ANALYST
·
2023
·Vol. 148
·期 15
·3518-3523
·
IF 4.2
Hao Gu,Guoxin Dai,Zhongqiu Teng,Lina Geng,Wei Xu
Liquid chromatography-tandem mass spectrometry (LC-MS/MS) is a universal method for the quantitative analysis of small molecular drugs in therapeutic drug monitoring (TDM). Alternatively, liquid chromatography-miniature mass spectrometry (LC-Mini MS) is a simple operating technique for quantitative analysis. However, the wide chromatographic peaks and long retention times of TDM samples using the LC-Mini MS system deteriorated the accuracy and efficiency of quantitative analysis. Here, an optimized electrospray ionization (ESI) interface setup with a splitter valve and a capillary needle (I.D. 30 μm and O.D. 150 μm) of the LC-Mini MS system was acquired. The chromatographic peaks were narrower and smoother and the retention time was shorter for TDM compounds. Furthermore, a quantitative analysis method for risperidone and the active metabolite 9-hydroxyrisperidone in plasma was developed based on this optimal LC-Mini MS setup. The results showed that the calibration curves of risperidone and 9-hydroxyrisperidone had good linear ranges of 2–100 ng mL−1 (R2 = 0.9931) and 2–100 ng mL−1 (R2 = 0.9915), respectively. Finally, the matrix effects, recoveries and stability of risperidone and 9-hydroxyrisperidone samples were analyzed. The results satisfied the requirements of quantitative validation in routine TDM procedures.
研究领域:
分析化学
·
药学
·
医学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
JOURNAL OF THE BRAZILIAN CHEMICAL SOCIETY
·
2017
·Vol. 28
·期 10
·1866-1873
·
IF 1.198
Yin Qinhong,Zhu Yanqin,Yang Yaling
Oleic acid modified Fe3O4 nanoparticles were proposed for magnetic solid-phase extraction coupled with ultra high-performance liquid chromatography-tandem mass spectrometry to determine risperidone (RISP) and 9-hydroxyrisperidone (9OHR) in biological samples. The effects of various experimental parameters including adsorbent amount, pH, adsorption time, eluent type and concentration were systematically investigated. Under optimal conditions, the calibration curve was linear within the concentration range of 0.2-200 ng mL-1 with the correlation coefficient (r) of 0.9962 and the lower limit of quantification was 0.06 ng mL-1 for RISP; the calibration curve was linear within the concentration range of 0.2-200 ng mL-1 with the correlation coefficient of 0.9956 and the lower limit of quantification was 0.04 ng mL-1 for 9OHR. The extraction recoveries were over 90.0% with relative standard deviation less than 5.0%. All these results suggested that magnetic extraction method can be used for enrichment and quantification of RISP and 9OHR in biological samples.
研究领域:
分析化学
·
药物分析
✓ 已验证
产品关联
DOI
高影响因子
TALANTA
·
2018
·
IF 4.244
Wen-Hua Ji,Yu-Shuang Guo,Xiao Wang,D.-S. Guo
An accurate, rapid, and sensitive method for the determination of risperidone and 9-hydroxyrisperidone in urine samples was developed by combining water-compatible magnetic molecularly imprinted solid-phase extraction with high performance liquid chromatography. Several variables relating to the efficiency of magnetic solid phase extraction were optimized, including the amount of adsorbent, adsorption time, type of elution solvent, and desorption time. The analytical performance of this method was validated under the optimized conditions. The linearity for risperidone and 9-hydroxyrisperidone was obtained in the range 1–2000 ng mL −1 with correlation coefficient ≥ 0.991. Limits of detection of risperidone and 9-hydroxyrisperidone are 0.21 ng mL −1 and 0.24 ng mL −1 , respectively. Recoveries at three spike levels (10, 100, and 1000 ng mL −1 ) ranged from 94.6% to 102.4% with relative standard deviations (%) ≤ 5.3. These results confirmed that this method can be successfully and facilely used to analyze the multi-residues of risperidone and 9-hydroxyrisperidone in urine samples with high efficiency and good sensitivity.
