Classification optimization of traditional Chinese medicine materials based on additive physical properties of powder / 中国中药杂志

According to the method of predicting the physical properties of oily powder based on the additive physical properties of Chinese medicinal powder, Dioscoreae Rhizoma and calcined Ostreae Concha with high sieve rate and good fluidity were mixed and crushed with Persicae Semen, Platycladi Semen, Raphani Semen, Ziziphi Spinosae Semen, and other typical oily materials with high fatty oil content in proportion to obtain 23 mixed powders. Fifteen physical properties such as bulk density, water absorption, and maximum torque force were measured, and the physical properties of typical oily powders were predicted. When the mixing and grinding ratio was in the range of 5∶1-1∶1, the r value in the correlation equation between the weighted average score of the mixed powder and the powder proportion ranged from 0.801 to 0.986, and the linearity was good, indicating that the method of predicting the physical properties of oily powder based on the additive physical properties of traditional Chinese medicine(TCM)powder was feasible. The results of cluster analysis showed that the classification boundaries of the five kinds of TCM materials were clear, and the similarity of the physical fingerprints of powdery and oily materials decreased from 80.6% to 37.2%, which solved the problem of fuzzy classification boundaries of powdery and oily materials due to the lack of representativeness of oily material model drugs. The classification of TCM materials was optimized, laying a foundation for optimizing the prediction model of the prescription of personalized water-paste pills.

Improvement on compactibility of the alcoholic extract of Zingiberis Rhizoma by co-spray drying with HPMC / 中国中药杂志

Aiming to solve the poor compactibility of the alcoholic extract of Zingiberis Rhizoma(ZR), this study explored the feasibility of its physical modification using co-spray drying with a small amount of hydroxypropyl methyl cellulose(HPMC). Based on the univariate analysis, the influence of two independent variables(the HPMC content in the product and the solid content of spray material) on the powder properties and tablet properties of the dried product was investigated by the central composite design. With the tensile strength and disintegration time of the tablets as the evaluation indexes, the optimal prescription was determined as follows: the HPMC content was 15% and the solid content of spray material was 25.6%. The accuracy of the regression model established for predicting tensile strength and disintegration time of tablets was verified, and the results revealed that the measured values were close to the predicted ones with deviations of 0.47% and-8.2%, indicating good prediction and reproducibility of the model. The tensile strength(4.24 MPa) of tablets prepared with the optimal prescription was 3.59 times that(1.18 MPa, far lower than the baseline of 2 MPa for qualified tablets) with the spray-dried powder of the ZR. On the other hand, due to the addition of HPMC, the disintegration time of tablets increased from 7.3 min to 24.6 min. On the whole, this study provided a new strategy to solve the common problem of poor compactibility of raw Chinese medicinal materials, which facilitated the successful preparation of Chinese medicinal tablets with high drug loads.

Quality value transmitting of volatile components in personalized preparations:a case study of Menthae Haplocalycis Herba / 中国中药杂志

Considering the characteristic chromatograms and quality value transmitting of three volatile components, this study investigated the changes in volatile components of Menthae Haplocalycis Herba in each heating process of personalized preparations and identified the critical control points for the application of volatile components from traditional Chinese medicine in such preparations. The characteristic chromatograms of volatile components in Menthae Haplocalycis Herba were established by gas chromatography, followed by the quantitative determination of three volatile components menthone, menthol, and piperitone and the comparison of retention rates of volatile components during the crushing, extraction, concentration and drying of preparation products and their change rules in characteristic peaks. The results showed that the volatile components of Menthae Haplocalycis Herba were reduced in each process. The loss rate was low in the crushing process when the volatile component peaks were present, but high in the extraction and concentration processes, manifested as the absence of partial component peaks and the presence of new component peaks. The changes in volatile components of Chuanxiong Chatiao Granule in the drying process were compared with those in Chuanxiong Chatiao Pill, both of which were prepared from the raw Menthae Haplocalycis Herba powder, and the findings demonstrated that Chuanxiong Chatiao Pill was superior to Chuanxiong Chatiao Granule. This study confirmed that the retention rates of volatile components in Menthae Haplocalycis Herba were mostly affected by the extraction and concentration processes, and the packing of preparations helped to reduce the loss of volatile components in Menthae Haplocalycis Herba powder, which has provided reference for the application of Chinese medicinal materials containing volatile components in the personalized preparations.

