Abstract:
:Drug solubility testing in biorelevant media has become an indispensable tool in pharmaceutical development. Despite this importance, there is still an incomplete understanding of how poorly soluble compounds interact with these media. The aim of this study was to apply the concept of the apparent solubilization capacity to fasted and fed state simulated intestinal fluid (FaSSIF and FeSSIF, respectively). A set of non-ionized poorly soluble compounds was studied in biorelevant media prepared from an instantly dissolving complex (SIF(™) Powder) at 37°C. The values of the solubilization capacity were different between FaSSIF and FeSSIF but correlated. Drug inclusion into the mixed micelles was highly specific for a given compound. The ratio of the FeSSIF to FaSSIF solubility was in particular considered and discussed in terms of the apparent solubilizing capacity. The apparent solubilization concept appears to be useful for the interpretation of biorelevant solubility tests. Further studies are needed to explore acidic and basic drugs.
journal_name
Pharm Dev Technoljournal_title
Pharmaceutical development and technologyauthors
Schwebel HJ,van Hoogevest P,Leigh ML,Kuentz Mdoi
10.3109/10837451003664099subject
Has Abstractpub_date
2011-06-01 00:00:00pages
278-86issue
3eissn
1083-7450issn
1097-9867journal_volume
16pub_type
杂志文章abstract::A colchicine release system utilizing biodegradable poly(phosphazenes) was investigated in vitro for intra-articular administration. Polymer degradation and drug release studies were performed on colchicine-loaded poly(phosphazenes) containing either imidazolyl (I-PPHOS) or ethyl glycinato (EG-PPHOS) side chain substi...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.3109/10837459809028479
更新日期:1998-02-01 00:00:00
abstract::Clinical trials of cholesterol ester transfer protein (CETP) peptide vaccine were stopped after disappointing results in humans due to the inadequacy of adjuvant aluminum hydroxide in stimulating the immune response against the self-antigen of CETP. To increase the efficacy of the CETP vaccine, we developed a novel li...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.1080/10837450.2019.1706181
更新日期:2020-04-01 00:00:00
abstract:CONTEXT:Teicoplanin is a glycopeptide antibiotic consisting of a combination of different active components. Clinical equivalence between different batches of this drug is not guaranteed by the present pharmacopeial specification of chemical composition based on an HPLC chromatogram. OBJECTIVE:To test a modification o...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.3109/10837450.2015.1035726
更新日期:2016-08-01 00:00:00
abstract::The aim of this work is to evaluate the feasibility of hydrophilic silica aerogels as drug carriers and to investigate the influence of the aerogels properties on the release rate of poorly water-soluble drugs. Hydrophilic silica aerogels of different densities were loaded with two model drugs, ketoprofen and griseofu...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.1081/pdt-200035804
更新日期:2004-11-01 00:00:00
abstract::The aim of this study was to investigate intravitreal injection of silk fibroin nanoparticles (SFNs) encapsulating bio-macromolecules, achieving enhanced drug bioavailability, and extended retention in retina. SFNs were prepared with regenerated silk fibroin using desolvation method with fluorescein isothiocyanate lab...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.1080/10837450.2018.1545236
更新日期:2019-06-01 00:00:00
abstract::Two polymorphs and three solvates of fluconazole were isolated and characterized by x-ray powder diffractometry, IR spectroscopy, differential scanning calorimetry (DSC), thermogravimetry, and their dissolution rates. The different forms were prepared by crystallization of the original powder in different solvents at ...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.1081/pdt-120015052
更新日期:2002-11-01 00:00:00
abstract::The purpose of this study was to assess the usefulness of waxy corn (maize) starch as a cofiller and diluent in pellets produced by aqueous extrusion-spheronization. Waxy corn starch was combined with microcrystalline cellulose (MCC) in the range of 20-50% of the entire composition. Pellets containing ordinary corn st...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.1081/pdt-100100521
更新日期:2000-01-01 00:00:00
abstract::Novel fast-disintegrating multi-unit tablets (FDMUTs) were prepared to modify the release of lornoxicam (a potent non-steroidal anti-inflammatory drug with a short half-life) as well as to combine the advantages of multi-unit systems with the cost-effectiveness of compressed tablets. The proposed FDMUTs consisted of s...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.3109/10837451003692595
