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 emulsion. Three microsphere formulations varying in copolymer composition were administered subcutaneously to rats. The blood plasma was analyzed for radioactivity content representing released lysozyme at various time points post-dose. The in vitro release was studied in phosphate-buffered saline. RESULTS:The encapsulation efficiency, calculated from the radioactivity in the outer water phase of the emulsion, varied from 60-87%. Depending on the PEG segment length and wt% PEGT, the lysozyme was released completely in vitro within 14 to 28 days without initial burst. 14C-methylated lysozyme could be detected in the plasma over the same time courses. The in vitro/in vivo correlation coefficients obtained from point-to-point analysis were greater than 0.96 for all microsphere formulations. In addition, less then 10% of administered radioactivity remained at dose site at 28 days for the microsphere formulations, indicating no notable retention of the protein at the injection site. CONCLUSION:The in vitro release in phosphate-buffered saline and the in vivo release in rats showed an excellent congruence independent of the release rate of 14C-methylated lysozyme from PEGT/PBT microspheres.
journal_name
Pharm Resjournal_title
Pharmaceutical researchauthors
van Dijkhuizen-Radersma R,Wright SJ,Taylor LM,John BA,de Groot K,Bezemer JMdoi
10.1023/B:PHAM.0000019303.12086.d1subject
Has Abstractpub_date
2004-03-01 00:00:00pages
484-91issue
3eissn
0724-8741issn
1573-904Xjournal_volume
21pub_type
杂志文章abstract:PURPOSE:Herein we report the discovery of a group of derivatized alpha-amino acids that increase the oral bioavailability of sodium cromolyn. METHODS:We prepared three N-acylated alpha-amino acids and used these compounds to demonstrate the oral delivery of cromolyn in an in vivo rat model. In vitro experiments, inclu...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1016034913181
更新日期:1996-02-01 00:00:00
abstract:PURPOSE:Generalizations based upon behavior of small molecules have established that a crystalline solid is generally much more stable toward chemical degradation than is the amorphous solid. This study examines the validity of this generalization for proteins using biosynthetic human insulin as the model protein. MET...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1012164520429
更新日期:1997-10-01 00:00:00
abstract:PURPOSE:To synthesize a trifluorinated bile acid that can be used for (19)F magnetic resonance imaging (MRI) of bile acid enterohepatic circulation, characterize its in vitro transporter affinity, stability, and (19)F-MRI signal, and assess its ability to concentrate in the gallbladder of C57BL/6 mice. METHODS:Target ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-012-0963-6
更新日期:2013-05-01 00:00:00
abstract:PURPOSE:To investigate the properties of phenylboronic acid-functional poly(amido amine) polymers (BA-PAA) in forming multilayered thin films with poly(vinyl alcohol) (PVA) and chondroitin sulfate (ChS), and to evaluate their compatibility with COS-7 cells. METHODS:Copolymers of phenylboronic acid-functional poly(amid...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-015-1688-0
更新日期:2015-09-01 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:PURPOSE:We have evaluated a new process, involving solution-enhanced dispersion by supercritical fluids (SEDS), for the production of polymeric microparticles. METHODS:The biodegradable polymers, Poly (DL-lactide-co-glycolide): copolymer composition 50:50 (DL-PLG), Poly (L-lactide) (L-PLA), Poly (DL-lactide) (DL-PLA) ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1018868423309
更新日期:1999-05-01 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:PURPOSE:To study the physical and release properties of different molecular weight (MW) pH- and temperature-responsive statistical terpolymers and beads of N-isopropylacrylamide (NIPAAm), butylmethacrylate (BMA) and acrylic acid (AA). METHODS:Random terpolymers of varying MW were synthesized with NIPAAm/BMA/AA of feed...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1018813700535
更新日期:1999-06-01 00:00:00
abstract:PURPOSE:The aim was to replace the traditional 21-day Caco-2 permeability protocol by a more high-throughput assay. METHODS:Caco-2 cells were seeded at high density in 96-well plates in novel cell culture boxes. After 7 days, drug permeability studies were performed. Samples were analyzed by a new UV detection method....
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/b:pham.0000008043.71001.43
更新日期:2003-12-01 00:00:00
abstract:PURPOSE:The present investigation describes a formulative study for the development of innovative drug delivery systems for bromocriptine. METHODS:Solid lipid nanoparticles (SLN) based on different lipidic components have been produced and characterized. Morphology and dimensional distribution have been investigated b...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-007-9514-y
更新日期:2008-07-01 00:00:00
abstract:PURPOSE:Short linear peptides have a high potential for delivering various drugs with therapeutic potential, including nucleic acids. Recently, we have shown that the cationic amphipathic histidine-rich peptide LAH4 (KKALLALALHHLAHLALHLALALKKA) possesses high plasmid DNA delivery capacities. Since such peptides are tho...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-010-0138-2
更新日期:2010-07-01 00:00:00
abstract::Unsymmetrical aryl(heteroaryl)methyl isopropyl ester analogues of nifedipine, in which the 2-nitrophenyl group at C-4 is replaced by a 2- or 3-pyridyl substituent, were synthesized and evaluated as calcium-channel antagonists using guinea pig ileal longitudinal smooth muscle. The point of attachment of the C-4 pyridyl...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1015941706008
更新日期:1990-09-01 00:00:00
abstract::The technique of Affinity capillary electrophoresis (ACE) is a useful tool to characterize complexation and partition equilibria. A wide range of applications in pharmaceutics has been presented: the determination of pKA values, of association constants between drugs and cyclodextrins or amphiphilic compounds as well ...
