Abstract：
:The objective of this study was to investigate the effect of the physiological parameters (pH, buffer capacity, and ionic strength) of the gastrointestinal (GI) fluid on the dissolution behavior of the class II weakly acidic (BCS class IIa) drug valsartan. A series of in vitro dissolution studies was carried out on Diovan® immediate release tablets using media that cover the physiological range of pH (1.2-7.8), buffer capacity (0-0.047 M/ΔpH), and ionic strength (0-0.4 mol/L) of the GI fluid during fasted and fed states using the conventional USP II apparatus. Valsartan exhibited pH- and buffer capacity-dependent dissolution behavior, where valsartan release was slow and incomplete in media simulating gastric fluid with low pH, and fast and complete in media simulating intestinal fluid with high pH. In addition, the rate of valsartan release increased with increasing the buffer capacity of the dissolution medium. In water and NaCl solutions, valsartan release was incomplete and the dissolution profiles were similar regardless of the ionic strength of the medium, indicating an ionic strength-independent dissolution behavior. These results highlight the significant effect of the physiological parameters of the GI fluid on the dissolution behavior of BCS class IIa drugs.
journal_name
Pharm Dev Technoljournal_title
Pharmaceutical development and technologyauthors
Hamed Rdoi
10.1080/10837450.2018.1536996subject
Has Abstractpub_date
2018-12-01 00:00:00pages
1168-1176issue
10eissn
1083-7450issn
1097-9867journal_volume
23pub_type
杂志文章abstract：:The investigation was aimed at developing thermodynamically stable topical delivery system of nanostructured lipid carrier of econazole nitrate (EN) for the treatment of deep seated fungal infection by improving its permeability. Fifteen formulations (F1-F15) of nanostructured lipid carriers (NLCs) were prepared by so...
journal_title：Pharmaceutical development and technology
pub_type： 杂志文章
doi：10.3109/10837450.2012.659256
更新日期：2013-05-01 00:00:00
abstract：:The current work aimed to develop low-density gastroretentive sponges loaded with alfuzosin HCl (ALF) to sustain the rate of drug release, improve its oral bioavailability and deliver it to the main site of absorption. Sponges were developed, according to a 23 full factorial design, by compression of the lyophilized A...
journal_title：Pharmaceutical development and technology
pub_type： 杂志文章
doi：10.1080/10837450.2020.1720235
更新日期：2020-06-01 00:00:00
abstract：:In pediatrics, it is crucial to ameliorate the unpleasant taste of oral pharmaceutical formulations in order to facilitate patient compliance. Scientists' attempt to develop modern products for children is included among the new trends in pharmaceutical technology. Designing the preparation procedures and selecting th...
journal_title：Pharmaceutical development and technology
pub_type： 杂志文章
doi：10.1080/10837450.2019.1609499
更新日期：2020-01-01 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：:The principal purpose of the present study was to prepare and characterize a complex drug delivery system consisting of Nafarelin-poly (3-hydroxybutyrate-co-3-hydroxyvalerate) (PHBV) nanoparticles (NPs) in combination with sodium alginate/poloxamer 407 in situ gel. Nafarelin-loaded PHBV NPs were prepared via double em...
journal_title：Pharmaceutical development and technology
pub_type： 杂志文章
doi：10.1080/10837450.2017.1321662
更新日期：2018-02-01 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：:Orally dissolving tablets (ODTs) represent one of the recent advances in drug delivery. The foremost objective of this study was to optimize the utilization of lubricant sodium stearyl fumarate in the preparation of dextromethorphan hydrobromide ODTs with enhanced taste-masking properties. The simple blending of sodiu...
journal_title：Pharmaceutical development and technology
pub_type： 杂志文章
doi：10.1080/10837450.2019.1579228
更新日期：2019-07-01 00:00:00
abstract：:Dynamic image analysis (DIA) was used to measure particle diameter (D50) of in-process samples removed during fluid bed coating. A single, rapid measurement gave D50 to within 4 mum. Samples removed at intervals of 2% weight gain were readily distinguishable by DIA and by their drug release profiles. Drug release was ...
journal_title：Pharmaceutical development and technology
pub_type： 杂志文章
doi：10.1080/10837450600770072
更新日期：2006-01-01 00:00:00
abstract：:Mefenamic acid (MA), a poorly water-soluble drug, was used as a model substance to investigate granules and tablet characteristics to be optimized for the loading volume of MA (0-74.1% v/v) in the formulation including lactose monohydrate/maize starch (7/3) as excipients. The compactibility of granules increased with ...
journal_title：Pharmaceutical development and technology
pub_type： 杂志文章
doi：10.1080/10837450701702941
更新日期：2008-01-01 00:00:00
abstract：:Pharmaceutical aerosols have the potential to prevent pulmonary infectious diseases. Liposomal amphotericin B (LAMB, Ambisome, Astellas Pharma US, Deerfield, IL, USA) is approved as an intravenous infusion for empiric treatment of presumed fungal infections in neutropenic, febrile patients, as well as patients infecte...
journal_title：Pharmaceutical development and technology
pub_type： 杂志文章
doi：10.3109/10837450.2011.591803
更新日期：2011-11-01 00:00:00
abstract：:This study investigates the physicochemical properties of glycyl-histidyl-lysine-copper (GHK-Cu) to support the development of a formulation for effective topical delivery. The solubility and distribution coefficients (log D) were investigated using conventional methods and GHK concentrations were quantified with a va...
