INTERNATIONAL JOURNAL OF PHARMACEUTICS
·
2025
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IF 5.2
Peizhuo Han,Lei Wang,Huimin Li,Changlin Yao,Yaqian Qu,Xu Zhang,Hanlin Zhao,Yaqi Ren,Bozhang Li,Lufeng Xu,Weiguo Song,Xutang Tao
Molnupiravir (MPV) is an oral antiviral drug widely used for the treatment of coronavirus disease 2019 (COVID-19). However, the commercial form I of MPV has a poor tabletability, greatly restricting its manufacture. To solve this problem, a new cocrystal named MPV-caprolactam (CPL) was discovered by melt crystallization, and its crystal structure was successfully determined by single crystal X-ray diffraction. Meanwhile, the formation mechanism of the MPV-CPL cocrystal was studied via the formation enthalpies, and the negative formation enthalpy (−27.61 J/g at 25 ℃) is responsible for the crystallization of the MPV-CPL cocrystal. Finally, the powder tableting properties of the MPV-CPL cocrystal were investigated, and the MPV-CPL cocrystal has superior tabletability, achieving a tensile strength of 2.06 ± 0.09 MPa at 262.5 MPa compression pressure — a 1.93-fold increase over pure MPV. The MPV-CPL cocrystal also shows good compressibility, compactibility, and plasticity. This work establishes two key advances: (1) melt crystallization is a supplement to solution methods, and it can produce pharmaceutical cocrystals that tend to form solvates in solution, and (2) the improvement in tabletability of MPV-CPL cocrystal overcomes the main barrier in developing MPV tablets, which makes it a promising candidate for developing MPV tablets.
研究领域:
药学
·
材料科学
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DOI
PubMed
高影响因子
JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS
·
2013
·
IF 2.947
Baogang Xie,Aihong Liu,Xiuzhong Fang,Ying Chen,Haijun Zhong
Determination of alendronate is crucial to routine quality control of alendronate tablets. However, tedious sample treatment processes such as derivatization were generally required by chromatographic separation of alendronate as its high polarity and no chromophore in the molecular structure. Here, we describe the use of 1 H NMR for the quantification of alendronate sodium in tablets. Linearity, recovery, selectivity and sensitivity of the assay were validated to be satisfactory with quick sample preparation and acquisition. The contents of alendronate sodium in tablets from five manufacturers were determined, the results showed that all assayed tablets fell within the range of 90.0–110.0% of the label claim and the relative standard deviation was less than 6.0%. The method was also successfully employed for alendronate tablet dissolution assay in this study.
研究领域:
药学
·
分析化学
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DOI
高影响因子
Journal of Spectroscopy
·
2020
·Vol. 2020
·期 1
·1308385
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IF 1.243
Yanlei Kang,Yushan Zhou,Qiaoyu Wu,Ning Wang,Jianguang Zhou
The nondestructive and high sensitive analysis of a low content of an active pharmaceutical ingredient (API) was a difficult problem, especially in a complex system of pharmaceutical formulations. In this paper, a rapid and no sample preparation method was developed, which used a 1064 nm Raman spectrometer to detect entecavir monohydrate (ETV-H) in Baraclude tablets. Entecavir was a drug approved by FDA for the treatment of chronic hepatitis B and became the first choice in the market. The wavelength selection results displayed that the signal-to-background ratio of the Raman spectrum with 1064 nm excitation wavelength was 14 times that of the commonly used 785 nm wavelength. The partial least squares (PLS) method was used to calibrate concentration models containing 0.1% to 1.0% w/w% ETV-H in calibration set samples. Different preprocessing methods were used to eliminate the background interference and extract more spectral information. Calibration samples were used to choose the best performing model. Then, all the calibration samples combined with the best performing models’ parameters successfully predicted the content of ETV-H in Baraclude tablets. Combining baseline processing and standard normal variate (SNV) with PLS, the model showed a good result with an R 2 of 0.973, RMSEC of 0.05%, and RMSEP of 0.03% on the spectral region of 1350–1700 cm −1 . The limit of detection of this model was 0.17%. These results showed that 1064 nm Raman spectroscopy technology could be an alternative analytical procedure to quantify low-content API in intact tablets.
