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1.
Braz. J. Pharm. Sci. (Online) ; 58: e18630, 2022. tab, graf
Article in English | LILACS | ID: biblio-1364418

ABSTRACT

Abstract The objective of the present investigation was to design, optimize and characterize the gastro retentive floating levofloxacin tablets and perform in-vivo evaluation using radiographic imaging. The floating tablets were prepared by using polymers i.e hydroxy propyl methyl cellulose (HPMC-K4M) and carbopol-940 individually and in combination by nonaquous granulation method. All the Formulations were evaluated for swelling index (S.I), floating behavior and in-vitro drug release kinetics. The compatibility study of levofloxacin with other polymers was investigated by FTIR, DSC, TGA and XRD. Results from FTIR and DSC revealed no chemical interaction amongst the formulation components. The optimized formulation (F11) showed floating lag time (FLT), total floating time (TFT) swelling index (S.I) of 60 sec, >16h and approximately 75 %, respectively. Moreover, F11 showed zero order levofloxacin release in simulated gastric fluid over the period of 6 h. X-ray studies showed that total buoyancy time was able to delay the gastric emptying of levofloxacin floating tablets in rabbits for more than 4 hours. In conclusion the optimized formulation (F11) can be used for the sustained delivery of levofloxacin for the treatment of peptic ulcer.


Subject(s)
Drug Liberation , Peptic Ulcer/classification , Tablets/pharmacology , X-Rays/adverse effects , In Vitro Techniques/instrumentation , Spectroscopy, Fourier Transform Infrared , Drug Compounding/instrumentation , Process Optimization/analysis , Levofloxacin/analysis , Gastric Emptying/drug effects
2.
Vitae (Medellín) ; 28(2): 1-9, 2021-05-18. Ilustraciones
Article in English | LILACS, COLNAL | ID: biblio-1363202

ABSTRACT

Background: Despite the high reactivity of the platinum electrode, the iodine-coated platinum electrode shows obvious inertness toward adsorption and surface processes. For that, iodine-coated platinum electrodes accommodate themselves to interesting voltammetric applications. Objectives: This study reports using the modified iodine-coated polycrystalline platinum electrode as a voltammetric sensor for ascorbic acid determination in pharmaceutical formulations. Methods: The developed voltammetric method based on recording cyclic voltammograms of ascorbic acid at iodine-coated electrode The optimized experimental parameters for the determination of ascorbic acid were using 0.1 M KCl as a supporting electrolyte with a scan rate of 50mV/s. Results: The anodic peak related to ascorbic acid oxidation was centered at nearly 0.28V. An excellent and extended linear dependence of the oxidative peak current on the concentration of ascorbic acid was observed in the range 2.84x10-3 - 5.68 mM. The limit of detection (LOD) and limit of quantitation (LOQ) were 1.0 µM and 3.01 µM, respectively, attesting to the method's sensitivity. The investigation for the effect of potential interference from multivitamin tablet ingredients (vitamins B1, B6, B12, folic acid, citric acid, sucrose, glucose, and zinc) indicated specific selectivity toward ascorbic acid and the absence of any electrochemical response toward these components. Recovery results in the range 98.93±2.78 - 99.98±5.20 for spiked standard ascorbic acid in pharmaceutical formulations further confirmed the potential applicability of the developed method for the determination of ascorbic acid in real samples. Conclusions: The developed method was successfully applied to the analysis of ascorbic acid (vitamin C), and the obtained results were in good agreement with the labeled values; besides, the statistical tests indicated no significant difference at p=0.05 with a 95% confidence level


