Optimization of the preparation process of Soft-shelled turtle blood lyophilized powder using Box-Behnken response surface methodology / 中国药房

OBJECTIVE To optimize the preparation process of Soft-shelled turtle blood lyophilized powder （STBLP）， and to provide a reference for improving the availability and quality stability of soft-shelled turtle blood （STB）. METHODS STBLP was prepared with vacuum freeze-drying. Taking the solubility as the index， the preparation process parameters of STBLP were optimized by single factor experiment and Box-Behnken response surface method. RESULTS The optimal freeze-drying process for STBLP was obtained： pre-freezing time of 4 h， total drying time of 13 h （before at 0 ℃）， and resolution drying temperature of 25 ℃. The average solubility of 3 batches of STBLP prepared according to the optimal process was 95.72% （RSD＝0.68%， n＝3）， the relative error of which was －0.97% to the theoretical solubility （96.66%）. CONCLUSIONS Optimized lyophilization process in this study are stable and feasible， the solubility of the prepared sample is high.

Methodology for adaptive decision--making research on manufacturing process of traditional Chinese medicine based on deep reinforcement learning / 中国中药杂志

The manufacturing process of traditional Chinese medicine is subject to material fluctuation and other uncertain factors which usually cause non-optimal state and inconsistent product quality. Therefore, it is necessary to design and collect the quality-rela-ted physical parameters, process parameters, and equipment parameters in the whole manufacturing process of traditional Chinese medicine for digitization and modeling of the process. In this paper, a method for non-optimal state identification and self-recovering regulation was developed for active quality control in the manufacturing process of traditional Chinese medicine. Moreover, taking vacuum belt drying process as an example, a DQN algorithm-based intelligent decision model was established and verified and the implementation process was also discussed and studied. Thus, the process parameters-based self-optimization strategy discovery and path planning of optimal process control were rea-lized in this study. The results showed that the deep reinforcement learning-based artificial intelligence technology was helpful to improve the product quality consistency, reduce production cost, and increase benefit.

Processing Magnoliae Officinalis Cortex with ginger juice: process optimization based on AHP-CRITIC weighting method and composition changes after processing / 中国中药杂志

The weight coefficients of appearance traits, extract yield of standard decoction, and total content of honokiol and magnolol were determined by analytic hierarchy process(AHP), criteria importance though intercrieria correlation(CRITIC), and AHP-CRITIC weighting method, and the comprehensive scores were calculated. The effects of ginger juice dosage, moistening time, proces-sing temperature, and processing time on the quality of Magnoliae Officinalis Cortex(MOC) were investigated, and Box-Behnken design was employed to optimize the process parameters. To reveal the processing mechanism, MOC, ginger juice-processed Magnoliae Officinalis Cortex(GMOC), and water-processed Magnoliae Officinalis Cortex(WMOC) were compared. The results showed that the weight coefficients of the appearance traits, extract yield of standard decoction, and total content of honokiol and magnolol determined by AHP-CRITIC weighting method were 0.134, 0.287, and 0.579, respectively. The optimal processing parameters of GMOC were ginger juice dosage of 8%, moistening time of 120 min, and processing at 100 ℃ for 7 min. The content of syringoside and magnolflorine in MOC decreased after processing, and the content of honokiol and magnolol followed the trend of GMOC>MOC>WMOC, which suggested that the change in clinical efficacy of MOC after processing was associated with the changes of chemical composition. The optimized processing technology is stable and feasible and provides references for the modern production and processing of MOC.

