Abstract:
:The objective of this study was to compare the dissolution behavior of tablets prepared from solid dispersions with and without drug-carrier interactions. Diazepam and nifedipine were used as model drugs. Two types of carriers were used; polyvinylpyrrolidone (PVP K12, K30 and K60) and saccharides (inulin 1.8 kDa, 4 kDa and 6.5 kDa). Solid dispersions with various drug loads were prepared by lyophilization. It was found that the drug solubility in aqueous PVP solutions was significantly increased indicating the presence of drug-carrier interaction while the drug solubility was not affected by the saccharides indicating absence of drug-carrier interaction. X-ray powder diffraction and modulated differential scanning calorimetry revealed that all solid dispersions were fully amorphous. Dissolution behavior of solid dispersion tablets based on either the PVPs or saccharides was governed by both dissolution of the carrier and drug load. It was shown that a fast drug dissolution of solid dispersions with a high drug load could be obtained with carrier that showed interaction with the drug.
journal_name
Pharm Dev Technoljournal_title
Pharmaceutical development and technologyauthors
Srinarong P,Kouwen S,Visser MR,Hinrichs WL,Frijlink HWdoi
10.3109/10837450903286529subject
Has Abstractpub_date
2010-09-01 00:00:00pages
460-8issue
5eissn
1083-7450issn
1097-9867journal_volume
15pub_type
杂志文章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::Microgels were prepared by cinnamic acid-gelatin (type B) conjugate (CA-GelB) and cinnamic acid-Pluronic F127 conjugate (CA-Plur). (1)H NMR confirmed that CA was conjugated to gelatin and the gelatin to CA residue molar ratio was estimated to be 1:4.7 by a colorimetric method. CA-Plur of which the CA residue to Plur m...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.3109/10837450.2014.999787
更新日期:2016-01-01 00:00:00
abstract::This study explored the application of chitosan-alginate (CA) and chitosan-pectin (CP) complex films as drug release regulator for the preparation of multiunit controlled-release diclofenac sodium capsules. Pellets containing drug and microcrystalline cellulose, in a ratio of 3:5, were prepared in a fluidized rotary g...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.1081/pdt-100002247
更新日期:2001-08-01 00:00:00
abstract::Vardenafil hydrochloride (VAR) is an erectile dysfunction treating drug. VAR has a short elimination half-life (4-5 h) and suffers low oral bioavailability (15%). This work aimed to explore the dual potential of VAR-dendrimer complexes as drug release modulators and oral bioavailability enhancers. VAR-dendrimer comple...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.1080/10837450.2018.1472611
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abstract::The formulation of betamethasone-17-valerate (BV) into topical medicines presents a significant challenge for the formulation chemist. The substance is susceptible to acid and base catalyzed isomerization in aqueous environments, which results in valerate transesterification from carbon 17 to carbon 21 of the steroid ...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.3109/10837450.2016.1143003
更新日期:2017-06-01 00:00:00
abstract::Ternary complexes of meloxicam (ML), a poorly water-soluble anti-inflammatory drug, with β-cyclodextrin (βCD) and polyethylene glycol (PEG) 6000 were prepared from an equimolar (ML-βCD) and 10% of PEG. Characterization of the ternary complex was carried out by differential scanning calorimetry and X-ray diffractometry...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.3109/10837450.2011.565347
更新日期:2012-09-01 00:00:00
abstract::The object of this study was to enhance the solubility, dissolution rate, and oral bioavailability of rutin by complexation with 2-hydroxypropyl-beta-cyclodextrin (HP-beta-CyD). The interaction of rutin with cyclodextrins (CyDs) was evaluated by the solubility, and ultraviolet (UV) and circular dichroism (CD) spectrop...
journal_title:Pharmaceutical development and technology
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doi:10.1081/pdt-100100556
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abstract::Purpose: Intestinal drug absorption is one of the main factors that govern the fraction of oral dose absorbed (Fa) of drugs. It is reported that oral absorption of bortezomib (BTZ) can be restricted by its low intestinal permeability. In this study, we aimed to evaluate the impact of self-nanoemulsifying drug delivery...
journal_title:Pharmaceutical development and technology
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更新日期:2020-03-01 00:00:00
abstract::In this study, chlorhexidine-loaded poly(ε-caprolactone) nanospheres (CHX-NS) were prepared and successfully coated on the urinary catheters. Properties of CHX-NS were evaluated including drug loading content and the nanosphere size. Effects of different lyoprotectants for long-term storage of CHX-NS were also investi...
journal_title:Pharmaceutical development and technology
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doi:10.1080/10837450.2018.1502317
更新日期:2019-04-01 00:00:00
abstract::Letrozole (LTZ), an aromatase inhibitor used for the treatment of hormonally-positive breast cancer in postmenopausal women, has poor water solubility, rapid metabolism, and a range of side effects. In this study, polymer-based nanoparticles (NPs) incorporating the drug have been designed and characterized, aimed to c...
journal_title:Pharmaceutical development and technology
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doi:10.1080/10837450.2018.1455698
更新日期:2019-02-01 00:00:00
abstract::We have proposed a theory indicating the correlation between the dissolution rate and the heat of solution of drug substances. The initial dissolution rates of the drug substances containing amorphous were predicted accurately from their heats of solution. In this report, the possibility for the theory to estimate the...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.1081/pdt-120002234
更新日期:2002-01-01 00:00:00
abstract::The objective of this study was to develop a floating, pulsatile, multiparticulate drug delivery system intended for chronopharmacotherapy of arthritis. The floating pulsatile drug delivery has the advantage that a drug can be released in the upper gastrointestinal tract after a definite time period of no drug release...