Antecedentes: A pesar de su alta reactividad, el electrodo de platino recubierto de yodo muestra una inercia evidente hacia la adsorción y los procesos superficiales. Por ello, los electrodos de platino recubiertos de yodo se adaptan a interesantes aplicaciones voltamétricas. Objetivos: Este estudio informa sobre el uso del electrodo de platino policristalino recubierto de yodo modificado como sensor voltamétrico para la determinación del ácido ascórbico en formulaciones farmacéuticas. Métodos: El método voltamétrico desarrollado se basa en el registro de voltamperogramas cíclicos del ácido ascórbico en el electrodo recubierto de yodo Los parámetros experimentales optimizados para la determinación del ácido ascórbico fueron utilizando KCl 0,1 M como electrolito de soporte con una velocidad de barrido de 50mV/s. Resultados: El pico anódico relacionado con la oxidación del ácido ascórbico se centró en casi 0,28V. Se observó una excelente y extendida dependencia lineal de la corriente del pico oxidativo con respecto a la concentración de ácido ascórbico en el rango 2,84x10-3 - 5,68 mM. El límite de detección (LOD) y el límite de cuantificación (LOQ) fueron 1,0 µM y 3,01 µM, respectivamente, lo que demuestra la sensibilidad del método. La investigación del efecto de la interferencia potencial de los ingredientes de las tabletas multivitamínicas (vitaminas B1, B6, B12, ácido fólico, ácido cítrico, sacarosa, glucosa y zinc) indicó una selectividad específica hacia el ácido ascórbico y la ausencia de cualquier respuesta electroquímica hacia estos componentes. Los resultados de recuperación en el rango de 98,93±2,78 - 99,98±5,20 para el ácido ascórbico estándar adicionado en formulaciones farmacéuticas confirmaron además la potencial aplicabilidad del método desarrollado para la determinación del ácido ascórbico en muestras reales. Conclusiones: El método desarrollado se aplicó con éxito al análisis de ácido ascórbico (vitamina C), y los resultados obtenidos coincidieron con los valores etiquetados; además, las pruebas estadísticas no indicaron diferencias significativas a p=0,05 con un nivel de confianza del 95%


Subject(s)
Humans , Drug Compounding , Cisplatin , Electrodes , Iodine
3.
Article in Chinese | WPRIM | ID: wpr-921635

ABSTRACT

In this paper, co-processed lactose SuperTab 40 LL was selected as fillers to study the preparation of musk sustained-release mini-tablets in the Xihuang multiple-unit drug release system. Musk sustained-release tablets containing different proportions of SuperTab 40 LL and MCC were prepared under various pressures, and then the compressibility and compactibility of these prescriptions were evaluated by Walker, Heckel and Ryshkewitch-Duckworth equations. In addition, the fluidity of the prescriptions was evaluated by parameters of Kawakita equation. There was a comprehensive analysis of the effect of SuperTab 40 LL on musk sustained-release mini-tablets combined with the appearance of SuperTab 40 LL and their tensile strength. The results shown that SuperTab 40 LL had better compression process through the Heckel equation, and the direct compression process of drug powders with excipients can be analyzed by the Kawakita and Ryshkewitch-Duckworth equations. As a new type of co-processed lactose, SuperTab 40 LL had a good fluidity and compactibility. SuperTab 40 LL may undergo particle crushing and plastic deformation during the compression process, which increased the contact area and bonding sites between the particles, and aggregated and shaped the mixed powder easy. Moreover, MCC showed a synergistic effect, and the combined application with SuperTab 40 ll could effectively improve the fluidity and compressibility of the musk sustained-release powder. When the ratio of SuperTab 40 LL and MCC was 2∶1, musk sustained-release mini-tablets had a high drug loading capacity and good compactibility in line with the design objectives.


Subject(s)
Delayed-Action Preparations , Drug Compounding , Excipients , Fatty Acids, Monounsaturated , Models, Theoretical , Powders , Tablets
4.
Article in Chinese | WPRIM | ID: wpr-921634

ABSTRACT

The high shear wet granulation(HSWG) process of Chinese medicine has a complicated mechanism. There are many influencing factors that contribute to this process. In order to summarize the manufacturability of different kinds of materials in HSWG, this paper constructed a material library composed of 11 materials, including 4 Chinese medicine extracts and 7 pharmaceutical excipients. Each material was described by 22 physical parameters. Several binders were employed, and their density, viscosity and surface tension were characterized. Combining empirical constraints and the principle of randomization, 21 designed experiments and 8 verification experiments were arranged. The partial least squares(PLS) algorithm was used to establish a process model in prediction of the median granule size based on properties of raw materials and binders, and process parameters. The surface tension and density of binders, as well as the maximum pore saturation were identified as key variables. In the latent variable space of the HSWG process model, all materials could be divided into three categories, namely the Chinese medicine extracts, the diluents and the disintegrants. The granulation of Chinese medicine extracts required low viscosity and low amount of binder, and the resulted granule sizes were small. The diluent powders occupied a large physical space, and could be made into granules with different granule sizes by adjusting the properties of binders. The disintegrants tended to be made into large granules under the condition of aqueous binder. The combination use of material database and multivariate modeling method is conducive to innovate the knowledge discovery of the wet granulation process of Chinese medicine, and provides a basis for the formulation and process design based on material attributes.