Preparation of personalized traditional Chinese medicine condensed water pill without excipients based on correlation between concentrate viscosity and molding quality / 中国中药杂志

To explore the correlation between concentrate viscosity and molding quality of personalized traditional Chinese medicine(TCM) condensed water pill, this study established a concentrate viscosity characterization method with rotational rheometry. Seven model prescriptions were respectively concentrated to different degrees and the viscosity of each concentrate was determined. The pre-sence of 'viscosity jump' in the middle stage of 'flag hanging' of all the model prescriptions implied that there might be an ideal viscosity range in the preparation of condensed water pill. The further study of 22 model prescriptions demonstrated that the optimum viscosity range of concentrate was 5-15 Pa·s(25 ℃) for approximately 82% of the prescriptions. About 18% of the prescriptions had a wide range, which might be caused by the high proportions of mineral and crustacean drugs in the crushing part and sugar and fibrous drugs in the decocting part. This study clarified the optimum viscosity range for concentrates of personalized TCM condensed water pills and achieved a preparation technology without any excipient, laying a foundation for the on-line control of the preparation.

Establishment of prediction model for personalized water-paste pills based on classification of traditional Chinese medicine materials / 中国中药杂志

The purpose of the present study was to investigate the relationship of the classification of traditional Chinese medicine(TCM) materials with the suitable binder concentration and dosage in the preparation of personalized water-paste pills and establish a model for predicting the binder concentration and dosage. Five representative TCM materials were selected, followed by mixture uniform design. The water-paste pills were prepared by extrusion and spheronization with hypromellose E5(HPMC E5) as the binder. The quality of intermediates and final products was evaluated, and the resulting data were subjected to multivariate statistical analysis. The prediction models for binder concentration and dosage were established as follows: binder concentration: Y_1=0.378 6 + 0.570 1X_A + 2.271 2X_B-0.894 5X_C-0.458 2X_D-1.145 4X_E(when Y_1 < 0, 10% HPMC E5 was required; when Y_1 > 0, 20% HPMC E5 was required), with the accuracy reaching up to 100%; binder dosage: Y_2=32.38 + 0.25X_A + 1.85X_B-0.013X_B~2-0.002 5X_C~2(R~2=0.932 6, P < 0.001). The results showed that the binder concentration and dosage were correlated positively with the proportion of fiber material but negatively with the proportions of sugar material and brittle material. Then the validation experiments were conducted with the prediction models and all the prescriptions could be successfully prepared at one time. These demonstrated that following the classification of TCM materials and the calculation of their proportions in the prescription, the established mathematical model could be adopted for predicting the binder concentration and dosage required in the preparation of personalized water-paste pills, which contributed to reducing the pre-formulation research and guiding the actual production of personalized water-paste pills.

Material classification of decoction pieces based on physical properties of powder / 中国中药杂志

Chinese medicinals feature different medicinal parts and enriched components, which makes their powders show obvious microscopic identification characteristics and specific physical properties. On this basis, the commonly used Chinese medicinals can be divided into several categories, such as powdery, fibrous, sugar, oil, and brittle materials, which is of great importance to the research and development of personalized Chinese medicinal preparation technology. However, the existing classification methods are highly subjective and thus difficult to meet the requirements for the development of personalized Chinese medicinal preparations with high quality. In this study, 55 representative Chinese medicinals, such as Dioscoreae Rhizoma and Leonuri Herba, were selected, and the physical properties of their powders were systematically characterized by comprehensive powder tester, torque rheometer, texture analyzer, etc., based on which a data set encompassing physical properties of these powders was built. The typical physical fingerprints of powders from the above 5 categories were established by multivariate statistical analysis. Then, the Chinese medicinals were classified according to the Euclidean distance between each of them and the typical value in the PCA score plot. For those with multiple material properties, whose classification boundary was fuzzy, the proportions of different types of materials were calculated with the combination of Euclidean distance, powder properties, microscopic identification characteristics, and chemical composition, so as to achieve the multivariate quantitative classification of Chinese medicinals. This lays the foundation for the further creation of intelligent personalized Chinese medicinal preparation technology.

