A comprehensive evaluation was conducted on 27 directly pulverized natural medicinal plant and mineral products (DP-NPs) by analyzing their fundamental and functional characteristics. Multiple analytical methods were employed to establish different classification systems or models, as well as to investigate the influence of powder properties upon critical tablet attributes. The results indicated that: (i) The fundamental properties of DP-NPs showed considerable variation (particularly in the mineral powders), e.g., wettability (contact angle, 64.7(o) to 121.7(o)) and flowability (angle of repose, 42.2(o) to 63.0(o)); (ii) a classification system for wet-granulation suitability was established with medium and high Liquid/Solid ratio powders (e.g., leaf powders) demonstrated suitability for granulation; (iii) powders were grouped into three categories based on tableting performance: Group 2 (the best: Lycii Fructus/FR3, TS = 3.56 MPa under 240 MPa) > Group 1 (e.g., Gypsum Fibrosum) > Group 3 (the worst: Lablab Semen Album, TS = 0.01 MPa under 240 MPa) using multiple analysis; (iv) powders were categorized into three classes according to their tablet disintegration kinetics: disintegrating (e.g., root powders), expansive (e.g., leaf powders), and dissolved (FR3) ones; and (v) Elastic Net Regression modeling revealed a positive correlation between tensile strength and disintegration time of tablets for the majority of DP-NPs, identifying key variables (e.g., yield pressure) influencing the two critical quality attributes. In summary, this study provides a systematic framework for understanding and predicting the behavior of DP-NPs in tablet production, establishing a scientific foundation for rational formulation design under the Quality by Design (QbD) paradigm.

This work aims to provide an effective and feasible solution for direct compaction (DC) production of high loading tablets of directly pulverized herb powders (DPPs). To confirm the generality of the solution, five DDPs with different and representative physical properties were selected to prepare modified composite particles (CPs) by liquid dispersion method with hydrophilic nano-silica (INS). The effects of key process factors were studied by setting (i) different dispersion liquid, i.e., water, 75 % ethanol, and anhydrous ethanol, and (ii) different initial particle sizes of DPPs. All DPPs were modified to meet the SeDeM expert system evaluation criteria which indicate the potential for DC. The tablet made by optimized CPs through continuous DC had less friability and more stable quality compared with the raw powder tablets. It was proved that the dispersion liquid would influence the amount and viscosity of the leaching liquor of the herbs, and, thus, affect the bonding strength of the drug and INS as well as the distribution of INS. However, the initial particle sizes affected little. Furthermore, the relationship between physical properties of powders as well as the moving trend were revealed by principal component analysis, and tablet quality was modelled by using the partial least-squares method.

Platycodonic Radix (PR) is a key herb in traditional Chinese prescriptions for pediatric respiratory disorders. However, its intense bitterness and persistent throat astringency reduce treatment compliance. This study established a mechanism-informed taste-masking strategy integrating chemical profiling, sensory evaluation, and formulation optimization. PR sensory characteristics were first quantified using human panels and an electronic tongue. Subsequently, PR water extracts were characterized by non-targeted profiling based on liquid chromatography-mass spectrometry (LC-MS). Putative bitter constituents were further screened using BitterX-assisted TAS2R molecular docking. The optimized formulation was then validated in two representative pediatric formulas containing the classical "PR-Glycyrrhiza uralensis Fisch." herb pair. LC-MS tentatively identified 308 compounds in PR decoctions, mainly carbohydrates and glycosides. Docking results indicated that platycodigenin, polygalacic acid, lactone-type platycodins, luteolin, and lignans show high affinity for human bitter taste receptors TAS2R14, TAS2R44, and TAS2R47, confirming a multi-component basis for PR bitterness. Among the excipients tested, 2-Hydroxypropyl-β-cyclodextrin (HP-β-CD) and xylitol were most effective. Mechanistically, HP-β-CD primarily suppressed residual bitterness and astringency, whereas xylitol improved initial mouthfeel. An optimized combination of 6.5 % HP-β-CD plus 10 % xylitol (w/w relative to PR) successfully transformed PR decoctions from "difficult to accept" to "sweet with no lingering bitterness", a shift corroborated by electronic tongue DFA plots. This strategy improved palatability in two representative pediatric formulas without altering the herbal composition. These findings demonstrate that 6.5 % HP-β-CD plus 10 % xylitol effectively alleviates both initial bitterness and throat irritation, offering a practical, non-destructive solution to enhance pediatric medication adherence in traditional phytotherapy.

