Abstract:
CONTEXT AND OBJECTIVE:The objective of the study was to develop a stable capsule formulation of ziprasidone hydrochloride which can be administered without regards to food intake. MATERIALS AND METHODS:The unstable anhydrous form of ziprasidone hydrochloride was stabilized employing hot-melt extrusion and further optimized by 32 central composite design. The formulation was optimized after establishing acceptable ranges for response variables like disintegration time, dissolution and impurity profile. A crossover fasted and fed in vivo study was conducted in human volunteers to assess the food-effect of optimized formulation vis-à-vis the marketed brand. RESULTS AND DISCUSSION:The optimized formulation met in-house specifications for various response variables. Further, high values of correlation coefficient vouch the adequate selection of experimental design and its high prognostic ability. In our study, no significant difference was observed between the Cmax and AUC values after administration of the optimized formulation in fasted and fed states. On the contrary, there was a statistically significant increase in the Cmax and AUC values after oral administration of Zeldox in fed state in comparison to fasted state. CONCLUSIONS:The present study describes the successful development of a stable formulation of 20 mg of ziprasidone devoid of any food-effects.
journal_name
Pharm Dev Technoljournal_title
Pharmaceutical development and technologyauthors
Banerjee S,Shankar KR,Prasad Y Rdoi
10.3109/10837450.2015.1055764subject
Has Abstractpub_date
2016-11-01 00:00:00pages
775-786issue
7eissn
1083-7450issn
1097-9867journal_volume
21pub_type
杂志文章abstract::ABSTRCT Felodipine has been widely used as a poorly water-soluble model drug for various studies to improve its oral bioavailability and in vivo efficacy. In this study, we developed amorphous solid dispersions (ASDs) via spray drying to enhance the bioavailability of felodipine through using natural zein protein as a...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.1080/10837450.2020.1809456
更新日期:2020-12-01 00:00:00
abstract::The present study was aimed to develop a matrix-type transdermal formulation of pentazocine using mixed polymeric grades of Eudragit RL/RS. The possible interaction between drug and polymer used were characterized by FTIR, DSC and X-RD. X-RD study indicates a change of state of drug from crystalline to amorphous in th...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.3109/10837450903188501
更新日期:2010-06-01 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::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
abstract::The purpose of this research was to design and develop a novel controlled-release bead formulation for oral administration with buffer crystals as a carrier for loading of fenoldopam mesylate, an intravenous antihypertensive agent, which provides an in vitro release rate of 30-50 mg/hr for 6-8 hr. Buffer crystals were...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.3109/10837459809028629
更新日期:1998-11-01 00:00:00
abstract::A carbopol 934P-based drug delivery system (AmDDS) was developed to achieve the dual-controlled delivery of Nonoxynol-9 (N-9), a spermicidal agent, and EDTA, a potentiator of spermicidal activity. This gel-type system made intimate contact with vaginal mucosa and maintained an effective drug concentration within the v...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.3109/10837459609029888
更新日期:1996-07-01 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 objective of this study was to develop and evaluate a novel microemulsion based gel formulation containing tazarotene for targeted topical therapy of acne. Psudoternary phase diagrams were constructed to obtain the concentration range of oil, surfactant, and co-surfactant for microemulsion formation. The optimized...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.3109/10837450.2015.1081610
更新日期:2016-12-01 00:00:00
abstract::The present study details the development of a small-scale spray-drying approach for the routine screening of amorphous solid dispersions (ASDs). This strategy aims to overcome the limitations of standard screening methodologies like solvent casting and quench cooling to predict drug-polymer miscibility of spray-dried...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.1080/10837450.2018.1534861
更新日期:2019-06-01 00:00:00
abstract::A novel analytical procedure has been developed for quantitative determination of levodopa and carbidopa in aqueous binary solutions acidified by HCl and without any other sample pretreatment. The method is based partially on least squares treatment of data obtained by attenuated total reflectance Fourier transform in...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.1080/10837450701481249
更新日期:2007-01-01 00:00:00
abstract::The purpose of this study was to improve the sensitivity and accuracy of quantitative analysis of polymorphic mixtures. Various techniques such as hand grinding and mixing (in mortar and pestle), air jet milling and ball milling for micronization of particle and mixing were used to prepare binary mixtures. Using these...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.3109/10837450903286511