Subject(s)
Drug Compounding , Excipients , Medicine, Chinese Traditional , Particle Size , Powders , Tablets , Technology, Pharmaceutical
5.
Chinese Journal of Biotechnology ; (12): 2256-2271, 2021.
Article in Chinese | WPRIM | ID: wpr-887794

ABSTRACT

The development of biotechnology and the in-depth research on disease mechanisms have led to increased application of enzymes in the treatment of diseases. In addition, enzymes have shown great potential in drug manufacturing, particularly in production of non-natural organic compounds, due to the advantages of mild reaction conditions, high catalytic efficiency, high specificity, high selectivity and few side reactions. Moreover, the application of genetic engineering, chemical modification of enzymes and immobilization technologies have further improved the function of enzymes. This review summarized the advances of using enzymes as drugs for disease treatment or as catalysts for drug manufacturing, followed by discussing challenges, potential solutions and future perspectives on the application of enzymes in the medical and pharmaceutical field.


Subject(s)
Biocatalysis , Biotechnology , Catalysis , Drug Compounding , Enzymes/metabolism
6.
Article in Chinese | WPRIM | ID: wpr-879124

ABSTRACT

In leading the high-quality development of Chinese medicine preparations, it is an important link to formulate the scientific, reasonable, and feasible guidelines for the change of Chinese medicines in accordance with the change characteristics and principles of the Chinese medicines is an important work to promote the Technical guidelines for the study of pharmaceutical changes in traditional Chinese medicines was formed by a broad consensus based on the characteristics and research results of the pharmaceutical changes in Traditional Chinese Medicines(TCM)with the principles of science and risk management. This guideline has clarified the basic principles and requirements for the evaluation of changes in TCM, specified the research and verification work of common change scenarios, defined the boundaries of changes in TCM, and proposed to encourage the use of new technologies, new methods, and new excipients that meet product characteristics. It will definitely promote the quality improvement and the secondary development of TCM. In this article, the revision background and main content of the guideline were introduced, and the main features of the Guideline were analyzed, in order to provide references for the industry.


Subject(s)
Consensus , Drug Compounding , Drugs, Chinese Herbal , Medicine, Chinese Traditional , Pharmaceutical Preparations , Quality Improvement
7.
Rev Rene (Online) ; 22: e59963, 2021. graf
Article in Portuguese | LILACS, BDENF | ID: biblio-1149524

ABSTRACT

RESUMO Objetivo identificar as atividades farmacológicas da manteiga de bacuri (Platonia insignis Mart.). Métodos revisão integrativa, realizada nas bases de dados Literatura Latino-americana e do Caribe em Ciências da Saúde, Cumulative Index to Nursing and Allied Health Literature, EMBASE, MEDLINE/PubMed, Web of Science, Cochrane Library e SCOPUS, sem delimitação temporal e de idioma. A seleção se constituiu de 13 ensaios pré-clínicos. A avaliação das informações ocorreu de forma descritiva, confrontando com os achados pertinentes. Resultados observou-se que 50,0% das publicações foram indexadas na MEDLINE/PubMed, maioria das publicações ocorreram na Inglaterra (61,5%), seguidas do Brasil e dos Estados Unidos, ambos com 13,3%. Destaca-se que 100,0% dos artigos foram ensaios pré-clínicos; atividades farmacológicas para antioxidante (38,4%) e antileishmanicidas (30,7%). Registrou-se que 38,4% dos ensaios apresentaram testes de toxicidade. Conclusão a manteiga de bacuri (Platonia insignis Mart.) apresentou atividades farmacológicas em ensaios pré-clínicos, como antioxidantes, antileshimaniose, anticonvulsivante e cicatrização de feridas.


ABSTRACT Objective to identify the pharmacological activities of bacuri butter (Platonia insignis Mart.). Methods an integrative review, carried out in the databases of Latin American and Caribbean Literature in Health Sciences, Cumulative Index to Nursing and Allied Health Literature, EMBASE, MEDLINE/PubMed, Web of Science, Cochrane Library and SCOPUS, without the time and language restriction. The selection consisted of 13 pre-clinical trials. The information assessment descriptively took place, comparing with the pertinent findings. Results it was observed that 50.0% of the publications were indexed in MEDLINE/PubMed, most publications were from England (61.5%), followed by Brazil and the United States, both with 13.3%. It is noteworthy that 100.0% of the articles were pre-clinical trials; pharmacological activities for antioxidants (38.4%) and antileishmanicides (30.7%). It was found that 38.4% of the trials presented toxicity tests. Conclusion bacuri butter (Platonia insignis Mart.) Showed pharmacological activities in pre-clinical trials, such as antioxidants, antileshimaniasis, anticonvulsant and wound healing.


