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 coated in a fluid-bed granulator with a blend of gastrointestinal (GI) insoluble/enteric Eudragit polymers (such as RSPM/S100 polymer blend), drug was layered on these polymer-subcoated buffer beads by a slurry coating process, and the drug-layered beads were subsequently overcoated using a blend of GI insoluble/enteric polymers. The release of fenoldopam and tartaric acid was monitored by a two-stage dissolution procedure using USP Apparatus 2 (paddles at 50 rpm) and HPLC methodologies. The overcoating of drug-layered tartaric acid crystals with Eudragit polymers with different permeabilities significantly affected the release of fenoldopam. However, even the least permeable polymer, Eudragit RS, could not sustain the release of tartaric acid beyond 2 hr, suggesting the need to subcoat freely water-soluble tartaric acid crystals prior to drug layering. By varying the type/ratios of the GI insoluble/enteric polymers for subcoat and overcoat, capsule formulations were developed, which released fenoldopam and tartaric acid at different rates. The use of Eudragit polymer blends at the optimized ratios for both subcoat and overcoat resulted in a significant retardation in the release of tartaric acid; still, the tartaric acid release was faster than that of fenoldopam, suggesting the need to use a less water-soluble fumaric or succinic acid crystals as the buffer. However, the technology described using tartaric acid crystals as the buffer will be highly useful for weakly basic drug substances with less stringent pH-dependent solubility profiles.
journal_name
Pharm Dev Technoljournal_title
Pharmaceutical development and technologyauthors
Venkatesh GMdoi
10.3109/10837459809028629subject
Has Abstractpub_date
1998-11-01 00:00:00pages
477-85issue
4eissn
1083-7450issn
1097-9867journal_volume
3pub_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
更新日期:2001-11-01 00:00:00
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::Films of gellan gum:pectin blends were prepared by solvent casting method. Gellan gum:pectin mass ratios were varied (4:1; 1:1; 1:4) at different concentrations (3% or 4%) and glycerol was used as plasticizer (1 or 2%). The films were thin (18-30 µm), translucent, flexible, and homogeneous. The surface pH was suitable...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.1080/10837450.2019.1682608
更新日期:2020-02-01 00:00:00
abstract::In the pharmaceutical industry, chemometrics is rapidly establishing itself as a tool that can be used at every step of product development and beyond: from early development to commercialization. This set of multivariate analysis methods allows the extraction of information contained in large, complex data sets thus ...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章,评审
doi:10.3109/10837450.2014.898656
更新日期:2015-01-01 00:00:00
abstract::Mechanically generated radicals were shown to affect short-term stability of a model pharmaceutical formulation during high-shear processing. A formulation containing an oxidatively sensitive drug, either amorphous or crystalline, and a polymeric excipient was high-shear mixed and the resulting short-term degradation ...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.1080/10837450802328869
更新日期:2008-01-01 00:00:00
abstract::Pulmonary delivery of peptides remains an important, noninvasive route of administration that is attractive because it offers high bioavailability and patient compliance. Optimization of particle characteristics for deposition in the deep regions of the lung after inhalation and retention of peptide stability are key ...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.3109/10837450.2015.1125924
更新日期:2017-09-01 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::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
更新日期:2013-11-01 00:00:00
abstract:PURPOSE:To investigate the influence of the pH of the dissolution medium on immediate release 850 mg metformin hydrochloride tablets. METHODS:A traditional wet granulation method was used to manufacture metformin hydrochloride tablets with or without a disintegrant. Tablet dissolution was conducted using the USP appar...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.3109/10837450.2014.892132
更新日期:2015-01-01 00:00:00
abstract::The physical-chemical processing variables affecting particle size following precipitation using the supercritical antisolvent (SAS) method were investigated by varying both the composition of the feed solvent and the structure of the solute, using a series of steroids. The key factor influencing particle size in thes...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.1080/10837450600561299
更新日期:2006-01-01 00:00:00
abstract::This article describes a method to quantitatively track the solvation of HPC in a non-aqueous solvent system during topical gel manufacture. Where visual observation and microscopy could not establish a trend, straight-forward rheological profiling demonstrated a correlation between increased solvation of hydroxypropy...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.1080/10837450.2018.1502319
更新日期:2019-04-01 00:00:00
abstract::When a nebulizer is evaluated by the Andersen Cascade Impactor (ACI), the flow rate is generally maintained at 28.3 L/min, as recommended by the manufacturer. However, the nebulizer flow rate that a patient inhales is only around 18 L/min. Because the drive flow of a nebulizer is approximately 6-8 L/min, the nebulized...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.1080/10837450701366937
