Abstract：
PURPOSE:To prepare a thermoreversible gel system able to work as a medium for crystallization at around 20°C, allowing easy retrieval of crystals by simply decreasing the gel temperature. Lactose was selected has model substance for crystallization. METHODS:Water solutions with different% of poloxamer 407, α-Lactose monohydrate, and ethanol were prepared and analysed by rheology to understand how the different components alter the gelling temperature. The systems with the required characteristics for lactose crystallization were prepared and the crystals recovered by cooling and then filtering the dispersion. RESULTS:Rheological analysis showed interaction between the poloxamer and lactose. Increasing the quantity of poloxamer or lactose lowered the gelation temperature while the addition of small amounts of ethanol had a modest effect on the same property. These data were used to identify the ideal concentration of the components in order to prepare a system matching the features of our purpose. Such system yielded high quality crystals, with well-defined geometry and narrow particle size distribution. CONCLUSION:Poloxamer is a very interesting polymer in that it is able to generate a reversible gelling medium from which crystals can be harvested by filtering, without the addition of any chemicals to promote the sol-gel transition.
journal_name
Pharm Resjournal_title
Pharmaceutical researchauthors
Cespi M,Bonacucina G,Casettari L,Mencarelli G,Palmieri GFdoi
10.1007/s11095-011-0606-3subject
Has Abstractpub_date
2012-03-01 00:00:00pages
818-26issue
3eissn
0724-8741issn
1573-904Xjournal_volume
29pub_type
杂志文章abstract：:Primaquine (I), a 6-methoxy-8-aminoqumoline derivative used for the treatment of malaria has previously been shown to be metabolized to 8-(3-carboxy-l-methyl-propylamino)-6-methoxyquinoline by both micro-organisms and laboratory rats. Reported herein is the synthesis of this novel metabolite. ...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/A:1016311616719
更新日期：1984-03-01 00:00:00
abstract：PURPOSE:The objective of the present work was to prepare safe and effective Ciclosporin A Lipid nanocapsule (CsA-LNC) eye-drops for the treatment of DED. METHODS:The phase-inversion method was used to prepared different sizes CsA-LNC. CsA biodistribution in ocular after topical administration in rabbits was analyzed b...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-020-02872-2
更新日期：2020-07-14 00:00:00
abstract：PURPOSE:This study aims to conduct an impact investigation in the hydrophobic-hydrophilic balance as an important factor for dissolution improvement of a hydrophilic carrier-based solid dispersion system. METHODS:Polymeric carriers with different hydrophobic to hydrophilic ratios were used to prepare several electrosp...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-019-2734-0
更新日期：2020-01-07 00:00:00
abstract：PURPOSE:Pulmonary antibiotic delivery is recommended as maintenance therapy for cystic fibrosis (CF) patients who experience chronic infections. However, abnormally thick and sticky mucus present in the respiratory tract of CF patients impairs mucus penetration and limits the efficacy of inhaled antibiotics. To overcom...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-016-1921-5
更新日期：2016-08-01 00:00:00
abstract：PURPOSE:PHBHHx (poly(3-hydroxybutyrate-co-3-hydroxyhexanoate)) is an excellent biomaterial for tissue repair. Here, we aim to develop a PHBHHx-based three-dimensional (3D) scaffold system for sustained delivery of proteins (insulin serves as a model protein). METHODS:The insulin-phospholipid complex (INS-PLC) was prep...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-012-0944-9
更新日期：2013-04-01 00:00:00
abstract：PURPOSE:The aim of the study was to evaluate organogel nanoparticles as a lipophilic vehicle to increase the oral bioavailability of poorly soluble compounds. Efavirenz (EFV), a Biopharmaceutical Classification System (BCS) Class II, was used as drug model. METHODS:Organogel nanoparticles loaded with EFV were formulat...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-020-02808-w
更新日期：2020-05-11 00:00:00
abstract：PURPOSE:To investigate the effect of tyrphostin 8 (T-8), a GTPase inhibitor, on transferrin receptor (TfR)-mediated transcytosis of insulin-transferrin (In-Tf) conjugate in cultured enterocyte-like Caco-2 cells and on gastrointestinal (GI) absorption of In-Tf in streptozotocin (STZ)-induced diabetic rats. METHODS:Caco...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1011032502097
