Abstract:
PURPOSE:The preparation of drug/cyclodextrin complexes is a suitable method to improve the dissolution of poor soluble drugs. The efficacy of the Controlled Particle Deposition (CPD) as a new developed method to prepare these complexes in a single stage process using supercritical carbon dioxide is therefore compared with other conventional methods. MATERIALS AND METHODS:Ibuprofen/beta-cyclodextrin complexes were prepared with different techniques and characterized using FTIR-ATR spectroscopy, powder X-ray diffractometry (PXRD), differential scanning calorimetry (DSC) and scanning electron microscopy (SEM). In addition, the influences of the processing technique on the drug content (HPLC) and the dissolution behavior were studied. RESULTS:Employing the CPD-process resulted in a drug content of 2.8+/-0.22 wt.% in the carrier. The material obtained by CPD showed an improved dissolution rate of ibuprofen at pH 5 compared with the pure drug and its physical mixture with beta-cyclodextrin. In addition CPD material displays the highest dissolution (93.5+/- 2.89% after 75 min) compared to material obtained by co-precipitation (61.3 +/-0.52%) or freeze-drying (90.6 +/-2.54%). CONCLUSION:This study presents the CPD-technique as a well suitable method to prepare a drug/beta-cyclodextrin complex with improved drug dissolution compared to the pure drug and materials obtained by other methods.
journal_name
Pharm Resjournal_title
Pharmaceutical researchauthors
Hussein K,Türk M,Wahl MAdoi
10.1007/s11095-006-9177-0subject
Has Abstractpub_date
2007-03-01 00:00:00pages
585-92issue
3eissn
0724-8741issn
1573-904Xjournal_volume
24pub_type
杂志文章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:Desmopressin acetate (DDAVP) is used parenterally and intranasally in the control of several diseases. Oral administration of DDAVP, while most desirable, is not practical presently due to low bioavailability. The objective of the present study was to explore the feasibility for employing oil-in-water MucoAdhes...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1016023111248
更新日期:1996-07-01 00:00:00
abstract:PURPOSE:Relatively large (>5 microm) and porous (mass density <0.4 g/cm3) particles present advantages for the delivery of drugs to the lungs, e.g., excellent aerosolization properties. The aim of this study was, first, to formulate such particles with excipients that are either FDA-approved for inhalation or endogenou...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1018910200420
更新日期:1999-11-01 00:00:00
abstract:PURPOSE:To investigate influence of inflammation on metabolism and pharmacokinetics (PK) of midazolam (MDZ) and construct a semi-physiologically based pharmacokinetic (PBPK) model to predict PK in mice with inflammatory disease. METHODS:Glucose-6-phosphate isomerase (GPI)-mediated inflammation was used as a preclinica...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-018-2447-9
更新日期:2018-06-21 00:00:00
abstract:PURPOSE:To characterize factor(s) contained in apical medium of primary cultured rat alveolar epithelial type II cell-like monolayers (RAECM-II) that enhance insulin absorption across alveolar epithelial cells. MATERIALS AND METHODS:Primary rat alveolar epithelial cell monolayers cultured on Transwells in the presence...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-007-9301-9
更新日期:2007-09-01 00:00:00
abstract:PURPOSE:To characterize the uptake mechanism of zidovudine (AZT), a nucleoside reverse transcriptase inhibitor, in syncytiotrophoblast cells using the TR-TBT 18d-1 cell line previously established by our group. MATERIALS AND METHODS:The effects of several transporter inhibitors on the initial and steady-state apical u...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-008-9564-9
更新日期:2008-07-01 00:00:00
abstract:PURPOSE:Ruthenium complex is a potentially theranostic agent for cancer imaging and therapy, however its application is limited due to poor water-solubility and lack of tumor selectivity. To overcome the above drawbacks, pH-sensitive nanocapsule as a novel targeting carrier was designed to deliver ruthenium complex for...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-016-2021-2
更新日期:2016-12-01 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 delivery of therapeutic nucleic acids to neurons has the potential to treat neurological disease and spinal cord injury. While select viral vectors have shown promise as gene carriers to neurons, their potential as therapeutic agents is limited by their toxicity and immunogenicity, their broad tropism, and the cos...
