Abstract:
:The effect of some processing and formulation variables on the stability of tablets containing a crystalline salt of a triazine derivative was studied. The salt has a relatively low melting point and a low microenvironmental pH due to the weakly basic nature of the parent compound (pKa = 4.0). This compound decomposes through acid-catalyzed hydrolysis. A full factorial design was used to study the effect of three variables on tablet stability: aqueous wet granulation, ball milling of the salt and filler prior to manufacturing, and the inclusion of sodium carbonate in the formulation as a pH modifier. In addition to the factorial design experiments, a batch of tablets was prepared by wet granulation, using sodium bicarbonate as the pH modifier. Stability of the drug in tablets was evaluated at 40 degrees C/75% relative humidity (RH) and at 40 degrees C/ambient humidity. Stability of tablets was adversely affected by wet granulation. However, stability was greatly improved by wet granulation in the presence of sodium carbonate. While sodium carbonate enhanced drug stability in the tablets, regardless of the manufacturing process, wet granulated tablets were more stable than tablets containing sodium carbonate and prepared without wet granulation. Similarly prepared tablets by using sodium bicarbonate were remarkably less stable compared with those containing sodium carbonate. The use of sodium bicarbonate as a pH modifier resulted in only marginal enhancement of tablet stability, suggesting that a higher microenvironmental pH than that provided by sodium bicarbonate is needed to maximize stability. Despite the low lattice energy of the salt and the potential for disruption of salt crystallinity by mechanical stress, milling did not appear to have an adverse effect on tablet stability under the current experimental conditions. This study shows that selection of the proper manufacturing process, in conjunction with the appropriate pH modifier, could be critical to dosage form stability.
journal_name
Pharm Dev Technoljournal_title
Pharmaceutical development and technologyauthors
Badawy S,Vickery R,Shah K,Hussain Mdoi
10.1081/pdt-200031417subject
Has Abstractpub_date
2004-08-01 00:00:00pages
239-45issue
3eissn
1083-7450issn
1097-9867journal_volume
9pub_type
杂志文章abstract::A comprehensive analytical solution that accounts for many factors and assumptions affecting drug concentration profile in the gastrointestinal tract was presented. A sensitivity analysis approach was utilized in order to investigate the importance of different parameters in the model. The partition coefficient is fou...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.1081/pdt-100000741
更新日期:2001-01-01 00:00:00
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 capac...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.3109/10837451003664099
更新日期:2011-06-01 00:00:00
abstract::The objective of this investigation was to formulate ocular inserts of gatifloxacin sesquehydrate to achieve controlled drug release. Drug reservoir was prepared using hydrophilic polymers, namely polyvinyl alcohol and polyvinyl pyrrolidone. The rate controlling membrane was prepared using hydrophobic ethyl cellulose ...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.3109/10837450.2010.502178
更新日期:2012-01-01 00:00:00
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::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
pub_type: 杂志文章
doi:10.1081/pdt-100101353
更新日期:1999-05-01 00:00:00
abstract::The present study was aimed to optimize capsulated unfolding type gastroretentive bilayer film constituting immediate release (IR) layer of amlodipine besylate and sustained release (SR) layer of atorvastatin calcium. A three-factor, three-level Box-Behnken-design was used to optimize bilayer film with dual-release ch...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.1080/10837450.2019.1705486
更新日期:2020-04-01 00:00:00
abstract::The interaction of 5-nitro-2-furfurilylidene benzhydrazide (5NFB), potential anti-trypanosomal compound, with micellar solutions was studied. The results indicated that 50 mug of 5NFB completely kills 20 million T. cruzi epimastigote cells within 3 days, whereas the same amount of benznidazole kills 30% of the cells a...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.1080/10837450701212727
更新日期:2007-01-01 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:INTRODUCTION:Theoretical models of the freeze-drying process are potentially useful to guide the design of a freeze-drying process as well as to obtain information not readily accessible by direct experimentation, such as moisture distribution and glass transition temperature, Tg, within a vial during processing. Previ...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.1081/pdt-35869
更新日期:2005-01-01 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::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::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::An anomalous peak was observed in the HPLC/UV analysis of a developmental drug product. High resolution LC/MS revealed that the mass of this degradant was 12 Da greater than the drug substance, corresponding to a net gain of a single carbon atom. The degradant was reproduced by incubating the drug substance with forma...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.3109/10837450.2012.696265
