Abstract：
:The purpose of this research was to develop and evaluate buccal mucoadhesive controlled release tablets of lercanidipine hydrochloride using polyethylene oxide and different viscosity grades of hydroxypropyl methylcellulose individually and in combination. Effect of polymer type, proportion and combination was studied on the drug release rate, release mechanism and mucoadhesive strength of the prepared formulations. Buccal mucoadhesive tablets were made by direct compression and were characterized for content uniformity, weight variation, friability, surface pH, thickness and mechanism of release. In order to estimate the relative enhancement in bioavailability one optimized formulation was evaluated in rabbits. Further, placebo tablets were also evaluated for acceptability in human subjects. Results indicated acceptable physical characteristics of designed tablets with good content uniformity and minimum weight variation. Drug release and mucoadhesive strength were found to depend upon polymer type, proportion and viscosity. The formulations prepared using poly ethylene oxide gave maximum mucoadhesion. The release mechanism of most formulations was found to be of anomalous non-Fickian type. In vivo studies of selected formulation in rabbits demonstrated significant enhancement in bioavailability of lercanidipine hydrochloride relative to orally administered drug. Moreover, in human acceptability studies of placebo formulations, the designed tablets adhered well to the buccal mucosa for more than 4 h without causing any discomfort. It may be concluded that the designed buccoadhesive controlled release tablets have the potential to overcome the disadvantage of poor and erratic oral bioavailability associated with the presently marketed formulations of lercanidipine hydrochloride.
journal_name
AAPS PharmSciTechjournal_title
AAPS PharmSciTechauthors
Charde S,Mudgal M,Kumar L,Saha Rdoi
10.1208/s12249-007-9031-7subject
Has Abstractpub_date
2008-01-01 00:00:00pages
182-90issue
1issn
1530-9932journal_volume
9pub_type
杂志文章abstract：:Top-spray fluidized bed granulation with axial fluidization airflow from the bottom of the granulator is well-established in the pharmaceutical industry. The application of swirling airflow for fluidized bed granulation was more recently introduced. This study examined the effects of various process parameters on the ...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-012-9906-0
更新日期：2013-03-01 00:00:00
abstract：:Polymeric films are safe and effective and can be used for vaginal administration of microbicide drug candidates. Dapivirine (DPV), an investigational and clinically advanced antiretroviral drug, was selected as a model compound for this study. We have previously developed and clinically tested a quick-dissolving DPV ...
journal_title：AAPS PharmSciTech
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更新日期：2019-06-26 00:00:00
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journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-013-9935-3
更新日期：2013-06-01 00:00:00
abstract：:Modifications to the surface chemistry, charge, and hydrophilicity/hydrophobicity of nanoparticles are applicable approaches to the alterations of the in vivo fate of intravenously administered nano-sized drug carriers. The objective of this study is to investigate the in vitro and in vivo antitumor efficacies of curc...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-020-01698-w
更新日期：2020-06-11 00:00:00
abstract：:A transdermal drug delivery system (TDDS) is generally designed to deliver an active pharmaceutical ingredient (API) through the skin for systemic action. Permeation of an API through the skin is controlled by adjusting drug concentration, formulation composition, and patch design. A bilayer, drug-in-adhesive TDDS des...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-020-01682-4
更新日期：2020-06-04 00:00:00
abstract：:Freeze-dried immunoglobulin G (IgG) incorporating trehalose and human serum albumin (HSA) was statistically evaluated regarding the existence of synergism between additives on the stability profile. The levels of HSA (X1) and trehalose (X2) were independent variables. Aggregation following the process (Y1), after 2 an...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-019-1509-6
更新日期：2019-10-28 00:00:00
abstract：:Spheroid formation mechanisms were investigated using extrusion-spheronization (ES) and rotary processing (RP). Using ES (cross-hatch), ES (teardrop), and RP (teardrop), spheroids with similar mass median diameter (MMD) and span were produced using equivalent formulation and spheronization conditions. During spheroniz...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/pt0801010