更新日期：2001-02-01 00:00:00
abstract：PURPOSE:This study aimed to investigate the impact of the size of X-ray iodinated contrast agent in nano-emulsions, on their toxicity and fate in vivo. METHODS:A new compound, triiodobenzoate cholecalciferol, was synthetized, formulated as nano-emulsions, and followed after i.v. administration in mice by X-ray imaging...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-015-1813-0
更新日期：2016-03-01 00:00:00
abstract：PURPOSE:Models to predict membrane-water partition coefficients (Kp) as a function of drug structure, membrane composition, and solution properties would be useful. This study explores the partitioning of dexamethasone (Dex) and its ionizable 21-phosphate (Dex-P) in liposomes varying in acyl chain length, physical stat...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-013-1143-z
更新日期：2013-12-01 00:00:00
abstract：PURPOSE:To test the hypothesis that coating particles with a highly bonding polymer is effective in improving tabletability of poorly compressible drugs. METHODS:Micronized acetaminophen (d (90) < 10 μm, Form I) was coated with 1%-10% (wt%) hydroxypropyl cellulose (HPC) by spray-drying. Phase nature of acetaminophen p...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-011-0518-2
更新日期：2011-12-01 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：:Magnetic nanoparticles are useful as contrast agents for magnetic resonance imaging (MRI). Paramagnetic contrast agents have been used for a long time, but more recently superparamagnetic iron oxide nanoparticles (SPIOs) have been discovered to influence MRI contrast as well. In contrast to paramagnetic contrast agent...
journal_title：Pharmaceutical research
pub_type： 杂志文章,评审
doi：10.1007/s11095-012-0711-y
更新日期：2012-05-01 00:00:00
abstract：PURPOSE:We evaluated the effect of luminal bacterial metabolism on intestinal absorption of azetirelin in rats. In vitro characteristics of bacterial metabolism of azetirelin were also investigated with the goal of overcoming the low stability of the peptidic drug against luminal microorganisms. METHODS:Plasma azetire...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1012141025938
更新日期：1997-08-01 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：:RNA interference (RNAi) strategies include double-stranded RNA (dsRNA), small interfering RNA (siRNA), short hairpin RNA (shRNA), and microRNA (miRNA). As this is a highly specific technique, efforts have been made to utilize RNAi towards potential knock down of disease-causing genes in a targeted fashion. RNAi has th...
journal_title：Pharmaceutical research
pub_type： 杂志文章,评审
doi：10.1007/s11095-011-0608-1
更新日期：2011-12-01 00:00:00
abstract：PURPOSE:Some patients are unable to generate the peak inspiratory flow rate (PIFR) necessary to de-agglomerate drug particles from dry powder inhalers (DPIs). In this study we tested the hypothesis that the acoustic parameters of an inhalation are related to the PIFR and hence reflect drug delivery. METHODS:A sensitiv...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-014-1371-x
更新日期：2014-10-01 00:00:00
abstract：PURPOSE:To prepare acylated exenatide analogues and investigate their biological properties for guiding the development of PLGA formulations of exenatide. METHODS:The acylated exenatide analogues were prepared by reaction with glycolic acid (GA), one constitutional unit of PLGA, and characterized by HPLC-MS/MS and Cir...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-014-1298-2
更新日期：2014-08-01 00:00:00
abstract：PURPOSE:In pharmacokinetic (PK)/pharmacodynamic (PD) modelling and simulations (M&S), omitting dropouts can cause inaccuracies in parameter estimation and clinical trial simulations (CTS). This study examines the impact of different imputation methods for missing data on the interpretation of model results, as well as ...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-014-1380-9
更新日期：2014-10-01 00:00:00
abstract：PURPOSE:The development of a physiologically based absorption model for orally administered drugs in rats is described. METHODS:Unlike other models that use a multicompartmental approach, the GI tract is modeled as a continuous tube with spatially varying properties. The mass transport through the intestinal lumen is ...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/b:pham.0000003373.72652.c0
