INTERNATIONAL JOURNAL OF PHARMACEUTICS
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2024
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IF 5.3
Yuqi Li,Jifeng Shi,Xinyu Zhang,Meng Ji,Yifei Ni,Ruiying Han,Zixuan Li,Yerong Xiong,Jiasheng Tu,Dongsheng He,Chunmeng Sun
Surface tension is a crucial functional indicator for various classes of pharmaceutical excipients, as highlighted in both the Pharmacopoeia of the People’s Republic of China (ChP) <9601 Guidelines for Functional Indicators of Pharmaceutical Excipients> and the United States Pharmacopoeia (USP) <1059 Excipient Performance>. However, there are few systematic studies on surface tension measurement of pharmaceutical excipients, resulting in a lack of stable parameter support in practical applications. In this study, we aim to fill this gap by exploring three different methods for measuring surface tension. These methods were carefully developed taking into account the actual measurement process and statistical theory, thus ensuring their applicability and reliability. Through comparative analyses, we have identified the most suitable measurement methods for different classes of pharmaceutical excipients. In addition, this paper describes the surface adsorption behavior of various excipients. Therefore, this study provides valuable guidance for the determination of surface tension and the study of surface adsorption behavior, which lays the foundation for further comprehensive research in the field of surface tension of pharmaceutical excipients and the improvement of general pharmacopoeia specification.
研究领域:
药学
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分析化学
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产品关联
DOI
PubMed
高影响因子
Annales Pharmaceutiques Francaises
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2020
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IF 0
Z. Osman,Y. Farah,H. Ali Hassan,S. Elsayed
Summary Objectives The aim of the current study was to compare the physicochemical and disintegrant properties of pearl millet starch with other starches using paracetamol as model drug. Methodology Determination of percentage yield, Physicochemical, micrometrics characteristics of starch/granules, drug excipients compatibility studies and evaluation of prepared paracetamol tablets were measured using official techniques. Results The yield of the millet starch ranged from 30 to 40%. Moisture content 8.77%, pH 5.7, Swelling capacity 1.2, Hydration capacity 1.748, Moisture uptake 11.8%, Amylose 24.6%, with poor flowability and compressibility. No significant difference in hardness, friability% & disintegration times for formulations containing millet starch to that containing potato and maize starch ( P > 0.05). Conclusion From the study, Millet seeds locally cultivated in Sudan gave a high yield of starch, has same physicochemical properties as maize and potato starch so can be used as an alternative to those starches.
研究领域:
药学
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材料科学
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DOI
XENOBIOTICA
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2020
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IF 1.902
Ruicong Ma,Gentao Li,Xue Wang,Yajuan Bi,Youcai Zhang
To date, relatively little is known about the interactions of pharmaceutical excipients with hepatic and renal drug uptake transporters. The present study was designed to systematically evaluate the effects of 16 commonly consumed excipients on human organic cation transporter 1 and 2 (hOCT1 and hOCT2), human organic anion transporter 1 and 3 (hOAT1 and hOAT3) and human organic anion transporting polypeptide 1B1 and 1B3 (hOATP1B1 and hOATP1B3).The inhibitory effects and mechanisms of excipients on transporters were investigated using in vitro uptake studies, cell viability assays, concentration-dependent studies, and the Lineweaver–Burk plot method.Triton X-100 is a non-competitive inhibitor for all six transporters. Tween 20 inhibits hOCT2, hOAT1, hOAT3, and hOATP1B3 in a mixed way, whereas it competitively inhibits hOATP1B1. The inhibition of Tween 80 is competitive for hOCT2, non-competitive for hOATP1B1 and hOATP1B3, and mixed for hOAT1 and hOAT3. Concentration-dependent studies identify Triton X-100 as a strong inhibitor of hOCT1 and hOCT2 with IC50 values of 20.1 and 4.54 μg/mL, respectively. Additionally, Triton X-100, Tween 20, and Tween 80 strongly inhibit hOAT3 with IC50 values ≤31.0 μg/mL.The present study is significant in understanding the excipient–drug interactions and provides valuable information for excipient selection in drug development.