Markovnikov hydroformylation of unactivated olefins represents a fundamental and highly valuable reaction for the formation of aliphatic branched aldehydes, but it remains challenging, because conventional hydroformylations typically exhibit anti-Markovnikov selectivity. Herein, we report a novel palladium-catalyzed Markovnikov hydroformylation of unactivated olefins to afford a series of branched aldehydes in high yields and with high regioselectivity. Crucial to the success of this reaction is the use of a unique neutral palladium catalyst coordinated with a novel (3',5'-bis(trifluoromethyl)-[1,1'-biphenyl]-2-yl)diphenylphosphane ligand, in conjunction with a silane-acetate acid system serving as the hydrogen surrogate. The mechanism of the reaction has been studied by several methods. The utility and versatility of this reaction are demonstrated by the efficient transformation of readily available olefins into high-value flavor and fragrance compounds.

By investigating three single herbal groups and seven validation groups, where Puerariae Lobatae Radix (PLR) extract was respectively combined with four directly pulverized natural plant powders (DP-NPPs) and three excipients, this study examined the effects of composition and process (wet co-processing and physical mixing) on powder tabletability, revealing a positive deviation (i.e., the measured tabletability exceeds the theoretical additive one) for co-processed powders (CPs) with high extract ratios. For example, the tensile strength of tablets of 80% PLR extract-20% DP Turpiniae Folium CP tableted under 100 MPa is 5.1 times of the theoretical value. To elucidate the underlying mechanism, the role of bonding area (BA), bonding strength (BS), and their interplay were explored. DP-NPPs exhibited poorer compressibility (BA) compared to extracts, whereas their σ0 (apparent BS) was unexpected significantly higher than that of extracts (e.g., σ0 of DP-PLR is 37.8 times that of PLR extract). The mechanism underlying the positive deviation can be categorized as the positive BS one (e.g., PLR-CP containing 67% extract) and the BA-BS synergistic one (e.g., Sophorae Flavescentis Radix CP containing 80% extract). Moreover, this study reveals that the threshold of extract ratio for CPs to exhibit positive deviation is governed by the BS and tabletability difference between DP-NPP and extract: the greater the BS difference and the smaller the tabletability difference, the lower the threshold. Overall, this study provides some theoretical evidence for the combined use of DP-NPPs with extracts in herbal tablets, and is conducive to the formulation and process design of herbal tablets.

Pheretima products are widely used, but the stenchy odor is a constraint to their application. In this study, 86 and 673 volatile components (VOCs) were identified in Pheretima and its extracts using headspace gas chromatography-ion mobility spectrometry (HS-GC-IMS) and headspace solid-phase microextraction-gas chromatography-mass spectrometry (HS-SPME-GC-MS), respectively. An increase in acid and amine contents after processing was found, which may explain the increased stenchy odor. Through orthogonal partial least squares discriminant analysis (OPLS-DA), 14 differential markers between aqueous and alcoholic extracts were screened, and 3-methylbutanal, pentanal, and trimethylamine were identified as the key differential odor components. Combined with relative odor activity value (ROAV) analysis, 10 key odor components were identified, including: 3-methylbutanal, 1-octen-3-ol, dimethyl trisulfide, (2E,6Z)-nona-2,6-dienal, methyl mercaptan, guaiacol, isobutyraldehyde, 1,8-cineole, 2-pentylfuran, and pentanal. This study provides theoretical support for the optimization of the odor of Pheretima-containing products and promotes their application.

