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1.
Braz. J. Pharm. Sci. (Online) ; 58: e18800, 2022. tab, graf, ilus
Article in English | LILACS | ID: biblio-1364431

ABSTRACT

Abstract Efavirenz is one of the most commonly used drugs in HIV therapy. However the low water solubility tends to result in low bioavailability. Drug nanocrystals, should enhance the dissolution and consequently bioavailability. The aim of the present study was to obtain EFV nanocrystals prepared by an antisolvent technique and to further observe possible effect, on the resulting material, due to altering crystallization parameters. A solution containing EFV and a suitable solvent was added to an aqueous solution of particle stabilizers, under high shear agitation. Experimental conditions such as solvent/antisolvent ratio; drug load; solvent supersaturation; change of stabilizer; addition of milling step and solvents of different polarities were evaluated. Suspensions were characterized by particle size and zeta potential. After freeze- dried and the resulting powder was characterized by PXRD, infrared spectroscopy and SEM. Also dissolution profiles were obtained. Many alterations were not effective for enhancing EFV dissolution; some changes did not even produced nanosuspensions while other generated a different solid phase from the polymorph of raw material. Nevertheless reducing EFV load produced enhancement on dissolution profile. The most important modification was adding a milling step after precipitation. The resulting suspension was more uniform and the powder presented grater enhancement of dissolution efficacy.


Subject(s)
Efficacy/classification , HIV/pathogenicity , Crystallization/instrumentation , Dissolution/methods , Particle Size , Solubility , Pharmaceutical Preparations/administration & dosage , Excipients/pharmacology , Dissolution/classification , Nanoparticles/administration & dosage , Methods
2.
Article in Chinese | WPRIM | ID: wpr-888098

ABSTRACT

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


Subject(s)
Drugs, Chinese Herbal , Excipients , Medicine, Chinese Traditional , Viscosity , Water
3.
Article in Chinese | WPRIM | ID: wpr-888097

ABSTRACT

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


Subject(s)
Drugs, Chinese Herbal , Excipients , Hypromellose Derivatives , Medicine, Chinese Traditional , Water
4.
Article in Chinese | WPRIM | ID: wpr-887985

ABSTRACT

With Sangtang Yin granule as model drug,and based on the strategy of " unification of medicines and excipients",the feasibility of preparing high drug loading granules with traditional Chinese medicine( TCM) raw powder as carrier was explored. The powder yield,particle size and particle size distribution,fillibility,flowability,hygroscopicity,reconstituability and other key physical properties relating to preparations of 8 herbs( Dioscoreae Rhizoma,Euryales Semen,Atractylodis Macrocephalae Rhizoma,Coicis semen,Poria,Puerariae Lobatae Radix,Puerariae Thomsonii Radix and Coicis Semen by stir-frying with bran) were studied after being smashed,and the feasibility of taking them as excipients of TCM granules was evaluated by co-spray drying,dry granulation and other preparation techniques. According to the results of the physical properties of raw powders,raw powders of Dioscoreae Rhizoma,Euryales Semen and Puerariae Thomsonii Radix had a high powder yield,uniform particle size distribution,good fillibility,poor hygroscopicity and good reconstitutability,with the feature of assisting granule forming. Compared with the prescription of spray dry powder Sangtang Yin without any excipient,the co-sprayed powder had a high yield,good fillibility and compressibility. The yield of dry granules prepared by co-spraying dry powder was increased by more than 10%,and the particles had a uniform color,good fluidity and dissolubility with the drug-loading rate up to 100%. Based on the physical characteristics of TCM raw powder combined with the analysis of the preparation process,Dioscoreae Rhizoma and Puerariae Thomsonii Radix raw powder were selected as the carriers of granule preparations,and Sangtang Yin granule without any excipient was successfully prepared. The findings provide a feasible idea for the preparation of TCM granules with a high drug loading capacity.


