VacciPharma 2020. V International Congress on Pharmacology of Vaccines

Dear colleagues: The Organizing Committee of the V International Congress on Pharmacology of Vaccines (VacciPharma 2020) organized by the Cuban Society of Pharmacology, BioCubaFarma and the International Union of Basic and Clinical Pharmacology (IUPHAR) would like to invite you to participate in this important event, scheduled for June 14 to 18, 2020 at the Convention Centre of the Melia Marina Varadero Hotel, Varadero Beach, Matanzas, Cuba. The Congress will be formed by different workshops and symposia such as: Meningococcal and Gonococcal vaccines Pneumococcal vaccines Pertussis and combined vaccines Enteric vaccines Leptospira vaccines Viral vaccines Animal models in vaccine development, QC and 3Rs Vaccine technology and bioprocess Vaccine technology transfers Patent, business and international cooperation VacciPharma 2020 is sponsored by: Cuban Society of Pharmacology (SCF) International Union of Basic and Clinical Pharmacology (IUPHAR) Latin-American Association of Pharmacology (ALF) PAHO / WHO BioCubaFarma National research centers: Finlay Vaccine Institute (IFV); Center of Genetic Engineering and Biotechnology (CIGB); Center of Molecular Immunology (CIM); Center for Control of Drugs, Equipment and Medical Devices (CECMED); National Center for Animal and Plant Health (CENSA); Tropical Medicine Institute Pedro Kourí (IPK); National Center for Biopreparations (BioCEN); Center for Drug Research and Development (CIDEM); Center for Clinical Trials (CENCEC); among others International Manufacturers and Companies The key objectives of the Congress are: To provide a progressive state-of-the-art report for scientists, manufacturers, governmental authorities and healthcare workers, who need to be updated about the latest scientific developments for human vaccines, including basic science, product development, market introduction, immunization programs and epidemiological surveillance. To promote the scientific collaboration among experts and institutions through the experience exchange, the presentation of results and the discussion on the conference topics. To accelerate progress in the development of vaccines and the acceptance and introduction of new methods and technologies. Opening lectures, oral presentations and posters will provide you the opportunity to be involved in a high quality congress to discuss about the progress in the field of vaccinology and pharmacology sciences. Deadline for registration and abstract submission: April 15th, 2020 Further information can be found at the VacciPharma 2020 Website: www.immunovaccipharma.com

Non-clinical study of the anxiolytic effect of Citrus aurantium L. essential oil in an inclusion complex with 2-hydroxypropyl-ß-cyclodextrin

Anxiety in the world population has increased significantly; the problem has encouraged studies regarding innovative alternatives for treatment. Research with Citrus aurantium L. essential oil (CEO) has revealed positive results with anxiolytic effects in both animals and humans. However, certain limitations affect its storage and preservation, its efficiency in therapy, and determination of adequate posologies. The potential use of cyclodextrins as drug carriers has been successfully explored. This study aims to assess the anxiolytic potential of a CEO/2-hydroxypropyl-ß-cyclodextrin (HP-ß-CD) inclusion complex. Preparation of the inclusion complex was performed using the Alpha 1-2 LDplus lyophilizer. To allow formation, and avoid loss of volatiles to the atmosphere, Limonene (LIM), the main compound in CEO, together with HP-ß-CD in a molar ratio of (1: 1M) was dispersed in ethanol for 36 hours using a laboratory shaker at room temperature (25°C). Non-clinical murine pharmacological tests were performed for anxiety assessment in experimental and control groups. To assess anxiety and motor impairment, the animals were evaluated using the elevated plus maze, open field, and rota-rod tests. Satisfactory results of the anxiolytic effect of the OEC complexed in HP-ß-CD were observed, with the indication of an potentiation of the effect with doses lower than 500 mg/kg and 250 mg/kg complexed, suggesting improvement in the anxiolytic properties of the OEC.

Intelligent and lean manufacturing for Chinese medicine:theory and its applications / 中国中药杂志

To cope with the " six major scientific problems" and the " five major technical challenges" of intelligent manufacturing and lean production of Chinese medicine( CM),we systematically proposed strategies,methods and the engineering theory of intelligent and lean manufacturing for CM by integrating the holistic view of traditional Chinese medicine and the concepts inspired from international advanced pharmaceutical technology. Moreover,the translational research of the theory and methods was successfully applied to six CMs such as Xuesaitong Injection. Several intelligent production lines were designed and built on the basis of the theory and methods,which greatly accelerated the digitalization,networking,and intelligence manufacture for CM. As a conclusion,the theory and applications provide technical demonstration for technical upgrading and high-quality development of CM industry.