Subject(s)
Benzophenones , Clusiaceae , Drug Compounding , Drug Synergism , Drug Therapy
8.
Rev. Ateneo Argent. Odontol ; 64(1): 18-21, 2021. ilus
Article in Spanish | LILACS | ID: biblio-1248258

ABSTRACT

Biomaterial de tercera generación con una tasa de degradabilidad en la zona perirradicular y del foramen apical, con una velocidad similar a la que emplea el organismo para formar tejido calcificado y sellar biológicamente el extremo apical del diente. Mediante el recurso tecnológico de la microencapsulación se produce la liberación lenta y controlada de Ca2+ retenido en la superficie y en el interior de las microesferas de alginato de calcio, sin que se modifique de manera significativa las propiedades reológicas básicas del biomaterial de obturación de conductos, tales como la compresibilidad, plasticidad, extensibilidad, fluidez, viscosidad cinemática, viscosidad de compresión y endurecimiento por trabajo (AU)


Third-generation biomaterial with a degradability rate in the periradicular area and the apical foramen, with a speed similar to that used by the body to form calcified tissue and biologically seal the apical end of the tooth. Through the technological resource of microencapsulation, the slow and controlled release of Ca2+ retained on the surface and inside the calcium alginate microspheres is produced, without significantly modifying the basic rheological properties of the duct sealing biomaterial, such as compressibility, plasticity, extensibility, flowability, kinematic viscosity, compression viscosity, and work hardening (AU)


Subject(s)
Humans , Periapical Diseases/therapy , Root Canal Filling Materials/therapeutic use , Biocompatible Materials , Rheology , Calcium Compounds , Tooth Apex , Drug Compounding , Alginates/chemistry , Microspheres
9.
Rev. fac. cienc. méd. (Impr.) ; 17(2): 25-30, jul.-dic. 2020.
Article in Spanish | LILACS, BIMENA | ID: biblio-1292409

ABSTRACT

La preparación y administración de medicamentos, es parte importante en el proceso de recuperación de la salud, se destaca entre las funciones relevantes de los profesionales y auxiliares de enfermería, incluye etapas críticas que deben garantizar la correcta y segura administración de los mismos. Existe carencia de revisiones bibliográficas que aborden la problemática de los errores de enfermería, aunque, investigadores en todo el mundo, han estudiado el impacto que genera el error en la preparación de medicamentos, siendo este uno de los principales problemas en el campo de la enfermería. Objetivo: conocer la relación entre la calidad técnica en la preparación de medicamentos, identificando características y tipos, con la frecuencia en los errores de enfermería. Material y Métodos: se realizó revisión bibliográfica, identificando once artículos científicos en las bases de datos PubMed, Scopus y SciELO. Se incluyeron estudios originales y observacionales, excluyendo revisiones sistemáticas, estudios duplicados y sin acceso libre a la información. Conclusión: los factores predominantes en los errores de enfermería, se deben a la confusión al momento de elegir el fármaco, error en el cálculo de dosis, sobrecarga de trabajo y déficit de conocimiento...(AU)


Subject(s)
Humans , Preparation Scales , Nursing Assistants , Drug Compounding/methods , Inappropriate Prescribing
10.
Article in English | WPRIM | ID: wpr-826321

ABSTRACT

BACKGROUND@#Currently, cancer is among the leading causes of morbidity and mortality in the world. Exposure to CDs may occur during drug preparation and mixing, during drug administration, during transport, and cleaning spills and waste disposal. Healthcare workers who prepare or administer antineoplastic drugs, or who work in areas where these drugs are used, can be exposed to these agents. This also affects the public around the exposed area if appropriate disposal system is not known. Several studies reported increased risks of leukemia and breast cancer among nurses handling CDs and not following safety guidelines. Because of the absence of studies in Ethiopia, the current study was conducted to determine the knowledge level of cytotoxic drug handling and associated factors among health professionals in the University of Gondar Comprehensive Specialized Hospital.@*METHODS@#The institutional-based cross-sectional study was conducted from June to August 2019. Epi info 7.1 was used for data entry and then exported into SPSS version 20 for computing, recording, and statistical analysis. Logistic regression was used to explain the relationship with independent variables.@*RESULTS@#Four hundred and twelve health professionals participated in the study with 53.4% males. The participants' mean age was 29.9 (± 5.43) years ranging from 20-60. Two hundred and twenty-three (54.1%) health professionals heard about cytotoxic drugs, and 52.7% (95% UI 47.8-57.8%) had good knowledge of cytotoxic drug handling. Being male sex (AOR = 1.84, 95% CI (1.13-3.00)), age of 29-31 (AOR = 1.99, 95% CI (1.03-3.84)), hearing information about cytotoxic drug handling (AOR = 2.53, 95% CI (1.43-4.47)), ever attended training on cytotoxic drug handling (AOR = 3.15, 95% CI (1.13-8.79)), ever taking courses related to cytotoxic drugs (AOR = 2.03, 95% CI (1.15-3.59)), and good practice (AOR = 3.24, 95% CI (1.95-5.37)) were significantly associated with knowledge towards cytotoxic drug handling. It is therefore imperative to train health professionals and to incorporate CDs handling related course contents while revising curricula to raise the knowledge of health professionals about proper cytotoxic drug handling.@*CONCLUSION@#Above half of the study participants scored higher than the median of the cytotoxic drug handling knowledge questions. Sex, age, information about cytotoxic drug handling, training, taking courses related to cytotoxic drugs, and good practice were significantly associated with knowledge towards cytotoxic drugs handling.


