Abstract:
:Moisture-sensitive pseudo-polymorphs with different stabilities were characterized, and their polymorphisms were monitored in the process of tableting and film coating by near-infrared (NIR) spectroscopy. In this study, we proved that we could successfully maintain the crystal form ratio in the tablet by controlling the moisture profile during the manufacture to sufficiently stabilize the drug product. Mitemcinal fumarate is an erythromycin derivative with two pseudo-polymorphic forms, hydrate and anhydrate. We characterized them by X-ray powder diffraction and water sorption isotherm plot analysis. Stability test revealed that the hydrate form is more stable than the anhydrate form. We established a quantitative method by using NIR and monitored the hydrate form ratio in the tablet during the tableting and coating process. The manufacturing room was controlled to between 40 and 60% RH. Although the hydrate form ratio just after the onset of tableting decreased to below 40%, 60% was obtained at the end of the final process which sufficiently retains stability. Transition of the hydrate form ratio during the manufacturing process was reasonable; this indicates that our NIR method is suitable for monitoring. Thus, NIR is one of the most suitable tools for in-process testing of these humidity-sensitive APIs.
journal_name
Int J Pharmjournal_title
International journal of pharmaceuticsauthors
Kamada K,Yoshimura S,Murata M,Murata H,Nagai H,Ushio H,Terada Kdoi
10.1016/j.ijpharm.2008.10.010subject
Has Abstractpub_date
2009-02-23 00:00:00pages
103-8issue
1-2eissn
0378-5173issn
1873-3476pii
S0378-5173(08)00696-0journal_volume
368pub_type
杂志文章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 aim of our research was to apply experimental design methodology in the development and optimization of drug release methods. Diclofenac sodium (2-[(2,6-dichlorophenyl)amino]benzeneacetic acid monosodium salt) was selected as a model drug and Naklofen retard prolonged release tablets, containing 100 mg of diclofen...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2004.07.041
更新日期:2005-03-03 00:00:00
abstract::Herein, a series of new amino acid-functionalized hollow mesoporous silica nanospheres (HMSNs) by post-grafting methods were prepared. These new materials were characterized by different techniques and were studied as matrices for the antineoplastic drug (cisplatin) transport and delivery. The results demonstrate that...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2019.118709
更新日期:2019-12-15 00:00:00
abstract::Natural compounds offer a wide spectrum of potential active substances, but often they have a poor bioavailability. To increase the bioavailability and bioactivity of the natural anti-inflammatory molecules curcumin and diplacone, we used glucan particles (GPs), hollow shells from Saccharomyces cerevisiae composed mai...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2020.119318
更新日期:2020-05-30 00:00:00
abstract:BACKGROUND:Perfluorocarbon-nanoemulsions (PFC-NE) made of PFC and phospholipids (PL) by homogenization are optimal for in vivo-19F labelling of monocytes and subsequently of inflamed tissues in magnetic resonance imaging (MRI). Necessary requirements for in vivo use of PFC-NE are sterility, suitable droplet sizes and t...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2019.118753
更新日期:2019-12-15 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
abstract::Blend uniformity analysis (BUA) is a routine and highly regulated aspect of pharmaceutical production. In most instances, it involves quantitative determination of individual components of a blend in order to ascertain the mixture ratio. This approach often entails the use of costly and sophisticated instrumentation a...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2012.07.073
更新日期:2012-11-15 00:00:00
abstract::In order to improve the dissolution and absorption properties of loviride, a poorly soluble antiviral agent, sucrose co-freeze-dried nanopowders were prepared, characterized and evaluated. Tween 80/poloxamer 188-stabilized nanosuspensions were produced on a laboratory scale using media milling. The milling process was...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2007.02.005
更新日期:2007-06-29 00:00:00
abstract::Vesicular systems have shown their ability to increase dermal and transdermal drug delivery. Their mechanism of drug transport into and through the skin has been investigated but remains a much debated question. Several researchers have outlined that drug penetration can be influenced by modifying the surface charge o...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2011.03.049
更新日期:2011-06-15 00:00:00
abstract::Dextran nanobubbles were prepared with a dextran shell and a perfluoropentan core in which oxygen was stored. To increase the stability polyvinylpirrolidone was also added to the formulation as stabilizing agent. Rhodamine B was used as fluorescent marker to obtain fluorescent nanobubbles. The nanobubble formulations ...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2009.07.010
更新日期:2009-11-03 00:00:00
abstract::The aerodynamic performance of a dry powder for inhalation depends on the formulation and the dry powder inhaler (DPI). In the case of capsule-based DPIs, the capsule also plays a role in the powder aerosolisation and the dispersion of the micronized drug during the inhalation. This study evaluated the impact of gelat...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2018.10.034
更新日期:2018-12-20 00:00:00
abstract::3-D ordered macroporous carbon with different polymer coatings were developed as new oral vaccine immunological systems. Poly dimethyl diallyl ammonium (PDDA), polyethyleneimine (PEI) and chitosan (CTS), three different polymers with electropositive or adsorption-promoting properties, were chosen as the coating materi...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2015.04.045
更新日期:2015-06-20 00:00:00
abstract::The need to be able to measure amorphous contents in crystalline powders is now recognised. In this review, calorimetric and gravimetric methods are reviewed in a way that should alert workers in the field to the theoretical, and practical considerations which are important to understanding how best to study crystalli...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章,评审