Characteristics and development assumptions of personalized traditional Chinese medicine granules / 中国中药杂志

Personalized traditional Chinese medicine(TCM) granules are positioned as a solid dosage form of TCM decoctions, boasting strong applicability and wide application range. The market prospect of personalized TCM granules is promising in that their preparation by mixed decoction makes up for the shortcoming of formula granules like the Chinese patent medicine granules and classical TCM prescription granules whose components cannot be changed flexibly. However, such factors as insufficient basic research, equipment mismatch, and low process commonality have limited their clinical application. After analyzing the characteristics of perso-nalized TCM granules, their production status, and the bottlenecks restricting their development, this paper pointed out the meaning and key points of developing a generalized preparation process for personalized TCM granules and affirmed the vital roles of the preparation and process prediction system and the on-line detection technology in improving the productivity of granulation. Finally, some assumptions on technology development for solving the specific problems of personalized TCM granules were shared to provide some ideas for the application and development of personalized TCM granules in clinical practice.

Application,problems,and development strategies of personalized traditional Chinese medicine preparations / 中国中药杂志

With the continuous improvement of people's living standards and the greatly accelerated pace of life, patients' requirements for traditional Chinese medicine(TCM) pharmaceutical care are constantly raised, and personalized TCM preparations used are increasing year by year. However, a series of problems, such as the bottleneck of preparation technology, the lack of preparation specifications, and the weak legal basis for supervision, have become prominent, leading to the uneven product quality of personalized pre-parations. This paper systematically summarized and analyzed the current situation and existing problems of personalized TCM preparations, including dosage form application, preparation technology, production equipment, quality standard, clinical application, and administration mode. Additionally, it put forward an inheritance and innovation research mode of personalized TCM preparation technology based on the physical fingerprint of raw materials and innovation research and intellectual property protection mode of "research-patent-technology-equipment-standard". Furthermore, innovative development strategies were proposed, such as the production standard system of clinical preparations based on the whole process traceability and the regional processing service mode of clinical preparations based on industry 4.0. The present study is expected to provide beneficial references for the inheritance and innovation development of personalized TCM preparations.

Improving compactibility properties of Lonicera Japonica Flos by Plasdone S-630 / 药学学报

To improve the fluidity and compactibility properties of raw powders of traditional Chinese medicine by particle modification technology, Lonicera Japonica Flos was used as a model drug, fluidized bed bottom spray technology was used, and Plasdone S-630 was used as a modifier to prepare modified particles. The powder properties, tablet compactibility parameters, disintegration time and dissolution were measured. The surface morphology of the powder particles before and after modification and compressed tablets were characterized by combining with scanning electron microscopy technology. The results showed that the particle size of Lonicera Japonica powder has been increased after particle modification, the fluidity, compressibility and compactibility of the powder have been improved to some extent, the disintegration time has also been reduced, and the dissolution in vitro is not affected. Therefore, this study can provide reference and ideas for the common problem that raw powder of traditional Chinese medicine that cannot meet the needs of preparation production due to poor powder properties such as fluidity and compressibility.

