Formulation development and systematic optimization of stabilized ziprasidone hydrochloride capsules devoid of any food effect.

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 Technol

authors

Banerjee S,Shankar KR,Prasad Y R

doi

10.3109/10837450.2015.1055764

subject

Has Abstract

pub_date

2016-11-01 00:00:00

pages

775-786

issue

7

eissn

1083-7450

issn

1097-9867

journal_volume

21

pub_type

杂志文章
  • The preparation of felodipine/zein amorphous solid dispersions and in vitro evaluation using a dynamic gastrointestinal system.

    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

    authors: Zhang H,Liu X,Ma X

    更新日期:2020-12-01 00:00:00

  • Eudragit-based transdermal delivery system of pentazocine: Physico-chemical, in vitro and in vivo evaluations.

    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

    authors: Chandak AR,Prasad Verma PR

    更新日期:2010-06-01 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

  • Glucose-sensitive gel rheology of dextran-concanavalin A mixtures suitable for self-regulating insulin delivery.

    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

    authors: Taylor MJ,Tanna S,Sahota TS

    更新日期:2010-01-01 00:00:00

  • Development of controlled-release SK&F 82526-J buffer bead formulations with tartaric acid as the buffer.

    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

    authors: Venkatesh GM

    更新日期:1998-11-01 00:00:00

  • In vitro permeation study of a mucoadhesive drug delivery system for controlled delivery of nonoxynol-9.

    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

    authors: Lee CH,Chien YW

    更新日期:1996-07-01 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

  • Novel microemulsion-based gel formulation of tazarotene for therapy of acne.

    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

    authors: Patel MR,Patel RB,Parikh JR,Patel BG

    更新日期:2016-12-01 00:00:00

  • Development of a small-scale spray-drying approach for amorphous solid dispersions (ASDs) screening in early drug development.

    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

    authors: Ousset A,Bassand C,Chavez PF,Meeus J,Robin F,Schubert MA,Somville P,Dodou K

    更新日期:2019-06-01 00:00:00

  • Simultaneous determination of levodopa and carbidopa in levodopa-carbidopa tablets by ATR-FTIR spectrometry.

    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

    authors: Khanmohammadi M,Mobedi E,Garmarudi AB,Mobedi H,Kargosha K

    更新日期:2007-01-01 00:00:00

  • Effect of sample preparation method on quantification of polymorphs using PXRD.

    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

    authors: Alam S,Patel S,Bansal AK

    更新日期:2010-09-01 00:00:00

  • Use of scoring to induce reproducible drug delivery from osmotic pulsatile tablets.

    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

    authors: Rahemba TR,Bell S,Connolly EK,Waterman KC

    更新日期:2009-01-01 00:00:00

  • Understanding drug-excipient compatibility: oxidation of compound A in a solid dosage form.

    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

    authors: Wu Y,Dali M,Gupta A,Raghavan K

    更新日期:2009-01-01 00:00:00

  • Development and evaluation of mathematical model to predict disintegration time of fast disintegrating tablets using powder characteristics.

    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

    authors: Goel H,Arora A,Tiwary AK,Rana V

    更新日期:2011-02-01 00:00:00

  • Evaluation of co-processed excipients used for direct compression of orally disintegrating tablets (ODT) using novel disintegration apparatus.

    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

    authors: Brniak W,Jachowicz R,Krupa A,Skorka T,Niwinski K

    更新日期:2013-03-01 00:00:00

  • "Prevention of structural perturbation and aggregation of hepatitis B surface antigen: screening of various additives".

    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

    authors: Tomar P,Giri N,Karwasara VS,Pandey RS,Dixit VK

    更新日期:2012-07-01 00:00:00

  • Effect of solid state transition on the physical stability of suspensions containing bupivacaine lipid microparticles.

    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

    authors: Li LC,Zhu L,Song JF,Deng JS,Bandopadhyay R,Wurster DE

    更新日期:2005-01-01 00:00:00

  • The impact of solid-state form, water content and surface area of magnesium stearate on lubrication efficiency, tabletability, and dissolution.

    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

    pub_type: 杂志文章

    doi:10.1080/10837450.2020.1839763

    authors: Calahan JL,Paul S,Yanez EG,DeNeve D,Sun CC,Munson EJ

    更新日期:2021-02-01 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

  • Characterization of nano oxaliplatin prepared by novel Fat Employing Supercritical Nano System, the FESNS®.

    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

    authors: Lee SJ,Kim YH,Lee SH,Hahn M

    更新日期:2012-03-01 00:00:00

  • The nonsteady state modeling of freeze drying: in-process product temperature and moisture content mapping and pharmaceutical product quality applications.

    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

    authors: Pikal MJ,Cardon S,Bhugra C,Jameel F,Rambhatla S,Mascarenhas WJ,Akay HU

    更新日期:2005-01-01 00:00:00

  • Iontophoretic enhancement of leuprolide acetate by fatty acids, limonene, and depilatory lotions through porcine epidermis.

    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

    authors: Rastogi SK,Singh J

    更新日期:2004-11-01 00:00:00

  • Construction and cellular uptake behavior of redox-sensitive docetaxel prodrug-loaded liposomes.

    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

    pub_type: 杂志文章

    doi:10.1080/10837450.2017.1287728

    authors: Ren G,Jiang M,Guo W,Sun B,Lian H,Wang Y,He Z

    更新日期:2018-01-01 00:00:00

  • Use of microcalorimetry and its correlation with size exclusion chromatography for rapid screening of the physical stability of large pharmaceutical proteins in solution.

    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

    authors: Burton L,Gandhi R,Duke G,Paborji M

    更新日期:2007-01-01 00:00:00

  • Dual drug nanocrystals loaded microparticles for fixed dose combination of simvastatin and ezetimibe.

    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

    pub_type: 杂志文章

    doi:10.1080/10837450.2019.1669181

    authors: Nandi S,Kaur A,Bansal AK

    更新日期:2020-01-01 00:00:00

  • Isotropic systems of medium-chain mono- and diglycerides for solubilization of lipophilic and hydrophilic drugs.

    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

    pub_type: 杂志文章

    doi:10.1081/pdt-120027422

    authors: Sari P,Razzak M,Tucker IG

    更新日期:2004-01-01 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

  • Well-plate freeze-drying: a high throughput platform for screening of physical properties of freeze-dried formulations.

    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

    authors: Trnka H,Rantanen J,Grohganz H

    更新日期:2015-01-01 00:00:00

  • A novel approach to increase oral drug absorption.

    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

    authors: Idkaidek NM,Abdel-Jabbar N

    更新日期:2001-01-01 00:00:00

  • Degradation of a pharmaceutical in HPLC grade methanol containing trace level formaldehyde.

    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

    authors: Zhong Q,Stowers S,Segraves NL,Ngim KK,Zhang K,Bostick T,Deese A,Chetwyn NP

    更新日期:2013-07-01 00:00:00