BACKGROUND:The ethanol extract of Pueraria lobatae Radix (EPL), a kind of medicinal herb powder with unacceptable behaviour (poor compactibility and slow dissolution rate), has the potential to be improved by double particle surface design by fluid-bed coating. This involves surface coating with plastic Hydroxypropyl Methylcellulose (HPMC) and surface pore formation induced by NH4HCO3. METHODS:The EPL drug was selected as the model for investigation. The formulation of the Composite Particles (CPs) was optimized using a central composite design. Subsequently, the pivotal tabletrelated attributes were contrasted between the optimized porous HPMC-coated EPL CPs and the pure HPMC-coated EPL CPs. Finally, the stability and applicability of the porous HPMC-coated EPL CPs were studied. RESULTS:The results demonstrated that (i) the optimized use levels of HPMC and NH4HCO3 for the porous CPs were 8.42% and 15.00% (w/w), respectively; (ii) the compactibility and tablet dissolution rate of the porous HPMC-coated EPL CPs were significantly enhanced in comparison to those produced from the pure HPMC-coated CPs; and (iii) the porous HPMC-coated CPs exhibited good stability and universal applicability in direct compaction. CONCLUSION:As a whole, the combination of polymeric coating and porous design proved effective in enhancing the compactibility and dissolution rate of EPL-based CPs while also rendering them suitable for direct compaction. These findings are conducive to the expansion of the application of fluidbed coating technology and the simultaneous improvement of the quality and efficacy of some drug tablets.

Twin-screw wet granulation (TSWG) is an innovative continuous granulation method in the pharmaceutical industry, yet research on its application for natural plant product (NPP) powders is limited. This study aims to investigate the TSWG processes of water extracted (W-E), ethanol extracted (E-E) and direct pulverization (D-P) NPP powders, as well as elucidate the forming mechanisms of different particles during the granulation. Principal component analysis was conducted on the physical properties of NPP and excipients powders, which identified three groups based on maximum liquid absorbency and torque rheological parameters. Granules from Group (1) were relatively dense with large particle size and low friability. In contrast, granules from Groups 2 and 3 were looser with small particle size and high friability. The granule forming mechanism revealed that W-E and E-E NPP powders partially dissolved and, after drying, formed rigid solid bridges that tightly bound the powder together. In contrast, the D-P NPP powders dispersed on the surface of droplets, creating internally porous and interconnected aggregates where the powder particles were held together mainly by intermolecular forces. Overall, this study systematically investigated the properties and TSWG process of NPP powders, and explained the forming mechanism of different NPP powders in TSWG. (c) 2025 The Society of Powder Technology Japan. Published by Elsevier B.V. and The Society of Powder Technology Japan. All rights are reserved, including those for text and data mining, AI training, and similar technologies.

In this study, berberine hydrochloride was combined with ion exchange resin to mask the unpleasant taste of berberine hydrochloride. The research uncovered the equation of berberine hydrochloride solubility in different beta-cyclodextrin concentrations at different temperatures, providing a foundation for selecting binding parameters. The effects of various factors on the reaction process were then investigated. Following that, the characteristics and taste evaluation were studied to verify the formation. at last, the in vitro release studies of chosen complexes were determined in solution mediums with pH values of 1.0, 4.5, and 6.8. The results revealed that Amberlite IRP69, which has a higher drug availability and a better taste-masking effect, was selected as the drug carrier. The optimal combined conditions are that the beta-cyclodextrin concentration is 0.06 mol & sdot;L- 1, the temperature is 65 degrees C, and the berberine hydrochloride concentration is 15 mg & sdot;mL- 1. Finally, in vitro release experiments of berberine hydrochloride and Amberlite IRP69 complex showed that the drug could be released more than 90 % in a medium with pH values of 1.0, 4.5, and 6.8. The research provided a method for preparing the berberine hydrochloride and resin complex, and the well-tasting complex was successfully prepared.