Subject(s)
Excipients , Medicine, Chinese Traditional , Particle Size , Powders , Pueraria , Rhizome
5.
Article in Chinese | WPRIM | ID: wpr-921763

ABSTRACT

Based on the defects in powder properties of the contents of Ziyin Yiwei Capsules, this study screened out the main medicinal slice powders causing the poor powdery properties, and introduced the powder modification process to improve the powdery properties of these slice powders, the pharmaceutical properties of the capsule contents, and the content uniformity of Ziyin Yiwei Capsules, so as to provide a demonstration for the application of powder modification technology to the preparation of Chinese medicinal solid preparations. Through the investigation on the powder properties of the contents of Ziyin Yiwei Capsules, it was clarified that the pulverized particle size of the capsule contents had a good correlation with the pulverization time. According to the measurement results of the powder fluidity and wettability, the quality defects of the capsule contents were caused by the fine powders of Taraxaci Herba and Lungwortlike Herba. "Core-shell" composite particles were prepared from medicinal excipients magnesium stearate and fine powders of Taraxaci Herba and Lungwortlike Herba slices after ultra-fine pulverization to improve the powder properties of the problematic fine powders. Powder characterization data including fluidity and wettability were measured, followed by scanning electron microscopy(SEM) and infrared ray(IR) detection. It was determined that the optimal dosage of magnesium stearate was 2%, and the compositing time was 3 min. The composite particles were then used as content components of the Ziyin Yiwei Capsules. The powder characteristics between the original capsule and the modified composite capsule including the particle size, fluidity, wettability, uniformity of bulk density, and uniformity of chromatism as well as the content uniformity and in vitro dissolution were compared. The results showed that the powder characteristics and content uniformity of the prepared composite capsule were significantly improved, while the material basis of the preparation was not changed before and after modification. The preparation process was proved to be stable and feasible. The powder modification technology solved the pharmaceutical defects that were easy to appear in the preparation of traditional capsules, which has provided experimental evidence for the use of powder modification technology for improving the quality of Chinese medicinal solid preparations and promoting the secondary development and upgrading of traditional Chinese medicinal dosage forms such as capsules.


Subject(s)
Capsules , Excipients , Particle Size , Powders , Wettability
6.
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
7.
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
8.
Article in Chinese | WPRIM | ID: wpr-828357

ABSTRACT

This paper explores Mongolian medicine processing methods and the use regularity of excipient by text mining techniques. Relevant books of Mongolian medicine processing were consulted to collect data on Mongolian medicine processing methods and excipient, and select data based on processing methods and excipient noun frequency statistics. Microsoft Excel 2010 software was used for statistical analysis and mining for the usage regularity of different types of Mongolian medicinal materials in different periods. And Cytoscape 3.6.1 software was used for visual presentation. The topological analysis showed the top five processing methods were net production, development, frying, calcining and cooking, and the top five processing excipient were fresh milk, wine, urine, cream and mineral borax. Frequency analysis showed that the plant medicinal materials were mostly recorded in the 18~(th) and 21~(st) centuries, especially in the 21 st century; the processing methods mostly contained water processing, repair processing and other methods. The mineral medicinal materials were mostly recorded in the 18~(th), 19~(th) and 21~(st) centuries; most of the processing methods were the fire processing method. The animal medicinal materials were recorded in the 18~(th), 19~(th) and 21~(st) century; the fire processing method occupied a major position, and the repair processing and the grinding processing were markedly increased in the 21~(st) century. In the use of excipient, liquid excipient were mostly used in plant medicines. Solid excipient were most commonly used in the 18~(th) century. Animal excipient were mostly used during the processing in the 18~(th) century. The use of liquid excipient gradually increased in the 19~(th) and 21~(st) centuries. This study summarizes the traditional processing methods of Mongolian medicine and the usage regularity of excipient, defines the characteristics of Mongolian medicine processing methods and excipient, and the characteristics of the combination of medicinal materials and excipient, so as to provide reference for the clinical use of Mongolian medicine.


Subject(s)
Data Mining , Excipients , Medicine, Mongolian Traditional , Records , Software
9.
Article in Chinese | WPRIM | ID: wpr-773162

