Asian Journal of Pharmaceutical Sciences
·
2017
·Vol. 12
·期 6
·580-585
·
IF 0
Shijie Wei,Jingbo Ren,Ning Li,Wuzhen Huo,Chongkai Gao
An LCC delivery system for Fenofibrate (Fen) was developed to improve its poorly oral bioavailability. Fen-LCC preparation methods were screened, and the prepared Fen-LCC was then characterized by a polarizing microscope and transmission electron microscopy (TEM). The spray drying technique was selected to dry and solidify particles into powder. The in vitro release of Fen-LCC was measured and in vivo pharmacokinetic experiments were carried out on rats after oral administration. Particles prepared through the high-temperature input method exhibited structural characteristics of LCC, and re-dissolved particles maintained the same features. The LCC delivery system can significantly improve in vitro release outcomes. After oral administration, AUCs of the suspension and LCC systems were measured at 131.6853 µg⋅h/ml and 1435.72893 µg⋅h/ml, respectively. The spray drying process presented here better maintains cubic structures, and the LCC system significantly improves bioavailability levels.
研究领域:
药剂学
·
药物递送系统
·
纳米医学
·
药代动力学
·
药物代谢
✓ 已验证
DOI
DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY
·
2019
·
IF 2.367
Jingwen Luo,Jiang Sun,Xiaoting Luo,Yinghui Wei,Hangsheng Zheng,Chaofeng Mu,Wenjie Yao
Objective: This article aims to design low molecular weight chitosan (LMWC)-based conjugates of Rhein (RH) by means of an amino acid linker (Alanine) for improved solubility and enhanced bioavailability.Significance: Rhein is a potential candidate for the therapy of kidney disease. However, the poor solubility, inadequate bioavailability, and lack of proper formulation restrict its clinical applicability. LMWC-drug conjugates offer the potential to improve the water-solubility of RH, increase its oral absorption, and thereby enhance its bioavailability.Methods: The conjugates were synthesized via a carbodiimide reaction and confirmed using UV-vis, FTIR, and 1H-NMR spectroscopy. The water-solubility and in vitro release properties were evaluated. Free RH and RH-LMWC conjugates were administered at an equivalent oral gavage dose of RH at 35 mg/kg for pharmacokinetic studies in Sprague Dawley rats.Results: The conjugates with RH content of 9.65% were successfully synthesized and featured a satisfactory water-solubility of 9.73 mg/mL, which exhibited a sustained release pattern over 72 h, and the enzymes present may promote the degradation of the conjugate to increase the release of Rhein. Oral administration of RH-LMWC conjugates to rats led to seven-folds and 3.1-folds increase in the T1/2 and AUC0–∞, respectively, as compared to RH suspension.Conclusion: The present work demonstrated that the RH-LMWC conjugates exhibited sustained release properties with outstanding oral bioavailability enhancements compared to administration of RH itself. Potentially, RH-LMWC conjugates may serve as a promising lead for developing a new platform for RH oral delivery.
研究领域:
药剂学
·
药物化学
·
生物医学工程
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Asian Journal of Pharmaceutical Sciences
·
2016
·Vol. 12
·期 2
·202-208
·
IF 0
Huiyan Shi,Chenzhi Hou,Liqiang Gu,Zhe Wei,Hang Xing,Meiyu Zhang,Shixiao Wang,Longshan Zhao,Kaishun Bi,Xiaohui Chen
The present study was designed to investigate the influence of the pretreatment of piperazine ferulate on pharmacokinetic parameters of methotrexate in methotrexate-induced renal injury rats. A simple and efficient high performance liquid chromatography coupled with mass spectrometry (HPLC-MS) method was developed to determine methotrexate in rat plasma. Methotrexate and syringic acid (internal standard) were extracted from rat plasma samples by protein precipitation with acetonitrile. The analysis was performed on a CAPCELL PAK C 18 column (150 mm × 4.6 mm, 5 µm) with acetonitrile and 5 mmol/l ammonium acetate aqueous (10:90, v/v ). The linear range was 5.0 × 10 −2 to 100.0 µg/ml for methotrexate. Other parameters were all within the acceptance criteria. The validated method was successfully applied the pharmacokinetic study of methotrexate between two methotrexate treated groups (with and without the pretreatment of piperazine ferulate). Compared with the methotrexate treated alone group, the pharmacokinetic parameters in the methotrexate with the pretreatment of piperazine ferulate group showed significantly lower MRT (0-t) , MRT (0-∞) and T 1/2 . Results suggested that methotrexate can be rapidly eliminated, cleared or metabolized in rat blood, which might be related to the pretreatment of piperazine ferulate. The method provided deeper insights into rational clinical use of methotrexate with the pretreatment of piperazine ferulate on cancer patients with renal dysfunction.