更新日期：2003-11-01 00:00:00
abstract：PURPOSE:Labrasol and Gelucire 44/14 are defined admixtures of acylglycerols and PEG esters which are substrates for digestive lipases. METHODS:We investigated their in vitro gastrointestinal lipolysis to understand which compounds are, after digestion, responsible for keeping poorly water-soluble drugs in solution. Th...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-009-9906-2
更新日期：2009-08-01 00:00:00
abstract：:Various carboxylic acid esters of the N-hydroxymethyl derivative of N-benzyloxycarbonylglycine benzylamide, used as a peptide-like model, were prepared and their decomposition kinetics studied in aqueous solution and in human plasma solutions. These N-acyloxymethylamide derivatives were found to undergo a facile decom...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1015839426229
更新日期：1991-10-01 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
abstract：PURPOSE:To study the influence of solid form on the behavior of the salt siramesine hydrochloride in aqueous environments. METHODS:The solubilities and dissolution rates of siramesine hydrochloride anhydrate and monohydrate were determined at pH 3.4 and 6.4, and precipitates were examined by X-ray powder diffraction. ...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-008-9783-0
更新日期：2009-04-01 00:00:00
abstract：PURPOSE:The objective of this study was to develop and characterize long-circulating, biodegradable, and biocompatible nanoparticulate formulation as an intracellular delivery vehicle. METHODS:Poly(ethylene glycol) (PEG)-modified gelatin was synthesized by reacting Type-B gelatin with PEG-epoxide. The nanoparticles, p...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1016486910719
更新日期：2002-07-01 00:00:00
abstract：PURPOSE:The study was performed for clarifying the mechanism of interaction between indoxyl sulfate (IS), a typical uremic toxin bound to site II, and site I-ligands when bound to human serum albumin (HSA). The effect of the N to B transition on the interactions was also examined. METHODS:Quantitative investigation of...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1011014629551
更新日期：2001-04-01 00:00:00
abstract：:A simple viscometric method was used to quantify mucin-polymer bioadhesive bond strength. Viscosities of 15% (w/v) porcine gastric mucin dispersions in 0.1 N HCl (pH 1) or 0.1 N acetate buffer (pH 5.5) were measured with a Brookfield viscometer in the absence (eta m) or presence (eta t) of selected neutral, anionic, a...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1015812615635
更新日期：1990-05-01 00:00:00
abstract：PURPOSE:With the aim of developing multivalent vaccines for single-injection, we examined the feasibility of combining antigens in biodegradable microspheres. Such vaccines are expected to improve vaccination coverage by reducing the number of vaccination sessions required to generate immunity. METHODS:Mono- and multi...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1020354809581
更新日期：2002-09-01 00:00:00
abstract：PURPOSE:To address the problem of precipitation of a poorly soluble drug during dissolution of highly soluble cocrystals by preparing granules intimately mixed with a water-soluble polymer. METHODS:Effectiveness of polymers as precipitation inhibitors during the dissolution of carbamazepine-nicotinamide (CBZ-NCT) cocr...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-019-2622-7
更新日期：2019-04-23 00:00:00
abstract：PURPOSE:To determine the factors influencing "solid solubility" and phase separation kinetics of drugs from amorphous solid dispersions. METHODS:Solid dispersions of griseofulvin-poly(vinyl pyrrolidone) (PVP) and indoprofen-PVP were prepared using solvent evaporation technique. Dispersions demonstrating single Tg were...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-004-1882-y
更新日期：2005-03-01 00:00:00
abstract：:A method to provide near-constant sustained release of high molecular weight, water-soluble proteins from polyanhydride microspheres is described. The polyanhydrides used were poly(fatty acid dimer) (PFAD), poly(sebacic acid) (PSA), and their copolymers [P(FAD-SA)]. P(FAD-SA) microspheres containing proteins of differ...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1018929531410
更新日期：1993-04-01 00:00:00
