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 characteristics. The selected independent variables were HPMC-K3, Eudragit RSPO, and Carbopol 934P and the responses were floating duration, swelling index, and in vitro release from SR layer in 8 h. The films were also assessed for pharmacotechnical characteristics, release kinetics, DSC, FTIR, and SEM. The pharmacokinetics of the drugs from the optimized formulation was compared with the marketed formulation in rabbits. The capsulated accordion film unfolded and provided SR of atorvastatin for 8 h (96.76% ± 0.71) and IR of amlodipine within 25 min (98.07% ± 0.62) for the optimized formulation (F14). The swelling index and floating duration for the optimized formulation were 140.48 ± 0.57 and 8.53 ± 0.10 h, respectively. Results of pharmacokinetics showed that faster absorption of amlodipine and improved bioavailability (2.16-fold) of atorvastatin in blood was made available through bilayer film. In vitro-in vivo correlation was established using numerical deconvolution method. It can be concluded that the capsulated gastroretentive system provided site specific simultaneous SR of antihyperlidemic drug and IR of antihypertensive drug as single pill that has therapeutic potential to manage cardiovascular risk.
journal_name
Pharm Dev Technoljournal_title
Pharmaceutical development and technologyauthors
Porwal A,Dwivedi H,Pathak Kdoi
10.1080/10837450.2019.1705486subject
Has Abstractpub_date
2020-04-01 00:00:00pages
416-431issue
4eissn
1083-7450issn
1097-9867journal_volume
25pub_type
杂志文章abstract::Elderly people, children and patients sometimes have difficulties swallowing tablets. To solve this problem, a novel method of preparing tablets that disintegrate rapidly in the mouth was developed. A tablet with high porosity is required for rapid disintegration, but such a tablet is generally fragile. To make a tabl...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.1081/pdt-120000287
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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
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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...
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journal_title:Pharmaceutical development and technology
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doi:10.1081/pdt-100000741
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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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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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journal_title:Pharmaceutical development and technology
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doi:10.3109/10837450.2016.1143003
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abstract::New microspheres containing hydrophilic core and hydrophobic coating as a controlled-release system with no toxic reagents were proposed. Water in oil in water (W/O/W) emulsion and solvent evaporation methods were used to make chitosan/ cellulose acetate (CCA) microspheres sized 200 - 400 microm. Ranitidine hydrochlor...
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abstract::Seven potential impurities, including by-products, starting materials and intermediates were identified in pharmaceutical substance quetiapine fumarate and characterized by spectroscopic methods (MS, IR, NMR). Based on these methods the structures of the impurities were assigned or confirmed as: impurity I: 2-(phenylt...
journal_title:Pharmaceutical development and technology
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doi:10.1080/10837450802409388
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journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
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abstract::The purpose of this study was to investigate the effect of the composition of a binary powder mixture on the bonding index, the brittle fracture index, and the strain index, as defined by Hiestand. The studies involved tensile strength and dynamic indentation hardness determinations of square compacts, the solid fract...
journal_title:Pharmaceutical development and technology
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doi:10.3109/10837459709022630
更新日期:1997-11-01 00:00:00
abstract::Objective: A polymer-based nanoparticle was constructed to target sorafenib delivery to colorectal carcinoma cells and decrease the side effects of the drug.Methods: Sorafenib-loaded nanoparticles (S-NPs) based on PEG-PLGA were prepared using a double emulsion solvent evaporation method. The properties of S-NPs were e...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.1080/10837450.2020.1718704
更新日期:2020-06-01 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
pub_type: 杂志文章
doi:10.1081/pdt-120022153
更新日期:2003-08-01 00:00:00
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journal_title:Pharmaceutical development and technology
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doi:10.3109/10837450.2016.1163393
更新日期:2017-09-01 00:00:00
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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
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journal_title:Pharmaceutical development and technology
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doi:10.1080/10837450.2019.1689401
更新日期:2020-02-01 00:00:00
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journal_title:Pharmaceutical development and technology
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doi:10.1080/10837450701481249
更新日期:2007-01-01 00:00:00
abstract::Substituting spacer by another in noninvasive ventilation (NIV) involves many variables, e.g. total emitted dose (TED), mass median aerodynamic diameter (MMAD), type of spacer, total lung deposition and total systemic absorption, which must be adjusted to ensure patient optimum therapy. Data mining based on artificial...
journal_title:Pharmaceutical development and technology
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doi:10.3109/10837450.2015.1116567
更新日期:2017-11-01 00:00:00
abstract::Microporous polymeric matrices prepared from poly(ɛ-caprolactone) [PCL] were evaluated for controlled vaginal delivery of the antiprotozoal agent (tinidazole) in the treatment of the sexually transmitted infection, trichomoniasis. The matrices were produced by rapidly cooling co-solutions of PCL and tinidazole in acet...
journal_title:Pharmaceutical development and technology
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更新日期:2019-03-01 00:00:00
abstract::A colchicine release system utilizing biodegradable poly(phosphazenes) was investigated in vitro for intra-articular administration. Polymer degradation and drug release studies were performed on colchicine-loaded poly(phosphazenes) containing either imidazolyl (I-PPHOS) or ethyl glycinato (EG-PPHOS) side chain substi...
journal_title:Pharmaceutical development and technology
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doi:10.3109/10837459809028479
更新日期:1998-02-01 00:00:00
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journal_title:Pharmaceutical development and technology
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doi:10.1080/10837450701702941
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journal_title:Pharmaceutical development and technology
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journal_title:Pharmaceutical development and technology
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更新日期:2014-12-01 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
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更新日期:2019-06-01 00:00:00
abstract::The purpose of this paper is to reject or to confirm the hypothesis that the influence of the water addition rate on the size and size distribution of pellets is caused by insufficient spreading of the added water at higher water addition rates. To overcome insufficient spreading of the added water, the agitation in t...
journal_title:Pharmaceutical development and technology
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doi:10.3109/10837459609031431
更新日期:1996-12-01 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
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abstract:PURPOSE:To evaluate four novel metrics that compare dissolution profiles and assess their performance characteristics by comparing dissolution profiles of FAST and SLOW immediate release metoprolol tartrate tablets. METHODS:The four novel metrics (rho, rho m, delta a, and delta s), along with f2, were applied to disso...
journal_title:Pharmaceutical development and technology
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doi:10.1081/pdt-120003493
更新日期:2002-05-01 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
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journal_title:Pharmaceutical development and technology
pub_type: 杂志文章,评审
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更新日期:2015-01-01 00:00:00
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更新日期:2018-02-01 00:00:00