ABSTRACT

Commercially available japonica rice and indica rice with different trade names were collected,and then based on the method of rice stir-frying,their many indexes were evaluated,for example the physical and chemical properties such as appearance color,grain type,broken kernel ratio,length-width ratio,1 000-grain weight,specific heat capacity,moisture content,amylose content,and protein content. The discriminant function analysis was used to determine the effective factors affecting the quality of rice as excipients. The results showed that two types of rice could be distinguished by rice color parameter a*,grain parameter circularity,1 000-grain weight and amylose content. These four effective factors can be used as the quality evaluation indexes for fried rice as excipients.Protein is one of the main components of rice,and its content affects the quality of rice. There is a significant difference in the protein content between japonica rice and indica rice. Therefore,protein content should be used as one of the evaluation indexes for rice quality. After comprehensive consideration,it is suggested that the red-green value a*shall not be less than 0. 50; the circularity not less than 53. 0,the 1 000-grain weight not less than 16. 0 g,the amylose content not less than 12. 0% and the protein content not less than4. 0% in the japonica rice; the red-green value a*shall not be lower than-1. 0,the circularity not less than 41. 0,the 1 000-grain weight not less than 13. 0 g,the amylose content not less than 9. 0% and the protein content not less than 3. 5% in the indica rice. In this study,the quality evaluation standards for rice as excipients( japonica rice,indica rice) were supplemented and improved,laying foundation for the development of quality standards for rice as excipients with the rice stir-frying method.


Subject(s)
Amylose , Cooking , Excipients , Food Quality , Hot Temperature , Oryza , Chemistry
10.
Hig. aliment ; 32(284/285): 128-132, out. 30, 2018. ilus, tab
Article in Portuguese | LILACS | ID: biblio-964418

ABSTRACT

Diversos alimentos são sistemas emulsionados, como a maionese, uma emulsão óleo em água que apresenta 70 a 80% de óleo. Devido à busca crescente do mercado consumidor por produtos mais saudáveis e nutritivos, diversos estudos têm sido realizados com o intuito de substituir e/ou reduzir o teor de alguns ingredientes na formulação de alimentos, em especial a gordura. Diante disso, o objetivo do presente estudo foi desenvolver e avaliar a estabilidade de emulsões tipo maionese contendo óleo de pequi (Caryocar brasiliense), fruto nativo do Cerrado rico em carotenóides, com diferentes concentrações de óleo (65, 45 e 25% m/m). Para as duas formulações com menor teor de óleo foram adicionados, separadamente, agentes espessantes (gomas guar ou xantana). As emulsões obtidas foram avaliadas em termos de sua microestrutura, pH, cor e estabilidade após 5 dias de armazenamento sob refrigeração ou à temperatura ambiente. Verificou-se que as emulsões obtidas apresentaram gotículas de óleo esféricas. Maior número de gotas foi observado na formulação com maior teor de óleo e maior polidispersidade foi percebida nas formulações com menor o teor de óleo. As emulsões apresentaram pH levemente ácido (4,14 a 4,22), sem diferença significativa entre as formulações. As formulações com goma e teor reduzido de óleo apresentaram maior luminosidade (L*) do que a formulação com 65% de óleo de pequi e sem goma. Resultado contrário foi observado para o parâmetro de cor a* (tonalidade de vermelho), o qual foi maior quanto maior o teor de óleo de pequi na formulação. Nenhuma diferença foi observada quanto o parâmetro b*. Não foram observadas alterações visuais nas formulações armazenadas à temperatura ambiente ou sob refrigeração por 5 dias, indicando a estabilidade das emulsões no período e condições avaliadas, exceto para emulsão com menor teor de óleo e presença de goma guar, que apresentou separação de fases após armazenamento à temperatura ambiente.


Several foods are emulsified systems, such as mayonnaise, an oil-inwater emulsion that has 70-80% oil. Due to the growing consumer market for healthier and more nutritious products, several studies have been carried out to replace and/or reduce the content of some ingredients in the formulation in food formulation, especially oil. The objective of the present study was to develop and evaluate the stability of emulsions like mayonnaise containing pequi oil (Caryocar brasiliense), a native fruit of the Cerrado rich in carotenoids, with different oil concentrations (65, 45 and 25%). For the two formulations with lower oil content, thickening agents (guar or xanthan gums) were added separately. The obtained emulsions were evaluated in terms of their microstructure, pH, color and stability after 5 days of storage under refrigeration or at room temperature. The emulsions were found to have spherical oil droplets. Higher number of drops was observed in the formulation with higher oil content, and higher polydispersity was observed in formulations with lower oil content. The emulsions showed slightly acid pH (4.14 to 4.22), with no significant difference between the formulations. The formulations with gum and reduced oil content showed higher brightness (L*) than the formulation with 65% pequi oil and without gum. The opposite result was observed for the color parameter a*, which was higher the higher the pequi oil content in the formulation. No difference was observed for the b* parameter. No visual changes were observed in the formulations stored at room temperature or under refrigeration after 5 days, indicating the stability of the emulsions in the period and conditions evaluated, except for emulsion with lower oil content and presence of guar gum, which presented phase separation after storage at room temperature.


