney. However, beca...

journal_title：Journal of pharmaceutical sciences

authors： Juhász V,Beéry E,Nagy Z,Bui A,Molnár E,Zolnerciks JK,Magnan R,Jani M,Krajcsi P

更新日期：2013-05-01 00:00:00

abstract：:In this study, we developed cationic microemulsions containing a protein transduction domain (penetratin) for optimizing paclitaxel localization within the skin. Microemulsions were prepared by mixing a surfactant blend (BRIJ:ethanol:propylene glycol 2:1:1, w/w/w) with monocaprylin (oil phase) at 1.3:1 ratio, and addi...

journal_title：Journal of pharmaceutical sciences

authors： Pepe D,McCall M,Zheng H,Lopes LB

更新日期：2013-05-01 00:00:00

abstract：:The nanosizing of poorly soluble drugs as a formulation strategy can eventually enhance their dissolution rate and bioavailability. Standard comminution techniques such as high-pressure homogenization (HPH) or wet bead milling have limitations in reaching the desired mean particle size. Combinative methods have been d...

journal_title：Journal of pharmaceutical sciences

authors： Salazar J,Müller RH,Möschwitzer JP

更新日期：2013-05-01 00:00:00

abstract：:Here, we report the structural characterization of several amorphous drugs made using the method of quenching molten droplets suspended in an acoustic levitator. (13) C NMR, X-ray, and neutron diffraction results are discussed for glassy cinnarizine, carbamazepine, miconazole nitrate, probucol, and clotrimazole. The (...

journal_title：Journal of pharmaceutical sciences

authors： Benmore CJ,Weber JK,Tailor AN,Cherry BR,Yarger JL,Mou Q,Weber W,Neuefeind J,Byrn SR

更新日期：2013-04-01 00:00:00

abstract：:This work investigated the feasibility of developing benznidazole (BZL) tablets, allowing fast, reproducible, and complete drug dissolution, by compressing BZL-Polyethylene Glycol (PEG) 6000 physical mixtures (PMs) and solid dispersions (SDs). SDs were prepared by the solvent evaporation method at different drug:polym...

journal_title：Journal of pharmaceutical sciences

authors： Leonardi D,Salomon CJ

更新日期：2013-03-01 00:00:00

abstract：:The aim of this study to administer hydrocortisone (HC) percutaneously in the form of polymeric nanoparticles (NPs) to alleviate its transcutaneous absorption, and to derive additional wound-healing benefits of chitosan. HC-loaded NPs had varied particle sizes, zeta potentials, and entrapment efficiencies, when drug-t...

journal_title：Journal of pharmaceutical sciences

authors： Hussain Z,Katas H,Amin MC,Kumulosasi E,Sahudin S

更新日期：2013-03-01 00:00:00

abstract：:Responses from the second Product Quality Research Institute (PQRI) Blend Uniformity Working Group (BUWG) survey of industry have been reanalyzed to identify potential links between formulation and processing variables and the measured uniformity of blends and unit dosage forms. As expected, the variability of the ble...

journal_title：Journal of pharmaceutical sciences

authors： Hancock BC,Garcia-Munoz S

更新日期：2013-03-01 00:00:00

abstract：:Avoiding unwanted immunogenicity is of key importance in the development of therapeutic drug proteins. Animal models are of less predictive value because most of the drug proteins are recognized as foreign proteins. However, different methods have been developed to obtain immunotolerant animal models. So far, the immu...

journal_title：Journal of pharmaceutical sciences

authors： Brenden N,Madeyski-Bengtson K,Martinsson K,Svärd R,Albery-Larsdotter S,Granath B,Lundgren H,Lövgren A

更新日期：2013-03-01 00:00:00

abstract：:AZ'0908 is a novel microsomal prostaglandin E synthase-1 inhibitor intended for oral administration. Pharmacokinetic experiments in rats showed that bioavailability was much lower than anticipated and increased following pretreatment with the nonspecific cytochrome P450 (CYP) inhibitor 1-aminobenzotriazole, presumably...