With the rapid development of buccal films (BFs), the demand for film-forming materials and preparation techniques has increased. Cellulose ethers (CEs) exhibit favorable properties, such as effective film formation, mucosal adhesion, and biocompatibility; as such, they are most commonly employed as film-forming materials, essential for BF fabrication. CE-based BFs, classified as orodispersible and buccal mucoadhesive films, can be prepared through solvent casting, inkjet printing, three-dimensional printing, electrospinning, and hot melt extrusion. Hydrophilic CE-based orodispersible films can rapidly dissolve or disintegrate upon contact with saliva to release drugs. High-viscosity or hydrophobic CEs can serve as protective layers for BFs, controlling the unidirectional release of drugs and mitigating the effects of saliva and buccal movements. These mucoadhesive films can firmly adhere to the buccal mucosa for an extended period, prolonging drug release time and enhancing bioavailability. CEs come in various types and grades, exhibiting different rheological and physicomechanical properties, which also provide options for customized design to specific patients. This review provides an overview of CE-based BF technology, analyzes the challenges and development directions of this film, and identifies key areas for scientific research, such as the interactions of bioadhesive materials in buccal mucosal drug delivery. The objectives of this review are to (i) highlight the value of their application in oral drug delivery and (ii) promote the broader adoption of BF-based patient-centric dosing.

Low-viscosity hydroxypropyl methylcellulose (HPMC) was obtained by electron beam irradiation, and its use as an excipient for improving the properties of spray dried pharmaceutical powders was investigated. The minimum molecular weight of HPMC which could maintain the capacity of encapsulation and powder modification was explored. As the irradiation dose was increased from 10 to 200 kGy, the molecular weight and viscosity of HPMC decreased linearly. However, its main structure and degrees of methoxy and hydroxypropyl substitution were not significantly affected. The irradiated HPMC could encapsulate particles during spray drying and, thus, modify powder properties. Furthermore, the water content of spray-dried powders with irradiated HPMC was lower than that with parent HPMC. After the spray-dried powder with irradiated HPMC was prepared into granules, their dissolution rate was also faster. However, in order to achieve high encapsulation, the molecular weight of HPMC should be ensured to be above 7.5 kDa. The designated low-viscosity HPMC obtained by electron beam irradiation is a suitable powder-modification material for use in spray drying, and it shows promise as a superior excipient in medicine, food, paint industries, among others.

In the process of preparing presonalized concentrated watered pills,the decoction needs to be concentrated by heat and mixed with medicinal slices or powder to prepare a wet mass.However,some of the traditional Chinese medicine(TCM)components are easily decomposed or transformed by heat.In order to optimize the preparation process of presonalized TCM concentrated watered pills and reduce the loss of heat-unstable components in prescriptions,this study uses five compound TCM prescriptions containing heat-unstable components as model prescriptions,namely the Linggui Zhugan Formula,Xiaochengqi Formula,Sanpian Formula,Xiaoer Qixing Formula,and Xiaoyao Formula.Based on the two kinds of preparation process of presonalized concentrated watered pills previously established by our research group,whole extract concentrated watered pills and concentrated watered pills without excipients are prepared,respectively.Characteristic maps are measured and compared with those of the corresponding decoction.The results show that the characteristic maps of the concentrated watered pills without excipients of the five model prescriptions are very close to those of the decoction,and the number of characteristic peaks and peak areas are higher than those of whole extract concentrated watered pills.In addition,the peak area of some peaks is higher than that of the corresponding decoction.Thus,it is recommended to select the preparation process of prescription-based concentrated watered pills without excipients based on the"unification of medicines and excipients"to preserve those heat-unstable components more effectively when the prescription contains a heat-unstable component of TCM.This study provides a basis for the subsequent reasonable development and application of presonalized TCM pills.

The study aimed to fingerprint the physical manufacturing properties of five commonly used acid sources in effervescent systems for designing the formulation and process of such systems. The hygroscopicity, texture properties, rheological torque, compressibility, tabletability, etc., were investigated to inspect 'powder direct compression (DC)' and 'wet granulation and compression' properties of citric (CA), tartaric (TA), malic (MA), fumaric (FA), and adipic acid (AA). The DC ability was evaluated by the SeDeM expert system. The results indicated that all acid powders failed to meet flowability requirements for DC, and plastic deformation dominated during compression. Furthermore, CA exhibited strong hygroscopicity and punch sticking, while MA demonstrated the best tabletability. TA had a large wet granulation space and was relatively the most suitable for DC. AA was extremely hygroscopic, and its flowability improved significantly as particle size increased. Finally, FA displayed the lowest hygroscopicity and ejection force as well as great compressibility and wet granulation space, and did not exhibit punch sticking, while the granule fragments dissolved slowly during disintegration. Generally speaking, the formulation or granulation affected the tabletability, indicating that pairing with other acids or suitable fillers could potentially improve its disadvantages. These multidimensional assessments effectively reduce the pre-exploration and enhance the efficiency of the development of effervescent systems.