研究领域:
分析化学
·
药物分析
·
环境科学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
JOURNAL OF MICROENCAPSULATION
·
2019
·
IF 2.04
Zhaoying Wu,Mengqing Zhao,Wei Zhang,Zhao Yang,Shuxin Xu,Qing Shang
The purpose of this study was to investigate the influences of drying methods on the risperidone (RIS) release profiles of RIS-loaded PLGA microspheres. These microspheres were fabricated with an O/W emulsion solvent evaporation method. The wet microspheres were dried with freeze drying and vacuum drying methods. The microspheres were mono-dispersed spheres with an average diameter of 100 μm. Studies found that drying methods had great influence on the porosity, morphology, and release profiles of RIS-loaded PLGA microspheres. Specifically, the freeze-dried microspheres had higher porosity (78.46 ± 1.64%) than those vacuum-dried ones (52.45 ± 2.68%), and they showed higher RIS release rates (p < 0.05). In the accelerated release tests (45 °C), these microspheres dried under the pressures of 700 mmHg and 200 mmHg gave faster release rates than those ones dried under the pressure of 450 mmHg. Importantly, the accelerated release test (45 °C) had a high correlation with the real-time test (37 °C) (R2 > 0.99). These studies exhibited a significance in the precise preparation of RIS-loaded PLGA microspheres.
研究领域:
药学
·
生物材料学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
POLYMERS FOR ADVANCED TECHNOLOGIES
·
2017
·Vol. 29
·期 1
·384-393
·
IF 1.907
Qing Shang,Aixin Zhang,Zhaoying Wu,Sijin Huang,Ruiqiong Tian
The aim of this study was to fabricate different risperidone (RIS)–loaded poly(lactic-co-glycolic acid) microspheres (PLGA MS) with various viscosity of PLGA polymers and investigate the RIS release profiles. Risperidone-loaded PLGA MS were fabricated via an oil/water–type emulsion solvent evaporation method, using ethyl acetate and benzil alcohol as the dispersed solvents. The PLGA (75:25) with the viscosity of 0.82, 0.93, and 1.10 dL/g was used in the fabrication. The morphology and the degradation of the RIS-PLGA MS were investigated with a scanning electron microscope. The distribution states of RIS in the PLGA MS were studied with differential scanning calorimetry. The residual of ethyl acetate and benzil alcohol in the resulting MS was monitored with gas chromatography. The in vitro release profiles of RIS from PLGA MS were also studied. Scanning electron microscope photographs illustrated that the obtained PLGA MS were monodisperse spheres with an average diameter of 100 μm. Gas chromatography results suggested that no residual ethyl acetate was left in the final RIS-PLGA MS, and the residue amount of benzil alcohol was about 1%. In vitro drug release profiles from the microsphere showed a substantially sigmoidal pattern of negligible initial burst up to 24 hours and minimal release (time lag) for 14 days. After the lag phase, slow release took a place up to 30 days, and then rapid release occurred sharply for about 2 weeks. The RIS release reached equilibrium around day 50. All release profiles showed the similar trend, and no significant difference was observed among these release profiles ( P > .05). This phenomenon indicated that RIS-loaded PLGA MS with the viscosity of 0.82 to 0.93 dL/g showed the optimal release behavior. However, no obvious differences were found among the MS obtained from the viscosity of 0.82 to 1.10 dL/g. These studies provided basis for the quality control in the industrial production of PLGA MS.
研究领域:
药剂学
·
生物材料学
✓ 已验证
产品关联
DOI
高影响因子
INTERNATIONAL JOURNAL OF PHARMACEUTICS
·
2025
·
IF 5.2
Bingwen Zhang,Haofan Liu,Yixuan Li,Tong Cao,Jinkuo Cao,Liandong Hu
This paper proposes a novel and efficient centrifugal microfluidic technology to prepare risperidone-loaded poly(lactic-co-glycolic acid) (PLGA) microspheres (RIS-MS). The effects of key parameters, including PLGA concentration and type, microchannel inner diameter and centrifugal speed on particle size, morphology and drug release were evaluated and optimized. The in vivo pharmacokinetic study of RIS-MS was conducted in rabbits. The results demonstrated that RIS-MS could be produced from microchannels with inner diameters of 170–210 μm at a centrifugal speed of 400 revolutions per minute (rpm) when the PLGA content is 15 % or higher. The mean plasma concentration of RIS-MS was more stable and C max of RIS-MS was significantly lower than that of the suspension group, and the RIS-MS could maintain the release of RIS in rabbits for up to 42 days. This study provided pioneering ideas for developing microspheres using centrifugal microfluidic technology. The optimized RIS-MS can make excellent sustained release and have the potential for the long-acting therapy of schizophrenia.