研究领域:
药理学
·
药物代谢
·
肾脏病学
·
肿瘤学
·
临床药学
·
分析化学
✓ 已验证
DOI
DRUG DELIVERY
·
2019
·
IF 3.829
Yanfei Tao,Fei Yang,Kuiyu Meng,Dongmei Chen,Yujuan Yang,Kaixiang Zhou,Wanhe Luo,Wei Qu,Yuanhu Pan,Zonghui Yuan,Shuyu Xie
In our previous study, enrofloxacin-loaded docosanoic acid solid lipid nanoparticles (SLNs) could be effectively delivered to cells in vitro. In this study, its properties and exploitation as possible oral and intramuscular sustained release formulations for pigs were studied after being made into suspension. The re-dispersed time and sedimentation rate of the nanosuspension were 55 s and 1, respectively. It showed good stability when stored away from light and sustained release in pH = 7.4 PBS buffer. The suspension exhibited no irritation at the injection site and good palatability. Compared with commercial injection and soluble powder, the nanosuspension increased the bioavailability of enrofloxacin by 1.63 and 2.38 folds, and extended the mean residence time (MRT) of the drug from 11.27 and 12.33 to 37.76 and 35.15 h after intragastric and intramuscular administration, respectively. These results suggest that docosanoic acid SLN suspension (DAS) might be a promising oral and intramuscular sustained release formulation to enhance the pharmacological activity of enrofloxacin.
研究领域:
兽医学
·
药物递送系统
·
药剂学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
JOURNAL OF FOOD BIOCHEMISTRY
·
2021
·Vol. 46
·期 1
·e14007
·
IF 2.72
Jing Liu,Zhongan Zhu,Yuhang Yang,Michael Adu-Frimpong,Lin Chen,Hao Ji,Elmurat Toreniyazov,Qilong Wang,Jiangnan Yu,Ximing Xu
A liposome of Licochalcone A (LCA-Liposomes) was purposively prepared to ameliorate the low in vivo availability and efficacy of LCA. Physical characterization of LCA-Liposomes was carried out mainly by determining particle size, morphology, zeta potential (Z-potential), and efficiency of LCA encapsulation (EE) via appropriate techniques. Also, the rate of LCA release in vitro and distribution in vivo (plasma and tissues) was evaluated. Evaluation of the antirenal activity of LCA-liposomes was carried out by establishing chronic renal failure (CRF) model in mice through intragastric administration of adenine (200 mg/kg) and subsequent determination of biochemical parameters and examination of tissue sections. Respectively, the mean size of liposomal particles, Z-potential and EE of LCA-Liposomes were 71.78 ± 0.99 nm, −38.49 ± 0.06 mV, and 97.67 ± 1.72%. Pharmacokinetic and tissue distribution studies showed that LCA-Liposomes could improve the availability of LCA in the blood and tissues, whereas during pharmacodynamics studies, the liposome effectively improved the therapeutic effect of LCA on CRF mice by potentially protecting the renal tissues while exhibiting antioxidant activity. In conclusion, LCA-Liposomes could effectively improve the bioavailability of LCA and provide platform for the development of LCA-related functional products. Practical applications As a traditional Chinese medicine, licorice is widely used in food and pharmaceutical industries. LCA is a small molecule flavonoid extracted from the root of licorice. In this study, LCA was loaded on liposome carriers, which significantly improved the water solubility and oral bioavailability, and proved that LCA-Liposomes have certain therapeutic effects on chronic renal failure, thereby providing a basis for the development of LCA into drugs or functional food in the future.