更新日期:2010-09-01 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::Drug-excipient compatibility studies lay the foundation for designing a chemically stable formulation for clinical and commercial development. This article describes the investigation of oxidative degradation encountered with compound A (a phenylalanine-drug complex) in a capsule dosage form. Two wet- granulation caps...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.1080/10837450903182140
更新日期:2009-01-01 00:00:00
abstract::The objective of the study was to develop a mathematical model for predicting the disintegration time of fast disintegrating tablets (FDTs) by estimating the powder characteristics of powder blend prior to compression. A combination of chitosan-alginate complex and glycine in the ratio of 50:50 was used for preparing ...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.3109/10837450903479996
更新日期:2011-02-01 00:00:00
abstract::The compendial method of evaluation of orodispersible tablets (ODT) is the same disintegration test as for conventional tablets. Since it does not reflect the disintegration process in the oral cavity, alternative methods are proposed that are more related to in vivo conditions, e.g. modified dissolution paddle appara...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.3109/10837450.2012.710238
更新日期:2013-03-01 00:00:00
abstract::The instability of protein and antigen(s) during encapsulation in biodegradable polymers by water-in-oil-in-water (w/o/w) encapsulation is well established. The aim of present study is to screen various additives to prevent the inactivation and loss of immunogenicity of HBsAg upon its exposure to the water/CH(2)Cl(2) ...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.3109/10837450.2010.546408
更新日期:2012-07-01 00:00:00
abstract::Bupivacaine lipid microparticles were prepared and evaluated as a parenteral sustained-release dosage form for postoperative pain management. Bupivacaine free base was incorporated into a molten tristearin matrix and lipid micro-particles were subsequently formed from this molten mixture by a spray-congealing process....
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.1081/pdt-54475
更新日期:2005-01-01 00:00:00
abstract::Magnesium stearate (MgSt) is a widely used pharmaceutical lubricant in tablet manufacturing. However, batch-to-batch variability in hydrate form and surface area can lead to inconsistency in tablet performance. In this work, several unique MgSt samples were studied: traditional monohydrate samples with high surface ar...
journal_title:Pharmaceutical development and technology
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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: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: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::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::A redox-responsive docetaxel (DTX) prodrug consisting of a disulfide linkage between DTX and vitamin E (DTX-SS-VE) was synthesized in our laboratory and was successfully formulated into liposomes. The aim of this study was to optimize the formulation and investigate the cellular uptake of DTX prodrug-loaded liposomes ...
journal_title:Pharmaceutical development and technology
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doi:10.1080/10837450.2017.1287728
更新日期:2018-01-01 00:00:00
abstract::The utility of microcalorimetry as a rapid screening tool for assessing the solution stability of high molecular weight pharmaceutical proteins was evaluated by using model recombinant antibodies, Protein I and Protein II. Changes in the transition midpoint, T(m), were monitored as a function of pH and/or in the prese...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.1080/10837450701212610
更新日期:2007-01-01 00:00:00
abstract::Dual drug nanocrystals loaded nano embedded microparticles (DNEMs) were prepared for fixed dose combination of simvastatin (SIM) and ezetimibe (EZE) using NanoCrySP technology. The purpose was to generate nanonized SIM and EZE dispersed in matrix of single crystallization inducing excipient and investigate their in vi...
journal_title:Pharmaceutical development and technology
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更新日期:2020-01-01 00:00:00
abstract::The aim of this study was to investigate isotropic mono- and diglyceride-based (MCMDG) systems, which are potential vehicles for injectable products containing both hydrophilic and lipophilic drugs. For two-component systems, MCMDG was mixed with various masses of water. For three-component systems, the samples were p...
journal_title:Pharmaceutical development and technology
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doi:10.1081/pdt-120027422
更新日期:2004-01-01 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
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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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更新日期:2015-01-01 00:00:00
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
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更新日期:2001-01-01 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
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更新日期:2013-07-01 00:00:00