Abstract:
:The object of this study was to enhance the solubility, dissolution rate, and oral bioavailability of rutin by complexation with 2-hydroxypropyl-beta-cyclodextrin (HP-beta-CyD). The interaction of rutin with cyclodextrins (CyDs) was evaluated by the solubility, and ultraviolet (UV) and circular dichroism (CD) spectrophotometries. The chemical and enzymatic stability of rutin was examined in an alkaline buffer solution and in rat small intestinal homogenates, respectively. Dissolution rates of rutin and its CyD complexes were measured by the dispersed amount method. In vivo absorption studies of rutin after oral administration via conventional tablet containing rutin alone or its beta-CyD complexes was performed on beagle dogs. The stability constants calculated from the phase solubility method increased in the order of HP-gamma-CyD < G2-beta-CyD < beta-CyD < HP-beta-CyD. Spectroscopic studies also revealed that HP-beta-CyD and beta-CyD formed a relatively more stable inclusion complex with rutin. The dissolution rates of rutin increased by the complexation with CyDs in the order of rutin alone < HP-beta-CyD < or = beta-CyD. HP-beta-CyD inhibited the hydrolysis of rutin in the alkaline buffer solution and the small intestinal homogenates of rats, suggesting that HP-beta-CyD may stabilize rutin in a gastrointestinal tract after oral administration. When the tablet containing rutin or its beta-CyD complexes was administered to beagle dogs, the plasma levels of homovanillic acid (HVA) (a major stable metabolite of rutin) after oral administration of HP-beta-CyD complex were much higher than in either that of rutin alone or in its beta-CyD complex. The in vivo absorption study suggests that HP-beta-CyD increased the oral bioavailability of rutin from the gastrointestinal tracts of beagle dogs because of the increase in solubility, faster dissolution rate, and gastrointestinal stability. HP-beta-CyD has a significant advantage with respect to providing high aqueous solubility while maintaining a lack of toxicity in oral pharmaceutical preparations of rutin.
journal_name
Pharm Dev Technoljournal_title
Pharmaceutical development and technologyauthors
Miyake K,Arima H,Hirayama F,Yamamoto M,Horikawa T,Sumiyoshi H,Noda S,Uekama Kdoi
10.1081/pdt-100100556subject
Has Abstractpub_date
2000-01-01 00:00:00pages
399-407issue
3eissn
1083-7450issn
1097-9867journal_volume
5pub_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 hygroscopicity of Brequinar sodium, an organ transplant immunosuppressant, at 75% relative humidity highly depends on the crystal form or crystallinity of the drug substance. Hygroscopicity and ease of water uptake of three lots of Brequinar sodium were investigated. Those lots contained different impurities at le...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.3109/10837459609031417
更新日期:1996-04-01 00:00:00
abstract:CONTEXT:Development and evaluation of thermosensitive and bioadhesive liquid suppositories containing ketoprofen (KP). OBJECTIVE:This study was conducted to develope thermosensitive and bioadhesive liquid suppositories containing KP using poloxamer and different bioadhesive polymers and to investigate their gelation t...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.3109/10837450.2013.846373
更新日期:2014-12-01 00:00:00
abstract::Drug solubility testing in biorelevant media has become an indispensable tool in pharmaceutical development. Despite this importance, there is still an incomplete understanding of how poorly soluble compounds interact with these media. The aim of this study was to apply the concept of the apparent solubilization capac...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.3109/10837451003664099
更新日期:2011-06-01 00:00:00
abstract::Drug release from hydroxypropyl methylcellulose (HPMC) hydrophilic matrix tablets is controlled by drug diffusion through the gel layer of the matrix-forming polymer upon hydration, matrix erosion or combination of diffusion and erosion mechanisms. In this study, the relationship between viscoelastic properties of the...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.1080/10837450.2016.1257022
更新日期:2018-11-01 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::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::Purpose: Intestinal drug absorption is one of the main factors that govern the fraction of oral dose absorbed (Fa) of drugs. It is reported that oral absorption of bortezomib (BTZ) can be restricted by its low intestinal permeability. In this study, we aimed to evaluate the impact of self-nanoemulsifying drug delivery...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.1080/10837450.2019.1699109
更新日期:2020-03-01 00:00:00
abstract::Nucleic acids therapeutic efficiency is generally limited by their low stability and intracellular bioavailability, and by the toxicity of the carriers used to deliver them to the target sites. Aminated poly(glycerol methacrylate) polymers are biodegradable and pH-sensitive polymers that have been used previously to d...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.1080/10837450.2017.1312443
更新日期:2018-04-01 00:00:00
abstract::The purpose of this work was to prepare and characterize Angiopep-2 functionalized ginsenoside-Rg3 loaded nanoparticles (ANG-Rg3-NP) and evaluate the therapeutic effect on C6 glioma cells. Nanoparticles were prepared by the emulsion solvent evaporation method. Angiopep-2 was functionalized to nanoparticles via a malei...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.1080/10837450.2018.1551901
更新日期:2020-03-01 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::The main objective of this research is to use the near-infrared diffuse reflectance method to evaluate and quantify the effects of hardness and porosity on the near-infrared spectras of tablets. To develop a model equation, validate the model and test the model predictive ability. Seven theophylline tablet formulation...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.1081/pdt-120024689