journal_title:Pharmaceutical development and technology
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doi:10.1080/10837450903095334
更新日期:2010-03-01 00:00:00
abstract::A novel flavonoid-polysaccharide conjugate was synthesized by free radical grafting of quercetin on starch. The covalent insertion of quercetin in the polymeric chain was confirmed by FT-IR, DSC and fluorescence analyses, while an estimation of the amount of quercetin bound per g of polymer was obtained by the Folin-C...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.3109/10837450.2010.546413
更新日期:2012-07-01 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
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更新日期:2020-04-01 00:00:00
abstract::The hygroscopicity of Brequinar sodium, an organ transplant immunosuppressant, at 75% relative humidity highly depends on the crystal form or crystallinity of the drug substance. Hygroscopicity and ease of water uptake of three lots of Brequinar sodium were investigated. Those lots contained different impurities at le...
journal_title:Pharmaceutical development and technology
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doi:10.3109/10837459609031417
更新日期:1996-04-01 00:00:00
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journal_title:Pharmaceutical development and technology
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doi:10.3109/10837450.2014.949268
更新日期:2015-01-01 00:00:00
abstract::The aim of this study was to prepare a highly porous multiparticulate dosage form containing cilostazol for gastroretentive drug delivery. The floating pellets were prepared with glyceryl behenate as a matrix former and camphor as a sublimating agent by extrusion/spheronization and sublimation under vacuum. Granules p...
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更新日期:2018-06-01 00:00:00
abstract::The aim of this study was to prepare various types of solid dispersions (SDs) by the hot-melt extrusion technique. Next, process analytical technology (PAT) such as Fourier transform-infrared (FT-IR) and Raman and near infrared (NIR) spectroscopy were applied to determine the solubilization effect. The SDs and its tab...
journal_title:Pharmaceutical development and technology
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更新日期:2020-06-01 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
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更新日期:2008-01-01 00:00:00
abstract:CONTEXT:Freeze-drying in presence of excipients is a common practice to stabilize biomacromolecular formulations. The composition of this formulation is known to affect the quality of the final product. OBJECTIVE:The aim of this study was to evaluate freeze-drying in well-plates as a high throughput platform for formu...
journal_title:Pharmaceutical development and technology
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doi:10.3109/10837450.2013.871028
更新日期:2015-01-01 00:00:00
abstract::A new approach to developing a drug-polymer mixed coat for highly water-soluble diltiazem pellets was investigated at different coating levels. Drug layering and the coating procedures were performed using a bottom spray fluidized bed coater. Drug pellets were coated with Eudragit NE40 (NE40) alone and in combination ...
journal_title:Pharmaceutical development and technology
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更新日期:2006-02-01 00:00:00
abstract::The purpose of this study was a comparative evaluation of miniaturized vs. University of Minnesota's (i.e., U of Minn. = Hiestand's) procedures for determining the tensile strength, indentation hardness, and bonding index (BI), one out of three Indices of Tableting Performance (ITP). Tableting properties of six direct...
journal_title:Pharmaceutical development and technology
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更新日期:2003-08-01 00:00:00
abstract::The aim of the present investigation was to develop and study topical gel delivery of curcumin for its anti-inflammatory effects. Carbopol 934P (CRB) and hydroxypropylcellulose (HPC) were used for the preparation of gels. The penetration enhancing effect of menthol (0-12.5% w/w) on the percutaneous flux of curcumin th...
journal_title:Pharmaceutical development and technology
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doi:10.1080/10837450802409438
更新日期:2009-01-01 00:00:00
abstract::In this study, we designed a polymersome system for the controlled release of methotrexate (MTX) as an anticancer drug with the objective of improving the loading efficiency of the drug in polymersomes as well as achievement of an efficient control on the release rate of drug from nanocarriers. We synthesized mono met...
journal_title:Pharmaceutical development and technology
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更新日期:2019-01-01 00:00:00
abstract::The physicochemical properties and enzymatic stability of esters of phenylephrone, synthesized on the basis of the chemical delivery system (CDS) concept, were studied as a new class of mydriatic agents. Potentiometrically determined ionization constants (pKa) of the novel compounds were in the range 7.19-7.21. The th...
journal_title:Pharmaceutical development and technology
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doi:10.1081/pdt-100101353
更新日期:1999-05-01 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
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更新日期:2019-11-01 00:00:00
abstract::The objective of the present work is to investigate the presence or absence of a critical concentration of maize starch according to the percolation theory for a truly ternary system with respect to a minimum disintegration time. The results of this study show that the application of percolation theory is not limited ...
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更新日期:2007-01-01 00:00:00
abstract::Stability of captopril in a controlled release formulation has been a challenge for some time. The sustained release of captopril from floating matrices has been studied varying the antioxidant load, the sodium bicarbonate proportion and the compaction pressure. Although in many cases the effect of compaction pressure...
journal_title:Pharmaceutical development and technology
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doi:10.1080/10837450903110737
更新日期:2009-07-22 00:00:00
abstract::The biopharmaceutical assessment of new drug candidates based on their chemical structure is important in drug discovery and development. The scope of this study is to focus on lipophilic drugs and to clarify the role of their chemical predictors on oral bioavailability in humans. First their chemical properties were ...
journal_title:Pharmaceutical development and technology
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doi:10.1080/10837450802626296
更新日期:2009-01-01 00:00:00
abstract::The purpose of this study was to develop a benchtop apparatus to simulate the scale-up of the moist-heat sterilization process of sodium carboxymethylcellulose (CMC) gel and identify critical process parameters that affect the sterilized gel viscosity. A 600-ml benchtop Parr reactor was modified and used to achieve go...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.1081/pdt-100101394
更新日期:1999-01-01 00:00:00