Subject(s)
Adult , Antineoplastic Agents , Cross-Sectional Studies , Drug Compounding , Ethiopia , Female , Health Knowledge, Attitudes, Practice , Health Personnel , Psychology , Humans , Male , Middle Aged , Young Adult
11.
Int. j. high dilution res ; 19(4): 2-9, 2020.
Article in English | LILACS, HomeoIndex | ID: biblio-1146533

ABSTRACT

IntroductionNosodes, the homeopathicpreparationssourcedfrom biological materials including clinical samples, cultures of organisms, and diseased tissues have been in use against the source-specific infections as well as other diseases. The nosodes have demonstrated some efficacy in managing epidemics, such as influenza, dengue, and leptospirosis.This article presents the need and process of development ofnosodes from the SARS-CoV-2 to explore its prophylactic and therapeutic potentials against certain related viral diseases.Materials and methodsA clinical sample of SARS-Cov-2 positive patient,based on the cycle threshold (CT) value of the qRT-PCR, heat-inactivated SARS-CoV-2, and spike glycoprotein all were processed for making nosodesas per the method described in Homoeopathy Pharmacopoeia of India.Molecular tests, such as qRT-PCR and sterility tests were performed to establish the live organisms, RNA material, and the absence of contamination.ResultsThree variants of CoronavirusNosodewere developed using a clinical sample,heat-inactivatedSARS-CoV-2, and spike glycoprotein.In potencies 3c and above, no detectableSARS-CoV-2 RNA material was found by PCR.The analytical results for nosodes were reported as compliant for sterility testing as per the IP.ConclusionThree variants of Coronavirus nosodes were preparedwhich need to be evaluated further through pre-clinical and clinical studies.(AU)


Subject(s)
Humans , Nosodes (Homeopathy)/pharmacology , Coronavirus Infections/therapy , Drug Compounding , Spike Glycoprotein, Coronavirus , Betacoronavirus , Virus Inactivation , Betacoronavirus/drug effects
12.
Gac. méd. Méx ; 155(2): 191-195, mar.-abr. 2019. tab, graf
Article in Spanish | LILACS | ID: biblio-1286482

ABSTRACT

Resumen La enfermedad de Menkes es una patología neurodegenerativa y letal debida a mutaciones génicas de la enzima ATP-7A trasportadora de cobre; se manifiesta por síntomas neurológicos y alteraciones del tejido conectivo de severidad variable. El uso subcutáneo oportuno de histidinato de cobre (Cu-His) es determinante en la calidad de vida. Se reportan las primeras experiencias en México en la síntesis y uso seguro de Cu-His en tres casos en los que corroboramos hipocupremia e hipoceruloplasminemia. Bajo asesoramiento del Hospital for Sick Children, Toronto, Canadá, elaboramos una solución de 500 µg/mL. En los tres casos aplicamos 250 µg de Cu-His, sin efectos indeseables relevantes durante 30 días y observamos las siguientes determinaciones séricas de cobre (Cu en µg/L) y ceruloplasmina (Cp en mg/dL): caso 1, Cu días 0 y 30, 8 y 504 µg/L; Cp días 0 y 30, 4 y 10.75 mg/dL; caso 2, Cu días 0 y 30, < 50 y 502, µg/L; Cp días 0 y 30, 2 y 15 mg/dL; caso 3, Cu días 0 y 30, 3 y 84.2 µg/L; Cp días 0 y 30, 4 y 10.7 mg/dL. En México es posible la síntesis segura de Cu-His y tratar la enfermedad de Menkes, la cual debe ser intencionalmente buscada.