Binder jet 3D printing composite bilayer tablet of extended-release printing technology in the study / 药学学报

Based on the dual needs of analgesia and anti-inflammation in trauma treatment, this study uses acetaminophen and moxifloxacin hydrochloride as active pharmaceutical ingredients and develops a composite bilayer tablet with a dual-phase drug release system by using binder jet 3D printing technology. Due to the complexity of the 3D printing process, there is an interaction between the various parameters. Through the optimization of the process, the relationship between the key process parameters can be determined more intuitively. In this study, the process of extended-release tablets was optimized to maintain the mechanical properties of the tablets while realizing the regulation of release. The full-factor experimental design of three central points 23 was used to analyze the factors that significantly affect the quality attributes of extended-release tablets and the interaction between factors. The optimal extended-release process parameters were obtained by the response optimizer: the inkjet quantity of the printing ink was 10 (about 13.8 pL), the powder thickness was 180 μm, and the running speed was 360 mm·s-1. The in vitro of release of 3D printed composite bilayer tablets showed that the in vitro of release of 3D printed tablets and commercially available tablets conformed to the Ritger-Peppas release model. The results of porosity showed that the immediate-release layer of the preparation has many pores and large pore size, and the dissolution of the immediate release layer within 15 min was greater than 85%. The internal pore size of the extended release layer is large, but it can still release slowly for up to 8 h, the mechanism may be related to the extended release of HPMC gelation. On the basis of verifying the rationality of the design goal of 3D printed composite bilayer tablets, this study also provides a theoretical basis for the preparation of 3D printing complex preparations.

Stability of human immunoglobulin(pH 4) for intravenous injection after process optimization / 中国生物制品学杂志

@#Objective To evaluate the stability of human immunoglobulin(pH 4)for intravenous injection(IGIV)after process optimization.Methods A filter plate and B filter membrane were used to filter the protein components in different separation stages to reduce the residue of immunoglobulin A(IgA)in the product in multi-batch large-scale production. The finished product was examined for the physical properties(appearance,visible foreign body,insoluble particle examination and thermal stability test)and the chemical properties[protein content,purity,molecular size distribution,titers of antiHBs,diphtheria antibody,prokallikrein activator(PKA),anti-complement activity(ACA),anti-A and anti-B hemagglutinin,and IgA residue]. The accelerated and long-term stability tests were performed.Results There was no significant difference in the key quality indicators between IGIV batches produced by the optimized process and the normal process,while the IgA residue decreased significantly(t = 3. 992 and 11. 215 respectively,each P < 0. 05). In the accelerated stability and long-term stability tests,all the test results of IGIV after process optimization were qualified,which met the relevant regulations in the third part of Chinese Pharmacopoeia(2020 edition).Conclusion IGIV after process optimization can effectively reduce IgA residue with good stability,which is of great significance for blood product manufacturers to improve the quality of IGIV products.

Construction of a mathematical model based on a genetic algorithm for an aptitude program in high school student optimization / Construção de modelo matemático baseado no algoritmo genético para otimização de um programa de aptidão em estudantes do ensino medio / Construcción de un modelo matemático basado en un algoritmo genético para la optimización de un programa de aptitudes en estudiantes de secundaria

ABSTRACT Introduction: The genetic algorithm is one of the essential theoretical mathematical models for simulating biological development. It is widely used in many fields such as engineering, medicine, and economics. Objective: Use the genetic algorithm as a mathematical model basis for optimization in the high school students' aptitude program. Methods: The selection method by competition is adopted to elect the random crossover of male crossover probability with high similarity to generate a new population. A genetic algorithm was proposed to adjust the crossover probability and dynamic mutation according to fitness, aiming to solve the problem of dynamic changes. A comparative analysis is performed between the nonlinear differential equations and the Levenberg-Marquardt method algorithm. Results: The algorithm improvement was obtained after analyzing the operation process and structuring of the traditional genetic algorithm; the mathematical model application revealed improvement in the motion accuracy model established by the genetic algorithm. Conclusion: The physical enhancement optimization scheme was tested and verified by a genetic algorithm and proves the research results hold theoretical feasibility. Evidence Level II; Therapeutic Studies - Investigating the results.