Development status and research strategy of traditional Chinese medicine temporary prescription preparation technology / 中国中药杂志

Temporary prescription preparation is the preparation processed into different dosage forms by relevant pharmacist according to the temporary preparation requirement and the personalized prescription made by the doctor in accordance with the syndrome differentiation and drug performance.It is an important part in personalized pharmaceutical services.Rational design of process route,production equipment and quality control method for the temporary prescription preparation,and establishment of technology research strategy and mode in accordance with the characteristics of traditional Chinese medicine temporary prescription preparations play an important role in promoting the development of the temporary prescription preparations.To promote the normalization,standardization and intelligent development of temporary prescription preparations,we would comprehensively summarize the significance,policy,technology characteristics,technology research status quo and existing problems in this paper,and put forward the research direction of temporary prescription preparation technology based on the physical properties of raw materials,equipment research strategy,and intelligent manufacturing technology.Thus it will push the inheritance and innovation of temporary prescription preparation.

Bioadhesive pellets of astragalosides: preparation and adhesive evaluation based on the physical properties of wet mass / 药学学报

Bioadhesive preparation can be attached to specific sites to control drug release rate, increase drug concentration and increase efficacy, which is based on natural or synthetic polymer material. In this paper, based on the physical properties of wet mass, a method for screening adhesion formulation was proposed, which was different from conventional way of screening optimal formulation, and astragalosides loaded bioadhesive pellets were prepared by extrusion-spheronization method (extrusion speed 30 r·min-1, spheronization speed 808 r·min-1, spheronization time 7.5 min) based on this formulation screening method, small living animal imaging technology and mucin from porcine stomach model were used to evaluate the in vivo and invitro adhesiveness behaviour of the pellets. According to the relationship between the physical properties of wet mass and the formability and adhesiveness of bioadhesive pellets, five key physical properties hardness (Ha), adhesiveness (Ad), springiness (Sp), cohesiveness (Co), chewiness (Ch) were selected as the index of screening optimal formulation, therefore a comprehensive evaluation model was established, which based on principal component analysis, to did digital ranking for these proposed adhesion formulation, the optimal formulation was determined: microcrystalline cellulose: (chitosan∶Carbomer 940 = 2∶1), the adhesive material dosage accounted for 20% of the excipient dosage, and the ratio of drugs to excipients was 1 : 4. All animal experiments have been approved by Ethics Committee of Shanghai University of Traditional Chinese Medicine. The in vivo and in vitro adhesive evaluation results showed the pellets had a clear advantage in intestinal adhesion over normal pellets, its also proved the scientificity and reliability of the method of screening bioadhesive formulation.

Application Status of Properties of Surface and Interface in Research on Pharmaceutical Preparations / 中国实验方剂学杂志

The surface and interface,as the transition region between two phases,belongs to the category of physical chemistry.At present,it is widely used in materials and other scientific fields.Meanwhile,this property also plays an important role in pharmaceutical research.The interface layer involved in the progress of pharmaceutical preparations is connected with the two-phase or three-phase between gas,liquid and solid closely.The interface effect will affect the final shaping of pharmaceutical preparations and the dissolution and absorption of drugs in the human body.In this paper,the surface and interface characteristics(specific surface area,surfacial and interfacial tension and surface Gibbs free energy) were compared,and the application of interface phenomena(wetting,solubilization and emulsification) in pharmaceutical research were introduced.From the points of view of the progress control of pharmaceutical preparations and the effectiveness of their products,the article expounds the important role of properties of surface and interface in the field of pharmaceutical preparations.Therefore,it is necessary to pay attention to the properties of surface and interface,one of the key physical properties of drugs,and to apply them in the pharmaceutical research.

A new device for determination of adhesive force and its application in predicting hot-melt sticking in spray drying of traditional Chinese medicine / 中国中药杂志

A new device was designed to measure adhesive force and predict whether traditional Chinese medicine extracts would appear hot-melt sticking in spray drying process．Based on the physical property tester as fundamental test platform, the device was fixed with a camera, a temperature and humidity sensor probe and a set of equipment for hot air. This device could simulate the dry environment of spray dryer and analyze the variables of testing solutions' adhesiveness against drying time. To establish and validate a model of predicting hot-melt sticking in spray drying, data was collected by using data mining. The results of this study proved that the device could be used to predict the hot-melt sticking in spray drying based on the adhesive force of materials (testing solutions). In addition, the study also found that the adhesiveness of the hot-melt sticking materials gradually increased with the evaporation of water, while that of non-sticking materials first increased and then rapidly decreased.

