Lubricating effects of cocoa butter and coconut oil in conventional paracetamol tablets

Background: Due to chemical instability of some Active Pharmaceutical Ingredients often caused by magnesium stearate and its impurities, it is expedient to research into some other materials especially of natural origin, which would probably exhibit better lubricating activity, chemically inactive, less bioactive and less prohibitive.Objective: This work is designed to examine the lubricating properties of cocoa butter and coconut oil as alternative lubricants in comparison with conventional lubricant - magnesium stearate at different concentrations in paracetamol tablets. Materials and Methods: Cocoa butter was extracted from the seeds of Theobroma cacao and coconut oil from the meat of matured coconuts harvested from the coconuts palm (Cocos nucifera).Physicochemical evaluation was carried out on the extracted oils. Thirteen different formulations were prepared using different lubricants; magnesium stearate, cocoa butter and coconut oil at 0 ­ 4 %w/w concentrations. The prepared granules were evaluated for various pre-compression characteristics (bulk density, tapped density, angle of repose, Hausner's quotient and Carr's index) and post-compression characteristics (weight variation, friability, hardness, disintegration and dissolution times).Results: Most of the values obtained from the evaluation of pre- and post- compression characteristics correlate with the pharmacopoeial limits. The values of disintegration time were observed to increase as the lubricant concentration increased but no direct relationship with dissolution time. Tablet hardness values decreased while friability increased as the lubricant concentration increased for all the batches. From the study, cocoa butter and coconut oil at 2 ­ 4 % exhibited effective lubricating effect in the formulation of paracetamol tablet with respect to their values of weight variation, friability, hardness, disintegration and dissolution times.Conclusion: Cocoa butter and coconut oil could be employed as good alternative lubricants to the conventional ones in pharmaceutical tablet formulation

Contrasting the crospovidones functionality as excipients for direct compression

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.

Isolation of hydrocarbonoclastic bacteria from bilge oil contaminated water

Two bacterial strains, i.e. Pseudomonas mendocina and Ochrobactnim sp. were isolated from bilge oil contaminated water of Mormugao harbour, Goa, India and grown in a culture medium with hexadecane as the sole carbon source. Pseudomonas mendocina was used in further studies as it was the dominant strain. This strain effectively degraded tetradecane, hexadecane and octadecane leaving a residual concentration of about 73%, 54% and 40% respectively in 120 h. Sequence analysis of the dominant bands from the denaturing gradient gel electrophoresis profiles revealed the differences between the genera of bilge oil contaminated sea water and its enrichment culture on hexadecane indicating a shift in community structure based on the type of substrate available. Pseudomonas mendocina amplified for the following catabolic genes namely C23O, nid and ndo. Based on the catabolic gene study the potential of the bacterial strain isolated, i.e. Pseudomonas mendocina seems to be interesting as it will be able to degrade polyaromatic hydrocarbons as well. Physicochemical properties of Pseudomonas mendocina indicates production of exopolysaccharides based on the value of its isoelectric point

Enzyme-catalyzed synthesis of ASGPR ligand-targeted modifier in non-aqueous medium / 药学学报

The asialoglycoprotein receptor (ASGPR) was used to mediate drug carrier for hepatic targeted drug delivery, this article showed the enzyme-catalyzed esterification of galactose and vinyl stearate and a kind of ASGPR ligand-targeted which was used to insert the surface of liposome has been synthesized. The structure of product has been confirmed by TLC, ESI-MS and 1H NMR. The factors of types and quantity of enzyme, organic solvents, molar ratio of substrate, temperature and time of reaction have been studied. Results showed when using acetone as reaction medium, the quantity of Novozym 435 immobilized lipase was 30 mg mL(-1), molar ratio of galactose to vinyl stearate was 1:5, and reacted at 60 degrees C for 12 h, the transformation of vinyl stearate reached more than 70%. This study provides a novel and efficient route to the synthesis of ligand-targeted modifier.

Mini-Transthoracic Supradiaphragmatic Approach to the Thoracolumbar Junction

Anterior reconstruction with instrumentation of the thoracolumbar junction (TLJ) offers: 1) the biomechanical advantage of immediate restoration of the load-bearing anterior column and 2) the ideal biological milieu for an optimal arthrodesis. The authors describe the mini-transthoracic supradiaphragmatic (MTTS) approach to the TLJ. Its technical feasibility is compared with that of the traditional transdiaphragmatic and thoracoscopic supradiaphragmatic approaches to this area of the spine. This technique was performed in 21 patients from 2004 to 2006. There were no surgical mortalities. The MTTS approach without the use of a thoracoscope was successfully employed in this study to treat patients with various lesions located at the TLJ. The diaphragmatic opening, even at its smallest diameter, provides excellent views of the operative field and avoids the significant morbidities associated with the traditional transdiaphragmatic approach.

