Formulation and evaluation of osmotic drug delivery system of ibuprofen

The authors are thankful to Mr.S.Sriram Ashok B.E, Correspondent, Sankaralingam Bhuvaneswari College of Pharmacy, Anaikuttam, Sivakasi, for providing necessary facilities to carry out the work.Aim: The present work was aimed to formulate and evaluate osmotic pump delivery system of Ibuprofen to provide a uniform concentration of drug at the absorption site and thereby maintain the plasma concentration within therapeutic range, which minimizes side effects and reduces the frequency of administration. Material and Methods: In the present work, 5 formulations (F1 to F5)of Ibuprofen osmotic drug delivery systems(ODDS) were prepared using two osmogens (NaCl and KCL) in two concentrations and a control F6 (without osmogens) by wet granulation technique. The excipients used in this study did not alter physicochemical properties of the drug, as tested by FTIR. Prior to compression, the prepared granules were evaluated for flow and compression characteristics. After compression, the tablets were evaluated for hardness, thickness, weight variation, friability, percentage of weight gain, drug content, in vitro release and stability studies. Results: The results revealed that the pre-compression and post-compression parameters are within the limits. Among all the formulations, F3 showed a controlled drug release of 63.54% at the end of 10th hour. The results of optimized formulation (F3) subjected to stability studies for 60 days at 27º±2ºC/60 ± 5% RH and 50º±2ºC/75 ± 5% RH showed that there was no significant change in the drug content and percentage drug release and the product was stable even after 2 months. Conclusions: From the study, it was concluded that Ibuprofen osmotic pump tablet prepared with potassium chloride (10%) as osmogent and cellulose acetate as coating polymer may be considered as a suitable alternative to currently available formulations of Ibuprofen.Objetivos: El objetivo del presente trabajo ha sido formular y evaluar el sistema de suministro de ibuprofeno mediante bomba osmótica para proporcionar una concentración uniforme de fármaco en el sitio de absorción y por lo tanto mantener la concentración plasmática dentro del intervalo terapéutico, lo que minimiza los efectos secundarios y reduce la frecuencia de administración. Material y Métodos: En el presente trabajo, 5 formulaciones (F1 a F5) de sistemas de administración de ibuprofeno osmótico (odds) se prepararon utilizando dos osmoagentes (NaCl y KCl) en dos concentraciones y un control (F6) (sin osmoagentes) por la técnica de granulación en húmedo. Los excipientes utilizados en este estudio no alteran las propiedades fisicoquímicas del fármaco, según lo testado por FTIR. Antes de la compresión, los gránulos preparados se evaluaron para la fluidez y la compresión. Después de la compresión, los comprimidos se evaluaron para la dureza, espesor, variación de peso, la friabilidad, el porcentaje de ganancia de peso, contenido de fármaco, la liberación in vitro y estudios de estabilidad. Resultados: Los resultados revelaron que los parámetros pre y post-compresión están dentro de los límites. Entre todas las formulaciones, F3 mostró una liberación controlada de fármacos de 63,54% al final de la décima hora. Los resultados de formulación optimizada (F3) sometido a estudios de estabilidad durante 60 días a 27º ± 2 °C/60 ± 5% HR y 50±2 °C/75 ± 5% HR mostraron que no hubo ningún cambio significativo en el contenido de fármaco y el porcentaje de liberación del fármaco y el producto fue estable incluso después de 2 meses. Conclusiones: En el estudio, se llegó a la conclusión de que la tableta de bomba osmótica ibuprofeno preparado con cloruro de potasio (10%) como osmoagente y acetato de celulosa como el polímero de revestimiento puede ser considerado como una alternativa adecuada actualmente disponibles para la formulaciones de ibuprofeno.Fund granted by College management and the research work was approved for the award of Degree of Master of pharmacy by The Tamilnadu Dr.MGR Medical University, Chennai, Indi