Abstract Menkes disease is a neurodegenerative and lethal pathology caused by gene mutations of the copper-transporting ATP-7A enzyme; it manifests itself by neurological symptoms and connective tissue changes of varying severity. Timely subcutaneous use of copper histidinate (Cu-His) is determinant for quality of life. We report the first experiences in Mexico on Cu-His synthesis and its safe use in 3 cases where hypocupremia and hypoceruloplasminemia were corroborated. With advice of the Hospital for Sick Children of Toronto Canada, we prepared a 500 µg/mL solution. In all three cases were 250 µg of Cu-His applied without relevant undesirable effects for 30 days. Serum copper (Cu, expressed in µg/L) and ceruloplasmin (Cp, in mg/dL) were determined: case 1, Cu days 0 and 30, 8 and 504 µg/L; Cp days 0 and 30, 4 and 10.75 mg/dL; case 2, Cu days 0 and 30, <50 and 502 µg/L; Cp days 0 and 30, 2 and 15 mg/dL; case 3, Cu days 0 and 30, 3 and 84.2 µg/L; Cp days 0 and 30, 4 and 10.7 mg/dL. In Mexico, it is possible to safely synthesize Cu-His and treat MD, which must be intentionally sought.


Subject(s)
Humans , Infant , Child, Preschool , Organometallic Compounds/administration & dosage , Quality of Life , Drug Compounding/methods , Histidine/analogs & derivatives , Menkes Kinky Hair Syndrome/drug therapy , Organometallic Compounds/adverse effects , Copper/blood , Pharmaceutical Solutions , Histidine/administration & dosage , Histidine/adverse effects , Mexico
13.
Article in Chinese | WPRIM | ID: wpr-773664

ABSTRACT

Aconitums,represented by Aconite Radix,Aconiti Lateralis Radix Praeparata and Aconiti Kusnezoffh Folium,is a kind of traditional Chinese medicine with a long medicinal history in China. They possess the significant toxicity and therapeutic effects simultaneously. Their potent effects of rescuing from dying,curing rheumatism,anti-inflammation,and analgesia make Aconitums highly regarded by physicians and pharmacists of various dynasties. However,countless poisoning cases caused by an irrational use of Aconitums were reported. In case of improper application and exceeding the therapeutic window,the acute cardiotoxicity and neurotoxicity would be caused,seriously threatening health and even life of the users. Therefore,the clinical application of Aconitums is limited to some extent. To avoid its toxicity and ensure the safety of medicinal use,Aconitums is usually used in a form of its processed products instead of the crude herbs,or combined with some other traditional Chinese medicines in a normal prescription. A proper processing and compatibility method can detoxicate its severe toxicity,reduce the adverse reactions,and also significantly broaden the indications and application range of Aconitums. This provides a guarantee for the secondary exploitation and utilization of Aconitums. In this paper,the traditional processing methods of Aconitums,along with the modern advancement were reviewed,and the mechanisms of detoxification by processing and compatibility were also illuminated. The physical detoxification mode and chemical detoxification mode were found as two main detoxification ways for Aconitums. In particular,the detoxification by hydrolysis,ion-pair,and saponification were three main means. The mechanisms illustrated in this paper can be a reference to the development of modern processing method and a guidance for appropriate use of Aconitums in clinical application.


Subject(s)
Aconitum , Chemistry , Toxicity , China , Drug Compounding , Methods , Drugs, Chinese Herbal , Chemistry , Toxicity , Medicine, Chinese Traditional , Plant Leaves , Chemistry , Plant Roots , Chemistry
14.
Article in Chinese | WPRIM | ID: wpr-773259

ABSTRACT

Extrusion-spheronisation method was used to prepare Rhus chinensis total phenolic acid pellets. The formula and preparation of R. chinensis total phenolic acid pellets were optimized. The formulas( drug loading capacity,diluent,wetting agent and anti-sticking agent) were determined by the single factor test with yield,appearance and performance as the indexes. The preparation was optimized by Box-Behnken design and response surface method,with the rate of extrusion,rate of spheronization and time of spheronization as the independent variables and the overall desirability value of yield,friability and roundness as the dependent variables. The optimal formula of pellets was as follows: drug loading capacity 28. 7%,MCC-lactose 9 ∶1,silicon dioxide as anti-sticking agent,and 60% ethanol as wetting agent. The optimal preparation was determined as follows: the rate of extrusion was 43 r·min-1,the rate of spheronization was 1 800 r·min-1,and the time of spheronization was 4 min. The absolute deviation between predicted value and estimated value under the conditions was less than 5. 0%,with a high degree of model fit. The preparation parameters obtained were accurate,reliable and reproducible. Under scanning electron microscopy( SEM),R. chinensis total phenolic acid pellets were uniform in diameter,round and smooth. The optimal formulation and process are stable and feasible for preparing R. chinensis total phenolic acid pellets.