journal_title：Journal of pharmaceutical sciences

authors： Bylund J,Bueters T

更新日期：2013-03-01 00:00:00

abstract：:The solvent-free melt electrospinning (MES) method was developed to prepare a drug delivery system with fast release of carvedilol (CAR), a drug with poor water solubility. To the authors knowledge, this is the first report for preparing drug-loaded melt electrospun fibers. Cationic methacrylate copolymer of Eudragit®...

journal_title：Journal of pharmaceutical sciences

authors： Nagy ZK,Balogh A,Drávavölgyi G,Ferguson J,Pataki H,Vajna B,Marosi G

更新日期：2013-02-01 00:00:00

abstract：:Literature data pertaining to the decision to allow a waiver of in vivo bioequivalence testing for the approval of immediate-release (IR) solid oral dosage forms containing efavirenz as the only active pharmaceutical ingredient (API) are reviewed. Because of lack of conclusive data about efavirenz's permeability and i...

journal_title：Journal of pharmaceutical sciences

authors： Cristofoletti R,Nair A,Abrahamsson B,Groot DW,Kopp S,Langguth P,Polli JE,Shah VP,Dressman JB

更新日期：2013-02-01 00:00:00

abstract：:Biopharmaceutics Classification System and Biopharmaceutics Drug Distribution Classification System are complimentary, not competing, classification systems that aim to improve, simplify, and speed drug development. Although both systems are based on classifying drugs and new molecular entities into four categories us...

journal_title：Journal of pharmaceutical sciences

authors： Benet LZ

更新日期：2013-01-01 00:00:00

abstract：:The growing interest of pharmaceutical companies toward the crystal morphology prediction of active pharmaceutical ingredients is a consequence of the dramatic effect of the crystal habit on the tableting behavior of drugs. In order to help the optimization of the industrial process, molecular mechanics calculations t...

journal_title：Journal of pharmaceutical sciences

authors： Li Destri G,Marrazzo A,Rescifina A,Punzo F

更新日期：2013-01-01 00:00:00

abstract：:We report a semiquantitative method for determining trace amounts (<1%) of thermodynamically stable forms in polymorphic mixtures, focusing on sample preparation effects on solid phase transitions. Tegafur [5-fluoro-1-(oxolan-2-yl)-1,2,3,4-tetrahydropyrimidine-2,4-dione] was used as a model material in this study. The...

journal_title：Journal of pharmaceutical sciences

authors： Bobrovs R,Actiņš A

更新日期：2012-12-01 00:00:00

abstract：:The aim of our study was to characterize and optimize a self-nanoemulsifying drug delivery system (SNEDDS) formulation by a three-factor, three-level Box-Behnken design (BBD) combined with a desirability function. The independent factors were the amounts of Capryol PGMC (X(1)), Tween 20 (X(2)), and Transcutol HP (X(3)...

journal_title：Journal of pharmaceutical sciences

authors： Marasini N,Yan YD,Poudel BK,Choi HG,Yong CS,Kim JO

更新日期：2012-12-01 00:00:00

abstract：:Arginine-glycine-aspartate (RGD) has been shown to be essential for the recognition of integrins overexpressed in tumor cells, especially during tumor invasion, angiogenesis, and metasis. In this study, a novel tetrapeptide, RGD-valine (RGDV), was designed and attached to the N position of 1-β-D-arabinofuranosylcytosi...

journal_title：Journal of pharmaceutical sciences

authors： Wang F,Cui C,Ren Z,Wang L,Liu H,Cui G

更新日期：2012-12-01 00:00:00

abstract：:X-ray diffraction and infrared spectroscopy measurements for the N,N-dimethylformamide (DMF) and dimethyl sulfoxide (DMSO) solvatomorphs of betulonic acid (BA) were investigated. BA [3-oxolup-20(29)-en-28-oic acid, C(30)H(46)O(3)] exhibits a wide spectrum of biological activities and is considered to be a promising na...

journal_title：Journal of pharmaceutical sciences

authors： Boryczka S,Jastrzebska M,Bębenek E,Kusz J,Zubko M,Kadela M,Michalik E

更新日期：2012-12-01 00:00:00

abstract：:A method is presented for determining the equilibrium solubility of a drug in a solid polymer at or near room temperature, which represents a typical storage temperature. The method is based on a thermodynamic model to calculate the Gibbs energy change ΔG(SS) associated with forming a binary drug-polymer solid solutio...