RESUMO Introdução: O algoritmo genético é um dos mais importantes modelos matemáticos teóricos para simulação de desenvolvimento biológico. É amplamente utilizado em muitos campos, tais como engenharia, medicina e economia. Objetivo: Utilizar o algoritmo genético como base de um modelo matemático para otimização no programa de aptidão nos estudantes do ensino médio. Método: Adota-se o método de seleção por competição para eleger o cruzamento aleatório da probabilidade de crossover masculino com grande semelhança para gerar uma nova população. Um algoritmo genético foi proposto para ajustar a probabilidade de crossover e mutação dinâmica de acordo com a aptidão física, visando resolver o problema das alterações dinâmicas. Efetua-se uma análise comparativa entre os resultados das equações diferenciais não-lineares e o algoritmo de Levenberg-Marquardt de quarta ordem. Resultados: O aperfeiçoamento do algoritmo foi obtido após a análise do processo de operação e estruturação do algoritmo genético tradicional, a aplicação do modelo matemático revelou melhora na precisão do modelo de movimento estabelecido pelo algoritmo genético. Conclusão: O esquema de otimização do aprimoramento físico foi testado e verificado por um algoritmo genético provando que os resultados da pesquisa possuem praticabilidade teórica.Nível de evidência II; Estudos Terapêuticos - Investigação de Resultados.

RESUMEN Introducción: El algoritmo genético es uno de los modelos matemáticos teóricos más importantes para la simulación del desarrollo biológico. Se utiliza ampliamente en muchos campos como la ingeniería, la medicina y la economía. Objetivo: Utilizar el algoritmo genético como base de un modelo matemático de optimización en el programa de aptitud para estudiantes de secundaria. Método: Se adopta el método de selección por competencia para elegir el cruce aleatorio de probabilidad de crossover masculino con alta similitud para generar una nueva población. Se propuso un algoritmo genético para ajustar la probabilidad de cruce y la mutación dinámica en función de la aptitud, con el fin de resolver el problema de los cambios dinámicos. Se realiza un análisis comparativo entre los resultados de las ecuaciones diferenciales no lineales y el algoritmo de Levenberg-Marquardt de cuarto orden. Resultados: La mejora del algoritmo se obtuvo tras el análisis del proceso de funcionamiento y estructuración del algoritmo genético tradicional, la aplicación del modelo matemático reveló la mejora de la precisión del modelo de movimiento establecido por el algoritmo genético. Conclusión: El esquema de optimización de la mejora física se probó y verificó mediante un algoritmo genético, demostrando que los resultados de la investigación tienen viabilidad teórica. Nivel de evidencia II; Estudios terapéuticos - Investigación de resultados.

Same-day discharge percutaneous coronary intervention. Where are we? / Intervenção coronária percutânea com alta no mesmo dia. Onde estamos?

With the evolution of percutaneous coronary intervention techniques and their greater safety, the use of radial access, the greater need to optimize resources in health management and the greater demand from patients for an agile service to solve their problems, the discharge on the same day after percutaneous coronary interventions have been gaining ground in the global scenario as a feasible strategy. The objective of this article was to demonstrate that there is already a scientific basis for this, which extends from the financial aspect, and the patient's experience, to the technical details related to the safety of the strategy. A structured protocol based on evidence and on the most recent recommendations from two major medical societies is also proposed. Selecting patients well, training the multidisciplinary team and educating the patient are fundamental parts for the success of the strategy.

Com a evolução das técnicas de intervenção coronária percutânea e sua maior segurança, o uso do acesso radial, a maior necessidade de otimização dos recursos na gestão em saúde e a maior cobrança por parte dos pacientes por um serviço ágil para resolução de seus problemas, a alta no mesmo dia após as intervenções coronárias percutâneas vem ganhando espaço no cenário global como uma estratégia factível. O objetivo deste artigo foi demonstrar que já há base científica para o assunto, a qual se estende desde a aspectos financeiros, à experiência do paciente até à questão técnica relacionada à segurança da estratégia. Propõe-se, ainda, um protocolo estruturado baseado em evidências e nas recomendações mais recentes de duas grandes sociedades médicas. Selecionar bem os pacientes, treinar a equipe multiprofissional e educar o paciente são partes fundamentais para o sucesso da estratégia.