Traditional Chinese medicine(TCM) placebos are simulated preparations for specific objects and the color simulation in the development of TCM placebos is both crucial and challenging. Traditionally, the prescription screening and pattern exploration process involves extensive experimentation, which is both time-consuming and labor-intensive. Therefore, accurate prediction of color simulation prescriptions holds the key to the development of TCM placebos. In this study, we efficiently and precisely predict the color simulation prescriptions of placebos using an image-based approach combined with Matlab software. Firstly, images of TCM placebo solutions are captured, and 13 chromaticity space values such as the L* a* b*, RGB, HSV, and CMYK values are extracted using Photoshop software. Correlation analysis and normalization are then performed on these extracted values to construct a 13×9×3 back propagation(BP) neural network model. Subsequently, the whale optimization algorithm(WOA) is employed to optimize the initial weights and thresholds of the BP neural network. Finally, the optimized WOA-BP neural network is validated using three representative instances. The training and prediction results indicate that, compared to the BP neural network, the WOA-BP neural network demonstrates superior performance in predicting the pigment ratios of placebos. The correlation coefficients for training, validation,testing, and the overall dataset are 0. 95, 0. 87, 0. 95, and 0. 95, respectively, approaching unity. Furthermore, all error values are reduced, with the maximum reduction reaching 99. 83%. The color difference(ΔE) values for the three validation instances are all less than 3, further confirming the accuracy and practicality of the WOA-BP neural network approach.

Improving the tableting-related properties (flowability, compressibility, compactibility, etc.) of pharmaceutical materials, especially active pharmaceutical ingredients (APIs), is critical for pharmaceutical manufacturing. A significant number of APIs and excipients exist in crystalline form. The polymorphisms and crystal habits of crystals will affect their physicochemical properties, pharmaceutical properties, bioavailability, and so on. In recent years, increasing modification methods for crystals, including cocrystallization, solvation, salting, and spherical crystallization, have concentrated on improving the solubility of materials. Besides, effects to tableting-related properties for pharmaceutical materials are reviewed herein. Layered, columnar/prismatic, spherical, and fragile hollow structures can be associated with excellent tabletability in most cases, while different polymorphs as well as block and needle shapes require further research on the presence or absence of active slip plane system and anisotropy, which are often related to better plasticity and consequently superior tabletability. Based on this, the theoretical methods of crystal morphology prediction are introduced. The solid-state transitions during tablet pharmaceutical manufacturing process due to moisture, heat, and mechanical strength during the tablet manufacturing process is also worth reviewing to help the controllability of crystal form in the final product. It is believed that a comprehensive understanding of crystals will help unlock the potential of more materials for practical production and clinical applications.

Based on high performance liquid chromatography-quadrupole time-of-flight tandem mass spectrometry(UPLC-Q-TOF-MSE)and molecular docking technique,bitter compounds of Ginkgo biloba extract(GBE)were characterized,and their relationship with bitter efficacy was investigated.Firstly,UPLC-Q-TOF-MSE was used for qualitative analysis of GBE components,and 60 chemical components were identified.These chemical components were molecular-docked with bitter receptors,and 26 bitter substances were se-lected,mainly flavonoids.Secondly,sensory and electronic tongue bitterness evaluation techniques were used to verify that total fla-vones of GBE were the main bitter substances,which was consistent with the molecular docking results.Finally,network pharmacology was used to predict and analyze bitter substances.The relationship between the target of bitter substance and bitter effect was explored.The key targets of bitter substances are CYP2B6,ALOX15,and PTGS2,etc.,and bitter substances may exert a bitter efficacy by ac-ting on related disease targets,indicating that bitter substances of GBE are the material basis of the bitter effect.In summary,the study indicated that the molecular docking technique had a guiding effect on the screening of bitter substances in traditianal Chinese medicine(TCM),and bitter substances of GBE had a bitter efficacy.It provides ideas and references for the study of the"taste-efficacy rela-tionship"of TCM in the future.

