Abstract：
:Fiber-optic near infrared (NIR) spectroscopy was used to investigate several key features of the polymorphic transitions observed during the crystallization and the filtration of SaC, an Active Pharmaceutical Ingredient (API) produced by Sanofi-Synthelabo. Using few samples, the spectroscopic data were calibrated to provide measurements of the polymorphic composition of the solid product which is likely to appear in two crystalline forms or in the amorphous state. Both qualitative and quantitative methods were successfully evaluated to characterize the API. The NIR spectroscopy measurement was then applied to investigate the kinetic behavior of the phase transition phenomena against various operating conditions. From the viewpoint of industrial process development several applications are presented. The effects of temperature and seed crystal habits on the rate of transition of filtration cakes are briefly investigated; and a study of the effect of residual water in the solvent on the transition occurring during filtration is more deeply analyzed. The experimental results demonstrate that highly valuable information can be provided by the NIR spectroscopy measurements, when one aims at understanding more deeply and optimizing the consequences of various and complex phenomena involved during the solid processing chain.
journal_name
Int J Pharmjournal_title
International journal of pharmaceuticsauthors
Févotte G,Calas J,Puel F,Hoff Cdoi
10.1016/j.ijpharm.2004.01.003keywords:
subject
Has Abstractpub_date
2004-04-01 00:00:00pages
159-69issue
1-2eissn
0378-5173issn
1873-3476pii
S037851730400016Xjournal_volume
273pub_type
杂志文章abstract：:CHF5633 (Chiesi Farmaceutici, Italy) is a synthetic pulmonary surfactant currently under clinical development for the treatment of Respiratory Distress Syndrome in premature infants. The product is composed of phospholipids in liposomal organization, together with two peptide analogues of human surfactant proteins B a...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2018.10.045
更新日期：2018-12-20 00:00:00
abstract：:The aim of this study was to investigate the equilibrium swelling properties in urea solutions of gamma-radiation induced polyelectrolyte copolymeric hydrogels consisting of acrylamide (AAm) and crotonic acid (CA). Poly(acrylamide-co-crotonic acid), poly(AAm-co-CA) hydrogels containing different amounts of CA were obt...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2005.05.026
更新日期：2005-09-14 00:00:00
abstract：:Amphipathic partial dendrimers having three lipidic (C(14)) chains coupled to dendritic lysine head groups with eight, 16 or 32 free terminal amino groups have been synthesised by solid-phase peptide synthesis. Liposomes were prepared with positive, negative and neutral charge using the dehydration-rehydration method ...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/s0378-5173(00)00635-9
更新日期：2001-02-19 00:00:00
abstract：:The effect of the protein stabilizers on the stability and aerosol performance of spray dried recombinant human growth hormone (SD rhGH) was investigated. rhGH solution was spray dried alone, with polysorbate 20 (at three concentrations of 0.05%, 0.01%, and 0.005%), Zn(2+) (by Zn(2+):rhGH molar ratio of 2:1 and 4:1), ...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2007.10.053
更新日期：2008-03-20 00:00:00
abstract：:In the present study, the features of two new thiolated polymers--the so-called thiomers--were investigated. Mediated by a carbodiimide cysteamine was covalently attached to sodium carboxymethylcellulose (Na-CMC) and neutralised polycarbophil (Na-PCP). Depending on the weight-ratio polymer to cysteamine during the cou...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/s0378-5173(01)00955-3
更新日期：2002-03-02 00:00:00
abstract：:The simultaneous skin permeation of drug and penetration enhancer have been studied in vitro. Simple formulations of mefenamic acid in PEG400 incorporating various proportions of ethanol or 1,8-cineole were prepared and applied to porcine ear skin in diffusion cells under infinite conditions. Receptor phases were assa...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2006.05.018
更新日期：2006-09-14 00:00:00