Preparation of curcumin nanocrystalline injection and evaluation of its in vivo and in vitro properties / 中国药科大学学报

@#In this study, the formulation and preparation process of curcumin nanocrystalline injection were optimized to improve curcumin dissolution rate and bioavailability in vivo.Media grinding method was used to prepare curcumin nanocrystals, and the particle size was used as the evaluation index.The Box-Behnken experimental design was used to optimize its formulation and preparation process, and to characterize its physical and chemical properties.In addition, the dissolution of nanocrystal with different particle sizes was investigated by the paddle method, and the pharmacokinetics in rats were studied.The experimental results showed that the optimal formula and process were obtained through Box-Behnken experimental design, and that uniform curcumin nanocrystals with an average particle size of 223.1 nm were obtained.The results of X-ray diffraction and differential scanning calorimetry analysis showed that the crystal form was stable during the preparation of nanocrystals. In vitro dissolution experiments with different particle sizes showed that the dissolution rate and the degree of dissolution would increase if the particle size was smaller.Pharmacokinetic studies in rats showed that cmax and AUC0-∞ of curcumin nanocrystal injection were 4.9 and 4.1 times that of curcumin raw materials, respectively.In summary, the curcumin nanocrystal injection developed in this research have a stable preparation process and can significantly improve the dissolution rate and bioavailability of the drug, which provides some ideas for the research on curcumin preparation.

Production of fatty acids by engineered Ogataea polymorpha / 生物工程学报

Fatty acids (FA) are widely used as feed stocks for the production of cosmetics, personal hygiene products, lubricants and biofuels. Ogataea polymorpha is considered as an ideal chassis for bio-manufacturing, due to its outstanding characteristics such as methylotroph, thermal-tolerance and wide substrate spectrum. In this study, we harnessed O. polymorpha for overproduction of fatty acids by engineering its fatty acid metabolism and optimizing the fermentation process. The engineered strain produced 1.86 g/L FAs under the optimized shake-flask conditions (37℃, pH 6.4, a C/N ratio of 120 and an OD600 of seed culture of 6-8). The fed-batch fermentation process was further optimized by using a dissolved oxygen (DO) control strategy. The C/N ratio of initial medium was 17.5, and the glucose medium with a C/N ratio of 120 was fed when the DO was higher than 30%. This operation resulted in a titer of 18.0 g/L FA, indicating the potential of using O. polymorpha as an efficient cell factory for the production of FA.

Practice of digital reform to optimize the decision-making mechanism of major issues in hospitals / 中华医院管理杂志

Digital reform serves as powerful driver for high-quality development of hospitals. Taking the problems existing in the decision-making mechanism of major issues as a breakthrough, a tertiary hospital used digital thinking to optimize the decision-making mechanism. The hospital took such means as optimizing the rules of procedure, strengthening the pre-decision assessment, clarifying the principle of " two initiatives" , improving the " No.1 issue" system, strengthening the linkage between the Party committee and meeting the president′s office meeting, and standardizing the supervision and implementation. By such means, the hospital successfully built a smart, efficient, coordinated, and closed-loop operation and management system, desirably strengthening the leadership and core role of the Party committee, enhancing the president′s overall management of business work, as well as improving the decision completion rate and feedback rate.