研究领域:
药理学
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药物开发
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制药学
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产品关联
DOI
PubMed
高影响因子
FERROELECTRICS
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2024
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IF 0.6
Chenghong Huang,Xiaorong Huang,Qi Yin,Xuehan Hu,Ying Fang,Hongjie Chen,Lin Zhang,Kang Yang,Hao Li,Fang Yang,Xiaoling Lu,Zeng Yang
Chitosan (CS) is lack of applications in pharmaceutical industry due to its lower compression density and instability during tablet process. This study mainly focus on the synthesis of ethyl vanillin incorporated CS(EV/CS) via Schiff base reaction and the evaluation of application as pharmaceutic excipient. Results of FT-IR showed that there is a typical amide peak in EV/CS that the 1640 cm−1 can be attributed to –C = N– bond and 1518 cm−1 can be attributed to backbone of benzene but not in CS raw material. Compared with the control, XRD of EV/CS have additional 2θ angle of 44°, 64° and 77° diffraction peaks except that the 2θ = 20° of EV is still existed. More slower weight loss of EV/CS than that of CS in the range of 248–760 °C is also demonstrated by TGA analysis. 1H NMR indicated there are intrinsic 7.5 and 7.1 ppm as well as emerging 4.2 ppm of chemical shift in EV/CS. The physical finger spectra from twelve indexes of EV/CS powder denotes quite differences in compressibility, fluidity and stability with that of CS. 5% content EV/CS of designed formulation can at most decrease the friability and disintegration time of the compressed tablet. In conclusion, the developed EV/CS is inclined to suitable for tablet as an excipient.
研究领域:
药学
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材料科学
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化学
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产品关联
DOI
高影响因子
MOLECULAR PHARMACEUTICS
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2021
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IF 4.939
Yiling Ruan,Xinran Li,Linjun You,Jungen Chen,Yueyue Shen,Junying Zhang,Yaozuo Yuan,Lifeng Kang,Chao Qin,Chunyong Wu
Growing evidence has shown that some pharmaceutical excipients can act on drug transporters. The present study was aimed at investigating the effects of 13 commonly used excipients on the intestinal absorption of metformin (MTF) and the underlying mechanisms using Caco-2 cells and an ex vivo mouse non-everted gut sac model. First, the uptake of MTF in Caco-2 cells was markedly inhibited by nonionic excipients including Solutol HS 15, polysorbate 20, polysorbate 40, polysorbate 60, polysorbate 80, and crospovidone. Second, transport profile studies showed that MTF was taken up via multiple cation-selective transporters, among which a novel pyrilamine-sensitive proton-coupled organic cation (H+/OC+) antiporter played a key role. Third, Solutol HS 15, polysorbate 40, and polysorbate 60 showed cis-inhibitory effects on the uptake of either pyrilamine (prototypical substrate of the pyrilamine-sensitive H+/OC+ antiporter) or 1-methyl-4-phenylpyridinium (substrate of traditional cation-selective transporters including OCTs, MATEs, PMAT, SERT, and THTR-2), indicating that their suppression on MTF uptake is due to the synergistic inhibition toward multiple influx transporters. Finally, the pH-dependent mouse intestinal absorption of MTF was significantly decreased by Solutol HS 15, polysorbate 20, polysorbate 40, polysorbate 60, polysorbate 80, and pyrilamine. In conclusion, this study revealed that a novel transport process mediated by the pyrilamine-sensitive H+/OC+ antiporter contributes to the intestinal absorption of MTF in conjunction with the traditional cation-selective transporters. Mechanistic understanding of the interaction of excipients with cation-selective transporters can improve the formulation design and clinical application of cationic drugs.