Research in technology of preparation and the stability in polysaccharide of aloe / 国际中医中药杂志

Objective To compare the contents in polysaccharide of aloe in gel of aloe with preparation in different processing methods on fresh aloe of outer cuticle and investigate their stability. It could provide technology of preparation of polysaccharide of aloe.Methods The aloe gel had been prepared through the fresh juicing method, and alcohol sinking was applied to abstract polysaccharides of aloe in proportion of sixty, seventy, eighty and ninety percent. The colorimetric method of anthracenone - thick sulfuric acid had been taken to determine contents of polysaccharide in different proportions by alcohol sinking. The contents of polysaccharide were compared among different processing methods in fresh aloe of outer cuticle, and then the stability on condition of different temperatures, pH and the reagent of reductant-oxidant with polysaccharides of aloe were investigated. Results The content abstracted from polysaccharide of aloe was the higher when the proportion was eighty percent and its character of powder was better. And content abstracted from polysaccharide of aloe with the outer cuticle was higher than that out of the outer cuticle. The powders from the polysaccharide of aloe with the outer cuticle were gray-green, gray-brown or gray-white. The powders from polysaccharide of aloe without the outer cuticle were partial-white, more well-distributed and delicate. The stability in polysaccharide of aloe was better with the condition of low temperature, reducing agent and the solution with pH from five to seven, while the stability was lower when in high temperature, oxidizing agent and the solution with strong acid and strong alkali. Conclusions The proportion of eighty percent with alcohol sinking, decorticating the outer cuticle of fresh aloe has the higher content and the better character in the polysaccharide of aloe.

Study on purification, concentration and drying technic of Fushubao gel / 国际中医中药杂志

Objective To study the purification, concentration and drying technology of Fushubao gel. Methods The purification technology of Fushubao gel was optimizing by the total retention rate of Rhein, emodin, physcion and purity of content. The concentration, drying technology of Fushubao gel was optimized by the transfering rate of Rhein, emodin, physcion and Berberine hydrochloride. Results Best refining technology included in the condition of the water extract of 0.2 g/ml at 70 ℃, the ZTC1+1-II clarifying agent B 0.6 ml/g was mixed10 min in a 70 ℃ water bath thermal insulation 30 min; And then agent A 0.3 ml/g was added and mixed 10 min in a 70 water bath thermal insulation 30 min; after 12 h, filter it. Best thickening, drying technology was in the vacuum for -0.08~-0.09 MPa, a temperature of 60 ℃, the pressure was reduced to concentrate its relative density about 1.05 and concentrated liquid spray was dryed. Conclusions The purification, concentration and drying technology of Fushubao gel is reasonable, and can be used in the production.

Chinese medicine industry 4.0：advancing digital pharmaceutical manufacture toward intelligent pharmaceutical manufacture / 中国中药杂志

A perspective analysis on the technological innovation in pharmaceutical engineering of Chinese medicine unveils a vision on "Future Factory" of Chinese medicine industry in mind. The strategy as well as the technical roadmap of "Chinese medicine industry 4.0" is proposed, with the projection of related core technology system. It is clarified that the technical development path of Chinese medicine industry from digital manufacture to intelligent manufacture. On the basis of precisely defining technical terms such as process control, on-line detection and process quality monitoring for Chinese medicine manufacture, the technical concepts and characteristics of intelligent pharmaceutical manufacture as well as digital pharmaceutical manufacture are elaborated. Promoting wide applications of digital manufacturing technology of Chinese medicine is strongly recommended. Through completely informationized manufacturing processes and multi-discipline cluster innovation, intelligent manufacturing technology of Chinese medicine should be developed, which would provide a new driving force for Chinese medicine industry in technology upgrade, product quality enhancement and efficiency improvement.

