Influence of molecular properties on oral bioavailability of lipophilic drugs - mapping of bulkiness and different measures of polarity.

abstract：:Objective: Tanshinone IIA (TSN) and Tetramethylpyrazine (TMP) were combined in a composite, oil-in-water nanoemulsions (TSN/TMP O/W NEs) was prepared to prolong in vitro and vivo circulation time, and enhance the bioavailability of TSN. Material and methods: Physicochemical characterization of TSN/TMP O/W NEs was char...

journal_title：Pharmaceutical development and technology

authors： Wang B,Hong L,Liu Y,Bedingfield SK,Zhang C,Peng C,Qian J,Zha L

更新日期：2019-12-01 00:00:00

abstract：:Co-solvent solubilization approach has been used to enhance the solubility of seven antidiabetic drugs: gliclazide, glyburide, glipizide, glimepiride, repaglinide, pioglitazone, and roziglitazone. Solubility in water, phosphate buffer (pH 7.4), six co-solvent solutions prepared in water as well as phosphate buffer (pH...

journal_title：Pharmaceutical development and technology

authors： Seedher N,Kanojia M

更新日期：2009-01-01 00:00:00

abstract：:The aim of this study was to prepare a highly porous multiparticulate dosage form containing cilostazol for gastroretentive drug delivery. The floating pellets were prepared with glyceryl behenate as a matrix former and camphor as a sublimating agent by extrusion/spheronization and sublimation under vacuum. Granules p...

journal_title：Pharmaceutical development and technology

authors： Hwang KM,Byun W,Cho CH,Park ES

更新日期：2018-06-01 00:00:00

abstract：:Oily liquid drugs are not convenient for oral administration. We developed a powder containing clofibrate (CF), a model of an oily drug, using aminoalkyl methacrylate copolymer (EPO) or methacrylic acid copolymer (L100). CF or a mixture of CF and soybean oil was emulsified with EPO or L100 aqueous solution. Using a hi...

journal_title：Pharmaceutical development and technology

authors： Fujii M,Kawakami A,Saito A,Tuchiya H,Koizumi N,Watanabe Y

更新日期：2016-12-01 00:00:00

abstract：:The objective of the study was to mask the unpleasant taste of captopril (CPT). Taste masking was achieved by complexation of CPT with a basic ion exchange resin, Dowex® 66, using the batch method. Dowex® 66 was used for the adsorption of CPT, and physical and chemical parameters of the CPT resinates complex were eval...

journal_title：Pharmaceutical development and technology

authors： Chikukwa MTR,Wesoly M,Korzeniowska AB,Ciosek-Skibinska P,Walker RB,Khamanga SMM

更新日期：2020-03-01 00:00:00

abstract：:An osmotic-controlled pulsatile delivery technology was developed for targeted drug delivery. This novel system consists of a tablet core surrounded by an osmotic coating that has been mechanically compromised in strategic locations to facilitate reliable drug release at a given time point after administration. The ta...

journal_title：Pharmaceutical development and technology

authors： Rahemba TR,Bell S,Connolly EK,Waterman KC

更新日期：2009-01-01 00:00:00

abstract：:A comprehensive analytical solution that accounts for many factors and assumptions affecting drug concentration profile in the gastrointestinal tract was presented. A sensitivity analysis approach was utilized in order to investigate the importance of different parameters in the model. The partition coefficient is fou...

journal_title：Pharmaceutical development and technology

authors： Idkaidek NM,Abdel-Jabbar N

更新日期：2001-01-01 00:00:00

abstract：:The objectives of this research were to evaluate the stability of lercanidipine in solution state and solid state and explore the compatibility of drug with oils, surfactants and cosurfactants as excipients. The effect of pH on the degradation in solution state was studied through pH-rate profile of lercanidipine in c...

journal_title：Pharmaceutical development and technology

authors： Parmar N,Amin S,Singla N,Kohli K

更新日期：2012-11-01 00:00:00

abstract：:The dry coating process was evaluated in terms of storage stability investigating drug release and agglomeration tendency of the different coated oral dosage forms; hydroxypropyl methylcellulose acetate succinate (HPMCAS) was used with triethylcitrate (TEC) as plasticizer and acetylated monoglyceride (Myvacet) as wett...

journal_title：Pharmaceutical development and technology

authors： Kablitz CD,Urbanetz NA

更新日期：2009-01-01 00:00:00

abstract：:Dynamic image analysis (DIA) was used to measure particle diameter (D50) of in-process samples removed during fluid bed coating. A single, rapid measurement gave D50 to within 4 mum. Samples removed at intervals of 2% weight gain were readily distinguishable by DIA and by their drug release profiles. Drug release was ...