研究领域:
药物分析
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光谱学
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制药工程
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DOI
高影响因子
COLLOIDS AND SURFACES A-PHYSICOCHEMICAL AND ENGINEERING ASPECTS
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2024
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IF 4.9
Na Liu,Ahamd Ali,Wanhang Jiang,Sara Toukouki,Shun Yao
Due to convenient use, adjustable composition and easy preparation, sorbent tablets are considered to have obvious characteristics in the field of separation, especially for water environmental pollutants . In this study, the green, facile and catalyst-free way was employed to synthesize deep eutectic solvent and ionic liquid@porous organic frameworks (DES@POF and IL@POF), which showed specific surface area and stability; and their adsorption capacities were 187.74 (ciprofloxacin) and 111.28 mg/g (carmine), respectively. Then the two complexes were mixed with diluent and pressed to become monolayer and bilayer composite tablets; especially, the latter had two sides like a coin, which were based on DES@POF and IL@POF, respectively. During the following studies, the tablets exhibited satisfied continuous working ability and adsorption efficiency (99.57% as the highest) for the selected antibiotics and pigments. The key influential factors for their preparation and performance were investigated systematically, and separation mechanisms as well as selectivity were also discovered. The whole process was well fitted by the Langmuir isotherm model and quasi second-order kinetic model . Such a kind of sorbent tablets can be reused and renewed, which can provide useful reference on the development for new forms of separation mediums.
研究领域:
环境科学
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材料科学
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DOI
高影响因子
Journal of Cleaner Production
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2020
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IF 7.246
Chen Chen,Xueting Feng,Shun Yao
As the new kind of adsorbent, a 0.15 g ionic liquid-multi walled carbon nanotubes (IL-MWCNTs) composite tablet was prepared for the continuous adsorption of tetracyclines (TCs) and heavy metal ions from their aqueous solutions for the first time. Benzothiazole ionic liquid ( N -butyl benzothiazole hexafluoroborate, [C 4 Bth][PF 6 ]) was found selective for these objects, which was loaded into MWCNTs before tabletting under 5–20 MPa. Preparation operation was easy and the optional magnetic core (0.6 mm × 8 mm) could make it revolve in solution stably for accelerating mass transfer. Then the novel composite tablet was comprehensively characterized by scanning electron microscopy, thermogravimetry , Zeta potential and spectral analysis. Afterwards, the effects of main factors on adsorption results were investigated. Under unoptimized conditions, the adsorption efficiency of TCs, Cr 6+ and Cu 2+ could reach 99.76%, 94.10% and 84.60% by single tablet, respectively. It was also found that the adsorbed TCs could enhance the subsequent adsorption of copper ions . The experimental data fit well with pseudo-second-order model and Langmuir model (R 2 ≥ 0.99). By elution with 5 mol/L NaOH solution, the newly prepared composite tablet could be recycled and more than 90% adsorbate could be removed.
研究领域:
环境科学
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材料科学
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产品关联
DOI
高影响因子
FOOD CHEMISTRY
·
2017
·
IF 4.529
Fenglian Wang,Minyi Cao,Nani Wang,Nadeem Muhammad,Shuchao Wu,Yan Zhu
Folic acid plays a significant role during periods of rapid cells division and growth. Pregnant women require folic acid daily, either from dietary supplements or folic acid tablets in order to prevent fetal neural tube defects. In this work, a simple coupled ultrahigh performance liquid chromatography and ion chromatography technique was developed for simultaneous determination of folic acid and inorganic anions in folic acid tablets. A reversed-phase C18 column was used as the pretreatment column for on-line separating inorganic anions from organics. Inorganic anions were concentrated in the concentration column. Under the optimal chromatographic conditions, good sensitivity and linear calibration-curves (r ≥ 0.9992) were obtained. Low detection limits were obtained in the range of 0.0032–0.40 mg L −1 for all analytes. Repeatability results were satisfactory with relative standard deviations less than 1.50% (n = 5). The developed method was utilized to analyze spiked folic acid tablet samples with good measured recoveries (92.4–107.4%).
研究领域:
分析化学
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医学
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药学
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DOI
PubMed
高影响因子
AAPS PHARMSCITECH
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2017
·Vol. 18
·期 6
·2329-2335
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IF 2.451
Yin Lifang,Wang Yong,Wang Cuifeng,Feng Min
Most therapeutic proteins are classified as class III drugs according to the Biopharmaceutical Classification System means that the low permeability across the intestinal epithelium is the rate-limited step for their oral absorption. Cationic chitosan nanoparticles have been found to open the tight junctions between epithelial cells. On the other hand, bioadhesive delivery devices could prolong the gastrointestinal residence time . In the present study, we developed a novel nano-reservoir bioadhesive tablets that combining the advantages of cationic nanoparticles and bioadhesive delivery devices anticipated achieving effective transport of sufficient protein drugs across the intestinal epithelium. The nano-reservoir in bioadhesive tablets was composed of chitosan nanoparticles (CS-NPs) loading a model protein drug bovine serum albumin (BSA). The formula of bioadhesive tablets was optimized by using rotatable central composite design and response surface methodology. The nano-reservoir, BSA-loaded CS-NPs, had an average particle diameter of 312.5 ± 12.89 nm and zeta-potential value of 26.76 ± 3.56 mV. Carboxymethyl chitosan added to the formula significantly ameliorated the tight junction damage of the Caco-2 cell monolayer induced by CS-NPs, meanwhile maintained the high transport efficiency of BSA. Permeability study exhibited that these nano-reservoir bioadhesive tablets combining the advantages of cationic nanoparticles and bioadhesive tablets significantly enhanced BSA transport through rabbit small intestine in comparison with either conventional bioadhesive tablets or CS-NPs. Therefore, these nano-reservoir bioadhesive tablets provided a great potential dosage form design for the oral delivery of protein drugs.