Preparation and process optimization of microbial organic copper as a feed additive / Preparação e otimização do processo de cobre orgânico microbiano como aditivo alimentar

As an essential trace element for animals, copper significantly contributes to the growth and health of animals. Compared to inorganic trace elements, organic trace elements are better supplements; notably, they are acquired through microbial transformation. Therefore, we screened for copper-enriched microorganisms from high copper content soil to obtain organic copper. Sodium diethyldithio carbamate trihydrate was applied as a chromogenic agent for determining micro amounts of intracellular copper through spectrophotometry. In total, 50 fungi were isolated after the successful application of the screening platform for copper-rich microbes. Following morphological and molecular biology analyses, the N-2 strain, identified as Aspergillus niger sp. demonstrated showed better copper enrichment potential than others. Notably, the strain tolerance to copper was nearly thrice that of Saccharomyces cerevisiae, up to 1600mg/L. The content of the organic bound copper was 22.84mg Cu/g dry cell. Using the Central Composite Design (CCD) response surface method, we optimized the fermentation condition (inoculation amount, 13%; temperature, 28(C; pH, 5.0). Compared to the original strain results under the single factor fermentation condition, we reported an increase by 24.18% under the optimized conditions. Collectively, these findings provide a reference for uncovering new and low-cost organic copper additives.(AU)

Como elemento traço essencial para os animais, o cobre contribui significativamente para o crescimento e saúde dos animais. Comparado aos oligoelementos inorgânicos, os oligoelementos orgânicos são melhores suplementos; notavelmente, eles são adquiridos através de transformação microbiana. Portanto, nós selecionamos microorganismos enriquecidos com cobre de solos com alto teor de cobre para obter cobre orgânico. O carbamato de sódio diethyldithio trihidratado foi aplicado como agente cromogênico para a determinação de micro quantidades de cobre intracelular através da espectrofotometria. No total, 50 fungos foram isolados após a aplicação bem sucedida da plataforma de triagem para micróbios ricos em cobre. Após análises morfológicas e de biologia molecular, a cepa N-2, identificada como Aspergillus niger sp. demonstrou um melhor potencial de enriquecimento de cobre do que outras. Notavelmente, a tolerância da estirpe ao cobre foi quase três vezes maior que a da Saccharomyces cerevisiae, até 1600mg/L. O conteúdo de cobre ligado orgânico era de 22,84mg Cu/g de célula seca. Usando o método de superfície de resposta Central Composite Design (CCD), nós otimizamos a condição de fermentação (quantidade de inoculação, 13%; temperatura, 28C; pH, 5,0). Em comparação com os resultados da deformação original sob a condição de fermentação de fator único, relatamos um aumento de 24,18% sob as condições otimizadas. Coletivamente, estas descobertas fornecem uma referência para descobrir novos aditivos de cobre orgânico de baixo custo.(AU)

Módulo Cartas Avales para el Sistema Informático Colpadi de la Unidad Central de Cooperación Médica. Cuba / Module Letters Guarantees for the Colpadi Computer System of the Central Unit for Medical Cooperation. Cuba

La Unidad Central de Cooperación Médica (UCCM) es un centro de excelencia del Ministerio de Salud Pública (MINSAP). Este centro se encarga de garantizar el cumplimiento de los compromisos internacionales contraídos por el MINSAP y el Gobierno de la República de Cuba, en el área de la cooperación médica a través de la asistencia técnica y docente. El objetivo de este desarrollo es implementar un módulo para el Sistema Integral para la Gestión de Información en la Colaboración Médica Cubana (Colpadi), que optimice el proceso de gestión de cartas avales que se generan en la UCCM. El trabajo que se desarrolla contribuye de forma positiva al concepto de excelencia de la institución. El proyecto tiene un enfoque cualitativo, con alcance descriptivo, de tipo retrospectivo y diseño no experimental, de corte transversal. Se emplean los métodos científicos de observación y análisis documental. Además, la implementación utilizando el Lenguaje Unificado de Modelado (UML) y la metodología RUP de desarrollo de software. Como resultado se obtiene un módulo, como parte del sistema informático Colpadi, que optimiza el proceso de gestión de cartas avales. Las cartas avales se entregan a los cooperantes internacionalistas del MINSAP en sus vacaciones y al finalizar su misión en el exterior. Con la implementación de la aplicación informática se obtienen varias ventajas como la automatización de los vuelos de entrada, las solicitudes automáticas para el procesamiento de las cartas avales, los reportes estadísticos y el tratamiento de la información(AU)