abstract：:Sodium salts are often used in drug formulation but their partial solubility parameters are not available. Sodium alters the physical properties of the drug and the knowledge of these parameters would help to predict adhesion properties that cannot be estimated using the solubility parameters of the parent acid. This ...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/s0378-5173(99)00374-9
更新日期：2000-01-20 00:00:00
abstract：:Particle detection and analysis techniques are essential in biopharmaceutical industries to evaluate the quality of various parenteral formulations regarding product safety, product quality and to meet the regulations set by the authority agencies. Several particle analysis systems are available on the market, but for...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2018.03.050
更新日期：2018-05-30 00:00:00
abstract：:Achieving stable, efficient and non-toxic pulmonary gene delivery is most challenging requirement for successful gene therapy to lung. Composite nanoparticles (NPs) of the poly(lactic-co-glycolic acid) (PLGA) and cationic polymer polyethyleneimine (PEI) is an efficient alternative to viral and liposomal vectors for th...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2017.03.094
更新日期：2017-05-30 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：:The aim of present study is to investigate the effect of poly(amidoamine) (PAMAM) dendrimer on skin permeation of 5-fluorouracil (5FU). Permeation studies were performed using excised porcine skin in a Franz diffusion cell and (14)C labeled 5FU samples were analyzed using liquid scintillation counter. Three different ...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2008.05.034
更新日期：2008-09-01 00:00:00
abstract：:The two polyhydroxy surfactants polyglycerol 6-distearate (Plurol(®)Stearique WL1009 - (PS)) and caprylyl/capryl glucoside (Plantacare(®) 810 - (PL)) are a class of PEG-free stabilizers, made from renewable resources. They were investigated for stabilization of aqueous solid lipid nanoparticle (SLN) and nanostructured...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2010.12.036
更新日期：2011-03-15 00:00:00
abstract：:The main objective of the study was to evaluate if the liquid crystalline cubic phase gel of glyceryl monooleate (GMO) protects insulin from agitation induced aggregation. The aggregation of Humulin(R), Regular Iletin I(R) and Regular Iletin II(R), in cubic phase GMO gels at 30 U/g of gel was compared with that in PBS...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/s0378-5173(99)00288-4
更新日期：1999-11-25 00:00:00
abstract：:The effect of dry granulation (roller compaction and slugging) on compactibility and tablet capping tendency in a formulation with macrolide antibiotic and microcrystalline cellulose (MCC) was investigated. Direct tableting of this formulation revealed a pronounced capping tendency. Both dry granulated systems exhibit...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2008.01.023
更新日期：2008-06-05 00:00:00
abstract：:Solid lipid nanoparticles (SLNs) conjugated with tamoxifen (TX) and lactoferrin (Lf) were applied to carry anticancer carmustine (BCNU) across the blood-brain barrier (BBB) for enhanced antiproliferation against glioblastoma multiforme (GBM). BCNU-loaded SLNs with modified TX and Lf (TX-Lf-BCNU-SLNs) were used to pene...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2015.12.054
更新日期：2016-02-29 00:00:00
abstract：:Progesterone-loaded poly(lactic) acid fibrous polymeric patches were produced using electrospinning and pressurized gyration for intra-vaginal application to prevent preterm birth. The patches were intravaginally inserted into rats in the final week of their pregnancy, equivalent to the third trimester of human pregna...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2020.119782
更新日期：2020-10-15 00:00:00
abstract：:The purpose of this study was to investigate the formation mechanism of colloidal nanoparticles after dispersion of probucol/polyvinylpyrrolidone (PVP)/sodium dodecyl sulphate (SDS) ternary ground mixture (GM) into water. Probucol, PVP and SDS were mixed at a weight ratio of 1:3:1 and ground for 30 min with a vibratio...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2007.10.052
更新日期：2008-03-20 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：:Superparamganetic iron oxide-based contrast agents in magnetic resonance imaging (MRI) have offered new possibility for early detection of lymph nodes and their metastases. According to important role of nanoparticle size in biodistribution, magnetite nanoparticles coated with different polyethylene glycol (PEG) conce...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2012.04.080