Subject(s)
Oils , Analysis of Variance , Emulsions , Industrialized Foods , Food Analysis , Dietary Fats , Statistical Analysis , Excipients , Food Technology
11.
Biosci. j. (Online) ; 34(4): 1017-1024, july/aug. 2018. tab
Article in English | LILACS | ID: biblio-967196

ABSTRACT

The toxic potential at the cellular level of industrialized Ginkgo biloba L. leaves was evaluated in meristematic cells of Allium cepa at concentrations of 0.1; 0.2 and 0.4 mg/ml. The industrialized products, from four pharmaceutical laboratories, were identified as A, B, C and D. Cell-level toxicity of dehydrated ginkgo leaf tea was also evaluated at concentrations of 0.15; 0.30 and 0.60 mg/ml. Dehydrated products were purchased from herbalists certified by ANVISA. The roots were exposed to teas and processed products for 24 and 48 hours. The results were submitted to the Chi-square test at 5%. However, industrialized ginkgo products at all concentrations caused antiproliferative effect. Also, the products purchased in pharmacies did not induce significant changes to root meristems. Therefore, industrialized ginkgo promoted cytotoxicity, however, they were not genotoxic to the bioassay used.


Avaliou-se, em células meristemáticas de raízes de Allium cepa, o potencial tóxico em nível celular de folhas de Ginkgo biloba L. industrializadas, nas concentrações 0,1; 0,2 e 0,4 mg/mL. Os produtos industrializados, oriundos de quatro laboratórios farmacêuticos, foram identificados como A, B, C e D. Também avaliou-se a toxicidade em nível celular de chás de folhas de ginkgo desidratadas, nas concentrações 0,15; 0,30 e 0,60 mg/mL. Os produtos desidratados foram adquiridos em ervanários certificados pela ANVISA. As raízes ficaram expostas aos chás e produtos industrializados por 24 e 48 horas. Os resultados obtidos foram submetidos ao teste Qui-quadrado, a 5%. No entanto, os produtos de ginkgo industrializados, em todas as concentrações, causaram efeito antiproliferativo. Ainda, os produto adquiridos em farmácias não induziram alterações em número significativo aos meristemas de raízes. Portanto, os ginkgos industrializados promoveram citotoxicidade, porém, não foram genotóxicos frente ao bioensaio utilizado.


Subject(s)
Cell Division , Ginkgo biloba , Excipients , Cytotoxins
12.
Caracas; s.n; 20170000. 90 p. Tablas.
Thesis in Spanish | LILACS, LIVECS | ID: biblio-1367183

ABSTRACT

Al momento de desarrollar un nuevo medicamento, la forma farmacéutica toma gran importancia representando un gran reto, la selección de los excipientes adecuados para obtener un producto que no se vea afectado en sus características organolépticas, ni físico químicas. La Autoridad Regulatoria implementa a través de normas y/o publicaciones oficiales, concentraciones, límites y advertencias para su empleo en la formulación. En el país rigen las Normas de la Junta Revisora de Productos Farmacéuticos, con el fin de obtener productos farmacéuticos que cumplan con estándares de calidad, seguridad y eficacia, lo que implica la necesidad de actualizar las Normas mencionadas, que datan del año 1998, en este estudio, el Capítulo XI "De los excipientes", aplicado a las formas farmacéuticas líquidas orales. La investigación se efectuó mediante análisis de fuentes secundarias de excipientes contemplados en la normativa nacional e internacional, a efecto de determinar comparación y vigencia; una vez analizadas se elaboró una lista en la cual se actualizan los excipientes. Una vez realizada la comparación de las dos listas de excipientes, se identificó los excipientes utilizados a nivel internacional y se procedió a la elaboración de la Lista de Excipientes ajustado a la necesidad actual.