Central Unit for Medical Cooperation (UCCM) is a center of excellence of the Ministry of Public Health (MINSAP). This center is in charge for guaranteeing compliance with the international commitments made by MINSAP and the Government of the Republic of Cuba, in the area of ​​medical cooperation through technical and educational assistance. This research contributes positively to the institution's concept of excellence. Its objective is to implement a module for the Colpadi computer system, which it optimizes the process for managing the guarantee letters generated at the UCCM. The research has a qualitative approach, with a descriptive scope, of a retrospective type and a non-experimental, cross-sectional design. Scientific observation and documentary analysis methods are used; as well as UML, and RUP software development methodology in its implementation. As a result, a module is obtained, as part of the Colpadi computer system, which it optimizes the guarantee letter management process. The letters of guarantee are delivered to the internationalist aid workers of the MINSAP, on their vacations and at the end of their mission abroad. With the implementation of the computer application, several advantages are obtained, such as the automation of the incoming flights, the automatic requests for the processing of the letters of guarantee, the statistical reports and the treatment of the information(AU)

Optimization of emergency management practice for emergent infectious diseases / 中华医院管理杂志

The study analyzed the application of failure mode and effect analysis(FMEA)in the emergency management of emergent infectious diseases. In February 2020, optimization of emergency management procedures for emergent infectious diseases was identified as the research theme. Subsequently, FMEA was applied to study the emergency management process of emergent infectious diseases and analyze corresponding potential failure modes in an infectious disease hospital. The appraisal identified four prioritized risk exposures to correct, including non-standardized personnel protection, delayed personnel arrival, unqualified specimens and inadequate ward preparation. Accordingly pertinent countermeasures were formulated. Three months after measures were taken, the risk priority numbers of the above four risks were decreased significantly. On the other hand, evident increase was found in the on-duty rate of emergency personnel, the rate of standard protection, the qualification rate of sample collection and disposal, as well as the serviceability rate of respirators, ECG monitors and protective equipment in emergency wards. The application of FMEA is conducive to optimizing the emergency response process of emergent infectious diseases, and to upgrading emergency management at large.

Optimization of polysaccharide extraction from Hippocampus by deep neural network and Box-Behnken design-response surface methodology / 中国中药杂志

In this paper, the extraction rate of crude polysaccharides and the yield of polysaccharides from Hippocampus served as test indicators. The comprehensive evaluation indicators were assigned by the R language combined with the entropy weight method. The Box-Behnken design-response surface methodology(BBD-RSM) and the deep neural network(DNN) were employed to screen the optimal parameters for the polysaccharide extraction from Hippocampus. These two modeling methods were compared and verified experimentally for the process optimization. This study provides a reference for the industrialization of effective component extraction from Chinese medicinals and achieves the effective combination of modern technology and traditional Chinese medicine.

Parameters optimization in Heparin affinity chromatography purification of human coagulation factor Ⅸ / 中国输血杂志

【Objective】 To optimize the purification conditions of heparin affinity chromatography in the purification of human coagulation factor Ⅸ by response surface method and establish the optimal chromatography process parameters. 【Methods】 The effect of sample loading temperature on purification efficiency was analyzed through single factor test. Three-factor three-level response surface method was used to optimize the chromatographic elution conditions. The Folin phenol method and the automatic hemagglutination analyzer were used to determine the total protein content and human coagulation factor Ⅸ titer, respectively. The purification effect was evaluated by activity index and process recovery rate. 【Results】 The optimized optimal chromatographic conditions were loading at 5 ℃, washing 4 CV, eluent formulation of sodium citrate 20 mmol/L, arginine hydrochloride 18.7 mmol/L, NaCl 611.6 mmol/L and pH 7.5; under this optimal setting, the recovery rate of the chromatographic process was (46.6±2.9) %, titer of factor Ⅸ rated to (68.4±4.7) IU/mL and specific activity was (62.8±3.3) IU/mg. 【Conclusion】 The optimized parameters of heparin affinity chromatography process by response surface method can produce better purification effect on human coagulation factor Ⅸ.

