Abstract:
:Cocrystallization of chlorbipram (ChBP), a novel phosphodiesterase-4 (PDE) inhibitor with water insoluble property developed in our lab, was performed to improve the physicochemical properties and bioavailability in the present study. Three new cocrystals with fumaric aicd (FA), gentisic acid (GA) and salicylic acid (SA) as coformers were synthesized and fully characterized by using the combination of multi-techniques. The cocrystals are phase stable even under high humidity conditions. In vitro study indicates that the solubility of ChBP-GA and ChBP-SA cocrystals increase to 3724.4 ± 58.7, 2897.4 ± 81.9 μg/mL in comparison with ChBP (2561.3 ± 150.4 μg/mL), the intrinsic dissolution rates (IDRs) of ChBP-GA and ChBP-SA cocrystals (721.3 ± 8.0, 614.4 ± 13.2 μg/min/cm2) are both higher than ChBP (537.9 ± 12.0 μg/min/cm2). The blood concentration peak values of ChBP-GA and ChBP-SA cocrystals (165.8 ± 50.9, 105.3 ± 35.6 ng/mL) are both higher than ChBP (51.3 ± 15.1 ng/mL) in in vivo evaluation. It presents the same order in in vitro/vivo study: ChBP-GA > ChBP-SA > ChBP > ChBP-FA. ChBP-FA cocrystal presents a longer elimination half life (t1/2 = 10.0 ± 2.6 h), which makes it a potential candidate for prolonged controlled release formulation. ChBP-GA and ChBP-SA cocrystals both present enhanced solubility and bioavailability in comparison with ChBP, making them a better candidate for the solid dosage formulation development.
journal_name
Int J Pharmjournal_title
International journal of pharmaceuticsauthors
Zhou J,Li L,Zhang H,Xu J,Huang D,Gong N,Han W,Yang X,Zhou Zdoi
10.1016/j.ijpharm.2019.118984subject
Has Abstractpub_date
2020-02-25 00:00:00pages
118984eissn
0378-5173issn
1873-3476pii
S0378-5173(19)31045-2journal_volume
576pub_type
杂志文章abstract::The present investigation describes a procedure for the synthesis of a glycidyl methacrylated derivative from galactomannan, GA-MA, and the respective hydrogel formation. The galactomannan (GA), raw material, was purified and dissolved in DMSO. After dissolution, 4-dimethyl-amino-pyridine (DMAP) and glycidyl methacryl...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2003.08.001
更新日期:2003-11-28 00:00:00
abstract::In the fluid bed agglomeration processes liquid distribution influences the agglomerate growth. We developed a new nozzle that produces uniform droplets, which allows droplets to be easily controlled in size independently of liquid- and airflow of the nozzle. It was found that the spray rate and the mixing in the spra...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/s0378-5173(99)00329-4
更新日期:2000-01-05 00:00:00
abstract::The present study puts forward a miniaturized high-throughput platform to understand influence of excipient selection and processing on the stability of a given drug compound. Four model drugs (sodium naproxen, theophylline, amlodipine besylate and nitrofurantoin) and ten different excipients were selected. Binary phy...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2012.08.025
更新日期:2013-08-30 00:00:00
abstract::The role of solvents in drug transport has not been properly addressed in the literature, despite its well known influence on drug permeation. Previously we have conducted thermodynamic and kinetic analyses to probe the molecular mechanisms of alcohol enhanced permeation. In the present study, the influence of tempera...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2011.08.037
更新日期:2011-11-28 00:00:00
abstract::The present study investigated the influence of in vitro dissolution conditions on the in vivo predictability of an amorphous solid dispersion of celecoxib (CCX) in the pH-sensitive polymer Eudragit® S 100. Different doses of a 25:75w/w% CCX:Eudragit® S 100 amorphous solid dispersion (CCX:EUD) were investigated. Durin...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2017.08.078
更新日期:2017-10-05 00:00:00
abstract::Liquid dosage forms, generally based on aqueous solutions, take an important role in drug administration. The approaches to a theoretical description of solvent and solubility properties have not yet proved completely satisfying. In this work, the Debye equation, which describes well polar and nonpolar molecules in an...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/s0378-5173(01)00771-2
更新日期:2001-08-28 00:00:00