At the time of developing a new drug, the pharmaceutical form is of great importance representing a great challenge, the selection of suitable excipients to obtain a product that is not affected in its organoleptic or physical chemical characteristics. The Regulatory Authority implements, through standards and / or official publications, concentrations, limits and warnings for its use in the formulation. In order to obtain pharmaceutical products that comply with quality, safety and efficacy standards, the Standards of the Pharmaceutical Products Review Board are in place, which implies the need to update the mentioned Standards, which date from 1998, in This study, Chapter XI "Of the excipients", applied to oral liquid pharmaceutical forms. The investigation was carried out by means of analysis of secondary sources of excipients contemplated in the national and international regulations, in order to determine comparison and validity; once analyzed a list was prepared in which the excipients are updated. After comparing the two lists of excipients, the excipients used at the international level were identified and the List of Excipients adjusted to the current need was drawn up.


Subject(s)
Humans , Pharmaceutical Preparations , Enacted Statutes , Products Registration , Excipients , Health Authorities , Legislation, Drug , Health Surveillance , Public Health
13.
Asia Pacific Allergy ; (4): 115-118, 2017.
Article in English | WPRIM | ID: wpr-750094

ABSTRACT

Intralesional triamcinolone acetonide injection is indicated for multiple skin conditions such as keloid scars, alopecia areata, and hypertrophic lichen planus. Immediate hypersensitivity reaction remains uncommon. We report on a 24-year-old woman who had received multiple intralesional injections with triamcinolone acetonide (Kenacort) plus lidocaine for keloid scar treatment without any reaction for the previous 10 years. The immediate reaction occurred 15 minutes after injection, with numbness on her face and 5 minutes later with urticaria on her chest wall and upper extremities, together with hypotension (blood pressure of 90/60 mmHg). Allergology workup revealed positive skin prick test for triamcinolone acetonide (Kenacort). Skin tests for other corticosteroids (hydrocortisone, methylprednisolone, and dexamethasone), excipients (carboxymethylcellulose, benzyl alcohol, and polysorbate 80) and lidocaine were negative, including subcutaneous challenge for lidocaine and oral challenge for carboxymethylcellulose. IgE-mediated hypersensitivity reaction must be considered in cases of multiple applications of triamcinolone acetonide injection.


Subject(s)
Adrenal Cortex Hormones , Alopecia Areata , Anaphylaxis , Benzyl Alcohol , Carboxymethylcellulose Sodium , Cicatrix , Drug Hypersensitivity , Excipients , Female , Humans , Hypersensitivity, Immediate , Hypesthesia , Hypotension , Injections, Intralesional , Keloid , Lichen Planus , Lidocaine , Methylprednisolone , Skin , Skin Tests , Thoracic Wall , Triamcinolone Acetonide , Triamcinolone , Upper Extremity , Urticaria , Young Adult
14.
Braz. j. pharm. sci ; 52(4): 735-740, Oct.-Dec. 2016. tab, graf
Article in English | LILACS | ID: biblio-951887

ABSTRACT

ABSTRACT Polymeric stabilizers have received attention in the preparation of nanostructured systems due to their ability to enhance formulation stability. Considering this, the objective of this work was to prepare poly(ε-caprolactone) nanocapsules using the pullulan as a polymeric stabilizer. The nanocapsules were prepared using the interfacial deposition method of preformed polymers and they were characterized in terms of pH, average diameter, polydispersity index, zeta potential, beclomethasone dipropionate content, encapsulation efficiency, photostability and drug release profiles. The formulations showed physicochemical characteristics consistent with nanocarriers for drug delivery such as: average diameter lower than 270 nm, polydispersity indexes lower than 0.2, negative zeta potential (-22.7 to -26.3 mV) and encapsulation efficiencies close to 100%. In addition, the nanocapsules were able to delay the beclomethasone dipropionate photodegradation under UVC radiation and by the dialysis bag diffusion technique, the nanocapsules were able to prolong the drug release. Thus, pullulan could be considered an interesting excipient to formulate polymeric nanocapsules.