Subject(s)
Drug Compounding , Methods , Hydroxybenzoates , Chemistry , Particle Size , Rhus , Chemistry , Solubility
15.
Article in Chinese | WPRIM | ID: wpr-773193

ABSTRACT

The taste is the key to the research and design for formulation prescription of traditional Chinese medicine buccal tablets( TCMBTs). TCMBTs are dissolved in the oral cavity in parallel with the release of the drug,providing a sufficient " time window" for the perception of various basic taste,tactile and retention. The overall taste is the result of competitive inhibition,comprehensive superposition and dynamic change of multiple tastes. Traditional evaluation methods rely mostly on recalled experience score,difficult to reflect the dynamic changes of taste for buccal tablets. Therefore,it is urgent to establish a new optimized model for taste evaluation and formulation prescription according to the formulation characteristics of TCMBTs. To this end,this paper proposed for the first time to construct a research method for the optimal formulation of TCMBTs based on temporal dominant description of sensations combined with multivariate statistical analysis: the sensory test of volunteers was carried out by temporal dominant description analysis method,and elements separation was conducted for the time and taste in the process of inclusion to form a temporal dominant descriptive score of multi-time points and multi-sensory attributes. Finally,the optimal formulation was obtained by multivariate statistical analysis. Taking the formulation prescription of Compound Caoshanhu Buccal Tablets as an example,the research ideas of this method were explained,and the optimal formulation prescription was obtained as follows,Glabrous Sarcandra Extract of 20. 0 g,mannitol of 24. 0 g,microcrystalline cellulose of 12. 0 g,aspartame of 1. 0%,menthol of 0. 7%,and menthol oil of 0. 7%. This study provides a new method for the taste evaluation and formulation research of TCMBTs,providing a new idea for the fine manufacturing and innovative development of TCM buccal tablets in the new era.


Subject(s)
Drug Compounding , Humans , Medicine, Chinese Traditional , Sensation , Solubility , Tablets , Taste
16.
Article in Chinese | WPRIM | ID: wpr-772683

ABSTRACT

OBJECTIVE@#The purpose of this study is to investigate the effects of different drying methods on the physical properties and drug delivery of chitosan microspheres.@*METHODS@#Three types of drying methods were utilized, including air drying and freeze drying after freezing at -20 ℃ (slow cooling) and at -80 ℃ (fast cooling). The physical properties of microspheres were characterized. Utilizing bovine serum albumin (BSA) as the model drug, the in-vitro release behaviors of drug-loaded beads were investigated.@*RESULTS@#By comparing the physical properties of the different drying methods, the microspheres' diameters, porosities, and surface area were observed to increase successively from air drying and slow cooling to fast cooling, whereas the pore size and the swelling and degradation rates varied. The drug-loading experiments revealed that the loading capacity of air-dried microspheres was the lowest and the release rate was the slowest. Although the loading capacity of fast cooling microspheres was high, an obvious burst release was observed. The loading capacity of slow cooling microspheres was similar to that of the fast cooling microspheres and the loaded BSA can be released continuously.@*CONCLUSIONS@#The results indicate that different drying methods can affect the physical properties of chitosan microspheres, which further influence drug loading and release.


Subject(s)
Chitosan , Drug Carriers , Drug Compounding , Microspheres , Particle Size
17.
Intestinal Research ; : 87-93, 2019.
Article in English | WPRIM | ID: wpr-740027

ABSTRACT

BACKGROUND/AIMS: Oral mesalazine is an important treatment for ulcerative colitis (UC), and non-adherence to mesalazine increases the risk of relapse. Controlled-release (CR) mesalazine has 2 formulations: tablets and granules. The relative acceptabilities of these formulations may influence patient adherence; however, they have not been compared to date. This study aimed to evaluate the acceptabilities of the 2 formulations of CR mesalazine in relation to patient adherence using a crossover questionnaire survey. METHODS: UC patients were randomly assigned to 2 groups in a 1:1 ratio. Patients in each group took either 4 g of CR mesalazine tablets or granules for 6 to 9 weeks, and then switched to 4 g of the other formulation for a further 6 to 9 weeks. The acceptability and efficacy were evaluated by questionnaires, and adherence was assessed using a visual analog scale. The difference in acceptabilities between the 2 formulations and its impact on adherence were assessed. RESULTS: A total of 49 patients were prospectively enrolled and 33 patients were included in the analysis. Significantly more patients found the tablets to be less acceptable than the granules (76% vs. 33%, P=0.0005). The granules were preferable to the tablets when the 2 formulations were compared directly (73% vs. 21%, P=0.004), for their portability, size, and numbers of pills. The adherence rate was slightly better among patients taking the granules (94% vs. 91%) during the observation period, but the difference was not significant (P=0.139). CONCLUSIONS: CR mesalazine granules are more acceptable than tablets, and may therefore be a better option for long-term medication.