研究领域:
制药工程
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生物医学工程
·
药理学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
JOURNAL OF PHARMACEUTICAL SCIENCES
·
2016
·
IF 2.641
Wei Weng,Peng Quan,Chao Liu,Hanqing Zhao,Liang Fang
The purpose of this work was to develop and design an appropriate drug-in-adhesive patch for transdermal delivery of risperidone (RISP). Various formulation factors were investigated by in vitro permeation study using excised rabbit skin. Increasing the drug concentration in the pressure sensitive adhesive (PSA) was used to enhance the drug permeation. To overcome the high crystallization tendency of the patch, several crystallization inhibitors such as PVP , PEG, and surfactants and fatty acids were evaluated by microscopy study. The mechanism of crystallization inhibition was investigated by differential scanning calorimetry , nuclear magnetic resonance spectrometer, and FT-IR studies. RISP and its active metabolite were determined after topical application of the optimized transdermal patch , and the in vivo pharmacokinetic parameters were compared with the intravenous administration group. The microscopy study indicated that fatty acid greatly inhibited the crystallization of RISP in PSA. The inhibition was attributed to the drug-additive interaction between amino group of RISP and the carboxyl group of fatty acid which was further confirmed by 1 H-NMR and FT-IR studies. The optimal permeation profile was obtained with the patches containing 5% RISP and 5% oleic acid in Duro-Tak ® 87-2287. The in vivo pharmacokinetic study exhibited a sustained absorption and metabolism profile and well correlated with the in vitro permeation data.
研究领域:
药剂学
·
药物传递系统
✓ 已验证
DOI
高影响因子
LAB ON A CHIP
·
2024
·
IF 6.1
Wenwen Chen,Hao Li,Xinyue Zhang,Yutao Sang,Zhihong Nie
Monodisperse biodegradable polymer microspheres show broad applications in drug delivery and other fields. In this study, we developed an effective method that combines microfluidics with interfacial instability to prepare monodispersed poly(lactic-co-glycolic acid)-b-polyethylene glycol (PLGA-PEG)/poly(lactic-co-glycolic acid) (PLGA) microspheres with tailored surface morphology. By adjusting the mass ratio of PLGA-PEG to PLGA, the concentration of stabilizers and the type of PLGA, we generated microspheres with various unique folded morphologies, such as “fishtail-like”, “lace-like” and “sponge-like” porous structures. Additionally, we demonstrated that risperidone-loaded PLGA-PEG/PLGA microspheres with these folded morphologies significantly enhanced drug release, particularly in the initial stage, by exhibiting a logarithmic release profile. This feature could potentially address the issue of delayed release commonly observed in sustained-release formulations. This study presents a straightforward yet effective approach to construct precisely engineered microspheres offering enhanced control over drug release dynamics.
研究领域:
药剂学
·
材料科学
·
药物递送系统
✓ 已验证
DOI
PubMed
高影响因子
INTERNATIONAL JOURNAL OF PHARMACEUTICS
·
2024
·
IF 5.3
Yuying Chen,Qingwei He,Huangjie Lu,Jie Yang,Jiongming Han,Ying Zhu,Ping Hu
This study addresses the challenging task of quantitatively investigating drug release from PLGA microspheres after in vivo administration. The objective is to employ Förster resonance energy transfer (FRET) to visualize drug-encapsulated microspheres in both in vitro and in vivo settings. The primary goal is to establish a quantitative correlation between FRET fluorescence changes and microsphere drug release. The study selects drugs with diverse structures and lipid solubility to explore release mechanisms, using PLGA as the matrix material. Clozapine and risperidone serve as model drugs. FRET molecules, Cy5 and Cy5.5, along with Cy7 derivatives, create FRET donor–acceptor pairs. In vitro results show that FRET fluorescence changes align closely with microsphere drug release, particularly for the Cy5.5-Cy7 pair. In vivo experiments involve subcutaneous administration of microspheres to rats, tracking FRET fluorescence changes while collecting blood samples. Pharmacokinetic studies on clozapine and risperidone reveal in vivo absorption fractions using the Loo-Riegelman method. Correlating FRET and in vivo absorption data establishes an in vitro – in vivo relationship (IVIVR). The study demonstrates that FRET-based fluorescence changes quantitatively link to microsphere drug release, offering an innovative method for visualizing and monitoring release in both in vitro and in vivo settings, potentially advancing clinical applications of such formulations.
