Abstract:
PURPOSE:The low aqueous solubility of many drugs impedes detailed investigation as the detection limit of standard testing routines is limited. This is further complicated within application relevant thin films typical used in patches or stripes for buccal or topical routes. METHODS:In this work a model system is developed based on spin - casting technique allowing defined clotrimazole and clotrimazole - polystyrene composite films preparation at a solid surface. Various highly sensitive techniques including quarz crystal microbalance (QCM), X-ray reflevtivity (XRR) and X-ray photon spectroscopy (XPS) are used to investigate the drug release over time into an aqueous media. RESULTS:The results reveal a steady drug release for both samples over the course of the experiments but with the release from the composite being significantly slower. In addition the dissolution rate of the clotrimazole sample initially increases up to 30 min after which a decrease is noted. XRR shows that this is a result of surface roughening together with film thickness reduction. The results for the composite show that the release in the composite film is a result of drug diffusion within the matrix and collapsing PS film thickness whereby XPS shows that the amount of clotrimazole at the surface after 800 min immersion is still high. CONCLUSION:It can be stated that the applied techniques allow following low mass drug release in detail which may also be applied to other systems like pellets or surface loaded nano-carriers providing information for processing and application relevant parameters.
journal_name
Pharm Resjournal_title
Pharmaceutical researchauthors
Ehmann HM,Winter S,Griesser T,Keimel R,Schrank S,Zimmer A,Werzer Odoi
10.1007/s11095-014-1368-5subject
Has Abstractpub_date
2014-10-01 00:00:00pages
2708-15issue
10eissn
0724-8741issn
1573-904Xjournal_volume
31pub_type
杂志文章abstract::The binding of diflunisal to hydroxypropyl-beta-cyclodextrin (HP beta CD), bovine serum albumin (BSA), human serum albumin (HSA), normal human plasma, and mixed solutions of HP beta CD/protein was studied at 25 degrees C, pH 7.4, by potentiometry using an electrode selective to diflunisal. The experimental data for di...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1018901912619
更新日期:1994-01-01 00:00:00
abstract:PURPOSE:Heparin immobilized porous poly(D,L-lactic-co-glycolic acid) (PLGA) microspheres were prepared for sustained release of basic fibroblast growth factor (bFGF) to induce angiogenesis. MATERIALS AND METHODS:Porous PLGA microspheres having primary amine groups on the surface were prepared using an oil-in-water (O/...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-006-9039-9
更新日期:2006-08-01 00:00:00
abstract:PURPOSE:A theory and computer programs running on Microsoft Excel for Windows for calculation of solution pH, buffer formula, and buffer capacity at a given ionic strength and temperature were developed. The theory does not limit the category of buffer components, the number of buffer components, or the number of ioniz...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1012037819211
更新日期:1997-03-01 00:00:00
abstract::Recently a new in vivo approach in man, using a regional intestinal perfusion technique, has been developed. The perfusion tube consists of a multichannel tube with two inflatable balloons, which are placed 10 cm apart. The tube is introduced orally and the time required for insertion and positioning of the tube is ap...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1015888813741
更新日期:1992-10-01 00:00:00
abstract::Although much effort has been devoted to opioid research since the identification of enkephalins, understanding of the physiological importance and mechanisms of action of endogenous opioids lags behind understanding of opiate alkaloids such as morphine. In recent years, several novel approaches have been refined with...
journal_title:Pharmaceutical research
pub_type: 杂志文章,评审
doi:10.1023/a:1015809702296
更新日期:1991-01-01 00:00:00
abstract::The absorption of insulin across the vaginal mucosa into the systemic circulation was studied in ovariectomized rats given subsequent estrogen treatment. Blood glucose levels were determined as an indirect measure of insulin absorption, and the effect of various enhancers on the hypoglycemic response was investigated....