Emprego do cloreto de polialumínio em estudos de tratabilidade de água de abastecimento via coagulação, floculação e sedimentação / Use of polyaluminium chloride in studies of water supply treatability through coagulation, flocculation, and sedimentation

RESUMO Cloreto de polialumínio (PAC) é um coagulante polimérico inorgânico pré-hidrolisado que tem se destacado no tratamento de água de abastecimento e residuária por formar um precipitado de Al(OH)3* rígido e pesado, além de ter baixo efeito no pH. A literatura, porém, ainda é escassa na correlação da química e da física do coagulante com otimizações de processo. Nesse sentido, o objetivo deste trabalho foi empregar o PAC em estudos de tratabilidade de água de abastecimento via coagulação, floculação e sedimentação. Para isso, inicialmente foi feito um modelamento matemático para ajuste de turbidez e pH e construídos diagramas de coagulação de turbidez e de cor aparente remanescentes com pH de 4,0 a 9,0 e dosagem de 10 a 120 mg.L-1 de PAC (0,6 a 6,9 mg.L-1 de Al3+). Também foram estudados diferentes gradientes de velocidade e tempos de mistura para a coagulação e a floculação. Os diagramas de coagulação apresentaram resultados satisfatórios na faixa de pH entre 7 e 9 com dosagem superior a 30 mg.L-1 de PAC (1,7 mg.L-1 de Al3+), e está relacionado com a solubilidade mínima do Al(OH)3*. Otimizações da coagulação e da floculação obtiveram melhora de até 79% da turbidez remanescente, redução de até 83% da área do sedimentador ou redução de até 67% na dosagem de PAC, em razão de um aumento do tamanho do floco produzido. Um conhecimento aprofundado da química e da física do processo relacionado ao uso do PAC pode, portanto, trazer benefícios ao seu uso.

ABSTRACT Polyaluminium chloride (PAC) is a pre-hydrolyzed inorganic polymeric coagulant that is being used widely in the treatment of water supply and wastewater by forming a hard and heavy Al(OH)3* precipitate, in addition to having a smaller effect on pH. The literature, however, is still scarce in correlating the chemistry and physics of the coagulant with process optimizations. The objective of this paper is to use PAC in studies of water supply treatability through coagulation, flocculation, and sedimentation. For this purpose, a mathematical modeling was initially performed to adjust turbidity and pH, and then remaining turbidity and apparent color coagulation diagrams were constructed with a pH of 4.0 to 9.0 and a dosage of 10 to 120 mg.L-1 of PAC (0.6 to 6.9 mg.L-1 of Al3+). Different gradients of velocity and mixing times for coagulation and flocculation were also studied. The coagulation diagrams indicated satisfactory results in the pH range between 7 and 9 with a dosage higher than 30 mg.L-1 of PAC (1.7 mg.L-1 of Al3+), and it is related to the minimum solubility of Al(OH)3*. Coagulation and flocculation optimizations achieved an improvement of up to 79% in the remaining turbidity, a reduction of up to 83% in the settler area or a reduction of up to 67% in PAC dosage, due to an increase in the size of the floc produced. An in-depth knowledge of the chemistry and physics of the process related to the use of PAC can, therefore, bring benefits to its use.