研究领域:
药剂学
·
生物医学工程
·
药理学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
JOURNAL OF MOLECULAR STRUCTURE
·
2025
·
IF 4.7
Chao Hao,Changping Fan,Lanting Gao,Mingyue Yin,Xue Jiang,Chenchen Wang,Xingyin Wang,Chaoyang Yin,Guisen Zhang,Jian Zhang
The present study aimed to prepare and evaluate a sustained-release microsuspension (MSP) of the antischizophrenic drug risperidone (RIS) via cocrystallization with kaempferol (KAE) (RIS-KAE-MSP). Cocrystal solvates of RIS and KAE in solvent systems of ethanol (EtOH), methanol (MeOH) and ethyl acetate (EA) were successfully prepared by solvent evaporation method. Cocrystal solvates prepared from 3 different solvent systems were characterized in detail using single-crystal X-ray diffraction (SCXRD), Hirshfeld surface analysis (HSA), Gas chromatography (GC), Karl Fischer titration (KFT), powder X-ray diffraction (PXRD), differential scanning calorimetry (DSC), thermogravimetric analysis (TGA) and Fourier transform infrared (FT-IR) spectroscopy. SCXRD successfully confirmed that RIS-KAE·0.4EtOH·2.6H₂O and RIS-KAE·MeOH are solvates. The dissolution rates of RIS from cocrystal solvates at pH 6.8 in 12 hours were 9.4-fold (RIS-KAE·0.4EtOH·2.6H₂O), 11.8-fold (RIS-KAE·MeOH) and 7.4-fold (RIS-KAE·EA·H₂O) lower than that of free RIS, showing significant sustained release behaviors. Furthermore, RIS-KAE·0.4EtOH·2.6H 2 O was prepared into microsuspensions (MSP), denoted as RIS-KAE-MSP, for I.M. injection. Pharmacokinetic (PK) results indicated that plasma RIS of RIS-KAE-MSP were still detectable by liquid chromatography-mass spectrometry (LC-MS) for as long as 45 days. In conclusion, cocrystallization with insoluble coformers is a promising strategy for long-term sustained release of RIS.
研究领域:
药剂学
·
药理学
·
晶体工程
·
药物递送
·
分析化学
✓ 已验证
产品关联
DOI
高影响因子
TALANTA
·
2024
·
IF 5.6
Hao Gu,Jiwen Li,Qiong Liang,Wei Xu
Modern solid phase microextraction (SPME) device linked with mass spectrometry (SPME-MS) has evolved from producing ion chronogram as flat noisy signal to as unimodal-like signal. We designed a SPME device, which is closer in morphology to LC column, linked it with a miniature mass spectrometer (SPME-Mini MS), and proposed a mathematical model that elution of compound from the SPME device is equivalent to overlay of elution of the compound from the infinite LC columns with the lengths between 0 and the length of the device and it can generate an ion chronogram as right-skew unimodal signal. Rhodamine B as analyte was used for experimental verification and its unimodal signal was used to fit the parameters of a computer simulation program based on the model. The experimental results and simulations empirically cross-confirmed that SPME-Mini MS can generate ion chronogram as clean right-skew unimodal signal. Furthermore, the SPME-Mini MS system was used for quantitative analysis of psychotropic drugs (i.e. risperidone and aripiprazole) in artificial urine. The results preliminarily demonstrated that the system can utilize area under unimodal signal for quantitative analysis and has potential to be applied for on-site, fast and accurate quantification of drugs and other compounds.
研究领域:
分析化学
·
质谱分析
·
药物分析
·
微萃取技术
✓ 已验证
产品关联
DOI
PubMed
高影响因子
ACS Omega
·
2024
·
IF 3.7
Liwen Wang,Ling Xin Yong,Say Chye Joachim Loo
This is the first study that explores blending polylactic acid (PLA) with various biomasses, including food wastes─brewer’s spent grain (BSG), spent coffee grounds (SCG), sesame cake (SC), and thermoplastic starch (TPS) biomass to create composite gastric floating drug delivery systems (GFDDS) through 3D printing. The aim is to investigate the influence of biomass percentage, biomass type, and printing parameters on their corresponding drug release profiles. 3D-printed (3DP) composite filaments were prepared by blending biomasses and PLA before in vitro drug release studies were performed using hydrophilic and hydrophobic model drugs, metoprolol tartrate (MT), and risperidone (RIS). The data revealed that release profiles were influenced by composite compositions and wall thicknesses of 3DP GFDDS capsules. Up to 15% of food waste could be blended with PLA for all food waste types tested. Delivery studies for PLA-food wastes found that MT was fully released by 4 h, exhibiting burst release profiles after a lag time of 0.5 to 1.5 h, and RIS could achieve a sustained release profile of approximately 48 h. PLA-TPS was utilized as a comparison and demonstrated variable release profiles ranging from 8 to 120 h, depending on the TPS content. The results demonstrated the potential for adjusting drug release profiles by incorporating affordable biomasses into GFDDS. This study presents a promising direction for creating delivery systems that are sustainable, customizable, and cost-effective, utilizing sustainable materials that can also be employed for agricultural, nutraceutical, personal care, and wastewater treatment applications.
研究领域:
材料科学
·
药剂学
·
可持续工程
·
生物医学工程
·
3D打印技术
✓ 已验证
DOI
高影响因子
危险品化学品经营许可证（带存储）