Abstract：
PURPOSE:The purpose of this study was to use a replicate designed trial to assess the overall, intra- and inter-subject variabilities in pharmacokinetic parameters of CGP 33101 after oral administration of tablets relative to that of powder suspended in water, and to determine the relative proportion of the intra-subject variance to the overall variability. METHODS:Sixteen healthy subjects were randomly assigned to four groups to receive tablets and suspension twice in four different treatment sequences. The plasma concentration-time profile of CGP 33101 was characterized in terms of Cmax, Tmax, and AUC. Bioavailability of tablets relative to suspension and intra- and inter-subject variability were assessed by statistical analysis. RESULTS AND CONCLUSIONS:The overall variabilities in absorption kinetics of CGP 33101 in healthy subjects were small with CV's of the population mean values for AUC and Cmax less than 26% for both tablets and suspension. Contribution of intra-subject variability to the overall variability was also small (approximately 20%). Both the overall and intra-subject variabilities of AUC and Cmax after suspension were larger than after the tablets. However, the differences in variability between tablets and suspension were not statistically significant (p > 0.05). The tablet formulation was bioequivalent to suspension in terms of rate and extent of absorption based on 90% conventional confidence intervals (for AUC and Cmax) and Wilcoxon rank-sum test (for Tmax).
journal_name
Pharm Resjournal_title
Pharmaceutical researchauthors
Cheung WK,Kianifard F,Wong A,Mathieu J,Cook T,John V,Redalieu E,Chan Kdoi
10.1023/a:1016275402723subject
Has Abstractpub_date
1995-12-01 00:00:00pages
1878-82issue
12eissn
0724-8741issn
1573-904Xjournal_volume
12pub_type
临床试验,杂志文章,随机对照试验abstract：PURPOSE:Nine common excipients were examined to determine their ability to cause disproportionation of the HCl salt of a a weakly basic compound. The goal was to determine which excipients were problematic and correlate the results to known properties such as surface pH, slurry pH, or molecular structure. Such a correl...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-013-1002-y
更新日期：2013-06-01 00:00:00
abstract：:Intranasal route continues to be one of the main focuses of drug delivery research. Although it is generally perceived that the nasal route could avoid the first-pass metabolism in liver and gastrointestinal tract, the role of metabolic conversions in systemic and brain-targeted deliveries of the parent compounds and ...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-010-0127-5
更新日期：2010-07-01 00:00:00
abstract：PURPOSE:To advance fundamental biological and translational research with the bacterium Neisseria gonorrhoeae through the prediction of novel small molecule growth inhibitors via naïve Bayesian modeling methodology. METHODS:Inspection and curation of data from the publicly available ChEMBL web site for small molecule ...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-020-02876-y
更新日期：2020-07-13 00:00:00
abstract：PURPOSE:SN-38, a potent chemotherapeutic drug, has not been used clinically because of its severe side effects and poor solubility. In this work, we aimed to evaluate the effect of dose and multiple injections of SN-38-loaded polymeric depots on antitumor efficacy and toxicity in vivo. METHODS:Preparation and characte...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-016-2011-4
更新日期：2016-12-01 00:00:00
abstract：:The effects of process and storage conditions of solid-state emulsions were studied. Oil-in-water emulsions may be prepared from solid state emulsions by adding an aqueous phase to the solid. Solid-state emulsions are prepared by processing an oil phase and an aqueous solution of matrix material via a solvent removal ...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1018983227234
更新日期：1993-07-01 00:00:00
abstract：PURPOSE:The purpose of this study was to evaluate an effect of the proteolytic enzyme papain on permeation of low molecular weight heparin (LMWH) in vitro and in vivo. MATERIALS AND METHODS:In vitro permeation studies were performed using rat small intestine as permeation barrier. In order to determine the ratio of pa...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-006-9226-8
更新日期：2007-05-01 00:00:00
