EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES
·
2021
·
IF 4.384
Jiawei Han,Luyuan Li,Zunting Pang,Meiling Su,Xiaoshuang He,Shuai Qian,Jianjun Zhang,Yuan Gao,Yuanfeng Wei
Amorphous curcumin (CUR) exhibited a decreased dissolution rate in comparison with the crystalline counterpart due to its gel formation during dissolution. The main purpose of the present study is to explore the mechanism of such gelation phenomenon. It was found that the dissolution of amorphous CUR and gel properties were influenced by the temperature and pH of the media. The formed gels were characterized by TPA, SEM, DSC, XRPD, FTIR and PLM. The results indicated that the gelation process led to the formation of a porous structure in which water molecules infiltrate, and entered into its supercooled liquid state with high viscosity when contacting aqueous media, accompanied by decreased T g and crystalline transformation. In addition, mixing with hydrophilic excipients (such as hydrophilic silica) accelerated the gel formation of amorphous CUR, while the addition of hydrophobic excipients (such as hydrophobic silica and magnesium stearate) could effectively weaken and even eliminate the gelation, hence significantly improving its dissolution. Furthermore, according to contact angle measurement and fluorescence microscope observation, hydrophilic excipients were found to be able to accelerate water entering into the interior of amorphous CUR, hence facilitating the gelation, while hydrophobic excipients would hinder water infiltration into the powder and thus achieve degelation. In conclusion, it is important to recognize that the gelation potential of some amorphous materials should be considered in developing robust amorphous drug product of high quality and performance.
研究领域:
药剂学
·
材料科学
✓ 已验证
DOI
PubMed
高影响因子
CHEMICAL ENGINEERING SCIENCE
·
2024
·
IF 4.1
Haifeng Lu,Liang Zhang,Hui Du,Xiaolei Guo,Haifeng Liu
Continuous manufacturing has intrigued many researchers in the pharmaceutical industry in the post-COVID-19 world. We experimentally studied the discharge characteristics of pharmaceutical excipients under vibrational excitation. The successful accurate dosing and filling of powders at fill rates of 0.6–15 mg/s was developed. A simple particle model includes fluid-grain coupling which is relevant to Faraday tilting resulting from gas trapped in the powder bed accurately predicts the discharge rate. A novel continuous micro mixing system was designed based on the discharge model. Any specified proportions can be realized by setting appropriate vibration parameters. The low variability (<2.5 %) in the content of components has verified the reliability of the mixing system. The continuous mixing performance was determined by the discharge characteristics. Yet the particle size distribution and cohesion lead to different mixing performances when the stability of micro feeding is satisfied. Reasonable process parameters for continuous mixing are determined and optimized.
研究领域:
制药工程
·
粉末力学
·
连续制造
✓ 已验证
DOI
高影响因子
Biomaterials Science
·
2021
·Vol. 9
·期 12
·4308-4316
·
IF 6.843
Jie Zhang,Zhengyu Liu,Haomin Wu,Ting Cai
Amorphous solids have been widely used to improve the solubility and oral bioavailability of poorly water-soluble drugs. Biocompatible polymeric materials are usually incorporated into formulations to inhibit the crystallization of high-energy amorphous drugs. Crystallization typically consists of two steps, nucleation and crystal growth. The impacts of polymeric excipients on the crystal growth of amorphous drugs have been intensively studied. However, the nucleation behaviors of amorphous drugs in the presence of polymers remain largely unexplored. Herein, we report that three chemically distinct polymers show significantly different effects on nucleation kinetics of amorphous fluconazole (FCZ), a classical antifungal drug. The addition of 10% w/w HPMCAS shows the largest inhibitory effect on the nucleation rates of FCZ, while the same amount of PVP has only a minor effect. Conversely, the nucleation rates for both polymorphs of FCZ are significantly increased in the presence of PEO. In addition, the polymeric additives are found to influence the kinetics of nucleation and crystal growth to a similar extent, suggesting that the two processes may share a similar kinetic barrier. The present study is helpful in the optimization of formulations of amorphous solid dispersions and understanding the nucleation behavior of polymorphic drugs.
研究领域:
药剂学
·
材料科学
✓ 已验证
DOI
PubMed
高影响因子
JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS
·
2024
·
IF 3.1
Min Zhou,Wei Wu,Hong Pu,Feng Chen,Chaofan Yi,Yuande Long
A long-term stability study using high performance liquid chromatography (HPLC) revealed an unidentified impurity in the bromhexine hydrochloride injection, which was employed as a mucolytic agent . Investigations into stress degradation and elemental impurities revealed one of the elemental impurities Fe 3+ in this injection as the primary generator of these impurities. This impurity, named N-carboxymethyl bromhexine, was a product formed during drug–excipient interaction between bromhexine and tartaric acid with Fe 3+ . The structure of the impurity was identified through ultra-high-performance liquid chromatography with diode array detector (UHPLC-DAD), liquid chromatograph mass spectrometer (LC-MS). Further, the formation mechanism of the impurity was discussed. Overall, this study elucidates the cause, origin, and mechanism of an unknown impurity in bromhexine hydrochloride injection, providing a basis for quality control for bromhexine hydrochloride injections and drug products containing both amine and tartaric acid.