Hydroxypropyl methylcellulose (HPMC) is an important polymeric excipient. Its versatility in terms of molecular weights and viscosity grades is the basis for its wide and successful application in the pharmaceutical industry. Low viscosity grades of HPMC (like E3 and E5) have been used as physical modifiers for pharmaceutical powders in recent years due to their unique physicochemical and biological properties (e.g., low surface tension, high Tg, strong hydrogen bonding ability, etc.). Such modification is the co-processing of HPMC with a drug/excipient to create composite particles (CPs) for the purpose of providing synergistic effects of functional improvement as well as of masking undesirable properties of the powder (e.g., flowability, compressibility, compactibility, solubility, stability, etc.). Therefore, given its irreplaceability and tremendous opportunities for future developments, this review summarized and updated studies on improving the functional properties of drugs and/or excipients by forming CPs with low-viscosity HPMC, analyzed and exploited the improvement mechanisms (e.g., improved surface properties, increased polarity, hydrogen bonding, etc.) for the further development of novel co-processed pharmaceutical powders containing HPMC. It also provides an outlook on the future applications of HPMC, aiming to provide a reference on the crucial role of HPMC in various areas for interested readers.

气味是中药的重要感官指标,与中药品质及药效作用直接相关.一些常用中药具有特殊的气味,也是其鉴别和品质评价的重要指标.从化学物质基础角度来说,挥发性化学成分的种类和含量差异,导致了不同中药气味的异同.研究中药气味的化学物质基础对中药的综合质量控制、临床应用辅助、科学内涵解释等中药现代研究具有重大意义,而目前阶段对中药气味的研究,主要集中在挥发油的成分、制剂工艺和药理作用方面,以及使用感官分析设备对中药气味进行现代表征和区分,而对中药气味的分类和化学物质基础尚未有较为系统的总结和介绍.本文从中药气味检测技术、气味的感官分类、气味的化学物质基础和中药制剂生产过程中气味的变化规律等方面对此主题进行综述,并对其研究方向进行展望.

Abstract In this study, hydroxypropyl Methylcellulose (HPMC) with lower viscosity was obtained by electron beam irradiation (EBI), and its physical modifiers for pharmaceutical powders was investigated when it was used during spray drying. After HPMC was irradiated at a dose of 150 kGy, the main structure of HPMC was not affected, and the substitution degree of methoxy and hydroxypropyl was not destroyed significantly. As the irradiation dose increased from 10 to 150 kGy, the molecular weight and viscosity of HPMC decreased continuously. The results of spray drying showed that HPMC could quickly migrate to the surface of the liquid medicine to cover droplets during spray drying and atomization, which improved the hygroscopicity and increased the softening point of spray-dried powder. And the powder water content is lower. After the powder is prepared into particles, the dissolution rate of particles is faster. Therefore, the modified powder exhibits better physical properties. The low viscosity HPMC obtained by electron beam irradiation is suitable for powder modification materials during spray drying, and is expected to be developed as excipient in traditional Chinese medicine and other industries.

腹泻型肠易激综合征(diarrhea-predominant irritable bowel syndrome,IBS-D)是肠易激综合征(irritable bowel syndrome,IBS)最常见的亚型.IBS-D的主要病因包括胃肠道炎症反应、内脏敏感性增加、脑-肠轴异常、肠道微生态紊乱、肠道屏障受损等.在这些病理进程中存在引发IBS-D的关键因子,因此可以寻找IBS-D发病的关键信号通路及关键信号因子,作为治疗IBS-D的生物靶标,通过抑制或调节这些生物靶标,以达到防治IBS-D的目的.研究显示,以中医药途径干预治疗IBS-D是一种安全且有效的方法,无论是单味中药或是中药复方,均显示对IBS-D的发病机制中的多种关键通路及关键信号因子具有调节作用.本文就中药对治疗IBS-D发病进程中的关键生物靶标的研究进展进行综述,为IBS-D治疗药物作用机制探索及新药开发提供思路.