Abstract：
:Establishing a method to evaluate the reliability of an optimal solution is an exciting challenge for the nonlinear response surface method. We reported previously that the bootstrap (BS) resampling technique and Kohonen's self-organizing map are promising tools for meeting this challenge. To understand the usefulness of these techniques further, we employed a formulation optimization study of photocrosslinked polyacrylic acid (PAA) hydrogel as a case study. In a series of experiments, a large number of optimal solutions were generated with BS resampling and they were classified into three distinct clusters with SOM clustering. Using analysis of Bayesian estimation, we clarified the mode of generating clusters; e.g., cluster 2 was distinguished by the difference in features between the BS optimal solutions and the original optimal solution, whereas cluster 3 was distinguished by the substantial change in the shape of the response surfaces. We concluded that cluster 1 represents the global optimal solution, and then estimated 95% confidence intervals of the optimal solutions using the BS optimal solutions. These findings prove that our method is a valid approach for evaluating nonlinear optimal solutions. This method has applications for establishing a science-based rationale for, and a design space in, pharmaceutical formulation development.
journal_name
Int J Pharmjournal_title
International journal of pharmaceuticsauthors
Onuki Y,Kikuchi S,Yasuda A,Takayama Kdoi
10.1016/j.ijpharm.2010.06.013subject
Has Abstractpub_date
2010-08-30 00:00:00pages
75-82issue
1-2eissn
0378-5173issn
1873-3476pii
S0378-5173(10)00441-2journal_volume
396pub_type
杂志文章abstract：:The purpose of this study was to explore whether it is possible to use hyper differential scanning calorimetry (HDSC) to detect and quantify low levels of amorphous content in samples that are mostly crystalline. HDSC uses scan rates that are much faster than conventional DSC, and consequently results in greater sensi...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2004.01.018
更新日期：2004-04-15 00:00:00
abstract：:The aim of this study was to provide preliminary validation of a new sublingual mucosal cell line (HO-1-u-1) for use as in vitro sublingual drug delivery screening of compounds involving passive diffusion. HO-1-u-1 cells were seeded on cell culture inserts. The ultrastructure and integrity of cell layers, inter-passag...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2006.10.012
更新日期：2007-04-04 00:00:00
abstract：:Understanding mechanical properties of pharmaceutical solids at the submicron scale can be very important to pharmaceutical research & development. In this paper, the hardness of individual particles of various pharmaceutical solids including sucrose, lactose, ascorbic acid, and ibuprofen was quantified using the atom...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2008.06.015
更新日期：2008-10-01 00:00:00
abstract：:Low density porous carriers are widely used in the pharmaceutical applications. Response surface methodology, using 3(2) factorial design was used to study drug adsorption on and its release patterns from microporous polypropylene (Accurel MP 1000) in the absence of additives. Ibuprofen, as model drug, was adsorbed on...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2006.09.013
更新日期：2007-02-22 00:00:00
abstract：:A disorder in the brain endothelium is thought to be closely related to the pathophysiology of brain diseases. A method for delivering nucleic acids (i.e. short interference RNA; siRNA) to the brain endothelium should be an attractive strategy for curing brain disorders. A liposomal nanoparticle containing a proton-io...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2014.02.016
更新日期：2014-04-25 00:00:00
abstract：:In a recent paper published in this journal, authors were perplexed by their results seemingly conflicting with our earlier findings [Sun, C.C., Himmelspach, M.W., 2006. Reduced tabletability of roller compacted granules as a result of granule size enlargement. J. Pharm. Sci. 95, 200-206]. After carefully reviewing th...