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::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::Hydrophobic porphyrins are potentially interesting molecules for the photodynamic therapy (PDT) of solid cancers or ocular vascularization diseases. Their pharmaceutical development is, however, hampered by their lipophilicity, which renders formulation difficult especially when intravenous administration is needed. E...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2004.07.029
更新日期:2004-11-22 00:00:00
abstract::The objective of this study was to identify key variables affecting the initial release (burst) and the encapsulation of leuprolide acetate-containing poly(lactide-co-glycolide) (PLGA) microparticles, which were prepared by the cosolvent evaporation method. Adjusting parameters, which affected the PLGA precipitation k...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2006.06.004
更新日期:2006-11-06 00:00:00
abstract::Platelet-rich plasma (PRP) is used in therapy for bone tissue repair because an abundance of osteogenesis-related growth factors can be released from the concentrated platelets. However, its clinical use is limited because growth factors, temporally released from PRP, are degraded rapidly. This study aimed to incorpor...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2018.06.020
更新日期:2018-08-25 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 aim of this study was to investigate the importance of liposome structure in oestradiol skin delivery as a tool for understanding the delivery mechanism from lipid vesicles. Liposomes of phosphatidylcholine (PC) (1), PC, sodium cholate; 86:14 w/w (II), PC, Span 80; 86.7:13.3 w/w (III) and PC, oleic acid: 84:16 w/w...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/s0378-5173(00)00493-2
更新日期:2000-08-25 00:00:00
abstract::Powder filled sachets containing a 3:1 (w/w) powder mixture of diacetylmorphine base and caffeine anhydrate were developed as a dosage form for smokable heroin used for the treatment of chronic, treatment-resistant heroin addicts. The powder mixture was filled into sachets using a micro dose auger filler machine. The ...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2004.07.007
更新日期:2004-11-05 00:00:00
abstract::The efficiency of drug depends not only on its potency but also on its ability to reach the target sites in preference to non-target sites. In this regard, protein assembled nanocarrier is the most promising strategy for intracellular anti-cancer drug delivery. The key motive of this study is to fabricate biocompatibl...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2020.119192
更新日期:2020-04-30 00:00:00
abstract:UNLABELLED:The aim of this study is to validate the ability of the disappearance model to predict absorption rates of insulin aspart in pigs. The disappearance model is used as a screening tool to estimate absorption rates after subcutaneous injections in humans or pigs especially of insulin and insulin analogues. The ...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2006.09.004
更新日期:2007-02-07 00:00:00
abstract::The effect of different preparation parameters were analyzed with respect to the rheological and pharmaceutical characteristics of hydrogel blend patches, as transdermal delivery formulation. Mixtures of pectin and gelatin were employed for the production of patches, with adjustable properties, following a two-step ge...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2013.06.081
更新日期:2013-09-15 00:00:00
abstract::The objective of the present study was to establish several methods for the introduction of thiol groups onto the surface of human serum albumin (HSA) nanoparticles. Besides the epsilon-amino groups of lysine, the carboxyl groups of asparaginic and glutaminic acid, and the carbonyl groups of the cross-linker glutarald...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/s0378-5173(00)00590-1
更新日期:2000-12-15 00:00:00
abstract::The aim of this work was to investigate the anti-tumor effect of paclitaxel (PTX)-loaded methoxy poly(ethylene glycol)-poly(ɛ-caprolactone) nanoparticles (MPEG-NP/PTX) against glioblastoma multiforme (GBM). MPEG-NP/PTX was prepared by the emulsion and evaporation technique with particle size of 72.5±2.2nm and did not ...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2010.10.005
更新日期:2010-12-15 00:00:00
abstract::Efficient delivery of small interfering RNA (siRNA) remains a challenging task in RNA interference (RNAi) studies. In this study, we used chitosan-graft-polyethylenimine (CHI-g-PEI) copolymer composed of chitosan and low molecular weight polyethylenimine (PEI) for the delivery of siRNA. The CHI-g-PEI carrier formed st...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2009.05.046