Course reform and thinking of the experimental teaching of pharmaceutical technology based on the case teaching / 中华医学教育探索杂志

The experimental teaching of Pharmaceutical Technology plays a critical role in improving the students' knowledge conversion,application,and innovation abilities in pharmaceutical engineering specialty.According to the problems existing in experimental teaching process,exploration and practice on the case teaching method and the student-centered teaching mode are introduced in this paper.The implementation of the teaching reform can effectively combine pharmaceutical technology theory with practice,and is conducive to the professional development of pharmaceutical engineering in our university.

Development of Huoxiang-Zhengqi oral emulsion / 国际中医中药杂志

Objective To determine a better technique for developing the Huoxiang-Zhengqi oral emulsion without ethanol. Methods The medicinal herb of prescription in Huoxiang-Zhengqi oral liquid was extracted, and the volatile oil was firstly sheared with lecithin by high speed shearing machine, and then was prepared by high-pressure homogenizer and finally was sterilized. The factors such as the amount of phospholipids, emulsifying temperature, shearing time, the times of high pressure homogenization and sterilization conditions were investigated. Results The optimization preparation process was that the volatile oil from Huoxiang-Zhengqi oral liquid was added into 50%lecithin and was dissolved in 70 ℃ water bath, then in 10 000 r/min high-speed shear. And in the phase of adding aqueous, it was sheared 5 min for the preparation of colostrum. In the high pressure homogenization machine, the first stage pressure was set at 800 bar and the second was at 80 bar, and based on the high pressure, colostrum was prepared by 8 times. Finally, the sterilization was 116 ℃, 30 min. The preparation was a brown clarified solution, which was qualified. Conclusion The preparation method was simple, stable, and easy to popularize.

An exploring research about preparation technology and released effect of tamsulosion hydrochloride sustained-released capsules / 中国药学杂志

OBJECTIVE: To study the preparation technology of tamsulosion hydrochloride sustained-release capsules and investigate the release degree in vitro. METHODS: The pellets containing tamsulosin hydrochloride were prepeared in the fluid-bed using bottom gush medicine. Then, it was coated with ethylcellulose aqueous dispersion (surelease), and in the following procedures, water-based acrylic resin enteric system (Acryl-EZE®) was used as coating material, hydroxypropylmethylcellulose E6 (HPMCE6) was considered as porous agent by fluid-bed. Based on the release degree in vitro, prescription influence factors were evaluated, as well as drug releases curve was compared, according to the single factor experiment. RESULTS: The preparation technology referred in our research was available to make tamsulosin hydrochloride sustained-release capsules, and drug release curve of self-made sustained-release capsules was similar to the commercial one. Additionally, the products reproducibility of intra-batch and inter-batch was excellent. CONCLUSION: The tamsulosin hydrochloride sustained-release capsules prepared in this study exhibited ideal sustained-release characteristics in vitro. The formulation is reasonable and feasible. It is suitable for industrial production.

The link between industry and social interests in health in Brazil's National Health Innovation System: the experience of the Brazilian National Institute of Traumatology and Orthopedics (INTO) / La interrelación entre intereses productivos y sociales en el Sistema Nacional de Innovación de la Salud: la experiencia del Instituto Nacional de Traumatología y Ortopedia (INTO) / Articulação entre os interesses produtivos e sociais da saúde no Sistema Nacional de Inovação de Saúde: a experiência do Instituto Nacional de Traumatologia e Ortopedia (INTO)

Abstract: This article has two parts. The first discusses the relationship between industry and health interests based on three different but non-mutually exclusive "logics": (a) independent; (b) divergent; and (c) convergent. The second part describes the experience at the Brazilian National Institute of Traumatology and Orthopedics (INTO) with a technology management model. The accumulated expertise in orthopedics at INTO can favor Brazil's domestic medical equipment industry without jeopardizing the country's social health needs. This means directing the production of feasible technologies adapted to the national reality, with a focus on safety and quality, without burdening the public coffers and by overcoming the country's dependency on imported products. The proposal is to promote socioeconomic development through a virtuous circle by attracting reserves and fomenting national competitiveness in domestic and foreign markets while improving social conditions and access to health.