journal_title:Pharmaceutical research
pub_type: 杂志文章,评审
doi:10.1007/s11095-007-9439-5
更新日期:2008-05-01 00:00:00
abstract::The transepithelial transport of arginine vasopressin (AVP) across cultured rat alveolar epithelial cell monolayers was studied. At 0.1 nM donor [125I]AVP, the radiolabel flux measured in the apical-to-basolateral (AB) direction was about 10 times greater than that in the reverse (BA) direction. HPLC analyses of the b...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1018918022865
更新日期:1994-11-01 00:00:00
abstract::Gallopamil is a calcium-channel antagonist with reported activity in experimental animals three to five times higher than that of verapamil. An automated high-performance liquid chromatographic (HPLC) method with fluorescence detection is described for the simultaneous determination of gallopamil and its metabolite no...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1016401405119
更新日期:1987-08-01 00:00:00
abstract:PURPOSE:To examine the inhibitory potential of enalapril [and other angiotensin converting enzyme (ACE) inhibitors] on glycylsarcosine (GlySar) transport by the high-affinity renal peptide transporter. METHODS:Studies were performed in rabbit renal brush border membrane vesicles in which the uptake of radiolabeled Gly...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1018847818766
更新日期:1999-05-01 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
pub_type: 杂志文章
doi:10.1023/a:1015880327911
更新日期:1992-07-01 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
pub_type: 杂志文章
doi:10.1007/s11095-020-02789-w
更新日期:2020-03-12 00:00:00
abstract::Significant efforts are made to characterize molecular liabilities and degradation of the drug substance (DS) and drug product (DP) during various product life-cycle stages. The in vivo fate of a therapeutic protein is usually only considered in terms of pharmacokinetics (PKs) and pharmacodynamics (PDs). However, the ...
journal_title:Pharmaceutical research
pub_type: 杂志文章,评审
doi:10.1007/s11095-019-2689-1
更新日期:2020-01-03 00:00:00
abstract:PURPOSE:The aim of the study is to determine the effect of experimental parameters on microinfusion through hollow microneedles into skin to optimize drug delivery protocols and identify rate-limiting barriers to flow. METHODS:Glass microneedles were inserted to a depth of 720-1080 microm into human cadaver skin to mi...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-005-8498-8
更新日期:2006-01-01 00:00:00
abstract:PURPOSE:Empirical formulae relate the mean size of primary droplets from jet and ultrasonic nebulizers to a fluid's physicochemical properties. Although the size selective "filtering" effects of baffling and evaporation may modify the secondary aerosol produced, this research sought to evaluate whether viscosity and su...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1016205520044
更新日期:1995-11-01 00:00:00
abstract:PURPOSE:The lack of effective delivery vehicles impedes in vivo applications of siRNA. The trimethyl chitosan-cysteine (TC) nanoparticles (NPs) were developed for in vivo delivery of tumor necrosis factor α (TNF-α) siRNA via oral gavage and intraperitoneal injection. METHODS:The nanoparticles formulated from TC conjug...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-013-1086-4
更新日期:2013-10-01 00:00:00
abstract:PURPOSE:To determine by pharmacokinetic (PK) means the role of erythropoietin-receptor (EPO-R) upregulation in fetuses on the elimination of erythropoietin (EPO). MATERIALS AND METHODS:Six fetal sheep were catheterized at a gestational age of 125-127 days and phlebotomized daily for 6 days. Paired tracer PK studies us...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-007-9295-3
更新日期:2007-09-01 00:00:00
abstract::The binding of 1-anilino-8-naphthalenesulfonate (ANS) to bovine serum albumin (BSA), human serum albumin (HSA), and human plasma has been studied by potentiometric titration utilizing a laboratory constructed ion selective electrode (ISE) of ANS. Three classes of ANS binding sites were found on BSA, HSA, and plasma at...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1015855613083
更新日期:1991-07-01 00:00:00
abstract::Gene delivery systems are designed to control the location of administered therapeutic genes within a patient's body. Successful in vivo gene transfer may require (i) the condensation of plasmid and its protection from nuclease degradation, (ii) cellular interaction and internalization of condensed plasmid, (iii) esca...