研究领域:
药理学
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药物递送
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药剂学
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细胞生物学
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药学
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产品关联
DOI
PubMed
高影响因子
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
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2024
·Vol. 26
·期 1
·72
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IF 4.9
Chaoji Li,Min Zhang,Yanni Zhao,Dan Yang,Mei Zhao,Leyuan Shang,Xiaodong Sun,Shuo Zhang,Pengjiao Wang,Xiuli Gao
Mycophenolic acid (MPA) is a commonly used immunosuppressant. In the human body, MPA is metabolized into mycophenolic acid 7-O-glucuronide (MPAG) and mycophenolic acid acyl-glucuronide (AcMPAG) mainly through liver glucuronidation, which involves UDP-glucuronosyltransferase (UGTs) and transfer proteins. Research has indicated that the pharmaceutical excipient PEG400 can impact drug processes in the body, potentially affecting the pharmacokinetics of MPA. Due to the narrow therapeutic window of MPA, combination therapy is often used, and PEG400 is widely used in pharmaceutical preparations. Therefore, investigating the pharmacokinetic influence of PEG400 on MPA could offer valuable insights for optimizing MPA’s clinical use. In this study, we examined the impact of a single oral dose of PEG400 on the blood levels of MPA in rats through pharmacokinetic analysis. We also investigated the distribution of MPA in various tissues using mass spectrometry imaging. We explored the potential mechanism by which PEG400 affects the metabolism of MPA using hepatic and intestinal microsomes and the Caco-2 cellular transporter model. Our findings reveal that the overall plasma concentrations of MPA were elevated in rats following the co-administration of PEG400, with the AUC0-tof MPA and its metabolite MPAG increasing by 45.53% and 29.44%, respectively. Mass spectrometry imaging showed increased MPA content in tissues after PEG400 administration, with significant differences in the metabolites observed across different tissues. Microsomal and transport experiments showed that PEG400 accelerated the metabolism of MPA, promoted the uptake of MPA, and inhibited efflux. In conclusion, PEG400 alters the in vivo metabolism of MPA, potentially through the modulation of metabolic enzymes and transport.
研究领域:
药理学
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免疫抑制剂
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药物代谢
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药用辅料
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体内和体外研究
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产品关联
DOI
PubMed
高影响因子
AAPS PHARMSCITECH
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2025
·Vol. 26
·期 7
·1-17
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IF 4
Tan Lihua,Jing Zhongli,Li Na,Yu Xuan,Liu Yi,Wang Meng,Ren Xiaoliang
This study introduced a novel vectorized Biopharmaceutics Classification System (BCS) model designed to evaluate the biopharmaceutical properties of active pharmaceutical ingredients (APIs) and their variations under different influencing factors. The model was validated using water-soluble supramolecular p -Sulfonatocalix[n]arenes (SCnA, n = 6, 8), promising pharmaceutical adjuvants, to enhance the solubility and bioavailability of a series of APIs in vitro . The binding interactions of SCnA with 22 alkaloids were assessed for their impact on solubility and permeability using the classical shake-flask method and the parallel artificial membrane permeability assay (PAMPA). To quantify the effects, the change in directional cosine (θ) for each API was calculated by measuring the ratio of the differences in x- and y-coordinates before and after binding. The linear distance and modulus length (r) changes for each API were determined using the Pythagorean theorem, enabling a quantitative assessment of the modifications in solubility and permeability. The potential changes in oral bioavailability pre- and post-binding were visualized using heat maps based on θ and r, highlighting significant improvements in the solubility of compounds such as allicin, tetrandrine, lycorisine, and others. These changes corresponded with shifts in BCS classification, indicating a positive relationship between SCnA concentration, cavity size, and enhanced solubility. The study also evaluated the influence of pH, and concentrations of host and guest, to assess the tolerance of SCnA for further pharmaceutical applications. Based on prior safety assessments, SCnA ( n = 6, 8) demonstrated significant potential as solubilizing excipients. The vectorized BCS model enabled precise, quantitative analysis of biopharmaceutical property variations without added experimental complexity, offering a tool for high-throughput screening of excipients in pharmaceutical formulation and processing. Graphical
研究领域:
药剂学
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药物递送
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生物药剂学
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超分子化学
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药用辅料
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体外研究
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产品关联
DOI
PubMed
高影响因子
危险品化学品经营许可证（带存储）