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 found to be the key parameter. Hence, for drugs stable in the intestinal wall, increasing partition coefficient only can lead to higher drug absorption. However, for drugs unstable in the intestinal wall, increasing partition coefficient and diffusivity is needed to counteract drug instability. On the other hand, the model is essentially insensitive to degradation in the intestinal lumen for degradation half lives greater than 0.7 min at a given intestinal length. However, a high model sensitivity to the rate of luminal degradation is obtained at higher intestinal length values. The proposed model can be used as a guide for oral drug delivery.
journal_name
Pharm Dev Technoljournal_title
Pharmaceutical development and technologyauthors
Idkaidek NM,Abdel-Jabbar Ndoi
10.1081/pdt-100000741subject
Has Abstractpub_date
2001-01-01 00:00:00pages
167-71issue
2eissn
1083-7450issn
1097-9867journal_volume
6pub_type
杂志文章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
更新日期:2012-03-01 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::The main objective of the present study was to improve bioavailability of diltiazem hydrochloride and decrease the frequency of dosage form administration by increasing the encapsulation efficiency of the drug, residence time of the dosage form at the site of absorption and sustained release of the drug from the deliv...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.1080/10837450802626304
更新日期:2009-01-01 00:00:00
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
pub_type: 杂志文章
doi:10.1080/10837450802409388
更新日期:2009-01-01 00:00:00
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 opti...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.3109/10837450.2015.1055764
更新日期:2016-11-01 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::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::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::A high-pressure homogenization method for the production of aqueous suspensions of poly(D,L-lactide) and poly(D,L-lactide-co-glycolide) was investigated. Depending on the production conditions it was possible to produce micro--as well as nanoparticulate systems without the use of organic solvents. The influence of dif...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.3109/10837459809009857
更新日期:1998-08-01 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::Novel buccal adhesive system (NBAS) containing Nimodipine (N) was prepared and evaluated by different parameters such as weight uniformity, thickness, hardness, surface pH, swelling index, mucoadhesive strength (MS), in vitro drug release and ex vivo drug permeation. Different formulations containing 5-20% Carbopol 93...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.3109/10837450903055494
更新日期:2010-03-01 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::This work aimed to incorporate Dexibuprofen (DXI), the pharmacologically active and more potent form of ibuprofen, into polymeric micelles based tablets with enhanced oral bioavailability. Thin film hydration technique was employed to prepare DXI polymeric micelles using Pluronic® F127 and/or P123 solutions in differe...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.3109/10837450.2013.823994
更新日期:2014-09-01 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::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::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::Vardenafil hydrochloride (VAR) is an erectile dysfunction treating drug. VAR has a short elimination half-life (4-5 h) and suffers low oral bioavailability (15%). This work aimed to explore the dual potential of VAR-dendrimer complexes as drug release modulators and oral bioavailability enhancers. VAR-dendrimer comple...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.1080/10837450.2018.1472611
更新日期:2019-03-01 00:00:00
abstract::The objective of this study was to investigate the effect of the physiological parameters (pH, buffer capacity, and ionic strength) of the gastrointestinal (GI) fluid on the dissolution behavior of the class II weakly acidic (BCS class IIa) drug valsartan. A series of in vitro dissolution studies was carried out on Di...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.1080/10837450.2018.1536996
更新日期:2018-12-01 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::Background: Clindamycin's bitter taste and odor is known to affect treatment adherence in children. Recently, a formulation of clindamycin HCl complexed with ion exchange resin IRP 69 was shown to mask the bitter taste. Because of the potential benefit of this formulation for children, a pilot study using a porcine mo...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章,随机对照试验
doi:10.1080/10837450.2019.1624771
更新日期:2019-10-01 00:00:00
abstract::Hypericin (Hyp), a natural hydrophobic and photoactive pigment, and methylene blue (MB), a hydrophilic cationic dye, are utilized as photosensitizer (PS) for photodynamic therapy of cancer. Bioadhesive and thermoresponsive polymeric systems can improve the drug availability by increasing the contact time between the s...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.1080/10837450.2019.1711394
更新日期:2020-04-01 00:00:00
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
更新日期:1996-07-01 00:00:00
abstract::The present study was carried out in order to mask the bitter taste of the Etoricoxib by complexation with cation-exchange resin, Indion 204. The drug resin complexes (DRC) were prepared by batch process and efficient drug loading was obtained by using inactivated form of resin in the drug-resin ratio 1:3.3 with 30 mi...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.3109/10837450903322787
更新日期:2010-09-01 00:00:00
abstract::Stability of captopril in a controlled release formulation has been a challenge for some time. The sustained release of captopril from floating matrices has been studied varying the antioxidant load, the sodium bicarbonate proportion and the compaction pressure. Although in many cases the effect of compaction pressure...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.1080/10837450903110737
更新日期:2009-07-22 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::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 formulation of betamethasone-17-valerate (BV) into topical medicines presents a significant challenge for the formulation chemist. The substance is susceptible to acid and base catalyzed isomerization in aqueous environments, which results in valerate transesterification from carbon 17 to carbon 21 of the steroid ...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.3109/10837450.2016.1143003
更新日期:2017-06-01 00:00:00
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
更新日期:2013-03-01 00:00:00
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) spectrop...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.1081/pdt-100100556
更新日期:2000-01-01 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