journal_title：International journal of pharmaceutics
pub_type： 评论,信件
doi：10.1016/j.ijpharm.2007.10.002
更新日期：2008-01-22 00:00:00
abstract：:Freeze-drying of three different forms of gene delivery systems was performed using a controlled two-step drying process and 10% sucrose as lyoprotectant. Complexes of pCMVL plasmid with transferrin-conjugated polyethylenimine, adenovirus-enhanced transferrinfection consisting of pCMVL/transferrin-polylysine complexes...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/s0378-5173(97)00244-5
更新日期：1997-11-28 00:00:00
abstract：:DNA fragments such as oligodeoxynucleotides (ODNs) are under investigation for a possible utilization in nuclear medicine. Until now, experiments on 99mTc-labeled ODNs in vitro or in vivo have required the application of time-consuming procedures to obtain and control the purity of the radiolabeled compound. A lyophil...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/s0378-5173(99)00293-8
更新日期：1999-11-15 00:00:00
abstract：:This study demonstrates the use of optical coherence tomography (OCT) to simultaneously characterize the roughness of the tablet core and coating of pharmaceutical tablets. OCT is a high resolution non-destructive and contactless imaging methodology to characterize structural properties of solid dosage forms. Besides ...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2017.12.023
更新日期：2018-01-30 00:00:00
abstract：:Amorphous nanoparticles are able to enhance the kinetic solubility and concomitant dissolution rates of BCS class II and BCS class II/IV molecules due to their characteristic increased supersaturation levels, smaller particle size and greater surface area. A DoE approach was applied to investigate formulation and spra...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2015.12.033
更新日期：2016-02-10 00:00:00
abstract：:The purpose of this investigation was to evaluate the performance of poly (amidoamine) (PAMAM) dendrimers, with three different surface groups, to be used as drug carriers. Drug-dendrimers complexes were investigated for solubility studies, dissolution studies, in vitro drug release studies, and for stability studies....
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2010.12.002
更新日期：2011-02-28 00:00:00
abstract：:Poly(methyl methacrylate) (PMMA) is used to fill the gap between the prosthesis and the surrounding bone in cemented arthroplasties. Biocompatibility problems related to bone cement application limit the clinical success of these cemented arthroplasties. Being the cement surface in close connection with the living bon...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2004.03.011
更新日期：2004-06-18 00:00:00
abstract：:In this study, a blend mixture of chitosan-ethylenediaminetetraacetic acid (CS 2 wt%-EDTA) at a weight ratio of 30/70 and polyvinyl alcohol (PVA) solution (10 wt%) was electrospun to produce fibrous mats with lysozyme (10, 20 and 30 wt%) used for wound healing. The morphology and diameter of the electrospun fiber mats...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2012.02.010
更新日期：2012-05-10 00:00:00
abstract：:We developed dual paclitaxel (PTX)/superparamagnetic iron oxide (SPIO)-loaded PLGA-based nanoparticles for a theranostic purpose. Nanoparticles presented a spherical morphology and a size of 240 nm. The PTX and iron loading were 1.84 ± 0.4 and 10.4 ± 1.93 mg/100 mg respectively. Relaxometry studies and phantom MRI dem...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2013.02.042
更新日期：2013-04-15 00:00:00
abstract：:We introduce a novel computational approach to designing passive drug delivery systems based on porous materials such as hydrogels. Our approach uses three tools: a method to establish the exact release pattern from all possible loading sites inside a given hydrogel; a method to generate a large number of hydrogel str...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2007.02.029
更新日期：2007-07-18 00:00:00
abstract：:Antibiotic-loaded acrylic bone cements (ALABCs) are well-established and cost-effective materials to control the occurrence of bone and joint infections. However, the inexistence of alternative antibiotics other than those already commercially available and the poor ability to bind to bone tissue hampering its biologi...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2015.05.038
更新日期：2015-07-25 00:00:00
abstract：:Low dose micro-tablets with acceptable quality attributes, specifically content uniformity (CU), would not only enhance the dose flexibility in the clinic, but also decrease excipient burden in pediatric population. Considering the CU challenges associated with directly compressed low dose micro-tablets, in this study...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2020.119571
更新日期：2020-09-25 00:00:00
abstract：:Several cationic compounds were screened as potential nasal absorption enhancers to increase intranasal absorption of a model drug, fluorescein isothiocyanate labeled dextran (MW 4.4 kDa, FD-4), without nasal membrane damage in rats. Their effects were compared with those of classical enhancers. Various cationic compo...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/s0378-5173(99)00100-3