Estudo descritivo sobre a antibioticoprofilaxia na rupturaprematura pré-termo de membranas / Perinatal results of antibioticprophyxalis with erythromycin in preterm premature rupture of the membranes

Objetivo: avaliar os resultados perinatais do uso profilático de estearato de eritromicina nas pacientesinternadas na unidade de gestação alto risco da Maternidade Carmela Dutra (MCD), Florianópolis–SC, com diagnóstico de ruptura prematura pré-termo de membranas (RPM). Métodos: estudo descritivo com análise de todas as pacientes internadas com o diagnóstico de RPM e com idade gestacional entre 20 semanas e 33 semanas e cinco dias. Foram excluídas da pesquisa gestantes com históriade hipersensibilidade à eritromicina, com sinais clínicos e/ou laboratoriais de corioamnionite, que estavam emtrabalho de parto ou que faziam uso de antibióticos no momento da internação. A amostra obtida entre 1º de abril de 2007 e 15 de maio de 2008 foi de 22 pacientes. Resultados e conclusões: o tempo médio de latência foi de 12 dias. Não houve casos confirmados decorioamnionite. Uma (4,54%) gestante desenvolveu quadro de endometrite puerperal. Não houve óbitos maternos. Dois (9,09%) recém-nascidos desenvolveram sepse. A taxa de óbito neonatal foi de 13,63%. Apesarda nossa pequena casuística, o uso de eritromicina nas pacientes com RPM parece estar associado a umadiminuição na taxa de corioamnionite.

Objective: The purposes of this study were to evaluate perinatal results of the prophylactic use of erythromycin to patients admitted in the high-riskgestation unit at Carmela Dutra Maternity Hospital, Florianópolis – SC with preterm premature rupture ofmembranes (PROM). Methods: We performed a descriptive analysis ofall patients with PROM and gestational age between 20 weeks and 33 weeks plus 5 days. Patients with erythromycin allergy, with chorioamnionitis signs orwomen who already being prescribed antibiotics were excluded from this study. Enrolment was from April 1,2007, until May 15, 2008. Twenty-two women had been followed up in this study. Results and Conclusions: The medium latency period was 12 days. There was not confirmed chorioamnionitis case. The occurrence of endometritis was 4,54%. There was not maternal death. The occurrence of neonatal sepsis was 9,09% and theoccurrence of neonatal deaths was 13,63%. Despite our small casuistry, the prophylactic use of erythromycinseems to reduce the chorioamnionitis rate.

The efficacy of erythromycin stearate in guttate psoriasis: A randomized, double-blind, placebo-controlled trial

Erythromycin is known to have both antibiotic and anti-inflammatory activity. It has been used to treat guttate psoriasis. A double-blind, placebo controlled trial was performed using 34 patients with guttate psoriasis at the Out Patient Department of the Philippine General Hospital. Each patient received either placebo or erythromycin stearate 1g in divided doses for 14 days. The response was graded according to the percentage change in Psoriasis Activity and Severity Index (PASI) score after 2 weeks. The results reveal similar baseline demographic characteristics between two treatment groups. After 2 weeks, the average PASI score change improved in the placebo group (9.1 to 8.5) and worsened in the treatment group (9.1 to 11.3). Using the two sample t-tests, there was no significant difference between the to treatment groups in terms of PASI score after 2 weeks. Thus, at present we cannot recommend antibiotic monotherapy in patients with guttate psoriasis.

Studies on chemical constituents of green algae Ulva pertusa / 中国中药杂志

<p><b>OBJECTIVE</b>To study the compounds from Ulva pertusa.</p><p><b>METHOD</b>The alga was extracted with ethanol, isolated and purified by column chromatography on silica gel and sephadex LH -20. All the compounds were identified on the basis of spectral analysis (including IR, MS, NMR).</p><p><b>RESULT</b>Seven compounds were elucidated as cis-asarone (1), trans-asarone (2), gamma-asarone (3), trans-phytol (4), phytyl-stearate (5), phytyl-acetate (6), isophytol (7).</p><p><b>CONCLUSION</b>All other compounds were isolated for the first time from U. pertusa, except for the compound 4.</p>

Quantitative characterization of adsorbed bovine serum albumin on modified surfaces of poly(ether urethane) materials using ATR-FT-IR spectroscopy / 生物医学工程学杂志

Attenuated total reflection (ATR) FT-IR spectroscopy was used to quantitatively characterize the extent of bovine serum albumin (BSA) adsorbed on the surface-coating-modified poly(ether urethane) (PEU) matrix. The two surface modifying additives (SMA) were respectively a tri-block-coupling-polymer of stearyl poly (ethylene oxide)-4,4'-methylene diphenyl diisocyanate-stearyl poly(ethylene oxide), for short MSPEO, and another similar block-coupling polymer with the Cibacron Blue F3G-A endgroups, for short cibaMPEO. The experiments of static BSA adsorption were composed by two parts. One was static isothermal adsorption, and the other was static adsorption kinetics. The quantitative characterization was based on the optical principles of FT-IR, method of experiment and index of the apparatus, by which the enhancement of BSA adsorption on the SMA-modified surfaces was confirmed.