更新日期:2013-07-01 00:00:00
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 physical stability of amorphous solid dispersions (SDs) is influenced by their storage conditions. The goal of this work was to investigate the factors affecting the recrystallization of drugs in SDs after storage under conditions of high temperature and high humidity. SDs of three drugs (dipyridamole, nifedipine ...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.3109/10837450.2013.795168
更新日期:2014-06-01 00:00:00
abstract:BACKGROUND:Oxaliplatin has long been used for the treatment of colorectal cancer via intra-venous infusion. In order to improve patient compliance, a solid dosage form for oral administration of oxaliplatin was prepared as nano-sized particles. METHOD:Nano oxaliplatin was prepared employing Fat Employing Supercritical...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.3109/10837450.2010.531735
更新日期:2012-03-01 00:00:00
abstract::Poor solubility and bioavailability of drugs are often affected by its microscopic structural properties. Nitrofurantoin (NF), a Biopharmaceutics Classification System class II item, has a low water solubility with low plasma concentrations. To improve its therapeutic efficacy, formulation strategy of solid dispersion...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.1080/10837450.2019.1689401
更新日期:2020-02-01 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::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: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
pub_type: 杂志文章
doi:10.3109/10837450.2013.871028
更新日期:2015-01-01 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 ...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.1080/10837450601166494
更新日期:2007-01-01 00:00:00
abstract::The effect of chemical enhancers (e.g., fatty acids, limonene, depilatory lotions) and iontophoresis was investigated on the in vitro permeability of leuprolide acetate through porcine epidermis. Franz diffusion cells and Scepter iontophoretic power source were used for the percutaneous absorption studies. Anodal iont...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.1081/pdt-200032986
更新日期:2004-11-01 00:00:00
abstract::Drug release from hydroxypropyl methylcellulose (HPMC) hydrophilic matrix tablets is controlled by drug diffusion through the gel layer of the matrix-forming polymer upon hydration, matrix erosion or combination of diffusion and erosion mechanisms. In this study, the relationship between viscoelastic properties of the...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.1080/10837450.2016.1257022
更新日期:2018-11-01 00:00:00
abstract::The main purpose of this work was to study the albendazole-cyclodextrins complexation equilibrium and to propose a suitable excipient to improve the solubility behavior and dissolution rate of albendazole. The complexation of albendazole with four cyclodextrins, alpha-CD, beta-CD, gamma-CD, and hydroxypropylated (HP)-...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.3109/10837459809009867
更新日期:1998-08-01 00:00:00
abstract::The present study reports the solid-state properties of Fluvastatin sodium salt crystallized from different solvents for comparison with crystalline forms of the commercially available raw material and United States Pharmacopeia (USP) reference standard. Fluvastatin (FLV) samples were characterized by several techniqu...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.3109/10837450.2012.727000
更新日期:2013-03-01 00:00:00
abstract::The general solubility equation (GSE) is the state-of-the-art method for estimating the aqueous solubilities of organic compounds. It is an extremely simple equation that expresses aqueous solubility as a function of only two inputs: the octanol-water partition coefficient calculated by readily available softwares lik...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.1080/10837450.2017.1321663
更新日期:2018-09-01 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::Mucosa has now been recognized as a potential site for both local and systemic delivery of therapeutics. Mucoadhesive drug delivery systems with customizable release profiles have recently gained considerable interest among formulation scientists to improve clinical outcomes of drugs. This review summarizes the curren...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.1080/10837450.2020.1753771
更新日期:2020-09-01 00:00:00
abstract::Aqueous concentrated plain mixtures of dextran and concanavalin A (con A) were examined for their rheological response to glucose for comparison with previously studied partially photopolymerized acrylic derivatives. Non-destructive oscillatory tests were undertaken within the linear viscoelastic range to examine the ...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.3109/10837450903002181
更新日期:2010-01-01 00:00:00