Wetting agent dosage screening for traditional Chinese medicine pellet based on torque rheological property / 中国中药杂志

With lubricant and bonding effect simultaneously, wetting agent has direct effect on properties of wet mass and extrudate, thus affecting the forming quality of pellets in extrusion-spheronization process. In this research, 25 representative kinds of traditional Chinese medicine(TCM) were selected as model drugs and 20%, 30% and 40% drug loading were set with MCC as their balling agent. The torque rheological curves were measured to get parameters such as maximum torque (Tmax) and corresponding water addition (WTmax) for these 75 raw materials by a mixer torque rheometer (MTR).The results showed that among 75 representative raw materials, 74 ones could be obtained for spherical pellets under the water addition of WTmax-2. corresponding to the second largest torque in torque rheological curve, suggesting that MTR could be used to select the optimal wetting agent dosage of TCM pellets. So the tedious and expensive pre-production work could be considerably reduced when TCM pellets were prepared.

Discussion on research and development of new traditional Chinese medicine preparation process based on idea of QbD / 中国中药杂志

Traditional processes are mostly adopted in traditional Chinese medicine (TCM) preparation production and the quality of products is mostly controlled by terminal. Potential problems of the production in the process are unpredictable and is relied on experience in most cases. Therefore, it is hard to find the key points affecting the preparation process and quality control. A pattern of research and development of traditional Chinese medicine preparation process based on the idea of Quality by Design (QbD) was proposed after introducing the latest research achievement. Basic theories of micromeritics and rheology were used to characterize the physical property of TCM raw material. TCM preparation process was designed in a more scientific and rational way by studying the correlation among enhancing physical property of raw material, preparation process and product quality of preparation. So factors affecting the quality of TCM production would be found out and problems that might occur in the pilot process could be predicted. It would be a foundation for the R&D and production of TCM preparation as well as support for the "process control" of TCMIs gradually realized in the future.

Pharmaceutical research progress of rhynchophylla based on chemical stability / 中国中药杂志

Rhynchophylla is a Chinese herb commonly used in clinical practice. It's also the primary herb of some famous Chinese herbal compound such as Tianma Gouteng decoction, and Lingyang Gouteng decoction. According the record from many previous materia medica literatures, rhynchophylla should be added later during decoction. Pharmaceutical research showed that rhynchophylla alkaloids were not stable. Which has resulted in many problems in the research and its application. For example, there was not a quantitative determination method in "Chinese Pharmacopoeia" of past and present versions, which seriously impacted its quality control and product application. Firstly, records from previous materia medica literatures and "Chinese Pharmacopoeia" were systematically sorted based on the chemical stability of rhynchophylla. Secondly, pharmaceutical research including chemical compositions and their stability, pharmacological effects, extraction process and quality analysis, was reviewed after reference of literatures published at home and abroad in recent decades. Positive reference and evidence for further research and development of rhynchophylla will be provided in the article.

Discrimination of traditional Chinese medicinal materials with different tastes based on electronic tongue / 中国中药杂志

<p><b>OBJECTIVE</b>To investigate the use of the electronic tongue in the evaluation of traditional Chinese medicinal materials with sour, bitter, sweet or salty tastes, and assess the possible application of the sensor in the evaluation of different tastes of traditional Chinese medicinal materials.</p><p><b>METHOD</b>Aqueous extracts of 22 traditional Chinese medicinal materials were measured by the electronic tongue. The data collected with the tongue was evaluated for discrimination of the samples with multivariate statistical methods: principal component analysis (PCA) and discriminant factor analysis (DFA).</p><p><b>RESULT</b>The electronic tongue was capable of discriminating between samples with different taste modalities and could also distinguish different samples eliciting the same basic taste. Twenty-two traditional Chinese medicinal materials could be classified into five clusters based on PCA. These differences seem to derive from the different tastes. DFA was applied to construct a model to discriminate traditional Chinese medicinal materials with different tastes. And the samples yielded about 88.2% accuracy for cross-validation.</p><p><b>CONCLUSION</b>We confirmed that the electronic tongue may provide an analytical procedure for classification of the samples with respect to tastes of the traditional Chinese medicinal materials.</p>