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1015892630637
更新日期:1992-07-01 00:00:00
abstract::Cyclosporine (CsA) is commercially available for oral administration as a solution in olive oil with alcohol and an emulsifier. To improve its variable absorption and low patient acceptability, several oral formulations were prepared and tested in vitro and in vivo in dogs. A tablet formulation prepared by direct comp...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1015815614959
更新日期:1991-04-01 00:00:00
abstract::The effect of different concentrations of polyvinyl alcohol 14000 and 72000 (PVA 14 and 72) on the activity of betamethasone and phenylephrine hydrochloride in the rabbit eye was investigated. The polymer of higher molecular weight exerts a more pronounced effect at relatively lower viscosities. Effects on the intraoc...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/A:1016398915965
更新日期:1986-08-01 00:00:00
abstract::Knowledge Management (KM) is a key enabler for achieving quality in a lifecycle approach for production of biopharmaceuticals. Due to the important role that it plays towards successful implementation of Quality by Design (QbD), an analysis of KM solutions is needed. This work provides a comprehensive review of the in...
journal_title:Pharmaceutical research
pub_type: 杂志文章,评审
doi:10.1007/s11095-016-2043-9
更新日期:2017-02-01 00:00:00
abstract:PURPOSE:The lack of water-solubility hampers the use of many potent pharmaceuticals. Polymeric micelles are self-assembled nanocarriers with versatile properties that can be engineered to solubilize, target, and release hydrophobic drugs in a controlled-release fashion. Unfortunately, their large-scale use is limited b...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/b:pham.0000029284.40637.69
更新日期:2004-06-01 00:00:00
abstract:PURPOSE:To analyze the effects of chemical enhancers and iontophoresis on the buccal transmucosal delivery of lidocaine and nicotine. METHODS:Porcine oral mucosal samples were pretreated with chemical enhancers before conducting 8-hr Franz diffusion-cell experiments. In studies addressing the influence of iontophoresi...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-011-0636-x
更新日期:2012-04-01 00:00:00
abstract:PURPOSE:Cell penetrating peptides (CPPs) were widely used as motifs for drug delivery to tumor. In former study, an RGD reverse sequence dGR was used to develop active-targeting liposome R8dGR-Lip, which showed well penetrating ability and treatment efficiency on glioma model. However, recurrence after tumor resection ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-018-2399-0
更新日期:2018-04-26 00:00:00
abstract:PURPOSE:The aim of the present study was to design a new mucosal drug delivery system composed of liposomes dispersed within a bioadhesive hydrogel containing methyl-beta-cyclodextrin (Me(beta)CD) for controlled drug release. METHODS:A hydrophilic model molecule, inulin, was encapsulated within positively charged and ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-005-4591-2
更新日期:2005-06-01 00:00:00
abstract::The effects of skin storage, skin preparation, skin pretreatment with a penetration enhancer, and skin barrier removal by adhesive tape-stripping on the concurrent cutaneous transport and metabolism of nitroglycerin (GTN) have been studied in vitro using hairless mouse skin. Storing the skin for 10 days at 4 degrees C...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1015822431178
更新日期:1992-03-01 00:00:00
abstract:PURPOSE:The structure-function relationship and mechanism of polycations as gene carriers have attracted considerable research interest in recent years. The present study was to investigate the relationship between polycation chain length and transfection efficiency (RCL-TE), and the corresponding mechanism by O-methyl...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-013-1211-4
更新日期:2014-04-01 00:00:00
abstract:PURPOSE:The purpose of this study was to obtain an in vitro/in vivo correlation for the sustained release of a protein from poly(ethylene glycol) terephthalate (PEGT)/poly(butylene terephthalate) (PBT) microspheres. METHODS:Radiolabeled lysozyme was encapsulated in PEGT/PBT microspheres via a water-in-oil-in-water emu...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/B:PHAM.0000019303.12086.d1
更新日期:2004-03-01 00:00:00
abstract:PURPOSE:To investigate the suitability of three antimicrobial peptides (AMPs) as cell-penetrating antimicrobial peptides. METHODS:Cellular uptake of three AMPs (PK-12-KKP, SA-3 and TPk) and a cell-penetrating peptide (penetratin), all 5(6)-carboxytetramethylrhodamine-labeled, were tested in HeLa WT cells and analyzed ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-014-1550-9
更新日期:2015-05-01 00:00:00
abstract:PURPOSE:Reverse micellar solutions of diclofenac sodium were encapsulated in soft gelatine capsules. On contact with aqueous media they exhibited an application induced transformation (AIT) into a semisolid system of liquid crystals (SSLC) which slows down drug release. The aim of the present paper was to study in vitr...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1012127829032