Subject(s)
Colitis, Ulcerative , Drug Compounding , Humans , Medication Adherence , Mesalamine , Patient Acceptance of Health Care , Patient Compliance , Prospective Studies , Recurrence , Tablets , Ulcer , Visual Analog Scale
18.
Article in Korean | WPRIM | ID: wpr-786522

ABSTRACT

PURPOSE: This study aimed to investigate the characteristics of poisoning drug ingested by younger children, and to compare the clinical outcome by drug forms.METHODS: This was a retrospective analysis based on medical records from the Emergency Department based Injury In-depth Surveillance (EDIIS) registry in Korea from January to December 2015. Patients aged 7 years or younger visiting the emergency department (ED) with drug poisoning were included. We classified the forms of drugs as tablets or syrup, and analyzed the characteristics by size, color, and shape. In addition, clinical outcomes and ED length of stay were compared according to the drug forms.RESULTS: A total of 308 cases were collected, and 202 patients finally were analyzed. Tablets and capsules (TACs) were more common than syrup (67.3% vs. 32.7%). Regarding clinical outcomes, patients who took TACs had higher admission rate (17.6% vs. 7.6%, P = 0.040) without a significant difference in ED length of stay compared to those who took syrups. While commonly ingested drugs in TACs were hormones, sedative and analgesics, frequent drugs in syrup were antihistamines and cold drugs. In 136 case of TACs, median long and short axes were 0.85 cm (interquartile range [IQR], 0.7–1.1 cm) and 0.72 cm (IQR, 0.59–0.82 cm), respectively. Chromatic TACs were 80 cases (58.8%) and more common than achromatic TACs. Round shapes were preferred than angular ones (96.3% vs. 3.7%).CONCLUSION: In younger children poisonings, the TACs showed higher incidence and admission rate compared to syrups. Especially, chromatic TACs and round shapes were preferred. Therefore, drugs with these characteristics need to be stored more carefully.


Subject(s)
Analgesics , Capsules , Child , Dosage Forms , Drug Compounding , Emergency Service, Hospital , Histamine Antagonists , Humans , Incidence , Korea , Length of Stay , Medical Records , Poisoning , Retrospective Studies , Tablets
20.
Acta cir. bras ; 33(12): 1052-1060, Dec. 2018. graf
Article in English | LILACS | ID: biblio-973489

ABSTRACT

Abstract Purpose: To establish a method for the preparation of zoledronate liposome and to observe its effect on inducing the apoptosis of rat liver Kupffer cells. Methods: Zoledronate was encapsulated in liposomes, and then the entrapment rate was detected on a spectrophotometer. The prepared Zoledronate liposome (0.01 mg/mL) was injected into the tail vein of SD rats. Three days later, the number of Kupffer cells (CD68 positive) in rat liver tissue was detected by immunohistochemistry. Flow cytometry was used to detect the apoptosis rate of the isolated liver Kupffer cell cultured in vitro. Results: The entrapment rate of Zoledronate was 43.4±7.8%. Immunohistochemistry revealed that the number of Kupffer cells was 19.3±2.1 in PBS group and 5.5±1.7 in Zoledronate liposome group, with a significant difference (P<0.05). The apoptosis rate of Kupffer cells was 4.1±0.8% in PBS group, while it was 9±2.2% and 23.3±5.9% in Zoledronate liposomes groups with different concentrations of Zoledronate liposome (P<0.05). Conclusions: Zoledronate liposomes can effectively induce the apoptosis of Kupffer cells in vivo and in vitro, and the apoptosis rate is related to the concentration of Zoledronate liposome. To establish a rat liver Kupffer cell apoptosis model can provide a new means for further study on Kupffer cell function.


Subject(s)
Animals , Male , Apoptosis/drug effects , Zoledronic Acid/pharmacology , Kupffer Cells/drug effects , Liver/cytology , Immunohistochemistry , Random Allocation , Cell Count , Reproducibility of Results , Treatment Outcome , Rats, Sprague-Dawley , Drug Compounding/methods , Flow Cytometry , Zoledronic Acid/administration & dosage , Zoledronic Acid/chemical synthesis , Liposomes/chemical synthesis
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