DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY
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2018
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IF 1.883
Yali Liu,Peng Li,Rong Qian,Tianyu Sun,Fangzhi Fang,Zonghua Wang,Xue Ke,Bohui Xu
The primary objective of this study was to mask bitter taste and decrease the disintegration time of carbinoxamine maleate (CAM) orally disintegrating tablets (ODTs). In order to screen the prescription of ODTs, a novel modified in vitro disintegration method (MIVDM) was developed to measure the in vitro disintegration time. In this method, different concentrations of ethanol served as disintegration medium in order to delay the in vitro water absorption and disintegration process of tablets. The MIVDM demonstrated good in vitro and in vivo correlation and proved more precise and discriminative than other reported methods. In this research, ion exchange resins (IERs) were used to mask bitter taste for improving mouthfeel. The drug-resin ratio and reaction temperature were investigated to obtain the optimum carbinoxamine resin complexes (CRCs). The characterization of CRCs revealed an amorphous state. ODTs were prepared by direct compression. Superdisintegrants and diluents of ODTs were screened first. Further optimization was carried out by using Box–Behnken design. The effect of (X1) mannitol/microcrystalline cellulose ratio, (X2) the amount of low-substituted hydroxypropylcellulose and (X3) the hardness was investigated for achieving the lowest (Y) in vitro disintegration time. Technological characterization, wetting time, water absorption ratio, and roughness degree were evaluated. The CRCs and ODTs proved successful taste-masking efficiency. The end product improved patients' compliance. The developed MIVDM was practical for commercial use.
研究领域:
药剂学
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药物递送系统
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制药技术
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产品关联
DOI
PubMed
高影响因子
INDUSTRIAL CROPS AND PRODUCTS
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2023
·
IF 5.9
Xiaowen Li,Dongdong Ye,Zhongrun Xiang,Huai Wang,Huiqing Wang,Yun Lu,Risheng Yao
Biocompatible cellulose has been used as a pharmaceutical excipient for several decades. However, there are still shortcomings, such as low drug loading, slow disintegration, and easy drug extraction. Herein, we describe a novel process for manufacturing cellulose nanomesh (CNM), a new structured nanocellulose with a high surface area of 98.37 m 2 g −1 and a high yield above 88%. This process combines mild acid vapor with a dilute enzymatic hydrolysis preparation method. The unique nanomesh structure clearly demonstrates benefits as superior drug carriers, including a high drug loading rate (>81.2%), miniaturizing volume, ultrafast disintegration time (<7 s), long-term sustained release (22 h), and also a strong drug-abuse deterrent effect. Our work suggests that the CNM produces great potential as a promising multi-functional drug carrier to realize tablet miniaturization, drug abuse-deterrent, and drug slow and controlled release.
研究领域:
制药工程
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材料科学
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生物医学工程
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产品关联
DOI
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
AAPS PHARMSCITECH
·
2022
·Vol. 23
·期 7
·1-12
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IF 4.026
Ye Qianyu,Ding Meilai,Zhang Ping,Wu Peng,Wang Yong,Selomulya Cordelia,Chen Xiao Dong
Compared to traditional drug release monitoring with manual sampling and testing procedures, low-field nuclear magnetic resonance (LF-NMR) imaging is a one-step, visual, non-destructive, and non-invasive measurement method. Here, we reported the application of LF-NMR to image the morphology, component, sub-diffusion, and spatial distribution of a solid oral formulation, Biyankang tablets, during dissolution in vitro . The drug ingredients with characteristic relaxation times were distinguished and localized based on the signal of standards, such as patchouli oil, Xanthium strumarium extract, and starch. The hydration, swelling, disintegration, and sub-diffusion of tablets in simulated gastric fluids (SGF) were visualized statically. All tablets showed similar expansion (37.4–42.0%) along the direction of thickness at 25 min and reached a full disintegration at 145 min, at pH 1.80–6.15, indicating pH-independent swelling and disintegration. Compared to that static immersion within 20 mL SGF, the tablet disintegration time was shortened by ~ 11% in 30 mL SGF. The application of shear reduced the time by ~ 28%, suggesting a major role of hydrodynamic condition in tablet dissolution. The ability to simultaneously visualize, distinguish, and localize drug ingredients using LF-NMR is expected to provide valuable information to develop drug release monitoring systems in vitro and potentially in vivo using small animal studies. Graphical abstract
研究领域:
药剂学
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药学
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生物物理学
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药物递送系统
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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
危险品化学品经营许可证（带存储）