journal_title：Journal of pharmaceutical sciences

authors： Bellantone RA,Patel P,Sandhu H,Choi DS,Singhal D,Chokshi H,Malick AW,Shah N

更新日期：2012-12-01 00:00:00

abstract：:RNA interference has emerged as a potentially powerful tool in the treatment of genetic and acquired diseases by delivering short interfering RNA (siRNA) or microRNA (miRNA) to target genes, resulting in their silencing. However, many physicochemical and biological barriers have to be overcome to obtain efficient in v...

journal_title：Journal of pharmaceutical sciences

authors： Guzman-Villanueva D,El-Sherbiny IM,Herrera-Ruiz D,Vlassov AV,Smyth HD

更新日期：2012-11-01 00:00:00

abstract：:A simulation study was done to determine if 72 h is the most informative sampling duration for bioequivalence (BE) determination in parallel-designed BE studies with drugs that have half-lives of at least 30 h. The impact of absorption and elimination half-lives on informative sampling was evaluated. Two-treatment par...

journal_title：Journal of pharmaceutical sciences

authors： El-Tahtawy A,Harrison F,Zirkelbach JF,Jackson AJ

更新日期：2012-11-01 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：:Biopharmaceuticals represent an important and growing class of medicines. Immunogenic responses to biopharmaceuticals in patients can sometimes result in reduced safety and efficacy. Although multiple factors are known to influence immunogenicity, our understanding of the complex underlying mechanisms remains imperfec...

journal_title：Journal of pharmaceutical sciences

authors： Bee JS,Goletz TJ,Ragheb JA

更新日期：2012-10-01 00:00:00

abstract：:Nephropathic cystinosis is a rare autosomal recessive disease characterised by raised lysosomal levels of cystine in the cells of all the organs. It is treated by the 6-h oral administration of the aminothiol, cysteamine, which has an offensive taste and smell. In an attempt to reduce this frequency and improve the tr...

journal_title：Journal of pharmaceutical sciences

authors： Buchan B,Kay G,Matthews KH,Cairns D

更新日期：2012-10-01 00:00:00

abstract：:Wounds, particularly burns, are prone to colonization of potentially life-threatening bacteria. Local delivery of antimicrobial agents in sufficient quantities and over longer period of time can reduce risk of burn infections. Mupirocin-in-liposomes-in-hydrogels were proposed as advanced delivery system for improved b...

journal_title：Journal of pharmaceutical sciences

authors： Hurler J,Berg OA,Skar M,Conradi AH,Johnsen PJ,Skalko-Basnet N

更新日期：2012-10-01 00:00:00

abstract：:Ensuring the health of street-involved children is a growing public health challenge. These children are vulnerable, neglected, and rarely a priority for basic service providers and governments. Sizable populations of street-involved children are present in major urban areas worldwide and current trends in urbanizatio...

journal_title：Journal of pharmaceutical sciences

authors： Osei-Twum JA,Wasan KM

更新日期：2012-10-01 00:00:00

abstract：:The physical stability of an immunoglobulin G4 monoclonal antibody (mAb) upon dilution into intravenous (i.v.) bags containing 0.9% saline was examined. Soluble aggregates and subvisible particles were observed by size-exclusion high-performance liquid chromatography (SE-HPLC) and light obscuration when formulated wit...

journal_title：Journal of pharmaceutical sciences

authors： Kumru OS,Liu J,Ji JA,Cheng W,Wang YJ,Wang T,Joshi SB,Middaugh CR,Volkin DB

更新日期：2012-10-01 00:00:00

abstract：:It is demonstrated that the fluid-phase thermodynamics theory conductor-like screening model for real solvents (COSMO-RS) as implemented in the COSMOtherm software can be used for accurate and efficient screening of coformers for active pharmaceutical ingredient (API) cocrystallization. The excess enthalpy, H(ex) , be...