journal_title:Pharmaceutical research
pub_type: 杂志文章,评审
doi:
更新日期:1999-11-01 00:00:00
abstract::Primaquine, an 8-aminoquinoline antimalarial, is shown to undergo unexpectedly rapid aromatic proton exchange with the medium. At a pH less than 4, the exchange of C-5 is so fast as to be unmeasurable by proton nmr methods. At a pH of 6-6.5 the half-time for exchange is 4 to 5 minutes. This unexpectedly high rate of e...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/A:1016356926714
更新日期:1984-07-01 00:00:00
abstract:PURPOSE:To investigate the potential of a novel lipid carrier, comprising beads of alpha-cyclodextrin and soybean oil, for topical drug delivery. Adapalene was chosen as a model drug to explore the ability of the beads to encapsulate and release a highly lipophilic compound. MATERIALS AND METHODS:Adapalene-loaded bead...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-007-9395-0
更新日期:2008-02-01 00:00:00
abstract:PURPOSE:The intratumoral heterogeneity observed in breast cancer (BC), in particular with regard to cell surface receptor expression, can hinder the success of many targeted cancer therapies. The development of novel therapeutic agents that target more than one receptor can overcome this inherent property of tumors and...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-019-2684-6
更新日期:2020-01-21 00:00:00
abstract::The transient dynamic swelling and dissolution behavior during the release of a growth hormone releasing peptide, [D-Trp2-D-Phe5]GHRP, from erodible, non-cross-linked poly(methyl methacrylate-co-methacrylic acid) (PMMA/MAA) beads has been investigated at pH 7.4 as a function of buffer concentration. Although the swell...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1018902404036
更新日期:1993-07-01 00:00:00
abstract::A new transdermal therapeutic system (TTS) for nitroglycerin is presented that controls release of the active substance by means of desorption and diffusion. The drug release, in the dosage range examined under sink conditions, is independent of electrolytes and pH of the aqueous acceptor medium, but it does depend on...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/A:1016361921803
更新日期:1985-01-01 00:00:00
abstract:PURPOSE:We investigated optimum formulation characteristics in the nasal absorption of salmon calcitonin (sCT) by incorporation of acylcarnitines. METHODS:Nasal sCT formulations were administered to anesthetized rats. Plasma calcium level was measured and pharmacological bioavailability (P.bioav) was calculated. RESU...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1016051600828
更新日期:1996-05-01 00:00:00
abstract:PURPOSE:Basal insulins with improved kinetic properties can potentially be produced using acylation by fatty acids that enable soluble, high-molecular weight complexes to form post-injection. A series of insulins, acylated at B29 with fatty acids via glutamic acid spacers, were examined to deduce the structural require...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-012-0739-z
更新日期:2012-08-01 00:00:00
abstract:PURPOSE:There is evidence that cholesterol affects the ATPase and transport functions of P-glycoprotein (P-gp). To study the influence of cholesterol on P-gp in a well defined lipid environment, we reconstituted P-gp in egg phosphatidylcholine (PhC) and PhC/cholesterol proteoliposomes with negligible residual amounts o...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-007-9326-0
更新日期:2007-11-01 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:A pattern fitting procedure using X-ray powder diffraction patterns was applied to study the crystallization kinetics of amorphous griseofulvin. From the optimized parameters obtained by pattern fitting, a change in the quantity and quality of griseofulvin crystals with crystallization was also investigated. M...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-006-9204-1
更新日期:2007-05-01 00:00:00
abstract:PURPOSE:Cannabinoids have been associated with tumor regression and apoptosis of cancer cells. Recently, we have shown that R(+)-methanandamide (R(+)-MA) induces apoptosis of H4 human neuroglioma cells via a mechanism involving de novo expression of the cyclooxygenase-2 (COX-2) enzyme. The present study investigated a ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-005-8815-2
更新日期:2006-01-01 00:00:00
abstract:PURPOSE:The objective of this study was to evaluate the in vivo consequences of glycyl-glutamate coadministration on gabapentin oral absorption. METHODS:Rats were administered gabapentin (10 mg/kg plus radiotracer) by gastric gavage, in the absence and presence of dipeptides, and by intravenous administration. Serial ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-007-9272-x
更新日期:2007-08-01 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::Prinomide tromethamine, a nonsteroidal antiinflammatory drug, was orally administered at doses of 250, 500, and 1000 mg every 12 hr for 28 days to healthy male volunteers. The pharmacokinetic behavior of prinomide and its primary plasma metabolite displayed nonlinear characteristics, while those of free prinomide and ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1018916811904
更新日期:1993-01-01 00:00:00
abstract::The stability of an antibiotic formulation (clindamycin phosphate in dextrose), which is stable at room temperature, was assessed by nonisothermal kinetic analysis at elevated temperatures. A preliminary study, conducted to establish apparent rate order, verified the appropriateness of a first-order kinetic model. The...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1015840320410
更新日期:1991-05-01 00:00:00
abstract:PURPOSE:In this study we aimed to evaluate adaptive designs (ADs) by clinical trial simulation for a pharmacokinetic-pharmacodynamic model in oncology and to compare them with one-stage designs, i.e., when no adaptation is performed, using wrong prior parameters. METHODS:We evaluated two one-stage designs, ξ0 and ξ*, ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-015-1693-3
更新日期:2015-10-01 00:00:00
abstract:PURPOSE:A Selegiline Transdermal System (STS) is under development for indications which may not be optimally or safely treated with oral selegiline. Studies were conducted to evaluate the in vitro penetration and skin metabolism of selegiline in order to better understand the toxicological findings and the observed pl...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1012051300130
更新日期:1997-01-01 00:00:00