Resumen: Este artículo está dividido en dos partes. En la primera, se discute cómo se relacionan los intereses productivos y la salud, a partir de tres "lógicas" o perspectivas diferentes, que no son mutuamente excluyentes: (a) independiente; (b) divergente; (c) convergente. En la segunda, se describe la experiencia del Instituto Nacional de Traumatología y Ortopedia (INTO) en el montaje de un modelo de gestión de tecnología. El conocimiento internalizado en ortopedia del INTO puede favorecer la industria nacional de equipos médicos, sin abandonar las necesidades sociales brasileñas en salud. Esto es, dirigir la producción de tecnologías viables y adaptadas a la realidad nacional, centrándose en la seguridad y calidad, sin ser onerosos para el erario público y abandonando la dependencia de productos importados. La propuesta es promover un progreso socioeconómico que construya un ciclo virtuoso, con el fin de atraer divisas y fomentar la competitividad nacional en mercados internos y externos, mejorando las condiciones sociales y de acceso a la salud.

Resumo: Este artigo está dividido em duas partes. Na primeira, discute-se como se relacionam os interesses produtivos e a saúde a partir de três "lógicas" ou perspectivas diferentes que não são mutuamente excludentes: (a) independente; (b) divergente e (c) convergente. Na segunda, descreve-se a experiência do Instituto Nacional de Traumatologia e Ortopedia (INTO) na montagem de um modelo de gestão de tecnologia. O conhecimento internalizado em ortopedia do INTO pode favorecer a indústria nacional de equipamentos médicos sem abandonar as necessidades sociais brasileiras de saúde. Isto é, direcionar a produção de tecnologias viáveis e adaptadas à realidade nacional, com foco em segurança e qualidade, sem onerar os cofres públicos e abandonando a dependência de produtos importados. A proposta é a de promover um desenvolvimento socioeconômico que construa um ciclo virtuoso, por atrair divisas e fomentar a competitividade nacional em mercados internos e externos, melhorando as condições sociais e de acesso à saúde.

Preparation technique of monolithic osmotic pump tablet containing inclusion complex of baicalein / 第二军医大学学报

Objective To use the inclusion technology for improving the solubility and dissolution rate of baicalein from monolithic osmotic pump tablet containing inclusion complex of baicalein by observing the effects of the core and coating on in vitro drug release. Methods Baicalein-inclusion complex was prepared by the inclusion technique, and its solubility and dissolution rate were determined. The percent of cumulative release was used to evaluate the drug release profile in vitro. Single factor analysis was used to study the effects of NaCl and PEO amounts, coating weight and plasticizer amount on drug release. Then orthogonal design was used to select the optimal formulation of monolithic osmotic pump tablet containing baicalein-inclusion complex. Results The solubility and dissolution rate of baicalein were greatly enhanced when prepared into inclusion complex. Orthogonal design results indicated that PEO content in the tablet core and plasticizer PEG 400 in the coating had significant effects on the drug release, and the optimum formulation was: baicalein-inclusion complex 180 mg, NaCl 100 mg, PEO 80 mg, coating weight 4% and plasticizer 9%. The tablets with optimized formula achieved the desired zero-order release profile (r=0.997 8) within 12 hours and the cumulative release was higher than 88%. Conclusion Monolithic osmotic pump tablet of baicalein has been successfully prepared using inclusion complex as the intermediate, and the release behavior accords with zero-order kinetics equation.

Investigation of formulation, preparation and stability of rosuvastatin calcium tablets / 第二军医大学学报

Objective To explore the formulation and preparation technique of rosuvastatin calcium tablets with satisfactory stability and reproducibility. Methods Using suitable formulations, we prepared the rosuvastatin calcium granulates by high shear mixer and fluid bed separately, and compared their influences on the granulate properties, tablet characteristics and dissolution. The reproducibility of formulation and preparation technique was investigated. Furthermore, the factors affecting the formulation were also investigated. Results Compared with the fluid bed, granulation using high sheer mixer was more suitable for preparing rosuvastatin calcium granulates. The selected formulation and preparation technique yielded 3 batches of rosuvastatin calcium tablets which met the quality requirement. The tablets had a comparable dissolution profiles to "Crestor " of AstraZeneca. The stability of rosuvastatin calcium was largely affected by the strong light, high humidity and high temperature. Conclusion The optimized formulation and preparation technique have good reproducibility for preparing rosuvastatin calcium tablets, which have good stability.

