The apparent solubilizing capacity of simulated intestinal fluids for poorly water-soluble drugs.

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 Technol

authors

Schwebel HJ,van Hoogevest P,Leigh ML,Kuentz M

doi

10.3109/10837451003664099

subject

Has Abstract

pub_date

2011-06-01 00:00:00

pages

278-86

issue

3

eissn

1083-7450

issn

1097-9867

journal_volume

16

pub_type

杂志文章
  • In vitro release of colchicine using poly(phosphazenes): the development of delivery systems for musculoskeletal use.

    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

    authors: Ibim SM,el-Amin SF,Goad ME,Ambrosio AM,Allcock HR,Laurencin CT

    更新日期:1998-02-01 00:00:00

  • Development of an effective liposomal cholesterol ester transfer protein (CETP) vaccine for protecting against atherosclerosis in rabbit model.

    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

    authors: Aghebati T,Arabsalmani M,Mohammadpour AH,Afshar M,Jaafari MR,Abnous K,Nazemi S,Badiee A

    更新日期:2020-04-01 00:00:00

  • About the equivalence between different batches of a glycopeptide drug.

    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

    authors: Boix-Montañes A,Garcia-Arieta A

    更新日期:2016-08-01 00:00:00

  • Dissolution rate enhancement by adsorption of poorly soluble drugs on hydrophilic silica aerogels.

    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

    authors: Smirnova I,Suttiruengwong S,Seiler M,Arlt W

    更新日期:2004-11-01 00:00:00

  • Silk fibroin nanoparticles for enhanced bio-macromolecule delivery to the retina.

    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

    authors: Yang P,Dong Y,Huang D,Zhu C,Liu H,Pan X,Wu C

    更新日期:2019-06-01 00:00:00

  • Solid-state characterization of fluconazole.

    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

    authors: Alkhamis KA,Obaidat AA,Nuseirat AF

    更新日期:2002-11-01 00:00:00

  • Waxy corn starch: a potent cofiller in pellets produced by extrusion-spheronization.

    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

    authors: Junnila R,Palviainen P,Heinämäki J,Myllärinen P,Forssell P,Yliruusi J

    更新日期:2000-01-01 00:00:00

  • Novel sustained-release fast-disintegrating multi-unit compressed tablets of lornoxicam containing Eudragit RS coated chitosan-alginate beads.

    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

    authors: Aburahma MH,Hamza Yel-S

    更新日期:2011-08-01 00:00:00

  • Robustness testing in pharmaceutical freeze-drying: inter-relation of process conditions and product quality attributes studied for a vaccine formulation.

    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

    authors: Schneid SC,Stärtzel PM,Lettner P,Gieseler H

    更新日期:2011-11-01 00:00:00

  • Encapsulation of plai oil/2-hydroxypropyl-β-cyclodextrin inclusion complexes in polyvinylpyrrolidone (PVP) electrospun nanofibers for topical application.

    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

    authors: Tonglairoum P,Chuchote T,Ngawhirunpat T,Rojanarata T,Opanasopit P

    更新日期:2014-06-01 00:00:00

  • A measurement of the unstirred aqueous boundary layer in a Franz diffusion cell.

    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

    authors: Miller MA,Kasting G

    更新日期:2012-11-01 00:00:00

  • Formulation and processing factors influencing the adhesion of film coats to tablet cores.

    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

    authors: Khan H,Fell JT,Macleod GS

    更新日期:2005-01-01 00:00:00

  • Co-solvent solubilization of some poorly-soluble antidiabetic drugs.

    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

    authors: Seedher N,Kanojia M

    更新日期:2009-01-01 00:00:00

  • The solution, solid state stability and kinetic investigation in degradation studies of lercanidipine: study of excipients compatibility of lercanidipine.

    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

    authors: Parmar N,Amin S,Singla N,Kohli K

    更新日期:2012-11-01 00:00:00

  • Evaluation of disintegrating time of rapidly disintegrating tablets by a paddle method.