doi:10.1016/s0378-5173(98)00335-4
更新日期:1999-03-15 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::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::The aim of this study was using Eudragit-cysteine conjugate to coat on chitosan microspheres (CMs) for developing an oral protein drug delivery system, having mucoadhesive and pH-sensitive property. Bovine serum albumin (BSA) as a protein model drug was loaded in thiolated Eudragit-coated CMs (TECMs) to study the rele...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2008.04.003
更新日期:2008-07-09 00:00:00
abstract::Delivery of poorly soluble drugs has been problematic due to its low absorption profile and bioavailability. In this work, ursodeoxycholic acid (UDCA), a poorly-soluble drug, was intercalated into inorganic nanovehicle, layered double hydroxides (LDHs), with a molecular level to enhance its solubility in biological fl...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2010.09.039
更新日期:2010-12-15 00:00:00
abstract::During the pharmaceutical development of pregabalin extended-release tablets, an unknown degradant at a relative retention time (RRT) of 11.7 was observed and its nominal amount exceeded the ICH identification threshold in an accelerated stability study. The aim of this study is to identify the structure and investiga...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2019.118910
更新日期:2020-02-15 00:00:00
abstract::New therapeutic strategies against inflammatory bowel disease (IBD) consider the usage of probiotics, prebiotics and synbiotics as beneficial for the intestinal microbial balance. Limitations of such an approach are addressed into difference in survival, persistence, colonization and variable effects among different p...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2017.05.049
更新日期:2017-07-15 00:00:00
abstract::Three-dimensional printing includes a wide variety of manufacturing techniques, which are all based on digitally-controlled depositing of materials (layer-by-layer) to create freeform geometries. Therefore, three-dimensional printing processes are commonly associated with freeform fabrication techniques. For years, th...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章,评审
doi:10.1016/j.ijpharm.2015.12.071
更新日期:2016-02-29 00:00:00
abstract::Hot-melt coating (HMC) as a solvent-free technology grants faster and more economic coating processes with reduced risk of dissolving the drug during the process. Moreover, traditional coating equipment can be modified to enable the HMC process. Despite the indubitable advantages and feasibility of the process, HMC is...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2017.08.086
更新日期:2017-11-30 00:00:00
abstract::Spray drying is a well-established technology to produce inhalable dry powders. However, the amorphous nature of the particles typically obtained from the process can lead to physically and chemically unstable products. The purpose of this study was to investigate whether spray-drying could be used as a manufacturing ...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2019.04.036
更新日期:2019-06-30 00:00:00
abstract::The concept of skin-specific drug delivery with a spatio-temporal control has just recently received concerns in dermatology. Inspired by the progress in smart materials and their perspective application in medicine science, development of stimuli responsive drug delivery systems with skin-specificity has become possi...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章,评审
doi:10.1016/j.ijpharm.2020.120081
更新日期:2021-01-05 00:00:00
abstract::We demonstrate a rapidly formed cubic liquid crystalline phase, i.e. typically 1g cubic phase in less than 1 min confirmed by X-ray diffraction, consisting of an ether lipid, 1-glyceryl monooleyl ether (GME), an aprotic solvent (propylene glycol or pentane-1,5-diol) and water. The efficacy of the cubic formulation was...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2013.05.047
更新日期:2013-08-16 00:00:00
abstract::The effect of mixing conditions on the flow curves of some clay-water dispersions was studied. Two Spanish fibrous phyllosilicates (sepiolite from Vicálvaro and palygorskite from Turón) and a commercial bentonite (Bentopharm Copyright, UK) were selected as model clays. The disperse systems were made up using a rotor-s...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/s0378-5173(99)00075-7
更新日期:1999-05-10 00:00:00
abstract::The work was aimed at developing an in vitro method able to provide rapid and reliable evaluation of drug absorption through buccal mucosa. Absorption simulator apparatus endowed with an artificial membrane was purposely developed by experimental design. The apparent permeation coefficient (Papp) through excised porci...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2018.06.032
更新日期:2018-08-25 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 overall aim of this study is to coat emulsion droplets with nanoparticles using a simple heterocoagulation process in aqueous dispersion and determine: the adsorption behavior and interfacial layer microstructure, droplet physical stability against flocculation and coalescence, and the release profile of a model l...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2006.06.044
更新日期:2006-10-31 00:00:00
abstract::In the pharmaceutical industry, in vitro dissolution testing ofsolid oral dosage forms is a very important tool for drug development and quality control. However, ion-pairing interaction between the ionic drugand surfactants in dissolution medium often occurs, resulting in inconsistent and incomplete drug release. The...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2017.10.063
更新日期:2018-01-15 00:00:00
abstract::Ibuprofen (IBU) was chosen as a model drug to investigate the drug delivery rate. Mesoporous MCM-41 has been charged with ibuprofen (MCM-41_IBU). Calcium alginate was applied to encapsulate free drug and the mesoporous material. The system with double barrier demonstrated a slower release of IBU than free ibuprofen-lo...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2014.06.037
更新日期:2014-09-10 00:00:00