Microemulsion based on Pterodon emarginatus oil and its anti-inflammatory potential

This article reports the development of a pharmaceutical product containing vegetable actives from a Brazilian medicinal plant. The possibility of forming a microemulsion using Pterodon emarginatus ("sucupira") oil was evaluated and the anti-inflammatory potential of this microemulsion was also examined. A formulation was developed using P. emarginatus oil, a mixture of ethoxylated Castor Oil (Ultramone(r) R-540/propylene glycol 2:1) (surfactant/cosurfactant) and distilled water at a ratio of 10:15:75, respectively. The microemulsion which was selected was then subjected to the preliminary stability test and analyzed in terms of average diameter of droplets, pH, zeta potential, and polydispersity index, on the 1st, 7th, 15th, and 30th days after preparation and stored at different temperatures (5 ± 2 °C, 25 ± 2 °C, and 40 ± 2 °C). The anti-inflammatory in vivo activity of both oil and formulation were evaluated, using the experimental model of croton oil-induced ear edema. The preliminary stability test showed that the microemulsion stored at 5 and 25 °C retained its original features throughout the 30-day period. The anti-inflammatory potential of both oil and formulation was shown to be statistically significant (p < 0.001), when compared to the control group, however, the microemulsion proved to be more effective (p < 0.05) than the oil when applied directly to the ear.

Descrevemos o desenvolvimento de um produto farmacêutico contendo ativo vegetal baseado em uma planta medicinal brasileira. Foi avaliada a habilidade de formação de uma microemulsão à base do óleo de Pterodon emarginatus (sucupira) e seu potential anti-inflamatório. Uma formulação foi desenvolvida utilizando o óleo de P. emarginatus, mistura de óleo de mamona etoxilado (Ultramona(r) R-540)/propilenoglicol (2:1) (tensoativo/cotensoativo) e água destilada, na proporção de 10:15:75, respectivamente. A microemulsão selecionada foi submetida ao teste preliminar de estabilidade e foi analisada quanto ao diâmetro médio das gotículas, pH, potential zeta e índice de polidispersão, no 1º, 7º, 15º e 30º dias após o preparo e foram estocadas em diferentes temperaturas (5±2 °C, 25±2 °C e 40±2 °C). Avaliaram-se a atividade anti-inflamatória in vivo do óleo de sucupira e da formulação, usando o modelo experimental do edema de orelha induzido pelo óleo de cróton. No teste preliminar de estabilidade observou-se que a formulação estocada a 5 °C e a 25 °C mantiveram suas características originais durante 30 dias. O potencial anti-inflamatório de ambos, óleo de sucupira e formulação foi estatisticamente significativo (p <0.001), quando comparado ao controle, porém a microemulsão foi mais eficiente (p <0.05) que o óleo aplicado diretamente nas orelhas dos animais.

Influence of process conditions on the physicochemical characteristics of cumaru (Amburana cearensis) powder produced by spray drying

The aim of the work was to study the spray-drying of ethanolic extract from Amburana cearensis (Allemão) A.C. Sm., Fabaceae, in order to obtain powders with better pharmacological and technological properties for herbal medicine. A 2³ fractional factorial statistical design was used to find adequate spray-drying operating conditions (inlet air temperature; feed flow rate and air flow rate) to produce A. cearensis powder with adequate concentration of active principles (amburoside and coumarin), low moisture content and high process yield. The HPLC analyses showed that the spray-drying powder of A. cearensis production did not cause alterations in the chromatographic profile when related to the fluid extract. The most significant factor that affected the amburoside concentration was air flow rate, while the concentration of coumarin, a thermolabile molecule, was influenced mainly by inlet air temperature. The moisture content of the spray-drying powder of A. cearensis varied from 3.72 to 5.85% (w/w), while the maximal process yield was 41.1% (w/w). The present study demonstrates for the first time the best operating conditions to produce A. cearensis extract powder that were adequate when related to the coumarin and amburoside concentrations and moisture content. However, additional studies are still needed to improve mainly it technological characteristics.