abstract：PURPOSE:The feasibility of using iontophoresis to enhance the permeation rate of a model peptide was investigated in vitro using hairless mouse skin. METHODS:Angiotensin 2 (AT 2) was employed as a permeant probe, using optimum iontophoresis conditions. A number of physicochemical parameters (donor ionic strength; vale...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1016254230155
更新日期：1995-07-01 00:00:00
abstract：PURPOSE:Calculation of the ideal solubility of a crystalline solute in a liquid solvent requires knowledge of the difference in the molar heat capacity at constant pressure of the solid and the supercooled liquid forms of the solute, delta Cp. Since this parameter is not usually known, two assumptions have been used to...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1012148910975
更新日期：1997-05-01 00:00:00
abstract：PURPOSE:The discovery of nano drug delivery system has rendered a great hope for improving cancer therapy. However, there are some inevitable obstacles that constrain its development, such as the physical and biological barriers, the toxicity of carrier materials and the physiological toxicity of drugs. Here, we report...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-019-2709-1
更新日期：2019-12-10 00:00:00
abstract：PURPOSE:The purpose of this study is to investigate the characteristics of pGlu-L-Dopa-Pro as a prodrug of L-Dopa. METHODS:pGlu-L-Dopa-Pro and L-Dopa-Pro were synthesized using the standard procedures of peptide synthesis. The conversion of pGlu-L-Dopa-Pro to L-Dopa was studied using pyroglutamyl aminopeptidase I and ...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1016239321494
更新日期：1995-07-01 00:00:00
abstract：PURPOSE:E-selectin is a cell adhesion molecule that is specifically expressed in the inflammatory vascular endothelium in response to cytokines such as IL-1 beta and TNF-alpha, and interacts with specific ligands containing sialyl Lewis X (Neu5Ac alpha 2-3Gal beta 1-4(Fuc alpha 1-3)GlcNAc-, SLex). In order to investiga...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1018849029727
更新日期：1999-02-01 00:00:00
abstract：:Photodegradation of solutions of metronidazole in the presence and absence of sodium urate was studied. Photodegradation appeared to follow zero-order kinetics and was found to be dependent on the pH, buffer species, sodium urate concentration, and light source. Complex formation between metronidazole and sodium urate...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1015851719579
更新日期：1989-01-01 00:00:00
abstract：:The plasma concentration-time profiles and pharmacokinetics were characterized for nicotine and its major metabolite, cotinine, after multiple daily application of a nicotine user-activated transdermal therapeutic system (UATTS) to nine healthy smokers. The volunteers abstained from smoking 24 hr prior to and during t...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1015810019076
更新日期：1991-03-01 00:00:00
abstract：PURPOSE:The purpose of this study was to characterize the amorphous state of ursodeoxycholic acid (UDCA) samples by using isothermal microcalorimetry, X-ray diffraction, infrared (IR) spectroscopy and solid state carbon 13 nuclear magnetic resonance (13C-NMR) spectroscopy, and to demonstrate the application of the ther...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1012114825513
更新日期：1997-06-01 00:00:00
abstract：:Losartan, an antihypertensive agent in clinical development, was found to exist in two enantiotropic polymorphic forms, a low-temperature stable form (Form I) and a high-temperature stable form (Form II), the temperatures at which they are stable being related to the transition temperature. X-ray powder diffraction pa...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1018973530443
更新日期：1993-06-01 00:00:00
abstract：PURPOSE:The objective of this study was to develop and evaluate a pulsatile drug delivery system based on an impermeable capsule body filled with drug and an erodible plug placed in the opening of the capsule body. METHODS:The erodible plugs were either prepared by direct compression followed by placing the tablets in...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1011940718534
更新日期：1998-03-01 00:00:00
abstract：:Esmolol hydrochloride degrades in aqueous solutions by the hydrolysis of a labile aliphatic carboxyester group. The products are methanol and ASL-8123. The resulting aliphatic carboxylic acid moiety (ASL-8123) has a pK of 4.80, which is within 1 pH unit of the pH of the formulation. ASL-8123 therefore acts as a "secon...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1015973425708
更新日期：1988-08-01 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