journal_title：Journal of pharmaceutical sciences

authors： Abramov YA,Loschen C,Klamt A

更新日期：2012-10-01 00:00:00

abstract：:Injectable controlled-release formulations are of increasing interest for the treatment of chronic diseases. This study aims to develop and characterize a polymeric matrix for intramuscular or subcutaneous injection, consisting of two biocompatible polymers, particularly suitable for formulating poorly soluble drugs. ...

journal_title：Journal of pharmaceutical sciences

authors： Meeus J,Chen X,Scurr DJ,Ciarnelli V,Amssoms K,Roberts CJ,Davies MC,van Den Mooter G

更新日期：2012-09-01 00:00:00

abstract：:Aerosolized medicine is one of the fastest growing areas in the pharmaceutical industry. Dry powder aerosols of pharmaceutical compounds are particularly attractive for the prevention and treatment of respiratory diseases but are also emerging as a treatment option for systemic diseases. Engineering particles in dry p...

journal_title：Journal of pharmaceutical sciences

authors： El-Gendy N,Selvam P,Soni P,Berkland C

更新日期：2012-09-01 00:00:00

abstract：:The clearance (Cl) and volume of distribution (V(ss)) of a lipophilic, lymphatically transported drug, halofantrine (Hf) have been evaluated after intravenous delivery to the systemic circulation in ex vivo lymph and plasma, and compared with the data obtained after administration of a lipid-based emulsion and a lipid...

journal_title：Journal of pharmaceutical sciences

authors： Caliph SM,Trevaskis NL,Charman WN,Porter CJ

更新日期：2012-09-01 00:00:00

abstract：:The purpose of this work was to study the permeability of two relatively lipophilic sulfenamide prodrugs of linezolid (clogP 0.85), N-(phenylthio)linezolid (1, clogP 2.77) and N-[(2-ethoxycarbonyl)ethylthio]linezolid (2, clogP 1.43), across Caco-2 cell monolayers. Both prodrugs were found to convert to linezolid in th...

journal_title：Journal of pharmaceutical sciences

authors： Nti-Addae KW,Guarino VR,Dalwadi G,Stella VJ

更新日期：2012-09-01 00:00:00

abstract：:A kinetic dialysis technique together with a radiolabeled chenodeoxycholate (CDC) was used to determine the existence of a relationship between the monomer concentration of CDC and the total CDC concentration in different CDC solutions containing 1 or 5 mM sulfobutylether (SBE)-β-cyclodextrin. On the basis of the natu...

journal_title：Journal of pharmaceutical sciences

authors： Liu CL,Chang CL,Jhou SY,Higuchi WI

更新日期：2012-08-01 00:00:00

abstract：:In the present study, a previously described sulfenamide prodrug of a basic antidiabetic drug, metformin, was evaluated further. This sulfenamide prodrug was designed to improve the permeability and consequently the oral absorption and bioavailability (F) of the highly water-soluble metformin. Bioactivation of the pro...

journal_title：Journal of pharmaceutical sciences

authors： Huttunen KM,Leppänen J,Vepsäläinen J,Sirviö J,Laine K,Rautio J

更新日期：2012-08-01 00:00:00

abstract：:The objective of this study was to determine reasons behind the low oral (p.o.) bioavailability of glucosamine. By using male Sprague-Dawley rats, the movement of glucosamine through everted gut, the effect of dose and glucose, and inhibition of a glucose transporter (GLUT2) by quercetin were studied. Glucosamine phar...

journal_title：Journal of pharmaceutical sciences

authors： Ibrahim A,Gilzad-kohan MH,Aghazadeh-Habashi A,Jamali F

更新日期：2012-07-01 00:00:00

abstract：:Thymoquinone (TQ) is the main bioactive component isolated from Nigella sativa essential oil and seeds and has been used for the treatment of inflammations, liver disorders, arthritis, and is of great importance as a promising therapeutic drug for different diseases including cancer. This paper reports the first exper...

journal_title：Journal of pharmaceutical sciences

authors： Lupidi G,Camaioni E,Khalifé H,Avenali L,Damiani E,Tanfani F,Scirè A

更新日期：2012-07-01 00:00:00