研究领域:
药学
·
药物分析
·
药物化学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Acta Biomaterialia
·
2025
·
IF 9.6
YiQing Shen,Xin Tan,Lin Zhou,ZiHan Sun,Min Han,Min liang,DongHang Xu
Although local anesthetics (LA) are non-addictive and effective in managing postoperative pain, their short-term effects limit their clinical utility. In this study, we constructed an in situ gel injection formulation with stearic acid-ropivacaine hydrophobic ion-pair (HIP) and glycerol monoglyceride (SA-ROP-GMS) for multiday postoperative pain management. As an in situ gel, SA-ROP-GMS avoids the burst release effect common to water-soluble small molecule drugs in liposomes and hydrogels. Meanwhile, the hydrophobic ion-pair formed by ropivacaine and stearic acid contributes to the gel's stabilization and slow-release properties. In vivo evaluation of mouse models of pain demonstrated that the formulation provided multiday analgesia. And the absence of systemic toxicity of SA-ROP-GMS was verified by histological and blood biochemical studies. This study demonstrated the safety and efficacy of an injectable ropivacaine formulation based on in situ gel. The materials used in SA-ROP-GMS are safe and easy to obtain, and the preparation process is simple and fast, providing a convenient and effective strategy for the development of single-dose long-acting local anesthetic products, which is of great significance for postoperative pain management. Statement of Significance More than 80% of patients experience severe postoperative pain, and poor pain control reduces recovery satisfaction while increasing the risk of chronic pain. In this study, we constructed an injectable in situ gel using all-small-molecule excipients for slow-release drug delivery for the first time. We designed a method to form a lipid drug coupling between ropivacaine and stearic acid (SA-ROP HIP), which was then combined with glyceryl monostearate (SA-ROP-GMS). SA-ROP-GMS maintained analgesia for nearly 10 days in a single dose, significantly improving ease of administration and patient compliance. In addition, the auxiliary ingredients used in this study are biocompatible and inexpensive. This formulation follows the trend of regional anesthesia and provides a new solution for postoperative pain management.
研究领域:
药剂学
·
疼痛管理
·
生物材料
✓ 已验证
产品关联
DOI
PubMed
高影响因子
INTERNATIONAL JOURNAL OF PHARMACEUTICS
·
2024
·
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
·
分析化学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
ACS Nano
·
2014
·
IF 12.033
Hanjun Sun,Nan Gao,Kai Dong,Jinsong Ren,Xiaogang Qu
Herein, an antibacterial system combining the “safe” carbon nanomaterials, graphene quantum dots (GQDs), with a low level of H2O2 has been put forward. It has been found that the peroxidase-like activity of GQDs originates from their ability to catalyze the decomposition of H2O2, generating ·OH. Since the ·OH has a higher antibacterial activity, the conversion of H2O2 into ·OH improves the antibacterial performance of H2O2, which makes it possible to avoid the toxicity of H2O2 at high levels in wound disinfection. All the experiments in vitro display that this intrinsic activity exerts a high enhancement of antibacterial activity of H2O2, and the designed system possessed broad spectrum of antibacterial activity against both Gram-negative (Escherichia coli) and Gram-positive (Staphylococcus aureus) bacteria. More importantly, to assess the antibacterial efficacy of the designed system in actual wound disinfection, the GQD-Band-Aids are prepared and show excellent antibacterial property with the assistance of H2O2 at low dose in vivo.
研究领域:
生物医学工程
·
材料科学
·
微生物学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS
·
2023
·
IF 3.4
Yu-ye Wang,Fan Yang,Jian Chen,Ying-jian Li,Jia Zhou,Xia Qing,Dong Yan,Xin Lu,Peng Zhou,Li Zhang
Lactose is one of the most commonly used pharmaceutical excipients . Depending on manufactures, the properties of lactose are very different, which could impact the pharmacokinetic behavior of drug products. Therefore, it is very important to trace the origin of pharmaceutical lactose in drug products which is valuable for prescription analysis. In this study, the carbon, hydrogen and oxygen isotope ratios ( δ 13 C, δ 2 H and δ 18 O) of thirty-four lactose from seven manufacturers were analyzed by elemental analysis-stable isotope ratio mass spectrometry (EA-IRMS). One-way analysis of variance (ANOVA) and Duncan's test indicated significant differences in isotope ratios of lactose from different origins. To identify the lactose manufacturer, a discrimination model was generated through linear discriminant analysis (LDA). Based on this model, the manufacturers of lactose used in three drug products were successfully identified. Our results suggested that the multidimensional analysis of δ 13 C, δ 2 H and δ 18 O of lactose provided a fast and effective method to trace the lactose manufacturer. In conclusion, this method can be used to analyze the prescription of the drug product quickly, which could speed up the development of generic drug product.