journal_title：Pharmaceutical development and technology

authors： Heinicke G,Schwartz JB

更新日期：2006-01-01 00:00:00

abstract：:Flecainide base is pharmaceutically active substance used for production of flecainide acetate which is known in market as Tambacor, Almarytm, Apocard, Ecrinal or Flecaine. It is determined that flecainide base forms four polymorphic forms abbreviated as Ib, IIb, IIIb and IVb. Flecainide base form Ib is thermodynamica...

journal_title：Pharmaceutical development and technology

authors： Veldre K,Eglīte Z,Actiņš A,Zvirgzdiņš A,Rozenberga L,Tamanis E

更新日期：2014-02-01 00:00:00

abstract：:Two polymorphs and three solvates of fluconazole were isolated and characterized by x-ray powder diffractometry, IR spectroscopy, differential scanning calorimetry (DSC), thermogravimetry, and their dissolution rates. The different forms were prepared by crystallization of the original powder in different solvents at ...

journal_title：Pharmaceutical development and technology

authors： Alkhamis KA,Obaidat AA,Nuseirat AF

更新日期：2002-11-01 00:00:00

abstract：:A prototype parenteral manufacturing facility based on isolation technology was designed, constructed, and commissioned at Warner-Lambert Co., Morris Plains, NJ, with emphasis on its application to research and development (R&D) settings. The facility contains closed isolators for holding, transferring, and manufactur...

journal_title：Pharmaceutical development and technology

authors： Krishna AK,Lodhi SA,Harris MR

更新日期：2000-01-01 00:00:00

abstract：:The hygroscopicity of Brequinar sodium, an organ transplant immunosuppressant, at 75% relative humidity highly depends on the crystal form or crystallinity of the drug substance. Hygroscopicity and ease of water uptake of three lots of Brequinar sodium were investigated. Those lots contained different impurities at le...

journal_title：Pharmaceutical development and technology

authors： Wu LS,Pang J,Hussain MA

更新日期：1996-04-01 00:00:00

abstract：:The purpose of this study was to assess the impact of impurities in formulation components, antioxidants, formulation pH, and processing/packaging on the extent of color change associated with oxidation of danofloxacin injectable. The methods used in this study include reversed-phase HPLC, UV-VIS spectrophotometry, at...

journal_title：Pharmaceutical development and technology

authors： Kasraian K,Kuzniar AA,Wilson GG,Wood JA

更新日期：1999-01-01 00:00:00

abstract：:Novel fast-disintegrating multi-unit tablets (FDMUTs) were prepared to modify the release of lornoxicam (a potent non-steroidal anti-inflammatory drug with a short half-life) as well as to combine the advantages of multi-unit systems with the cost-effectiveness of compressed tablets. The proposed FDMUTs consisted of s...

journal_title：Pharmaceutical development and technology

authors： Aburahma MH,Hamza Yel-S

更新日期：2011-08-01 00:00:00

abstract：:The utility of microcalorimetry as a rapid screening tool for assessing the solution stability of high molecular weight pharmaceutical proteins was evaluated by using model recombinant antibodies, Protein I and Protein II. Changes in the transition midpoint, T(m), were monitored as a function of pH and/or in the prese...

journal_title：Pharmaceutical development and technology

authors： Burton L,Gandhi R,Duke G,Paborji M

更新日期：2007-01-01 00:00:00

abstract：:In this study, we developed a one-step method to prepare ibuprofen fast- and sustained-release complex preparation. It was based on a double jets electrospinning process. Ibuprofen, a poorly water-soluble drug, was electrospun into fibers with polyvinyl pyrrolidone and hydroxypropyl methyl cellulose by two jets, respe...

journal_title：Pharmaceutical development and technology

authors： Che X,Xue J,Zhang J,Yang X,Wang L

更新日期：2020-07-01 00:00:00

abstract：:The aim of this study was to investigate early formulation screening in small scale with a miniaturized fluid bed device. Altogether eight different batches were granulated in a Multipart Microscale Fluid bed Powder processor (MMFP) with constant process conditions using electrostatic atomization. Atomization voltage ...

journal_title：Pharmaceutical development and technology

authors： Kivikero N,Murtomaa M,Antikainen O,Hatara J,Juppo AM,Sandler N

更新日期：2011-08-01 00:00:00

abstract：:The present study was carried out in order to mask the bitter taste of the Etoricoxib by complexation with cation-exchange resin, Indion 204. The drug resin complexes (DRC) were prepared by batch process and efficient drug loading was obtained by using inactivated form of resin in the drug-resin ratio 1:3.3 with 30 mi...