pub_type： 杂志文章
doi：10.1007/s11095-006-9644-7
更新日期：2006-04-01 00:00:00
abstract：PURPOSE:The objective of this study is to evaluate the feasibility of using coated microneedles to deliver vaccines into the oral cavity to induce systemic and mucosal immune responses. METHOD:Microneedles were coated with sulforhodamine, ovalbumin and two HIV antigens. Coated microneedles were inserted into the inner...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-014-1335-1
更新日期：2014-09-01 00:00:00
abstract：PURPOSE:To demonstrate that polyanhydride copolymer chemistry affects the uptake and intracellular compartmentalization of nanospheres by THP-1 human monocytic cells. METHODS:Polyanhydride nanospheres were prepared by an anti-solvent nanoprecipitation technique. Morphology and particle diameter were confirmed via scan...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-008-9760-7
更新日期：2009-03-01 00:00:00
abstract：PURPOSE:To develop novel biomineral-binding liposomes (BBL) for the prevention of orthopedic implant associated osteomyelitis. METHODS:A biomineral-binding lipid, alendronate-tri(ethyleneglycol)-cholesterol conjugate (ALN-TEG-Chol), was synthesized through Cu(I)-catalyzed Huisgen 1,3-dipolar cycloaddition (a versatile...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-012-0812-7
更新日期：2012-11-01 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
pub_type： 杂志文章
doi：10.1007/s11095-016-1861-0
更新日期：2016-05-01 00:00:00
abstract：PURPOSE:Deposition characteristics of MDI and DPI aerosols were compared throughout the conducting airways for the first time using a combination of in vitro experiments and a newly developed stochastic individual path (SIP) model for different inhalation profiles. METHODS:In vitro experiments were used to determine i...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-012-0691-y
更新日期：2012-06-01 00:00:00
abstract：:A rapid quantitative, enantioselective HPLC method for the analysis of the four stereoisomers, (+) and (-) erythro and (+) and (-) threo forms, of mefloquine has been developed using a Chiralpak Ad analytical column containing amylose tris-3,5-dimethylphenyl carbonate coated on silica gel and hexane/ethanol/diethylami...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1015832912774
更新日期：1992-12-01 00:00:00
abstract：:Knowledge of comparative solubility profiles of a base and its hydrochloride salt is important in selecting one form over the other for dosage form design. The studies with two model bases, namely, tiaramide and papaverine, showed that, except during phase transition from a base to a salt or vice versa, the pH-solubil...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/A:1016382426347
更新日期：1985-03-01 00:00:00
abstract：PURPOSE:The purpose of the present study was to investigate changes of blood-brain barrier (BBB) and brain parenchymal protein expression due to type II diabetes mellitus (T2DM) induced by a high-fat diet (HFD) by using SWATH-based quantitative proteomics. METHODS:Mice were fed a HFD for 2 or 10 weeks, and then SWATH-...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-019-2674-8
更新日期：2019-07-31 00:00:00
abstract：:The pharmacokinetics of Sb was examined in 29 patients with cutaneous leishmaniasis following the intramuscular administration of a dose of sodium stibogluconate equivalent to 600 mg of Sb. Blood was sampled at different time intervals from each patient and Sb was measured in whole blood by electrothermal atomic absor...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1016251023427
更新日期：1995-01-01 00:00:00
abstract：PURPOSE:Study on curcumin dissolved in natural deep eutectic solvents (NADES) was aimed at exploiting their beneficial properties as drug carriers. METHODS:The concentration of dissolved curcumin in NADES was measured. Simulated gastrointestinal fluids were used to determine the concentration of curcumin and quantum c...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-019-2643-2
更新日期：2019-06-03 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
pub_type： 杂志文章
doi：10.1007/s11095-013-1033-4
更新日期：2013-07-01 00:00:00
abstract：PURPOSE:To investigate the ability of various polymers to inhibit the crystallization of amorphous felodipine from amorphous molecular dispersions in the presence of absorbed moisture. METHODS:Spin coated films of felodipine with poly(vinylpyrrolidone) (PVP), hydroxypropylmethylcellulose acetate succinate (HPMCAS) and...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-007-9331-3
更新日期：2008-04-01 00:00:00