更新日期:1997-12-01 00:00:00
abstract::A method of immobilizing urokinase on albumin microspheres has been developed. Laser scattering, which was used to follow particle size from the initial emulsification stage to the final aqueous resuspension of the microsphere stage, showed that particle coalescence and crosslinking were critical parameters in manufac...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1015855622459
更新日期:1992-06-01 00:00:00
abstract::The pentahydrate (alpha form) of cefazolin sodium (CEZ) exhibited sharp X-ray diffraction peaks, while the dehydrated alpha form showed weak but distinct diffraction peaks. As expected the amorphous form exhibited a diffuse and halo diffraction pattern. The X-ray procedure to estimate the degree of crystallinity of CE...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1015984300692
更新日期:1988-07-01 00:00:00
abstract::Biotherapeutics, including recombinant or plasma-derived human proteins and antibody-based molecules, have emerged as an important class of pharmaceuticals. Aggregation and immunogenicity are among the major bottlenecks during discovery and development of biotherapeutics. Computational tools that can predict aggregati...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-011-0414-9
更新日期:2011-05-01 00:00:00
abstract:PURPOSE:To evaluate the impact of intestinal first-pass metabolism (Fg) by cytochrome P4503A (CYP3A) and uridine 5'-diphosphate-glucuronosyltransferases (UGT) on in vivo oral absorption of their substrate drugs. METHODS:CYP3A and UGT substrates were orally administered to portal-vein cannulated (PV) rats to evaluate t...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-014-1489-x
更新日期:2015-02-01 00:00:00
abstract:PURPOSE:In the present work, we developed water-in-oil (w/o) nanoemulsions for the intravesical administration of cisplatin. METHODS:The nanoemulsions were made up of soybean oil as the oil phase and Span 80, Tween 80, or Brij 98 as the emulsifier system. alpha-Terpineol and oleic acid were incorporated as permeation ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-009-9947-6
更新日期:2009-10-01 00:00:00
abstract::The in situ rat gut technique was used to study the effects of hypothermia on the intestinal absorption of a 1 mg/ml solution of sodium pentobarbital in 0.01 M phosphate buffer (pH 6.0). Male Sprague-Dawley rats weighing between 300 and 370 g were exposed to an atmosphere of helox (helium:oxygen, 80:20) at 0-4 degrees...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1016416413780
更新日期:1987-06-01 00:00:00
abstract:PURPOSE:To investigate whether conjunctival epithelial cells express transport processes for opioid peptides. METHODS:We monitored the uptake of [(3)H]deltorphin II and [(3)H]DADLE, two hydrolysis-resistant synthetic opioid peptides, in the rabbit conjunctival epithelial cell line CJVE and elucidated the characteristi...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-008-9709-x
更新日期:2009-05-01 00:00:00
abstract::Animal models are used commonly in various stages of drug discovery and development to aid in the prospective assessment of drug-drug interaction (DDI) potential and the understanding of the underlying mechanism for DDI of a drug candidate. In vivo assessments in an appropriate animal model can be very valuable, when ...
journal_title:Pharmaceutical research
pub_type: 杂志文章,评审
doi:10.1007/s11095-010-0157-z
更新日期:2010-09-01 00:00:00
abstract:PURPOSE:Several phenomena in tablets indicate that an inhomogeneous pore distribution is formed during the compaction process. Examples are lamination and the capping of corners. In order to gain an understanding of the relation between structure and compact properties, analyzing the structure in a location dependent m...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-005-5280-x
更新日期:2005-08-01 00:00:00
abstract::This paper describes an investigation of the use of poly(lactic/glycolic acid) polymers for long-term delivery of high molecular weight, water-soluble proteins. Poly(lactic/glycolic acid) (PLGA) microspheres, containing (fluorescein isothiocyanate)-labeled bovine serum albumin and (fluorescein isothiocyanate)-labeled ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1015841715384
更新日期:1991-06-01 00:00:00
abstract::The release of lithium carbonate incorporated into polymethylmethacrylate, polyvinyl chloride, hydrogenated vegetable oil, and carbomer matrix tablets was studied in vitro. The formulation containing 10% carbomer showed a sustained-release profile comparable to that of a standard, commercially available, sustained-rel...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1015863204732
更新日期:1990-04-01 00:00:00
abstract::Physicochemical effects caused by intestinal fluids on drugs in the gastrointestinal (GI) tract can be a contributing factor in food induced changes in bioavailability. To identify physicochemical properties of gemfibrozil that may be altered by endogenous and dietary lipids, in vitro studies were conducted in model s...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1018967401000
更新日期:1994-12-01 00:00:00