研究领域:
药学
·
分析化学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
POLYMER
·
2022
·
IF 4.432
Yuan Liu,Fei Hu,Shuo Wang,Mengmeng Xu,Qianqian Yu,LinGe Wang
Polymersomes (polymeric vesicles) are non-viral delivery vehicles self-assembled from block copolymers (BCPs), holding promising potential in biomedical applications. Despite the higher chemical stabilities of the BCPs, lyophilization is still required for the long-term preservation of the polymersomes and their encapsulated drugs. However, formulation and processing parameters can affect the efficiency of the lyophilization. In this work, we present an approach to evaluate the integrity of polymersomes based on Fluorescence Resonance Energy Transfer (FRET) for rapid optimization of the lyophilization parameters. Specifically, Coumarin 6 (C6) and Nile red (NR)-encapsulated polymersomes were fabricated separately and mixed together for lyophilization. Upon reconstitution, FRET was detected for polymersomes which lost integrity during the lyophilization or reconstitution. The evaluation was carried out for poly(ethylene glycol)- b -poly(lactic acid) (PEG- b -PLA) polymersomes lyophilized with eight different excipients , and the results showed that the best polymersomes integrity could be achieved with the addition of hydroxypropyl-beta-cyclodextrin (HP-β-CD). We believe the approach described here would greatly facilitate the optimization of the polymersomes lyophilization, accelerating the translation of polymersomes to practical applications.
研究领域:
生物医学工程
·
药物递送系统
·
材料科学
✓ 已验证
产品关联
DOI
高影响因子
Annales Pharmaceutiques Francaises
·
2020
·
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
·
材料科学
✓ 已验证
DOI
JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY
·
2020
·
IF 2.734
Jing Yuan,Jieyu Wu,Tianxiang Yin
Ionic liquids have recently been found to be effective ingredient in formulation of transdermal drug delivery system . In this work, we synthesized two cholinium-animo acid based ionic liquids CHAAILs, cholinium glycinate [Ch][Gly] and cholinium analinate [Ch][Ala], and investigated their ability to enhance the solubility and permeation of model drug ibuprofen . The solubility measurements showed that slight amount of CHAAILs can significantly increase the solubility of ibuprofen. Besides, the effective enhancement of permeation of ibuprofen across polyethersulfone (PES) membrane was clearly presented at low concentration (0.8 wt%) of CHAAILs. It is more valuable that the addition of CHAAILs brings little cytotoxicity. Therefore, [Ch][Gly] and [Ch][Ala] can be served as green and effective constituents in transdermal drug delivery system.
研究领域:
药剂学
·
药物递送系统
·
分子药理学
·
生物药剂学
·
药物代谢
✓ 已验证
DOI
高影响因子
POWDER TECHNOLOGY
·
2014
·
IF 2.269
En-Yu Xu,Jing Guo,Ying Xu,Hao-Ying Li,Peter C. Seville
Two areas attracting considerable attention when developing effective pulmonary drug delivery systems include the improvement of aerosolisation efficiency of the inhaled formulation and the controlled release of drug from the formulation following deposition within the lung. In this study, four saccharides were employed as excipients in the preparation of spray-dried powder formulations for the pulmonary drug delivery. Beta-cyclodextrin-, starch-, and sodium carboxymethylcellulose (NaCMC)-based spray-dried powders showed a significant (one-way ANOVA, Duncan's test, p < 0.05) increase in lower stage drug deposition in the Next Generation Impactor (NGI) when compared to lactose-based spray-dried powders. Furthermore, NaCMC-based spray-dried powder formulations exhibited a sustained drug release profile in dissolution testing; approximately 80% of salbutamol sulphate was released after an hour, whereas drug from the lactose-based spray-dried powder formulation was released within 5 min. Our results clearly demonstrate that the inclusion of NaCMC in spray-dried powder formulations increases the aerosolisation efficiency of the powder and also offers the potential for sustained drug release, which may be of benefit in the treatment of local and systemic conditions.
研究领域:
药剂学
·
药物递送系统
✓ 已验证
产品关联
DOI
高影响因子
危险品化学品经营许可证（带存储）