更新日期：1999-08-05 00:00:00
abstract：:This paper describes a systematic approach to select optimum stabilizer for the preparation of nano-crystalline suspensions of an active pharmaceutical ingredient (API). The stabilizer can be either a dispersant or a combination of dispersant and wetting agent. The proposed screening method is a quick and efficient wa...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2014.09.048
更新日期：2014-12-10 00:00:00
abstract：:Previous in vivo studies using PEG 400 showed an enhancement in the bioavailability of ranitidine. This study investigated the effect of PEG 200, 300 and 400 on ranitidine transport across Caco-2 cells. The effect of PEG polymers (20%, v/v) on the bi-directional flux of (3)H-ranitidine across Caco-2 cell monolayers wa...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2011.02.059
更新日期：2011-05-16 00:00:00
abstract：:3D-printing technology is growing in importance due to increased availability and a wider range of applications. Here, we prepared and evaluated a hot melt pneumatic (HMP) 3D-printed QR (Quick Response)-coded orodispersible film (QRODF) containing a poorly water-soluble aripiprazole (ARP). Moreover, QRODF was formulat...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2020.119405
更新日期：2020-06-30 00:00:00
abstract：:A simple and rapid method for radiolabeling of three types of Ag NPs has been performed using 125I isotope, with high labeling yields, >90% without disturbing the optical properties. All the factors affecting labeling yield were studied. In order to monitor the in-vivo tissue uptake of radiolabeled Ag NPs using γ-rays...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2017.06.044
更新日期：2017-08-30 00:00:00
abstract：:In this note we describe the substitution of the phospholipid component in classical ISCOMs (immune-stimulating complexes) with the cationic lipid dioleoyl-trimethyl-ammonium-propane (DOTAP). The self-assembled colloidal structures formed by DOTAP, Quil-A and cholesterol were characterised using transmission electron ...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2006.09.029
更新日期：2007-03-06 00:00:00
abstract：:A biodegradable porous starch foam (BPSF) was developed for the first time as a carrier in order to improve the dissolution and enhance the oral bioavailability of lovastatin - defined as a model poorly water soluble BCS type II drug. In this paper, BPSF was prepared by the solvent exchange method and characterized by...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2010.09.040
更新日期：2011-01-17 00:00:00
abstract：:Cyclodextrin-containing polymers have proved themselves to be useful for controlled release. Herein we describe the preparation of membranes of poly(methylmethacrylate) (PMMA) containing hydroxypropyl-beta-cyclodextrins (HP-beta-CDs) using a supercritical CO(2)-assisted phase inversion method, for potential applicatio...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2009.04.029
更新日期：2009-07-06 00:00:00
abstract：:Dendrimers are considered versatile carriers especially for the treatment of diseases like cancer, AIDS, malaria etc. Cancer is a worldwide threat particularly in developing countries. A breakthrough research in this regard is a prime requirement. In the present study, folic acid was conjugated to fifth generation pol...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2010.04.002
更新日期：2010-06-30 00:00:00
abstract：:To understand the quality, efficacy, and safety of liposomal drugs, it is necessary to develop a robust and accurate method for the separation and the quantification of unencapsulated and liposome-associated drugs (or liposomal encapsulated drugs). Conventional methods involve separation of unencapsulated and liposome...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2018.07.019
更新日期：2018-10-05 00:00:00
abstract：:We have evaluated a miniaturized in vitro method, based on the μDISS Profiler™ technique that enables on-line monitoring of drug release from a 21 μl sample with 10 ml of release medium. Four model drugs in eight clinically used formulations, including both solid and non-solid drug delivery systems, were investigated....
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2015.03.076
更新日期：2015-01-01 00:00:00
abstract：:The objective of this study was to evaluate mucoadhesive properties and gastrointestinal transit of microspheres made of oppositely charged dextran derivatives and cellulose acetate butyrate (CAB). The microspheres were prepared by emulsion solvent evaporation method. A reference microsphere was made of lactose instea...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/s0378-5173(03)00159-5
更新日期：2003-06-04 00:00:00
abstract：:Praziquantel (PZQ) is effective against all known species of Schistosomes that infect humans. The failure of mass treatment of schistosomiasis has been attributed to the fact that therapy is not sufficiently long-lasting. This effect may be due to the low bioavailability of PZQ that has a low hydrosolubility and fast ...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2005.02.009
更新日期：2005-05-13 00:00:00