更新日期：2007-02-09 00:00:00
abstract：:Pentoxifylline (PTX), an anti-hemorrhage drug used in the treatment of intermittent claudication, is extensively metabolized by the liver resulting in a reduction of the therapeutic levels within a short duration of time. Self-nano-emulsifying drug delivery system (SNEDDS) is well reported to enhance the bio-absorptio...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-020-01644-w
更新日期：2020-04-21 00:00:00
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journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/pt040338
更新日期：2003-01-01 00:00:00
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journal_title：AAPS PharmSciTech
pub_type： 杂志文章,评审
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更新日期：2017-07-01 00:00:00
abstract：:Nanoparticles fabricated from the biodegradable and biocompatible polymer, polylactic-co-glycolic acid (PLGA), could be a promising system for targeting ocular drug delivery. The objective of this work was to investigate the possibility of encapsulating brinzolamide in PLGA nanoparticles in order to be applied as a su...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-017-0710-8
更新日期：2017-10-01 00:00:00
abstract：:Pellet manufacturing by extrusion/spheronization is quite common in the pharmaceutical field because the obtained product is characterized by a high sphericity as well as a narrow particle size distribution. The established mechanisms only consider deformation of the initially fractured particles but do not account fo...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-010-9532-7
更新日期：2010-12-01 00:00:00
abstract：:The purpose of this research was to evaluate a new wireless and battery-free sensor technology for invasive product temperature measurement during freeze-drying. Product temperature is the most critical process parameter in a freeze-drying process, in particular during primary drying. The product temperature over time...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-008-9099-8
更新日期：2008-01-01 00:00:00
abstract：:Nanoparticles, of the poorly water-soluble drug, itraconazole (ITZ), were produced by the Advanced Evaporative Precipitation into Aqueous Solution process (Advanced EPAS). This process combines emulsion templating and EPAS processing to provide improved control over the size distribution of precipitated particles. Spe...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-012-9817-0
更新日期：2012-09-01 00:00:00
abstract：:We have designed a microemulsion (ME) containing Ketoprofen (KET) for anti-inflammatory effect evaluated using the rat paw edema model. The ME was prepared by adding propylene glycol (PG) loaded with 1% KET/water (3:1, w/w), to a mixture of sorbitan monooleate and polysorbate 80 (47.0%) at 3:1 (w/w) and canola oil (38...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-017-0749-6
更新日期：2017-10-01 00:00:00
abstract：:The purpose of this study was to develop and validate a rapid, sensitive, and specific reversed-phase high-performance liquid chromatography method for the quantitative determination of native tenofovir (TNF) for various applications. Different analytical performance parameters such as linearity, precision, accuracy, ...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-011-9735-6
更新日期：2012-03-01 00:00:00
abstract：:Next to the coating formulation, process conditions play important roles in determining coating quality. This study aims to develop an operational window that separates layering from agglomeration regimes and, furthermore, the one that leads to the best coating quality in a fluidized bed coater. The bed relative humid...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-009-9250-1
更新日期：2009-01-01 00:00:00
abstract：:The impact of pharmaceutical materials properties on drug product quality and manufacturability is well recognised by the industry. An ongoing effort across industry and academia, the Manufacturing Classification System consortium, aims to gather the existing body of knowledge in a common framework to provide guidance...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章,评审
doi：10.1208/s12249-018-1198-6
更新日期：2018-11-01 00:00:00
abstract：:The aim of the study is to examine thermal behavior of water within reticulated structure of bacterial cellulose (BC) films by sub-ambient differential scanning calorimetry (DSC). BC films with different carbon source, either manitol (BC (a)) or glycerol (BC (b)), were produced by Acetobacter xylinum using Hestrin and...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-008-9104-2