journal_title:Pharmaceutical research
pub_type: 杂志文章,评审
doi:10.1023/a:1012187414126
更新日期:1997-07-01 00:00:00
abstract:OBJECTIVES:We recently demonstrated that fibrin-based tissue engineered blood vessels (TEV) exhibited vascular reactivity, matrix remodeling and sufficient strength for implantation into the veins of an ovine animal model, where they remained patent for 15 weeks. Here we present an approach to improve the mechanical pr...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-007-9499-6
更新日期:2008-05-01 00:00:00
abstract::Sodium taurodihydrofusidate (STDHF) is one of the most promising absorption enhancers for nasal delivery of peptide drugs. Drugs and additives in nasal formulations should not interfere with the self-cleaning capacity of the nose by the ciliary epithelium. Measured in vitro on human adenoid tissue with a photoelectric...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1015872617511
更新日期:1990-02-01 00:00:00
abstract:PURPOSE:The main goal of this research was to assess the mechanical properties of APIs' polymorphic forms at the single-crystal level (piroxicam, famotidine, nifedipine, olanzapine) in order to predict their bulk deformational attributes, which are critical for some pharmaceutical technology processes. METHODS:The mec...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-014-1475-3
更新日期:2015-02-01 00:00:00
abstract::The use of microdialysis sampling to study the binding of drugs to plasma proteins was evaluated. Microdialysis sampling is accomplished by placing a short length of dialysis fiber in the sample and perfusing the fiber with a vehicle. Small molecules in the sample, such as drugs, diffuse into the fiber and are transpo...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1015955503708
更新日期:1990-10-01 00:00:00
abstract:PURPOSE:Effects of polyvinylpyrrolidone (PVP) molecular weight on the solid-state intermolecular interactions among probucol/PVP/sodium dodecyl sulfate (SDS) ternary ground mixtures (GM) and the formation of nanoparticles were investigated by solid-state NMR spectroscopy. MATERIALS AND METHODS:Ternary GMs of probucol ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-006-9089-z
更新日期:2006-11-01 00:00:00
abstract:PURPOSE:To investigate how likely two extended release formulations are to be bioequivalent when they demonstrate f2 similarity. METHOD:Dissolution profiles were simulated using the Weibull model and varying model parameters around those of a reference profile. The f2 values were calculated for the comparisons of each...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-011-0377-x
更新日期:2011-05-01 00:00:00
abstract:PURPOSE:Nasal delivery is a favorable route for vaccination against most respiratory infections, as antigen deposited in the nasal turbinate and Waldeyer's ring areas induce mucosal and systemic immune responses. However, little is known about the nasal distribution of the vaccines, specifically for infants. METHODS:A...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-020-02976-9
更新日期:2021-01-15 00:00:00
abstract::One of the authors has his name incorrectly indexed in PubMed and SpringerLink as "Laird Forrest M" (last name "Laird Forrest"). His name should index as "Forrest M. Laird" with last name as "Forrest". ...
journal_title:Pharmaceutical research
pub_type: 杂志文章,已发布勘误
doi:10.1007/s11095-018-2463-9
更新日期:2018-07-25 00:00:00
abstract::A liposomal formulation of methylprednisolone (L-MPL) was developed to improve localization of this immunosuppressant in lymphatic tissues. Liposomes containing MPL were formulated from a mixture of phosphatydylcholine and phosphatydylglycerol (molar ratio, 9:1) and sized by extrusion through a 0.1-micron membrane. Ma...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1018954704886
更新日期:1993-10-01 00:00:00