更新日期:2009-08-13 00:00:00
abstract::Current treatment for pelvic organ prolapse (POP) and stress urinary incontinence (SUI) involves transvaginal implantation of surgical mesh, conventionally made of polypropylene (PP). However, it has recently become apparent that the mechanical properties of PP are unsuitable, resulting in serious complications such a...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2020.120145
更新日期:2021-01-25 00:00:00
abstract::We prepared an injectable depot system for the long-term delivery of alendronate using a solid/water/oil/water multiple emulsion technique with poly(lactic-co-glycolic acid) as a carrier. The microparticles were spherical with smooth surfaces, ranging from 20 to 70 μm in size. The microspheres (ALD-HA-RG504H-MC70) wer...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2015.01.020
更新日期:2015-03-01 00:00:00
abstract::Semifluorinated alkanes (SFAs) have been described as potential excipients for pulmonary drug delivery, but proof of their efficacy is still lacking. We tested whether SFA formulations with the test drug ibuprofen can be nebulised and evaluated their pharmacokinetics. Physico-chemical properties of five different ibup...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2011.10.051
更新日期:2012-01-17 00:00:00
abstract::A procedure is developed that allows particles inhaled with realistic breath patterns to be sized by cascade impaction at a constant flow rate. This procedure is then used to examine the difference between particle sizes obtained with constant flow rate (step profile) versus actual-subject breath patterns for two dry ...
journal_title:International journal of pharmaceutics
pub_type: 临床试验,杂志文章
doi:10.1016/s0378-5173(00)00569-x
更新日期:2000-12-04 00:00:00
abstract::The purpose of this work was to develop a practical and scalable method to encapsulate the hydrophobic antibiotic thiostrepton (TST) in sterically stabilized micelles (SSM). Using the conventional method of thin-film hydration, we encapsulated up to 5 drug molecules per SSM (diameter ∼ 16 nm). However, since this meth...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2018.12.001
更新日期:2019-02-10 00:00:00
abstract::It has been reported that the degree of particle agglomeration in fluidized bed coating is greatly affected by the spray mist size of coating solution. However, the mist size has generally been measured in open air, and few reports have described the measurement of the mist size in a chamber of the fluidized bed, in w...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/s0378-5173(98)00370-6
更新日期:1999-02-01 00:00:00
abstract::A simple and readily manoeuverable method for preparing immuno-magnetic liposomes that indigenously contain binding sites for attaching other molecules like antibodies on their exterior surface is described. In this method magnetic unilamellar vesicles are prepared from a mixture of phosphatidylcholine, cholesterol, s...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/s0378-5173(00)00667-0
更新日期:2001-03-14 00:00:00
abstract::Cationic liposomes spontaneously interact with negatively charged plasmid DNA to form a transfection competent complex capable of promoting the expression of a therapeutic gene. This work aims to improve the understanding of the poorly defined mechanisms and structural rearrangements associated with the lipid-DNA inte...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/s0378-5173(99)00117-9
更新日期:1999-06-25 00:00:00
abstract::This work focuses on the relevance of antibacterial nanofibers based on a polyelectrolyte complex formed between positively charged chitosan (CHT) and an anionic hydroxypropyl betacyclodextrin (CD)-citric acid polymer (PCD) complexing triclosan (TCL). The study of PCD/TCL inclusion complex and its release in dynamic c...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2016.09.060
更新日期:2016-11-20 00:00:00
abstract::Na-deoxycholate (Na-DOC) forms a viscous thixotropic gel when in contact with excess buffer systems. The resulting gels have been tested as novel drug carrier systems for topical use. The influence of differing amounts of mannitol, glycerol and xylitol on the viscous modulus (G"/Pa) was evaluated by oscillatory measur...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/s0378-5173(99)00170-2
更新日期:1999-08-05 00:00:00