研究领域:
药剂学
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生物医学工程
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DOI
PubMed
高影响因子
CARBOHYDRATE POLYMERS
·
2025
·
IF 12.5
Huibin Zhang,Yaqin Hou,Zebang Hu,Guowen Zhang,Shunjing Luo,Chengmei Liu,Zhongxia Li,Tingting Chen
Maintaining probiotic viability during storage and gastrointestinal transit is crucial for supplement efficacy. This study was to investigate the protective effects of modified arabinoxylan (AX) by feruloylation in tablets. AX was feruloylated with various ferulic acid (FA) contents (0–106 mg/g) into high (H-FAX), medium (M-FAX), and low (L-FAX) FA content matrices. Tube inversion test revealed that increased FA content reduced the critical concentration for gel formation, with H-FAX showing gelation at 25 % w/v compared to 35 % w/v for L-FAX. The FAX matrices demonstrated superior protection of probiotic during tablet compression compared to conventional excipients, maintaining viability above 7.95 × 10 9 CFU/tablet. Higher FA content improved mechanical properties resulted in better probiotic survival rates in simulated gastric (pH 2.0) and intestinal (pH 7.2) conditions. Storage at 4 °C maintained probiotic viability above 4.67 × 10 9 CFU/tablet for 12 months. The FAX matrix's protective barrier slowed probiotic release and shielded cells from harsh gastrointestinal conditions, while bound ferulic acid's antioxidant effects enhanced survival, ensuring effective colon delivery. These findings demonstrate that FAX matrices' potential in probiotic tablet formulations, with FA content being critical for optimizing protection. This work provides new insights for developing improved probiotic delivery tablets using naturally derived polymers.
研究领域:
食品科学
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生物工程
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药剂学
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DOI
PubMed
高影响因子
INTERNATIONAL JOURNAL OF PHARMACEUTICS
·
2021
·
IF 5.875
Yu Zheng,Feihuang Deng,Bo Wang,Yue Wu,Qing Luo,Xianghao Zuo,Xin Liu,Lihua Cao,Min Li,Haohui Lu,Senping Cheng,Xiaoling Li
Three-dimensional printing (3DP) technology offers unique advantages for pharmaceutical applications. However, most of current 3D printing methods and instrumentations are not specifically designed and developed for pharmaceutical applications. To meet the needs in pharmaceutical applications for precision, compatibility with a wide range of pharmaceutical excipients and drug materials without additional processing, high throughput and GMP compliance, an extrusion-based 3D printer based on Melt Extrusion Deposition (MED™) 3D printing technology was developed in this study. This technology can process powder pharmaceutical excipients and drugs directly without the need of preparing filament as required by FDM 3D printing. Six different tablet designs based on compartment models were used to demonstrate the precision and reproducibility of this technology. The designed tablets were fabricated using the GMP-compliant MED™ 3D printer and were evaluated in vitro for drug release and in vivo for selected designs using male beagle dogs. Tablet designs with one or more compartments showed versatile release characteristics in modulating the release onset time, release kinetics, duration of release and mode of release. Multiple drugs or formulations were fabricated into a single tablet to achieve independent release kinetics for each drug or to fine-tune the pharmacokinetic profile of a drug. Building upon the theoretical analysis of models, precision and reproducibility of MED™ 3D printing technology, a novel product development approach, 3D printing formulation by design (3DPFbD®) was developed to provide an efficient tool for fast and efficient pharmaceutical product development. The MED™ 3D printing represents a novel and promising technology platform encompassing design and development of modified drug release products and has potential to impact the drug delivery and pharmaceutical product development.