Subject(s)
Polysaccharides/classification , Biological Products/classification , Excipients , Nanocapsules/statistics & numerical data , Drug Delivery Systems , Diffusion
15.
Article in English | WPRIM | ID: wpr-21482

ABSTRACT

PURPOSE: This study aimed to investigate community pharmacists' knowledge and certainty of adverse effects and contraindications of pharmaceutical products to estimate the risk of error. Factors influencing their knowledge and certainty were also investigated. METHODS: The knowledge of community pharmacists was assessed in a cross-sectional design using a multiple-choice questions test on the adverse effects and contraindications of active pharmaceutical ingredients and excipients from May 2014 to March 2015. Self-rated certainty scores were also recorded for each question. Knowledge and certainty scores were combined to estimate the risk of error. RESULTS: Out of 315 subjects, 129 community pharmacists (41.0%) completed the 30 multiple-choice questions test on active ingredients and excipients. Knowledge on active ingredients was associated with the year of graduation and obtaining a licence to practice pharmacy. Knowledge on excipients was associated with the degree obtained. There was higher risk of error in items on excipients than those on ingredients (P<0.01). CONCLUSION: The knowledge of community pharmacists in Palestine was insufficient with high risk of errors. Knowledge of community pharmacists on the safety issues of active ingredients and excipients need to be improved.


Subject(s)
Cross-Sectional Studies , Excipients , Humans , Pharmaceutical Preparations , Pharmaceutical Services , Pharmacists , Pharmacy
16.
Braz. j. pharm. sci ; 51(3): 745-753, July-Sept. 2015. graf
Article in English | LILACS | ID: lil-766324

ABSTRACT

The present study was planned to investigate the influence of polyethylene glycols (PEGs) on the activity and expression of P-glycoprotein (P-gp). Sub-toxic concentrations of PEGs in Caco-2 cells were determined using the MTT test assay. Then the measurement of Rhodamine-123 (Rho-123) uptake, a P-gp fluorescence substrate, in Caco-2 cells confronting PEG 400 (1% and 2% w/v), PEG 4000 (2% and 4% w/v), PEG 6000 (2% and 4% w/v), PEG 10000 (2% and 4% w/v), PEG 15000 (1% and 2% w/v), and PEG 35000 (2% and 4% w/v) overnight was taken to elucidate whether non-toxic concentrations of PEGs are able to impact P-gp activity. Furthermore, western blotting was carried out to investigate P-gp protein expression. The results showed that PEG 400 at concentrations of 1% (w/v) and 2% (w/v) and PEG 6000 at the concentration of 4% (w/v) are notably capable of blocking P-gp. Based on the obtained results it is concluded that the mentioned excipients could be used to obstruct P-gp efflux transporter in order to increase the bioavailability of co-administered substrate drug.


O presente estudo foi planejado para investigar a influência de polietileno glicóis sobre a atividade e expressão da P- glicoproteína (P-gp) . Concentrações sub-tóxicas de PGPs e em células Caco-2 foram determinadas por meio do ensaio de MTT. Em seguida, efetuou-se a a medida de captura de Rodamina-123 (Rho-123), um substrato fluorescente de P-gp, em células Caco-2, confrontando com PEG 400 (1% e 2% m/v), PEG 4000 (2% e 4% m/v) e PEG 6000 (2% e 4% m /v), PEG 10000 (2% e 4% w/v), PEG 15000 (1% e 2% m/v), e PEG 35000 (2% e 4% m/v). Essa medida foi efetuada durante a noite, para saber se as concentrações não tóxicas de excipientes são capazes de influenciar a actividade da P-gp. Além disso, realizou-se o western blotting para investigar a expressão da proteína P-gp. Os resultados mostraram que o PEG 400, nas concentrações de 1% (m/v) e 2% (m/v), e PEG 6000, na concentração de 4% (m/v) são capazes de bloquear P-gp. Com base nos resultados conclui-se que os excipientes mencionados poderiam ser utilizados para obstruir o efluxo por P-gp, a fim de aumentar a biodisponibilidade de do fármaco co-administrado.