Estudo químico das cascas do caule de Ziziphus joazeiro Martius / Chemical constituents of stem bark of Ziziphus joazeiro Martius

Nas identificacöes de lupeol, ácido betúlinico, cafeína e estearato de glicerila, isolados das cascas do caule de Ziziphus joazeiro Martius, empregaram-se além de técnicas espectroscópicas usuais, observaçöes anotadas durante o processo de extraçäo, isolamento e purificaçäo dessas substâncias. Análise cromatográfica frente a padräo autêntico foi, também, utilizada.

Tensoativos nao ionicos na estabilidade das suspensoes de estearato e palmitato de cloranfenicol e estearato e estolato de eritromicina / Nonionic surfactants on the suspensions stability of chloramphenicol stearate and chloramphenicol palmitate and erythromycin stearate and erythromycin estolate

A homogeneidade das suspensoes farmaceuticas e de importancia fundamental na terapeutica, no aspecto da correta e constante dosagem a cada administracao. A influencia dos tensoativos nao ionicos foi estudada na estabilidade das suspensoes de estearato e palmitato de cloranfenicol e estearato e estolato de eritromicina. Os tensoativos utilizados nas formulacoes foram na forma nao associada ("polisorbato 20, polisorbato 40, polisorbato 60, polisorbato 80") e associada ("span"/polisorbato 20, "span"/polisorbato 40, "span"/polisorbato 60, "span"/polisorbato 80) com os niveis de E.H.L. (equilibrio hidrofilo-lipofilo) de 10, 11, 12, 13, 14, 14,9, 15, 15,6 e 16,7. A estabilidade das preparacoes foi avaliada por meio dos seguintes parametros: valor de pH; densidade; viscosidade; aspectos do sobrenadante e sedimento; tempo de ressuspensao; volume de sedimento; e teor dos farmacos. O periodo de observacao foi de 15 semanas para a primeira e segunda etapa e de 52 semanas para a terceira. Na analise dos resultados aplicou-se estudo estatistico que indicou haver interacoes entre as variaveis. Em relacao aos parametros analiticos houve influencia dos farmacos suspensos dos tensoativos e dos valores de E.H.L. As caracteristicas fisicas mais influenciadas foram viscosidade, volume de sedimento e ressuspensao

Assessment of Occupational Exposure to Cadmium in Korea / 대한산업의학회지

Twenty-four factories registered at the Ministry of Labor as factories using or producing cadmium in 1991 were investigated to know the present state of occupational exposure to cadmium in 1992. Nine factories among 24 stopped using or changed to other substances and 1 factory didn't produce any more, but delivered it to other factories through imports. Therefore, only 14 factories were producing or using cadmium. But, alloying materials were uspplied to about 20 and more factories, however, they couldn't be investigated because of limited information. Three factories had less than 50 workers were 3, 6 had 50-300 and 5 had more than 300. About 167 workers were exposed to cadmium. According to the classification by process, there were 4 alloy processes, 2 refinary, 2 elctroplating, 2 dry cell making, 1 industrial battery and 1 copper refinary. 8 factories used metal cadmium, 3 cadmium oxide, 2 cadmium sulfide, and 1 cadmium hyroxide. One factory was importing cadmium stearates only and supplying them to the PVC making factories. The amount of metal cadmium producing in 2 refinary factories was about 50-65 ton per month. The other cadmium compounds were imported. According to exposure level of cadmium in air of the 10 factories examined, each factory could be divided into high, moderate and low exposure groups. 1 battery recycling factory and 3 alloy factories were in the high exposure group and their mean air concentrations were 0.06679, 0.05481, 0.02492, and 0.003mg/m3, respectively. Refinary and industrial battery making factories were in the middle exposure group and their mean air concentrations were 0.00773 and 0.00613 mg/m3, respectively. Finally, low exposure group were copper smelting, dry cell case making, duplicator drum making and electroplating factory and their mean air concentrations were 0.00096, 0.00071, 0.00057 and 0.00054 mg/m3 respectively.