    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

    authors: Que L,Wu W,Cheng X,Hu T

    更新日期:2006-01-01 00:00:00

  • Development and in vivo evaluation of baicalin-loaded W/O nanoemulsion for lymphatic absorption.

    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

    authors: Xu Q,Zhou A,Wu H,Bi Y

    更新日期:2019-11-01 00:00:00

  • Relating formulation variables to in vitro dissolution using an artificial neural network.

    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

    authors: Ebube NK,McCall T,Chen Y,Meyer MC

    更新日期:1997-08-01 00:00:00

  • Casein hydrolysate as a rapid and/or enteric dissolving additive for oral drugs.

    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

    authors: Imai T,Nishiyama T,Shameem M,Otagiri M

    更新日期:1998-05-01 00:00:00

  • Physicochemical stability of bioadhesive thermoresponsive platforms for methylene blue and hypericin delivery in photodynamic therapy.

    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

    authors: Borghi-Pangoni FB,Junqueira MV,Bruschi ML

    更新日期:2020-04-01 00:00:00

  • Interaction of [D-Trp6, Des-Gly10] LHRH ethylamide and hydroxy propyl beta-cyclodextrin (HPbetaCD): thermodynamics of interaction and protection from degradation by alpha-chymotrypsin.

    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

    authors: Koushik KN,Bandi N,Kompella UB

    更新日期:2001-11-01 00:00:00

  • Application of Design Expert for the investigation of capsaicin-loaded microemulsions for transdermal delivery.

    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

    authors: Duangjit S,Chairat W,Opanasopit P,Rojanarata T,Ngawhirunpat T

    更新日期:2016-09-01 00:00:00

  • A proposal for a drug product Manufacturing Classification System (MCS) for oral solid dosage forms.

    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

    authors: Leane M,Pitt K,Reynolds G,Manufacturing Classification System (MCS) Working Group.

    更新日期:2015-01-01 00:00:00

  • Conjugates of TAT and folate with DOX-loaded chitosan micelles offer effective intracellular delivery ability.

    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

    authors: Zhang S,Liu Y,Gan Y,Qiu N,Gu Y,Zhu H

    更新日期:2019-02-01 00:00:00

  • Stability of Octastatin, a somatostatin analog cyclic octapeptide, in aqueous solution.

    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

    authors: Jang SW,Woo BH,Lee JT,Moon SC,Lee KC,DeLuca PP

    更新日期:1997-11-01 00:00:00

  • Phase transition of a microemulsion upon addition of cyclodextrin - applications in drug delivery.

    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

    authors: Thakur SS,Solloway J,Stikkelman A,Seyfoddin A,Rupenthal ID

    更新日期:2018-02-01 00:00:00

  • In vitro/in vivo correlation and modeling of emitted dose and lung deposition of inhaled salbutamol from metered dose inhalers with different types of spacers in noninvasively ventilated patients.

    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

    authors: Hussein RRS,M A Ali A,Salem HF,Abdelrahman MM,Said ASA,Abdelrahim MEA

    更新日期:2017-11-01 00:00:00

  • The prediction of variability occurring in fluidized bed coating equipment. I. The measurement of particle circulation rates in a bottom-spray fluidized bed coater.

    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

    authors: Cheng XX,Turton R

    更新日期:2000-01-01 00:00:00

  • The absorption of (99m)Tc-alendronate given by rectal route in rabbits.

    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

    authors: Asikoğlu M,Ozguney I,Ozcan I,Orumlu O,Guneri T,Koseoğlu K,Ozkilic H

    更新日期:2008-01-01 00:00:00

  • Formulation and evaluation of meloxicam niosomes as vesicular carriers for enhanced skin delivery.

    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

    authors: El-Menshawe SF,Hussein AK

    更新日期:2013-07-01 00:00:00

  • Dry adsorbed emulsion of simvastatin: optimization and in vivo advantage.

    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

    authors: Dixit RP,Nagarsenker MS

    更新日期:2007-01-01 00:00:00