Subject(s)
Caco-2 Cells , ATP Binding Cassette Transporter, Subfamily B, Member 1/analysis , Polyethylene Glycols/analysis , Biological Availability , Excipients/classification , Rhodamine 123
17.
Rev. chil. pediatr ; 86(4): 224-235, ago. 2015. ilus
Article in Spanish | LILACS | ID: lil-764078

ABSTRACT

Los pilares terapéuticos del niño con shock séptico se mantienen en el tiempo, sin embargo, se han incorporado nuevos conceptos, siendo importante que el pediatra y el intensivista tengan conocimiento a cabalidad de ellos. La reanimación con fluidos es una intervención fundamental, no obstante, aún no se ha establecido un tipo de fluido ideal, presentando cada uno limitaciones específicas, no existiendo evidencia sobre la superioridad de un tipo de fluido. Si a pesar de una adecuada resucitación con fluidos persiste el shock, el inicio de inótropos y/o vasopresores está indicado. En caso de refractariedad al uso de vasopresores, nuevos fármacos vasoactivos pueden ser empleados y el uso de hidrocortisona debe considerarse en niños con sospecha de insuficiencia suprarrenal. Existe controversia respecto a la transfusión de glóbulos rojos o el nivel óptimo de glucemia, no existiendo consenso en el valor umbral para el uso de estos hemocomponentes o el inicio de insulina, respectivamente. Asimismo, la utilización de la hemofiltración de alto volumen (HFAV)aún permanece controversial, requiriendo mayores estudios para su recomendación en forma rutinaria en el curso de un shock séptico refractario. El soporte nutricional es primordial, ya que la desnutrición es una grave complicación que debe ser prevenida y tratada adecuadamente. El objetivo de la presente revisión es entregar una actualización en los más recientes avances en tratamiento del shock séptico en la población pediátrica.


Essential therapeutic principles in children with septic shock persist over time, although some new concepts have been recently incorporated, and fully awareness of pediatricians and intensivists is essential. Fluid resuscitation is a fundamental intervention, but the kind of ideal fluid has not been established yet, as each of these interventions has specific limitations and there is no evidence supportive of the superiority of one type of fluid. Should septic shock persists despite adequate fluid resuscitation, the use of inotropic medication and/or vasopressors is indicated. New vasoactive drugs can be used in refractory septic shock caused by vasopressors, and the use of hydrocortisone should be considered in children with suspected adrenal insufficiency, as it reduces the need for vasopressors. The indications for red blood cells transfusion or the optimal level of glycemia are still controversial, with no consensus on the threshold value for the use of these blood products or the initiation of insulin administration, respectively. Likewise, the use of high-volume hemofiltration is a controversial issue and further study is needed on the routine recommendation in the course of septic shock. Nutritional support is crucial, as malnutrition is a serious complication that should be properly prevented and treated. The aim of this paper is to provide update on the most recent advances as concerns the treatment of septic shock in the pediatric population.


Subject(s)
Chemistry, Pharmaceutical/methods , Tablets/chemistry , Technology, Pharmaceutical/methods , Bone Screws , Cellulose/chemistry , Desiccation/methods , Excipients/chemistry , Particle Size , Pressure , Starch/analogs & derivatives , Starch/chemistry , Stearic Acids/chemistry , Temperature , Water/chemistry
18.
Braz. j. pharm. sci ; 51(1): 27-33, Jan-Mar/2015. tab, graf
Article in English | LILACS | ID: lil-751352

ABSTRACT

This work reports the preparation of tablets by direct compression of sodium alendronate-loaded microparticles, using pullulan as filler. The tableting properties of pullulan were compared with those of microcrystalline cellulose and lactose. Pullulan tablets showed low variations in average weight, thickness and drug content. Moreover, these tablets exhibited a higher hardness compared to the other excipients. In vitro release studies showed that only pullulan was capable to maintain gastroresistance and release properties of microparticles, due to its ability to protect particles against damage caused by compression force. Thus, pullulan was considered an advantageous excipient to prepare tableted microparticles.


Neste trabalho relata-se a preparação de comprimidos pela compressão direta de micropartículas contendo alendronato de sódio, utilizando o pullulan como diluente. As propriedades dos comprimidos de pullulan foram comparadas com as de comprimidos de celulose microcristalina e de lactose. Os comprimidos de pullulan mostraram baixa variação no peso médio, espessura e teor. Por outro lado, estes apresentaram altos valores de dureza comparados aos preparados com os outros excipientes. Através dos estudos de liberação in vitro pode-se observar que apenas o pullulan foi capaz de manter a gastrorresistência e as propriedades de liberação das micropartículas, o que se deve à sua capacidade de proteger as partículas do dano causado pela força de compressão. Dessa forma, o pullulan foi considerado um excipiente vantajoso para a preparação de comprimidos microparticulados.