研究领域:
制药工程
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药物递送系统
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生物医学工程
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产品关联
DOI
PubMed
高影响因子
SPECTROCHIMICA ACTA PART A-MOLECULAR AND BIOMOLECULAR SPECTROSCOPY
·
2021
·
IF 4.098
Xueqing Guo,Yang Liu,Wenjuan Dong,Qin Hu,Yong Li,Shaomin Shuang,Chuan Dong,Lishuai Cai,Xiaojuan Gong
Azithromycin (AZM) 1 is one of the most widely used antibiotics. AZM abuse is easy to cause great harm to human body, so developing a rapid and sensitive method to detect AZM is of great importance. Herein, 3-aminothiophenol as only reaction precursor, nitrogen and sulfur co-doped carbon quantum dots (N,S-CQDs) 2 were fabricated by one-step hydrothermal carbonization method. All characteristics demonstrate that N,S-CQDs possess good water solubility, high fluorescence stability and low cytotoxicity. Without being disturbed by amino acids and drugs, the most interesting finding is that AZM can efficiently quench the fluorescence of N,S-CQDs by a synergistic effect of electrostatic interaction and static quenching. A fluorescent probe for the detection of AZM was constructed with high selectivity and good sensitivity, achieving two linear ranges of 2.5–32.3 μM and 37.2–110 μM and a limit of detection of 0.76 µM. The proposed fluorescent method was used for the detection of AZM in cells with fulfilling results. More importantly, the fluorescent probe was successfully used to the detection of AZM in tablets and human urine with recovery rate and relative standard deviations of 98.2–104.8% and 0.04–3.46%, respectively, which was confirmed by the standard method of HPLC-UV. This finding illustrates the usefulness and feasibility of N,S-CQDs as an effective fluorescent probe for the detection of AZM in tablets and human urine, which is helpful for supervising and guiding pharmacy.
研究领域:
药物分析
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荧光材料
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生物医学工程
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产品关联
DOI
PubMed
高影响因子
ANALYST
·
2019
·Vol. 144
·期 23
·6989-7000
·
IF 4.019
Alula Yohannes,Shun Yao
The application of ionic liquids (ILs) for the separation of bioactive compounds from various sample matrices is a burgeoning area. Here, a class of porous materials called metal–organic frameworks (MOFs) were combined with tropine-based ILs having structural similarity with natural tropane alkaloids for the quantitative analysis of Huashansheng tablets. Three MOFs (MIL-101, HKUST-1 and ZIF-8) were used to form the composite with the a tropine-based IL (N-propyl-substituted tropine hexafluorophosphate, [C3tr][PF6]), using the ship-in-a-bottle (SIB) synthesis approach. The performance of the hybrid IL/MOF composite (IL@MOF) was evaluated as a potential sorbent for application in the dispersive solid-phase-extraction-based enrichment of tropane alkaloids, followed by chromatographic analysis. It was found that [C3tr][PF6]@MIL-101 exhibited excellent adsorption capacity, and the extraction results showed satisfactory recoveries in the range of 91.5–104.7% (RSD < 5%). Further, the limit of detection went down to 10–20 μg L−1 with a linear range from 100–500 μg L−1, which proved that an adsorbent with the same nucleus as the target objects would be more suitable and efficient for their later extraction.
研究领域:
分析化学
·
药物分析
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产品关联
DOI
PubMed
高影响因子
JOURNAL OF RAMAN SPECTROSCOPY
·
2015
·Vol. 46
·期 7
·605-609
·
IF 2.671
Si-Yu Long,Zeng-Ping Chen,Yao Chen,Ru-Qin Yu
With p -thiocresol as internal standard, quantitative analysis of captopril, a synthetic angiotensin converting enzyme inhibitor, was achieved by the combination of the multiplicative effects model with surface-enhanced Raman spectroscopy (SERS). The multiplicative effects model was adopted to correct the detrimental effects caused by the heterogeneity in the physical properties of enhancing substrate (i.e. Ag nano-particles). Experimental results showed that the calibration model built on the SERS spectra of the calibration captopril samples prepared with ultrapure water could attain quite satisfactory concentration predictions for captopril in both real-world tablet samples and plasma samples. The recovery rates were in the range of 94.3% to 109.8%, which were in substantial agreement with the corresponding results of LC-MS/MS. The limit of detection and limit of quantification were estimated to be 0.149 and 0.451 μM, respectively. The proposed approach has advantages of relatively low cost, simplicity, high sensitivity and good accuracy and therefore can be further developed and extended to a routine method for the quantification of captopril in complex systems. Copyright © 2015 John Wiley & Sons, Ltd.
研究领域:
分析化学
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药物分析
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生物医学
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产品关联
DOI
高影响因子
危险品化学品经营许可证（带存储）