研究领域:
药剂学
·
药理学
·
分子药理学
·
药物代谢
·
纳米医学
·
中药药理学
✓ 已验证
DOI
高影响因子
Journal of Analytical Methods in Chemistry
·
2022
·Vol. 2022
·期 1
·2565494
·
IF 2.594
Qiulong Zhao,Chunxue Wang,Jiaxin Cheng,Hui Yan,Ling Wang,Dawei Qian,Jinao Duan
According to the sixth edition of China’s “New Coronavirus Diagnosis and Treatment Plan (NCDTP),” ReDuNing injection (RDN) was firstly introduced to treat severe and critical COVID-19, whereas its combination with broad-spectrum antibiotics was suggested to take with extreme caution and full reasons. Therefore, we aim to describe the pharmacokinetics of seven active phytochemicals and semiquantification of nine relevant metabolites in ReDuNing injection (RDN) after combining with cefuroxime sodium (CNa) for injection in rat plasma. Male Sprague–Dawley rats were randomly assigned to six groups, and they were intravenously administered, respectively, with different prescriptions of RDN (2 mL/kg) and CNa (225 mg/kg). At different time points (0.03, 0.08, 0.17, 0.24, 0.33, 0.50, 0.67, 1, and 6 h) after administration, the drug concentrations of iridoids glycosides, organic acids, and metabolites in rat plasma were determined using ultrahigh-pressure liquid chromatography coupled with linear ion rap-orbitrap tandem mass spectrometry (UHPLC–LTQ–Orbitrap–MS), and main pharmacokinetic parameters were estimated by noncompartment model. The results showed that there were differences in pharmacokinetic parameters, AUC (0-t) , T 1/2 , C max , CL of iridoids glycosides, and organic acids, after the intravenous administration of the different combinations of RDN and CNa. Moreover, different combinations of the injections also resulted in different curves of relative changes of each metabolite. The obtained results suggested that RDN and CNa existed pharmacokinetic drug–herb interactions in rats. The findings not only lay the foundation for evaluating the safety of RDN injection combined with CNa but also make contributions to clinically applying RDN injection combined with CNa, which works potentially against severe forms of COVID-19.
研究领域:
药理学
·
药物代谢
·
中药学
·
临床药学
·
分析化学
·
病毒学
·
转化医学
✓ 已验证
DOI
高影响因子
SPECTROCHIMICA ACTA PART A-MOLECULAR AND BIOMOLECULAR SPECTROSCOPY
·
2016
·
IF 2.653
Xue-Dong Xiao,Lin Shi,Li-Hui Guo,Jun-Wen Wang,Xiang Zhang
The supramolecular interaction between the water-soluble pillar[5]arene (WP[5]) as host and dopamine hydrochloride (DH) as guest was studied by spectrofluorometry . The fluorescence intensity of DH gradually decreased with increasing WP[5] concentration, and the possible interaction mechanism between WP[5] and DH was confirmed by 1 H NMR, 2D NOESY , and molecular modelling. Based on significant DH fluorescence, a highly sensitive and selective method for DH determination was developed for the first time. The fluorescence intensity was measured at 312 nm, with excitation at 285 nm. The effects of pH, temperature, and reaction time on the fluorescence spectra of the WP[5]-DH complex were investigated. A linear relationship between fluorescence intensity and DH concentration in the range of 0.07–6.2 μg mL − 1 was obtained. The corresponding linear regression equation is Δ F = 25.76 C + 13.56 (where C denotes the concentration in μg mL − 1 ), with the limit of detection equal to 0.03 μg mL − 1 and the correlation coefficient equal to 0.9996. This method can be used for the determination of dopamine in injection and urine samples. In addition, the WP[5]-DH complex has potential applications in fluorescent sensing and pharmacokinetics studies of DH.
研究领域:
分析化学
·
超分子化学
·
药物代谢
·
生物分析
·
药代动力学
✓ 已验证
DOI
高影响因子
INTERNATIONAL JOURNAL OF PHARMACEUTICS
·
2019
·
IF 4.213
Qian Du,Jianqiu Chen,Guojun Yan,Fannan Lyu,Jie Huang,Jin Ren,Liuqing Di
This study compared the in vitro and in vivo effects of different aliphatic acid grafted N -trimethyl chitosan (TMC) surface-modified nanostructured lipid carriers (NLC) by oral delivery. Medium-chain fatty acids, decylic acids (DA), and long-chain fatty acids, palmitic acids (PA) were selected as contrasting objects. TMC, DA grafted TMC (DA-TMC), and PA grafted TMC (PA-TMC) were successively synthesized. Kaempferol loaded NLC (KNLC), KNLC coated with DA-TMC (DA-TMC-KNLC) and PA-TMC (PA-TMC-KNLC) were fabricated, respectively. KNLC were subspherical in shape at nano-size limits. The particle size increased from 93.6 to 125.5 nm and the zeta potential changed from negative to positive due to surface-modification. The KNLC surface-modified with different aliphatic acid grafted TMC displayed a diverse release profiles at the simulative physiological environment, which contrasted that of KNLC. Pharmacokinetic studies demonstrated that the nanoparticles all could improve the AUC values and prolong blood retention times compared to that of kaempferol suspensions. Cell uptake and in situ intestinal perfusion experiments revealed that DA-TMC-KNLC and PA-TMC-KNLC could remarkably enhance cellular uptake of kaempferol into Caco-2 cells and drug absorption in each intestinal segment in comparison with KNLC, repectively. Wherein, DA-TMC-KNLC exhibits the greatest uptake and absorption efficiency as compared to kaempferol suspensions, KNLC and PA-TMC-KNLC. Collectively, DA-TMC surface-modified NLC might serve as a potential drug carrier for oral delivery of water-insoluble flavonoid ingredients.