Preparation and quality evaluation of dispersible tablets of isoflavonoids from Belamcanda chinensis / 第二军医大学学报

Objective: To investigate the preparation technique and quality evaluation of dispersible tablets of isoflavonoids from Belamcanda chinensis. Methods: With the disintegrating time taken as index, the formula of isoflavonoid dispersible tablets was optimized by orthogonal experiment, and the influencing factors were observed. Three batches of samples were made using the optimized prescription, and the quality evaluation was done by examining the disintegration time, dissolution rate, and dispersing uniformity. Results: The optimized formula was A2B2C2. The contents of crospovidone(A), gelling starch(B) and gum arabic(C) were 12%, 14% and 3%, respectively. As crospovidone and gelling starch, the ratios before granulation to after pre-compress were all 2:1. The products formulated by the optimum techniques disintegrated in 30 s and dissolved in 45 min, which, together with the dispersing uniformity, met the quality criteria of dispersed tablets. Conclusion: The dispersible tablets prepared in this study have a good distribution homogeneity and a higher dissolution rate. The preparation is simple and suitable for industrial production.

Estudio de compatibilidad química del extracto seco de Rhizophora mangle L y diferentes excipientes farmacéuticos por análisis térmico / Study of chemical compatibility of Rhizophora mangle L. dry extract and of different pharmaceutical excipients using thermal analysis

En el presente trabajo se aplicó una de las técnicas más representativas que conforman el análisis térmico, la calorimetría diferencial de barrido, para estudiar la compatibilidad entre el extracto seco de Rhizophora mangle L y distintos excipientes preseleccionados para la obtención de formulaciones a partir de esta especie vegetal. Se obtuvo como resultado la no interacción química entre el extracto vegetal seco y los excipientes

In present paper authors applied one of the more representative techniques conforming the thermal analysis, the differential scanning clometry to study the compatibility among the Rhizophora mangle L dry extract and different excipients selected to obtain the formulae from this vegetal species. As result, it was possible to obtain the non-chemical interaction between the dry vegeral extract and the excipients ones

Implants as drug delivery devices for the treatment of eye diseases / Implantes como dispositivos de distribuição de medicamentos para o tratamento de doenças oculares

The treatment of diseases affecting the posterior segment of the eye is limited by the difficulty in transporting effective doses of drugs to the vitreous, retina, and choroid. Topically applied drugs are poorly absorbed due to the low permeability of the external ocular tissues and tearing. The blood-retina barrier limits drug diffusion from the systemic blood to the posterior segment, thus high doses of drug are needed to maintain therapeutic levels. In addition, systemic side effects are common. Intraocular injections could be an alternative, but the fast flowing blood supply in this region, associated with rapid clearance rates, causes drug concentration to quickly fall below therapeutic levels. To obtain therapeutic levels over longer time periods, polymeric sustained-drug release systems implanted within the vitreous are being studied for the treatment of vitreoretinal disorders. These systems are prepared using different kinds of biodegradable or non-biodegradable polymers. This review aims to demonstrate the main characteristics of these drug delivery implants and their potential for clinical application.

O tratamento de doenças do segmento posterior do olho é limitado pela dificuldade no transporte de doses efetivas de fármacos para o vítreo, retina e coróide. Os fármacos aplicados topicamente são pouco absorvidos por causa da baixa permeabilidade dos tecidos oculares externos e ao lacrimejamento. Embora a administração sistêmica seja capaz de transportar fármacos para o segmento posterior do olho, as barreiras hemato-aquosa e hematorretiniana dificultam a absorção e, normalmente, são necessárias doses elevadas, as quais estão geralmente associadas a potenciais efeitos adversos. Injeções intravitreais são capazes de transportar fármacos para o segmento posterior do olho, mas é uma técnica invasiva, pouco tolerada pelos pacientes e apresenta riscos de infecções oculares e danos aos tecidos. Visando a obtenção de níveis terapêuticos adequados de fármacos no segmento posterior do bulbo do olho por longos períodos, sistemas de liberação poliméricos implantados diretamente no vítreo estão sendo investigados para o tratamento de várias doenças vítreo-retinianas. Esses implantes podem ser preparados a partir de diferentes polímeros biocompatíveis, biodegradáveis ou não-biodegradáveis. Nesta revisão, as principais características destes implantes transportadores de fármacos são descritas, expondo suas potencialidades de aplicação clínica.