更新日期：2012-08-20 00:00:00
abstract：:The objective of the present study was to synthesize and investigate the transgene expression efficacy of quaternized derivatives of aminoglycoside polymers in different cancer cell lines. A series of glycidyltrimethylammonium chloride (GTMAC) derivatives of aminoglycoside polymers (GTMAC-AM polymers), containing vary...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2015.04.026
更新日期：2015-07-15 00:00:00
abstract：:The effect of carrier surface properties on drug particle detachment from carrier crystals during inhalation with a special test inhaler with basic air classifier has been studied for mixtures containing 0.4% budesonide. Carrier crystals were retained in the classifier during inhalation and subsequently examined for t...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/s0378-5173(03)00264-3
更新日期：2003-07-24 00:00:00
abstract：:Here we explore the opportunity to design and then produce tailored release of therapeutic drugs from microcapsules. By use of "building blocks," formed from well characterized microcapsule populations, an inverse design algorithm has been developed that provides an optimal (in a least squares sense) combination of bu...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2009.09.010
更新日期：2010-01-04 00:00:00
abstract：:The objective was to quantify drug loss due to cold flow (CF) in marketed estradiol transdermal drug delivery systems (TDDS), and study its influence on the in vitro flux and drug transfer across contacting skin. TDDS samples (products-A and B) were induced with CF at 25 and 32°C/60% RH by applying 1-kg force for 72h....
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2014.10.013
更新日期：2014-12-30 00:00:00
abstract：:To reduce systemic bleeding risks during anticoagulant treatment, a new concept named "precise anticoagulation" was proposed to localize the effects of anticoagulants via the targeted delivery of prodrugs to the coagulation site. In this study, the fusion protein Annexin V-hirudin 3-ABD (hAvHA) was constructed to achi...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2020.119869
更新日期：2020-09-10 00:00:00
abstract：:A relatively high molecular weight of 4-arm star PELA was obtained by ring-opening polymerization of l-lactic acid O-carboxyanhydride with 4-arm-PEG in the presence of DMAP as an initiator. The results via(1)H NMR and (13)C NMR show that the end of the star PELA chain is a hydroxyl group and the central core is a PEG ...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2015.05.074
更新日期：2015-08-01 00:00:00
abstract：:Oral absorption of lopinavir (LPV) is limited due to P-glycoprotein (P-gp) and multidrug resistance-associated protein2 (MRP2) mediated efflux by intestinal epithelial cells. Moreover, LPV is extensively metabolized by CYP3A4 enzymes. In the present study, dipeptide prodrug approach was employed to circumvent efflux p...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2014.09.035
更新日期：2014-12-10 00:00:00
abstract：:Using twin-screw granulation as particle size enlargement technique, the effect of modifying the screw configuration (number of mixing zones, configuration of kneading block) on granule quality, tablet properties and mixing efficiency was investigated. The amount of oversized agglomerates and yield was significantly i...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2008.01.012
更新日期：2008-05-22 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：:The aim of this work was to develop a tablet for the buccal delivery of the poorly soluble drug carvedilol (CAR), based on poly(ethyleneoxide) (PEO) as bioadhesive sustained-release platform and hydroxypropyl-beta-cyclodextrin (HPbetaCD) as modulator of drug release. As first, PEO tablets loaded with CAR/HPbetaCD bina...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2006.03.031
更新日期：2006-08-17 00:00:00
abstract：:A novel, efficient delivery system for iron (Fe2+) was developed using the alginate biopolymer. Iron loaded alginate nanoparticles were synthesized by a controlled ionic gelation method and was characterized with respect to particle size, zeta potential, morphology and encapsulation efficiency. Successful loading was ...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2016.09.053
更新日期：2016-11-20 00:00:00