journal_title：Pharmaceutical development and technology

authors： Patra S,Samantaray R,Pattnaik S,Barik BB

更新日期：2010-09-01 00:00:00

abstract：:An approach for cancer treatment is modulation of tumor microenvironment. Based on the role of extracellular matrix in cell modulation, fabrication of textured materials mimicking extracellular matrix could provide novel opportunities such as determining cancer cell behaviour. With this background, in this work, we ha...

journal_title：Pharmaceutical development and technology

authors： Yaşayan G,Mega Tiber P,Orun O,Alarçin E

更新日期：2020-12-01 00:00:00

abstract：:The first-line therapy for moderate to severe benign prostatic hyperplasia is the oral therapy by alfuzosin hydrochloride. Unfortunately, the oral therapy of alfuzosin is associated with several route-specific systemic side-effects. The current study was aimed to develop a prototype transdermal patch system for alfuzo...

journal_title：Pharmaceutical development and technology

authors： Nair AB,Vaka SR,Gupta S,Repka MA,Murthy SN

更新日期：2012-03-01 00:00:00

abstract：:The main objective of this study was to design positively charged Levofloxacin Hemihydrate (Levo-h)-loaded nanoparticles with improved entrapment efficiency and antibacterial activity. PLGA alone or in combinations with Eudragit® RLPO or RS30D with or without positively charged inducing agent; 1,2-dioleoyl-3-trimethyl...

journal_title：Pharmaceutical development and technology

authors： Hasan AA,Sabry SA,Abdallah MH,El-Damasy DA

更新日期：2016-09-01 00:00:00

abstract：:The high initial burst release of a highly water-soluble drug from poly (D,L-lactide-co-glycolide) (PLGA) microparticles prepared by the multiple emulsion (w/o/w) solvent extraction/evaporation method was reduced by coating with an additional polymeric PLGA layer. Coating with high encapsulation efficiency was perform...

journal_title：Pharmaceutical development and technology

authors： Ahmed AR,Elkharraz K,Irfan M,Bodmeier R

更新日期：2012-01-01 00:00:00

abstract：:The objective of this study was to develop a floating, pulsatile, multiparticulate drug delivery system intended for chronopharmacotherapy of arthritis. The floating pulsatile drug delivery has the advantage that a drug can be released in the upper gastrointestinal tract after a definite time period of no drug release...

journal_title：Pharmaceutical development and technology

authors： Gaikwad M,Belgamwar VS,Tekade A,Gattani S,Surana S

更新日期：2010-03-01 00:00:00

abstract：CONTEXT AND OBJECTIVE:The objective of the study was to develop a stable capsule formulation of ziprasidone hydrochloride which can be administered without regards to food intake. MATERIALS AND METHODS:The unstable anhydrous form of ziprasidone hydrochloride was stabilized employing hot-melt extrusion and further opti...

journal_title：Pharmaceutical development and technology

authors： Banerjee S,Shankar KR,Prasad Y R

更新日期：2016-11-01 00:00:00

abstract：:The aim of this study was to investigate isotropic mono- and diglyceride-based (MCMDG) systems, which are potential vehicles for injectable products containing both hydrophilic and lipophilic drugs. For two-component systems, MCMDG was mixed with various masses of water. For three-component systems, the samples were p...

journal_title：Pharmaceutical development and technology

authors： Sari P,Razzak M,Tucker IG

更新日期：2004-01-01 00:00:00

abstract：BACKGROUND:Oxaliplatin has long been used for the treatment of colorectal cancer via intra-venous infusion. In order to improve patient compliance, a solid dosage form for oral administration of oxaliplatin was prepared as nano-sized particles. METHOD:Nano oxaliplatin was prepared employing Fat Employing Supercritical...

journal_title：Pharmaceutical development and technology

authors： Lee SJ,Kim YH,Lee SH,Hahn M

更新日期：2012-03-01 00:00:00

abstract：:The use of rice bran (RB), soybean (SB) or sunflower seed (SF) oils to prepare lipid-core nanocapsules (LNCs) as controlled drug delivery systems was investigated. LNCs were prepared by interfacial deposition using the preformed polymer method. All formulations showed negative zeta potential and adequate nanotechnolog...

journal_title：Pharmaceutical development and technology

authors： Rigo LA,Frescura V,Fiel L,Coradini K,Ourique AF,Emanuelli T,Quatrin A,Tedesco S,Silva CB,Guterres SS,Pohlmann AR,Beck RC

更新日期：2014-11-01 00:00:00

abstract：:This study examines the effect of the degree of methoxylation (DM) and particle size on compression properties and compactibility of pectin powders. A powder classification system based on sequential handling of compression parameters was applied. A single size fraction (90-125 μm) of pectin powders with DM values ran...

journal_title：Pharmaceutical development and technology

authors： Salbu L,Bauer-Brandl A,Alderborn G,Tho I

更新日期：2012-05-01 00:00:00