Dissolução de comprimidos e péletes de liberação prolongada empregando-se os métodos da pá e Bio-Dis / Dissolution of sustained release tablets and pellets using the paddlle and Bio-Dis methods

Matrizes hidrofílicas de diclofenaco sódico e de cetoprofeno foram preparadas por meio de compressão direta ou granulação úmida seguida de compressão, utilizando-se hipromelose para modular a dissolução do fármaco. Foram também obtidos péletes de liberação prolongada de cetoprofeno, mediante extrusão-esferonização e revestimento, em leito fluidizado, com Kollicoat® EMM 30D. Um planejamento fatorial 22 foi usado para elucidar os efeitos de variáveis de formulação sobre os perfis de liberação do fármaco a partir dos sistemas em estudo, determinados empregando-se os métodos da pá e/ou Bio-Dis. No caso dos comprimidos matriciais, os efeitos do grau de viscosidade e concentração de hipromelose foram investigados. Para os péletes, avaliou-se os efeitos da granulometria e ganho de peso em revestimento. A influência do pH sobre a liberação do fármaco a partir dos sistemas preparados foi também estudada, usando-se meios de dissolução com pH 1,2-7,2. Os métodos ANOVA e teste de Tukey (comparação estatística entre porcentuais de fármaco dissolvido e/ou eficiência de dissolução), f1, f2 e Weibull foram usados para caracterizar e comparar os perfis de dissolução. O grau de viscosidade e concentração de hipromelose influenciaram a liberação de diclofenaco sádico e cetoprofeno a partir das matrizes em estudo, sendo a concentração do polímero o fator principal que governou o processo. A granulação alterou os perfis de dissolução de cetoprofeno em relação às matrizes obtidas por compressão direta, diminuindo a velocidade e modificando o mecanismo de liberação. No caso dos péletes, o ganho de peso em revestimento foi o parâmetro que exerceu maior efeito sobre a liberação do cetoprofeno, enquanto a granulometria apenas influenciou os perfis de dissolução dás formulações com maior ganho de peso em revestimento. A liberação do fármaco a partir dos sistemas em estudo aumentou com a elevação do pH, o que ocorreu devido à solubilidade pH-dependente do cetoprofeno e diclofenaco sódico.

Diclofenac sodium and ketoprofen hydrophilic matrices were prepared by direct compression or wet granulation followed by compression, using hypromellose to modulate the drug dissolution. Sustained release ketoprofen pellets were also obtained by extrusion-spheronization and fluidized bed coating with Kollicoat® EMM 30D. A 22 factorial design has been used to elucidate the effects of formulation variables on the drug release profiles from the systems in study, determined using the paddle method and Bio-Dis. In the case of matrix tablets, the effects of the viscosity grade and concentration of hypromellose were investigated. For the pellets, the effects of granulometry and weight gain were evaluated. The influence of the pH value on the drug release from the prepared systems was also studied, using pH 1,2-7,2 dissolution media. ANOVA and Tukey's test (statistical comparison between percentages of drug dissolved and/or dissolution efficiency), f1, f2 and Weibull methods were used to characterize and compare the dissolution profiles. The concentration and viscosity grade of hypromellose influenced the ketoprofen and diclofenac sodium release from the studied matrices, being the polymer concentration the main factor that has governed the process. Granulation has modified the dissolution profiles of ketoprofen in relation to the matrices obtained by direct compression, reducing the rate and modifying the mechanism of drug release. In the pellets case, weight gain was the main factor that has influenced the ketoprofen release, while ganulometry has only influenced the dissolution profiles of the formulation with the highest weight gain. Drug release from the systems under study increased with the increase of the pH value of the medium because of the diclofenac sodium and ketoprofen pH-dependent solubility.

Extracting Technology of Kanggan Qudu Ling Granule / 中药新药与临床药理

Objective:To investigate the effects of various deco cting times,and frequencies on the main active components of Radix et Rhizoma Rh ei and Rhizoma Coptidis decocting together so as to determine the best extractin g technology.Methods:Orthogonal method was used to screen the extracting techno logy and TLC scanning to determine the content of main active components. Conclu sion: Proper decocting frequency and adding water volume will increase the yield of the main active components.

The Technology of Extracting Semen Cassiae from Jueming Jiangzhi Powder / 中药新药与临床药理

The technology,of extracting Semen Cassiae from Jueming Jiangzhi Powder was investigated.The perceutages of extra ction and preservation of anthraquinone were used to select the methods of extra ction, concentration and drying of Semen Cassiae. The optimal procedure was set as follows:the large-size powder of Semen Cassiae was extracted with 50% alcohol for three times, then the extracted liquid was concentrated by vacuum evaporati on and finally dried by spraying.