Optimization of infiltration process of Astragali Radix based on HPLC-DAD- ELSD and response surface design / 中草药

Objective: To optimize the infiltration process of Astragalus (Astragalus membranaceus var. mongholicus) medicinal materials by Box-Behnken response surface method. Methods: Based on the HPLC-DAD-ELSD and response surface design method, the qualified rate of decoction pieces, the content of index components and bending inspection were used as comprehensive inspection indicators, and the three factors of infiltration were selected for response surface experimental design to optimize the infiltration process of Astragalus medicinal materials parameter. Results: The best infiltration process was as following: infiltration temperature was 20 ℃, with water addition of 1:0.988 for 6 h. Under this process, the qualified rate of Astragalus pieces was 95.81%, the content of calycosin-7-glucoside was 0.072%, and the content of astragaloside IV was 0.276 %. Combining fingerprint analysis and heat map analysis, the material basis of A. membranaceus var. mongholicus changed during the infiltration process. The infiltration parameters should be strictly controlled during the infiltration process to ensure uniform quality of the pieces. Conclusion: The optimized Astragalus medicinal material infiltration process is stable and feasible with good reproducibility, which can provide a reference for the mass production process development of Astragalus medicinal slices.

Synthesis and synthetic process optimization of the enterovirus 71 3C protease inhibitor NK-1.8k / 国际药学研究杂志

Objective: To synthesize the enterovirus 71 3C protease inhibitor NK-1.8k and optimize the synthetic process. Methods: With N-Boc-L-glutamic acid dimethyl ester as the starting material, the target compound NK-1.8k was synthesized via the substitution, reductive amination, deprotection, amide condensation, hydrolysis, and reduction reactions. Compared with the original synthetic route, the tandem string type in the important intermediate 5 synthesis was changed to parallel type, thereby the total synthetic reactions were condensed from seven steps to six steps, and some post-processing methods were also optimized. Results: The structures of intermediates and the target compound were confirmed by MS and 1H NMR data, and the total yield of the target compound synthesis was increased to 13.3% from 10.7% of the original route. Conclusion: The synthetic route established in this article for NK-1.8k is reasonable and feasible, the raw materials used are cheap and easily available, the operation is simple, most of the reaction conditions are mild and controllable, the post-processing is simple, the intermediates are easy to separate and purify, the steps are short, and the yield is high. This method provides a valuable reference for the further synthesis of NK-1.8k and similar products.

Synthesis and syntehtic process optimization of mTOR protein inhibitor Torin2 / 国际药学研究杂志

Objective: To synthesize the mammalian target of sirolimus(mTOR)inhibitor Torin2 and optimize the synthetic process. Methods: Starting from p-bromoaniline, the target product was obtained through amino bonding, cyclization, chlorination, bonding with 3-aminotoluene ring, oxidation, cyclization and Suzuki reaction. The synthetic conditions for the key intermediates 3 and 8 as well as the final product Torin2 were optimized by the orthogonal experiment. Results and Conclusion: The structures of the intermediates and the target compound were confirmed by MS and 1H NMR data. The total yield of the target compound synthesis increased from 3% to 18%, and no column chromatography was required for the target compound separation and purification, which thus makes it suitable for industrial production.

Synthesis and synthetic process optimization of a specific dipeptidyl peptidase-Ⅳinhibitor vildagliptin / 国际药学研究杂志

Objective: To investigate and optimize the synthetic process of specific dipeptidyl peptidase-Ⅳ(DPP-Ⅳ)inhibitor vitagliptin. Methods: The aimed synthetic route was conceived by the literature survey according to the advantages and disadvantages of the reported synthetic routes. The key process parameters were determined by the orthogonal test or single factor test for the main intermediates in the speed limiting step. Results: The structures of intermediates and target compound were confirmed by MS and 1H NMR data. The overall yield of the target compound was 38.5%. Conclusion: The synthetic process has the advantages of lower cost, simple operation and mild reaction condition, and the yield has been improved by optimizing the crystallization solvent, which should be more suitable for industrial production.