更新日期:2007-01-01 00:00:00
abstract::Alpha lipoic acid (ALA), an active substance in anti-aging products and dietary supplements, need to be masked with an edible polymer to obscure its unpleasant taste. However, the high viscosity of the ALA molecules prevents them from forming microcomposites with masking materials even in supercritical carbon dioxide ...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.3109/10837450.2015.1049707
更新日期:2016-09-01 00:00:00
abstract::The purpose of this study was to develop a method to prepare Metoprolol Succinate (MS) sustained release pellets and compress them into pellet-containing tablets without losing sustained release property. The drug layered pellets were coated with Eudragit NE 30D to obtain a sustained release (SR) property. The mechani...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.3109/10837450.2015.1081612
更新日期:2016-12-01 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 paddle method for measurement of the disintegrating time of orally disintegrating tablets with rizatriptan benzoate as a model drug was evaluated. The paddle method employed a dissolution test assembly with tablets immersed in disintegrating medium through a fastened sinker. Paddle stirring rate, opening of the sink...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.1080/10837450600767649
更新日期:2006-01-01 00:00:00
abstract::The aim of this study was to prepare various types of solid dispersions (SDs) by the hot-melt extrusion technique. Next, process analytical technology (PAT) such as Fourier transform-infrared (FT-IR) and Raman and near infrared (NIR) spectroscopy were applied to determine the solubilization effect. The SDs and its tab...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.1080/10837450.2020.1723023
更新日期:2020-06-01 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::The contact time of a vehicle on the cornea is of utmost importance for ophthalmic drug delivery. The poor bioavailability and therefore poor therapeutic response exhibited by the conventional ophthalmic solutions due to pre-corneal elimination of a drug may be overcome by the use of the in situ gel forming systems, w...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.3109/10837450903262033
更新日期:2010-07-01 00:00:00
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
pub_type: 杂志文章
doi:10.3109/10837459709022630
更新日期:1997-11-01 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:CONTEXT:Bioadhesiviness of polyacrylic acid polymers make them promising hydrogels to design topical drug delivery systems, allowing a close contact with biological substrate as well as an enhanced local concentration gradient, both factors that may improve the biological performance of the drugs. AIM:Texture and bioa...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.3109/10837450.2014.882941
更新日期:2015-06-01 00:00:00
abstract::In this study, chlorhexidine-loaded poly(ε-caprolactone) nanospheres (CHX-NS) were prepared and successfully coated on the urinary catheters. Properties of CHX-NS were evaluated including drug loading content and the nanosphere size. Effects of different lyoprotectants for long-term storage of CHX-NS were also investi...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.1080/10837450.2018.1502317
更新日期:2019-04-01 00:00:00
abstract::Colorectal cancer (CRC) is the third most common cause of cancer-related death in both men and women. Often, surgical intervention remains the choice in treating CRC. Traditional dosage forms used for treating CRC deliver drug to wanted as well as unwanted sites of drug action resulting in several adverse side effects...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章,评审
doi:10.3109/10837450.2012.696268
更新日期:2012-09-01 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::A preliminary study of the feasibility of using near-infrared spectroscopy (NIRS) for the offline simultaneous determination of metoprolol tartrate (MTP) and hydrochlorothiazide (HTZ) in powders and tablets has been carried out. An industrial tableting process was simulated using an instrumented tablet press replicato...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.3109/10837450.2014.949268
更新日期:2015-01-01 00:00:00
abstract::The aim of the present work was to investigate the possibility of achieving buccal delivery of a problematic drug, acyclovir, from films based on chitosan hydrochloride (HCS) and polyacrylic acid sodium salt (PAA). At first, the ionic interaction between HCS and PAA in distilled water was investigated by means of rheo...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.1081/pdt-120018490
更新日期:2003-01-01 00:00:00
abstract::In the current study, we demonstrate a structured approach to downstream process development for spray dried amorphous solid dispersions. Direct compression is generally not suitable due to typically poor flow of spray dried powders in tablets. Roller compaction (RC) is therefore the method of choice to enable spray d...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.1080/10837450.2020.1863985
更新日期:2021-01-04 00:00:00
abstract::In this study, we designed a polymersome system for the controlled release of methotrexate (MTX) as an anticancer drug with the objective of improving the loading efficiency of the drug in polymersomes as well as achievement of an efficient control on the release rate of drug from nanocarriers. We synthesized mono met...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.1080/10837450.2018.1425433
更新日期:2019-01-01 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