Subject(s)
Alendronate/pharmacokinetics , Excipients/classification , Polysaccharides/classification , Tablets/pharmacokinetics , Solid Waste Grinding
19.
Braz. j. pharm. sci ; 51(1): 155-171, Jan-Mar/2015. tab, graf
Article in English | LILACS | ID: lil-751368

ABSTRACT

Specific values of technological properties of excipients allow the establishment of numerical parameters to define and compare their functionality. This study investigates the functionality of Polyplasdones XL and XL10. Parameters studied included tablet disintegration profiles, compactibility profiles and powder flow. The results allowed the establishment of quantitative surrogate functionalities of technological performance, such as absolute number, and as a value relative to the known microcrystalline cellulose type 102. Moreover, the establishment of an explicit functionality to improve the technological performance of two diluents and a model drug was investigated, as was setting up of these functionalities, as quantitative values, to determine the input variables of each material and its probable functionality in a drug product. Disintegration times of pure Polyplasdone XL and its admixtures were around half that of Polyplasdone XL10. The improvement in tablet compactibility was 25-50% greater for Polyplasdone XL10 than Polyplasdone XL. Crospovidones proportions of up to 10% have little effect on the flow properties of other powders, although pure Polyplasdone XL10 and its admixtures display compressibility indexes about 20% greater than Polyplasdone XL. The observed results are in line with a smaller particle size of Polyplasdone XL10 compared to Polyplasdone XL.


Os valores específicos de propriedades tecnológicas de excipientes permitem o estabelecimento de parâmetros numéricos para definir e comparar a sua funcionalidade. Este estudo investiga a funcionalidade dos excipientes. Os parâmetros estudados foram perfis de desintegração dos comprimidos, perfis de compactação e fluxo de pó. Os resultados permitiram expressar o desempenho tecnológico através de valores absolutos e valores relativos à conhecida celulose microcristalina tipo 102. Do mesmo modo, permitiram estabelecer uma funcionalidade explícita para melhorar o desempenho tecnológico de dois diluentes e um fármaco modelo. A criação destas funcionalidades, como valores quantitativos, permite conhecer as variáveis de entrada de cada material e sua provável funcionalidade em um medicamento. Os tempos de desintegração do Poliplasdone XL e das suas misturas são cerca da metade do observado para as misturas com o Poliplasdone XL10. Melhoria da compressão de comprimidos que contêm Polyplasdone XL10 é 25-50% maior do que o Polyplasdone XL. Crospovidonas em proporções de até 10% têm pouco efeito sobre as propriedades de fluxo dos outros pós embora o Poliplasdone XL10 e suas misturas exibam índices de compressibilidade cerca de 20% maior do que o Poliplasdone XL. Os resultados observados estão em sintonia com o menor tamanho de partícula do Poliplasdone XL10, em comparação com o Poliplasdone XL.


Subject(s)
Excipients , International Classification of Functioning, Disability and Health/classification , Tablets/analysis , Stearates/analysis , Tablets/pharmacokinetics
20.
Acta Pharmaceutica Sinica ; (12): 1342-1345, 2015.
Article in Chinese | WPRIM | ID: wpr-320079

ABSTRACT

To study the effects of surfactants on wettability of excipients, the contact angles of six types of surfactants on the surface of two common excipients and mixture of three surfactants with excipients were measured using hypsometry method. The results demonstrated that contact angle of water on the surface of excipients was associated with hydrophilcity of excipients. Contact angle was lowered with increase in hydrophilic groups of excipient molecules. The sequence of contact angle from small to large was starch < sodium benzoate < polyvinylpyrrolidone < sodium carboxymethylcellulose < sodium alginate < chitosan < hydroxypropyl methyl cellulose <magnesium stearate. In addition, surfactants both in droplets and mixed in excipients significantly reduced the contact angle of excipients, and their abilities to lower contact angle varied. The results of the present study offer a guideline in the formulation design of tablets.


Subject(s)
Chemistry, Pharmaceutical , Excipients , Chemistry , Hydrophobic and Hydrophilic Interactions , Surface-Active Agents , Chemistry , Tablets , Water , Wettability
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