更新日期：2008-01-01 00:00:00
abstract：:The purpose of the present investigation is to formulate and evaluate proniosomal transdermal carrier systems for flurbiprofen. Proniosomes were prepared using various non-ionic surfactants, namely span 20 (Sp 20), span 40 (Sp 40), span 60 (Sp 60) and span 80 (Sp 80) without and with cholesterol at percentages ranging...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-008-9114-0
更新日期：2008-01-01 00:00:00
abstract：:Atropine sulfate (AS) fast-disintegrating sublingual tablets (FDSTs) were tested for AS sublingual permeation's feasibility as a potential alternative dosage form to treat organophosphates (OP) toxicity. More than 12,000 OP pesticide toxicity cases were reported in the USA from 2011 to 2014. AS is the recommended anti...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-019-1420-1
更新日期：2019-06-21 00:00:00
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journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/pt040228
更新日期：2003-01-01 00:00:00
abstract：:The aim of this study was to investigate the effects of a type of hydrophobic moiety, extent of N-substitution (ES), and degree of quaternization (DQ) of chitosan (CS) on the transepithelial electrical resistance and permeability of Caco-2 cells monolayer, using fluorescein isothiocyanate dextran 4,400 (FD-4) as the m...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章
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更新日期：2010-06-01 00:00:00
abstract：:Cyclodextrins (CDs) are used in oral pharmaceutical formulations, by means of inclusion complexes formation, with the following advantages for the drugs: (1) solubility, dissolution rate, stability, and bioavailability enhancement; (2) to modify the drug release site and/or time profile; and (3) to reduce or prevent g...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章,评审
doi：10.1208/s12249-011-9690-2
更新日期：2011-12-01 00:00:00
abstract：:The objective of this study was to prepare and evaluate terbutaline sulphate (TBS) bi-layer tablets for once-daily administration. The bi-layer tablets consisted of an immediate-release layer and a sustained-release layer containing 5 and 10 mg TBS, respectively. The sustained-release layer was developed by using Comp...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-015-0404-z
更新日期：2016-06-01 00:00:00
abstract：:Buccal bioadhesive films, releasing topical drugs in the oral cavity at a slow and predetermined rate, provide distinct advantages over traditional dosage forms. The aim of present study was to prepare and evaluate buccal bioadhesive films of clotrimazole for oral candidiasis. The film was designed to release the drug...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-008-9083-3
更新日期：2008-01-01 00:00:00
abstract：:The aim of this study was to introduce smectite clay matrices as a drug delivery carrier for the development of amorphous solid dispersions (ASD). Indomethacin (IND) was processed with two different smectite clays, magnesium aluminium and lithium magnesium sodium silicates, using hot melt extrusion (HME) to prepare so...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-020-01813-x
更新日期：2020-10-08 00:00:00
abstract：:The objective of the present investigation was to reduce the bitterness with improved dissolution, in acidic medium (pH 1.2), of mefloquine hydrochloride (MFL). Microparticles were prepared by coacervation method using Eudragit E (EE) as polymer and sodium hydroxide as precipitant. A 3(2) full factorial design was use...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-008-9052-x
更新日期：2008-01-01 00:00:00
abstract：:Posaconazole is a triazole antifungal drug that with extremely poor aqueous solubility. Up to now, this drug can be administered via intravenous injection and oral suspension. However, its oral bioavailability is greatly limited by the dissolution rate of the drug. This study aimed to improve water solubility and diss...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-016-0497-z
更新日期：2017-01-01 00:00:00
abstract：:This study focused on the chemical stability of the cephalosporin (6R, 7R)-7-(1-pentafluorophenoxyacetamido)-3-[2-(5-methyl-1,3,4-thiodiazolyl)thiomethyl]-Delta(3)-cephem-4-carboxylic acid, sodium salt (cephem 1) formulation after electron beam (e-beam) irradiation. The cephem 1 concentrations of samples irradiated at...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/pt020423
更新日期：2001-11-19 00:00:00