Pharmaceutical study on multi-component traditional Chinese medicines / 中国中药杂志

Due to the limitation of science and technology in ancient times, traditional Chinese medicines (TCMs) could have prepared only in traditional dosage forms, such as pills, powders, ointments and pellets. Though studies on multi-component TCMs have become one of major development orientations of TCM, the druggability of their preparations has always been neglected. On the basis of two key difficulties--the integration of studies on multi-component TCMs and TCM theory as well as the evaluation on their druggability, the essay proposes methods and technologies that can be adopted in studies on multi-component TCM preparations, including the characteristic physicochemical property of multi-component TCMs and its correlation with forming process, the release-modified micro pill preparation technology based on prescription-symptom-dosage, and the evaluation technology on release of release-modified micro pill components based on mathematical set model.

Determination of rhynchophylline and isorhynchophylline in Uncaria rhynchophylla by HPLC / 中国中药杂志

<p><b>OBJECTIVE</b>To explore an HPLC method for determination of rhnchophylline and isorhnchophylline in Uncaria rhnchophylla.</p><p><b>METHOD</b>An HPLC method has been developed for determination of rhnchophylline and isorhnchophylline. The transformation of rhnchophylline and isorhnchophylline after heating was also studied by HPLC-ESI-MS.</p><p><b>RESULT</b>Good linearities of rhynchophylline and isorhynchophylline were 0.064-5.100, 0.064-5.110 mg, respectively. The average recoveries were from 87.51% to 88.83% for rhynchophylline and from 107.9% to 113.9% for isorhynchophylline. The recoveries of rhynchophylline and isorhnchophylline reference solutions after extraction were 12.60% and 40.00% in the reflux extraction procedure, respectively. While in the ultrasonic extraction procedure, the average recoveries of rhynchophylline and isorhynchophylline was from 99.48% to 103.2% and from 97.00% to 99.59%, resepectively. The recoveries of rhynchophylline and isorhnchophylline reference solutions after extraction were 47.08% and 51.03%, respectively. The unqualified recovery could be elucidated by HPLC-ESI-MS analysis, indicating that trhynchophylline could be transformed mostly into isorhynchophylline and a little amount of unkown composition, while isorhynchophylline could be transformed into rhynchophylline isocorynoxeine, corynoxeine and 22-O-beta-D-glucopyranosyl isocorynoxeinic acid during the extraction procedure.</p><p><b>CONCLUSION</b>Ultrasonic extraction procedure was more sutble for HPLC determination of the content of rhynchophylline and isorhynchophylline in U. rhnchophylla, however, the recovery problems should be paid attention to when it comes to the determination.</p>

Preparation of ferulic acid, senkyunolide I and senkyunolide H from Ligusticum chuanxiong by preparative HPLC / 中国中药杂志

Preparative HPLC was used to prepare ferulic acid, senkyunolide I and senkyunolide H from Ligusticum chuanxiong. The separation was conducted on a Shim-Pack Prep-ODS (20.0 mm x 250 mm, 5 microm) column with the mobile phase of methanol-0.2% glacial acetic acid (50:50)at the flow rate of 5 mL x min(-1). The detection wavelength was 278 nm, and the purity of each compound was detected by HPLC analysis. Spectral data analyses including UV, ESI-MS and NMR were used to identify their structures. This method is simple, fast, which is suitable for preparation of standard reference of ferulic acid, senkyunolide I and senkyunolide H from L. chuanxiong and can meet the requirement of new drug research and development.