更新日期:2011-08-01 00:00:00
abstract:CONTEXT:The recent US Food and Drug Administration (FDA) legislation has introduced the evaluation of the Design Space of critical process parameters in manufacturing processes. In freeze-drying, a "formulation" is expected to be robust when minor deviations of the product temperature do not negatively affect the final...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.3109/10837450.2011.581287
更新日期:2011-11-01 00:00:00
abstract::The aim of this study was to prepare electrospun polyvinylpyrrolidone (PVP)/2-hydroxypropyl-β-cyclodextrin (HPβCD) nanofiber mats and to incorporate plai oil (Zingiber Cassumunar Roxb.). The plai oil with 10, 20 and 30% wt to polymer were incorporated in the PVP/HPβCD solution and electrospun to obtain nanofibers. The...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.3109/10837450.2013.788659
更新日期:2014-06-01 00:00:00
abstract::The unstirred aqueous boundary layer (ABL) thickness was determined for modified Franz diffusion cells using three test compounds--parathion, 4-hexylresorcinol, and 2,4-dinitrochlorobenzene (DNCB). Steady-state fluxes through one, two, and three dialysis membranes in series were achieved in donor-saturated, infinite-d...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.3109/10837450.2011.572895
更新日期:2012-11-01 00:00:00
abstract::The effect of six factors: spray gun, formulation, inlet temperature, atomizing air pressure, fan air pressure, and gun-bed distance, on the final adhesion of the film coat to the tablet core were assessed. The method used was based on an experimental design, Resolution IV, that allowed the main effects to be free fro...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.1081/pdt-49692
更新日期:2005-01-01 00:00:00
abstract::Co-solvent solubilization approach has been used to enhance the solubility of seven antidiabetic drugs: gliclazide, glyburide, glipizide, glimepiride, repaglinide, pioglitazone, and roziglitazone. Solubility in water, phosphate buffer (pH 7.4), six co-solvent solutions prepared in water as well as phosphate buffer (pH...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.1080/10837450802498894
更新日期:2009-01-01 00:00:00
abstract::The objectives of this research were to evaluate the stability of lercanidipine in solution state and solid state and explore the compatibility of drug with oils, surfactants and cosurfactants as excipients. The effect of pH on the degradation in solution state was studied through pH-rate profile of lercanidipine in c...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.3109/10837450.2011.580758
更新日期:2012-11-01 00:00:00
abstract::A paddle method for measurement of the disintegrating time of orally disintegrating tablets with rizatriptan benzoate as a model drug was evaluated. The paddle method employed a dissolution test assembly with tablets immersed in disintegrating medium through a fastened sinker. Paddle stirring rate, opening of the sink...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.1080/10837450600767649
更新日期:2006-01-01 00:00:00
abstract::Background: Lymphatic formations that effectively eradicate the virus in the lymphatic system will be therapeutically advantagous in hepatitis B virus (HBV) infection. Lipid-based formulation is often used to deliver drug via the lymphatic system. Baicalin nanoemulsion may be a promising drug delivery system for impro...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.1080/10837450.2019.1646757
更新日期:2019-11-01 00:00:00
abstract::The purpose of this paper was to investigate the effect of several experimental variables on the ability of a neural network to predict in vitro dissolution rate as a function of product formulation changes. Neural network software was trained with sets of hypothetical and experimental data consisting of 4-15 formulat...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.3109/10837459709031442
更新日期:1997-08-01 00:00:00
abstract::Two types of casein hydrolysates, casein A (mean peptide length 3.3) and casein B (mean peptide length 17.4) were prepared by the enzymatic hydrolysis of casein, and their effects on in vitro dissolution rates and oral bioavailability of drugs were evaluated. The in vitro dissolution behavior of the kneaded mixture of...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.3109/10837459809028499
更新日期:1998-05-01 00:00:00
abstract::Hypericin (Hyp), a natural hydrophobic and photoactive pigment, and methylene blue (MB), a hydrophilic cationic dye, are utilized as photosensitizer (PS) for photodynamic therapy of cancer. Bioadhesive and thermoresponsive polymeric systems can improve the drug availability by increasing the contact time between the s...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.1080/10837450.2019.1711394
更新日期:2020-04-01 00:00:00