更新日期:2003-01-01 00:00:00
abstract::The effect of some processing and formulation variables on the stability of tablets containing a crystalline salt of a triazine derivative was studied. The salt has a relatively low melting point and a low microenvironmental pH due to the weakly basic nature of the parent compound (pKa = 4.0). This compound decomposes...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.1081/pdt-200031417
更新日期:2004-08-01 00:00:00
abstract::This study investigates the physicochemical properties of glycyl-histidyl-lysine-copper (GHK-Cu) to support the development of a formulation for effective topical delivery. The solubility and distribution coefficients (log D) were investigated using conventional methods and GHK concentrations were quantified with a va...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.3109/10837450.2014.979944
更新日期:2016-03-01 00:00:00
abstract::In this study, the degradation of Octastatin, a cyclic octapeptide analog of somatostatin, was examined as a function of pH, temperature, buffer, and ionic strength by reversed-phase gradient high-performance liquid chromatography. Degradation of Octastatin followed a first-order kinetics. Various buffer species such ...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.3109/10837459709022640
更新日期:1997-11-01 00:00:00
abstract::The current work aimed to develop low-density gastroretentive sponges loaded with alfuzosin HCl (ALF) to sustain the rate of drug release, improve its oral bioavailability and deliver it to the main site of absorption. Sponges were developed, according to a 23 full factorial design, by compression of the lyophilized A...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.1080/10837450.2020.1720235
更新日期:2020-06-01 00:00:00
abstract::The purpose of this research was to prepare various injectable, protein (cytochrome c)-loaded biodegradable poly(lactide-co-glycolide) (PLGA) devices by a novel microencapsulation method and to compare their characteristics. Syringeable mixtures of polymer and protein solidified upon injection when coming in contact w...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.1081/pdt-100100535
更新日期:2000-01-01 00:00:00
abstract::A novel flavonoid-polysaccharide conjugate was synthesized by free radical grafting of quercetin on starch. The covalent insertion of quercetin in the polymeric chain was confirmed by FT-IR, DSC and fluorescence analyses, while an estimation of the amount of quercetin bound per g of polymer was obtained by the Folin-C...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.3109/10837450.2010.546413
更新日期:2012-07-01 00:00:00
abstract::The effect of six factors: spray gun, formulation, inlet temperature, atomizing air pressure, fan air pressure, and gun-bed distance, on the final adhesion of the film coat to the tablet core were assessed. The method used was based on an experimental design, Resolution IV, that allowed the main effects to be free fro...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.1081/pdt-49692
更新日期:2005-01-01 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
pub_type: 杂志文章
doi:10.1080/10837450.2019.1669181
更新日期:2020-01-01 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
pub_type: 杂志文章
doi:10.3109/10837459609031431
更新日期:1996-12-01 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::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::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
更新日期:2013-07-01 00:00:00
abstract::Oily liquid drugs are not convenient for oral administration. We developed a powder containing clofibrate (CF), a model of an oily drug, using aminoalkyl methacrylate copolymer (EPO) or methacrylic acid copolymer (L100). CF or a mixture of CF and soybean oil was emulsified with EPO or L100 aqueous solution. Using a hi...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.3109/10837450.2015.1086370
更新日期:2016-12-01 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
pub_type: 杂志文章
doi:10.1080/10837450701557246
更新日期:2007-01-01 00:00:00
abstract::The interaction of 5-nitro-2-furfurilylidene benzhydrazide (5NFB), potential anti-trypanosomal compound, with micellar solutions was studied. The results indicated that 50 mug of 5NFB completely kills 20 million T. cruzi epimastigote cells within 3 days, whereas the same amount of benznidazole kills 30% of the cells a...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.1080/10837450701212727
更新日期:2007-01-01 00:00:00
abstract::We have proposed a theory indicating the correlation between the dissolution rate and the heat of solution of drug substances. The initial dissolution rates of the drug substances containing amorphous were predicted accurately from their heats of solution. In this report, the possibility for the theory to estimate the...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.1081/pdt-120002234
更新日期:2002-01-01 00:00:00
abstract::Quality by design (QbD) is an essential part of the modern approach to pharmaceutical quality. This study was conducted in the framework of a QbD project involving ramipril tablets. Preliminary work included identification of the critical quality attributes (CQAs) and critical process parameters (CPPs) based on the qu...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.3109/10837450.2012.705294
更新日期:2013-02-01 00:00:00
abstract::There is as yet no commercialized preparation for oral administration of flecainide acetate (FA) to children. In such cases, manipulation of commercial tablets is the usual practice in pharmacy services of hospitals and compounding pharmacies, to provide a suitable dosage form for this vulnerable pediatric population ...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.1080/10837450.2016.1238484
更新日期:2018-12-01 00:00:00