journal_title：Pharmaceutical development and technology
pub_type： 杂志文章
doi：10.3109/10837450.2014.979944
更新日期：2016-03-01 00:00:00
abstract：:This study examines the effect of the degree of methoxylation (DM) and particle size on compression properties and compactibility of pectin powders. A powder classification system based on sequential handling of compression parameters was applied. A single size fraction (90-125 μm) of pectin powders with DM values ran...
journal_title：Pharmaceutical development and technology
pub_type： 杂志文章
doi：10.3109/10837450.2010.535831
更新日期：2012-05-01 00:00:00
abstract：PURPOSE:BMS-196843 (Oncostatin M) is a therapeutic recombinant protein in development. Scale-up process changes led to unexpected instability of the bulk drug substance solution during storage. A product with an apparent higher MW than the parent protein was observed by the size-exclusion chromatography (SEC). This stu...
journal_title：Pharmaceutical development and technology
pub_type： 杂志文章
doi：10.1081/pdt-100002202
更新日期：2001-01-01 00:00:00
abstract：:Fixed dose combination (FDC) products are common in the treatment of hypertension, diabetes, human immunodeficiency virus, and tuberculosis. They make it possible to combine two or more drug molecules with different modes of pharmacological actions in a single dosing unit and optimize the treatment. From a patient per...
journal_title：Pharmaceutical development and technology
pub_type： 杂志文章,评审
doi：10.3109/10837450.2012.660699
更新日期：2013-11-01 00:00:00
abstract：:Mechanically generated radicals were shown to affect short-term stability of a model pharmaceutical formulation during high-shear processing. A formulation containing an oxidatively sensitive drug, either amorphous or crystalline, and a polymeric excipient was high-shear mixed and the resulting short-term degradation ...
journal_title：Pharmaceutical development and technology
pub_type： 杂志文章
doi：10.1080/10837450802328869
更新日期：2008-01-01 00:00:00
abstract：:The first-line therapy for moderate to severe benign prostatic hyperplasia is the oral therapy by alfuzosin hydrochloride. Unfortunately, the oral therapy of alfuzosin is associated with several route-specific systemic side-effects. The current study was aimed to develop a prototype transdermal patch system for alfuzo...
journal_title：Pharmaceutical development and technology
pub_type： 杂志文章
doi：10.3109/10837450.2010.522585
更新日期：2012-03-01 00:00:00
abstract：:The purpose of this research was to prepare various injectable, protein (cytochrome c)-loaded biodegradable poly(lactide-co-glycolide) (PLGA) devices by a novel microencapsulation method and to compare their characteristics. Syringeable mixtures of polymer and protein solidified upon injection when coming in contact w...
journal_title：Pharmaceutical development and technology
pub_type： 杂志文章
doi：10.1081/pdt-100100535
更新日期：2000-01-01 00:00:00
abstract：CONTEXT:Development and evaluation of thermosensitive and bioadhesive liquid suppositories containing ketoprofen (KP). OBJECTIVE:This study was conducted to develope thermosensitive and bioadhesive liquid suppositories containing KP using poloxamer and different bioadhesive polymers and to investigate their gelation t...
journal_title：Pharmaceutical development and technology
pub_type： 杂志文章
doi：10.3109/10837450.2013.846373
更新日期：2014-12-01 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：: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：:To improve the solubility and bioavailability of oridonin (ORI), glycerol monooleate lipid (GMO)- or phytantriol (PYT)-Poloxamer 407-propylene glycol-water systems were firstly used to develop cubosomes containing ORI for oral delivery. These cubosomes prepared through the fragmentation of bulk gels under homogenizati...
journal_title：Pharmaceutical development and technology
pub_type： 杂志文章
doi：10.3109/10837450.2015.1121496
更新日期：2017-05-01 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：:The objective of this study was to prepare pellets of thyme (Thymus vulgaris L.), stinging nettle (Urtica dioica L.) and sage (Salvia officinalis L.) dry extracts by extrusion-spheronization technique to improve technological properties and investigate dissolution profiles of pellets covered different levels of pH-sen...
journal_title：Pharmaceutical development and technology
pub_type： 杂志文章
doi：10.3109/10837450.2014.920355
更新日期：2015-11-01 00:00:00
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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：: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：: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：: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：:Quality by design (QbD) is an essential part of the modern approach to pharmaceutical quality. This study was conducted in the framework of a QbD project involving ramipril tablets. Preliminary work included identification of the critical quality attributes (CQAs) and critical process parameters (CPPs) based on the qu...
journal_title：Pharmaceutical development and technology
pub_type： 杂志文章
doi：10.3109/10837450.2012.705294
更新日期：2013-02-01 00:00:00
abstract：:An osmotic-controlled pulsatile delivery technology was developed for targeted drug delivery. This novel system consists of a tablet core surrounded by an osmotic coating that has been mechanically compromised in strategic locations to facilitate reliable drug release at a given time point after administration. The ta...
journal_title：Pharmaceutical development and technology
pub_type： 杂志文章
doi：10.1080/10837450902838692
更新日期：2009-01-01 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