abstract:PURPOSE:The purpose of this study is to investigate the mechanisms and thermodynamics of the interaction between hydroxypropyl beta-cyclodextrin (HPdetaCD) and [D-Trp6, des-Gly10] LHRH ethylamide (deslorelin), a peptide drug. METHODS:We used UV and fluorescence spectroscopy to study the interaction of HPbetaCD and des...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.1081/pdt-120000297
更新日期:2001-11-01 00:00:00
abstract::Our previous study reported that the Design Expert® Software showed a beneficial role in the development of microemulsions (ME) for transdermal drug delivery. To fully confirm the reproducibility and the reliability of simultaneous optimal ME formulations, the optimal ME formulations predicted by the Design Expert® So...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.3109/10837450.2015.1048552
更新日期:2016-09-01 00:00:00
abstract::This paper proposes the development of a drug product Manufacturing Classification System (MCS) based on processing route. It summarizes conclusions from a dedicated APS conference and subsequent discussion within APS focus groups and the MCS working party. The MCS is intended as a tool for pharmaceutical scientists t...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章,评审
doi:10.3109/10837450.2014.954728
更新日期:2015-01-01 00:00:00
abstract::The key for better antitumor efficacy is to improve the specificity of antitumor drugs for tumor cells and diminish their cytotoxicity to normal tissues. Targeted nanoparticles as antitumor drug delivery system can resolve this problem. In this study, we prepared folate and TAT (arginine-rich cell-penetrating peptide)...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.1080/10837450.2018.1469147
更新日期:2019-02-01 00:00:00
abstract::In this study, the degradation of Octastatin, a cyclic octapeptide analog of somatostatin, was examined as a function of pH, temperature, buffer, and ionic strength by reversed-phase gradient high-performance liquid chromatography. Degradation of Octastatin followed a first-order kinetics. Various buffer species such ...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.3109/10837459709022640
更新日期:1997-11-01 00:00:00
abstract::This study reports on the impact of cyclodextrin addition on the phase behavior of microemulsion systems. Three distinct oil-in-water microemulsions were formulated and subjected to increasing concentrations of various cyclodextrins. The prepared formulations underwent visual, textural and microscopic characterization...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.1080/10837450.2017.1371191
更新日期:2018-02-01 00:00:00
abstract::Substituting spacer by another in noninvasive ventilation (NIV) involves many variables, e.g. total emitted dose (TED), mass median aerodynamic diameter (MMAD), type of spacer, total lung deposition and total systemic absorption, which must be adjusted to ensure patient optimum therapy. Data mining based on artificial...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.3109/10837450.2015.1116567
更新日期:2017-11-01 00:00:00
abstract::The purpose of this work was to investigate the effect that changes in design and process variables had on the movement of particles around a fluidized bed coating apparatus. To measure the mean and variance of the particle cycle time distribution (CTD), the number of passages taken by a magnetic tracer particle throu...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.1081/pdt-100100546
更新日期:2000-01-01 00:00:00
abstract::Alendronate sodium (ALD) is a bisphosphonate medication used in the treatment and prevention of osteoporosis. Absorption of ALD as oral formulation is very poor (0.5%-1%). Its bioavailability can decrease with food effect. It has some gastrointestinal adverse effects such as gastritis, gastric ulcer, and esophagitis. ...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.1080/10837450801949509
更新日期:2008-01-01 00:00:00
abstract:CONTEXT:Skin delivery of Meloxicam (MX) offers several advantages over the oral route which is associated with potential side effects. OBJECTIVES:The aim of this study was to develop transdermal MX in niosomes. MATERIALS AND METHODS:Vesicles prepared by thin film hydration method were characterized and the acute anti...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.3109/10837450.2011.598166
更新日期:2013-07-01 00:00:00
abstract::In the present study, Simvastatin was incorporated in emulsion of soybean oil and propylene glycol monocaprylate as oily phase and Tween 80 and Cremophor EL as surfactants and also their mixtures. Dry adsorbed emulsions were prepared by using colloidal silicon dioxide in varying proportions to adsorb the liquid emulsi...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.1080/10837450701557246
更新日期:2007-01-01 00:00:00