研究领域:
药剂学
·
药物递送
·
纳米技术
·
药代动力学
·
胶体与界面科学
✓ 已验证
DOI
高影响因子
BULLETIN OF THE KOREAN CHEMICAL SOCIETY
·
2018
·Vol. 39
·期 5
·657-664
·
IF 0.522
Nai-Di Tan,Jian-Hang Yin,Yaqing Yuan,Lei Meng,Na Xu
Herein, a novel bright-green and highly fluorescent polyethyleneimine capped copper nanoclusters (CuNCs@PEI) has been hydrothermally synthesized, which is employed as a fluorescence probe to determine rifampicin. Under optimum synthetic conditions, the morphology, surface chemistry and optical features of resulting CuNCs@PEI are well characterized by transmission electron microscopy, Fourier transform infrared spectroscopy, UV–Vis absorption spectra, transient and steady-state fluorescence. In comparison to previous reports, the new species with a larger diameter of approximately 3 nm exhibit higher fluorescence quantum yield (QY) up to nearly 10.7%, and demonstrate tolerability to extreme pH, high ionic strengths as well as long-term UV irradiation. These excellent optical properties ascribe to unique grain size and surface chemical features of products, which are further discussed in this work. In addition, we employed as-prepared CuNCs@PEI to detect rifampicin based on fluorescence quenching phenomenon. The fluorescence intensity of probe is linearly proportional to rifampicin over the concentration rage from 0 to 20 μM, where the limit of detection (LOD) is 50 nM. Besides, this probe can be also used to assay rifampicin in serum samples with satisfactory recoveries.
研究领域:
分析化学
·
纳米生物技术
·
药物分析
·
分子诊断
·
转化医学
·
药代动力学
✓ 已验证
DOI
高影响因子
JOURNAL OF MATERIALS SCIENCE-MATERIALS IN MEDICINE
·
2017
·Vol. 28
·期 5
·67
·
IF 2.325
Li Wenyan,Huo Mengmeng,Sen Chaudhuri Arka,Yang Chen,Cao Dazhong,Wu Zhenghong,Qi Xiaole
Currently, polysaccharide-based hydrogels are widely studied macromolecular networks to modify drug dissolution from controlled-releasing matrix tablets. Among them, polyelectrolyte complexes (PEC) films consisted of chitosan (CS) and sodium alginate (SA) could be obtained via spontaneously assembling under physiological gastrointestinal environment. Here, we utilized these self-assembled PEC films as an efficient coating materials to develop controlled-released matrix tablets through compression coating process, with paracetamol (APAP) as model drug. The constitutive and morphology characteristic studies on these PEC films illustrated that the mixture of CS and SA with the weight ratio of 1:1 would be an promising outer layer for compression-coating tablets. In addition, the in vitro drug releasing behavior experiments demonstrated that the optimized compression coating tablets displayed satisfied zero-order drug releasing profits. Furthermore, the in vivo pharmacokinetic studies of these APAP loaded compression-coated tablets in New Zealand rabbits gave that the T max (12.32 ± 1.05 h) was significantly prolonged ( p < 0.01), compared to that (0.89 ± 0.26 h) of common APAP tablets (Jinfuning ® ) after oral administration. These studies suggest that the compression-coated tablets with self-assembled PEC film as coating outer layer may be a promising strategy for peroral controlled release delivery system of water soluble drugs. Graphical
研究领域:
药剂学
·
生物材料
·
药物递送系统
·
药代动力学
·
胃肠药理学
✓ 已验证
DOI
高影响因子
危险品化学品经营许可证（带存储）