GASTRO RETENTIVE NON-FLOATING DRUG DELIVERY APPROACH: A REVIEW

Gastro retardation is attractive approach to enhance bioavailability of narrow absorption window drugs. Drug retardation in stomach is more beneficial for certain gastro intestinal disorders like gastro esophageal reflex disease, ulcer and other gastro intestinal conditions. Gastric site retardation is one of the challenging technique, however various techniques are applied to keep the drug and achieve the enhancement of bioavailability. To achieve gastro retentive commonly two approaches are considered, they are floating drug delivery system and non-floating gastro retentive drug delivery system. The floating drug made-up by low density polymers, this approach was not fit many of the drug molecule and floating drug has some limitations like sufficient level fluids in stomach and not to be dosed just before going to bed. In this review describe the various high density (sinking) system (non-floating) drug delivery systems like super porous hydrogels, expanding system, bio/mucoadhesives system, and magnetic system and mechanism, desirable drug characters, advantages and disadvantages. Keyword: Bioavailability, gastro retentive, magnetic system, mucoadhesive, non-floating and sinking system

Formulation and In-vitro evaluation of liposomal drug delivery system of metformin HCl

Metformin is widely used for the treatment of diabetes; the intention of the present study was to formulate Metformin HCl liposomes for a sustained drug delivery system. It have the advantages of dose reduction, less dosing frequency, minimize the side effect, prolong the action of drug and thus achieve better patient compliance. The liposomes were prepared by physical dispersion and ether injection method. Soya lecithin and cholesterol were used for encapsulating the drug, it facilitates to release the medicaments in sustained manner. Chloroform, ether and methanol were used as a solvent. Phosphate buffer pH 6.8 was used as a hydration medium for loading the drug. The final liposome was evaluated in various quality parameters of drug entrapment efficiency, morphological analysis, particle size analysis, in-vitro drug release studies and stability studies. In the two methods of metformin liposome formulation the ether injection method showed prolonged action when compared to physical dispersion method. In the parameters of drug entrapment and stability physical dispersion method was shows better results. Keywords: Physical dispersion, ether injection, soya lecithin, cholesterol, morphological analysis, metformin

New method of predicting optimum surfactant structure for EOR

textChemical enhanced oil recovery (CEOR) has gained a rapid momentum in the recent past due to depleting reserves of “easy-oil” and soaring oil prices. Hence, CEOR is now being considered for several candidates with varied oils and reservoir conditions, which demands the need for large hydrophobe surfactants. A new class of thermally and chemically stable large hydrophobe surfactant, Guerbet alkoxy carboxylates (GAC) has been tested. Unlike Guerbet alkoxy sulfates, GAC are stable at all pH and can be extremely useful in cases where alkali usage is prohibitive. They also exhibit synergistic behavior with internal olefin sulfonates (IOS) and alkyl benzene sulfonates (ABS), with the mixture showing enhanced calcium tolerance than the individual surfactants. Furthermore, in an attempt to diversify the raw material base, a new class of hydrophobe, viz. tristyrylphenol (TSP) based on petrochemical feed stock has also been developed and evaluated. Given the fact that there are hundreds of surfactants that can be tested for a particular candidate, the difficulty often lies in choosing the right surfactant to begin with. In an attempt to simplify that, a new correlation to predict the optimum surfactant structure has been developed. It relates the optimum surfactant structure to the formulation variables like oil properties, salinity, and temperature, including the parameters like PO and EO for new-generation surfactants. The correlation can serve as a guideline in choosing the optimum surfactant and will help in improving our understanding of the relationship among variables affecting the optimum surfactant structure. Surfactant retention is an important factor affecting the economics of chemical flooding and has to be studied carefully. Using an extensive data obtained from core flood studies a new correlation for predicting surfactant retention including the variables like pH, TAN, salinity, mobility ratio, temperature, co-solvent, and surfactant molecular weight has been developed. All these are new and highly significant advance in the optimization of chemical EOR processes that will greatly reduce the time and cost of the effort required to develop a good formulation as well as to improve its performance.Petroleum and Geosystems Engineerin

Adsorption of Methylene Blue, Bromophenol Blue, and Coomassie Brilliant Blue by α-chitin nanoparticles

Expelling of dyestuff into water resource system causes major thread to the environment. Adsorption is the cost effective and potential method to remove the dyes from the effluents. Therefore, an attempt was made to study the adsorption of dyestuff (Methylene Blue (MB), Bromophenol Blue (BPB) and Coomassie Brilliant Blue (CBB)) by α-chitin nanoparticles (CNP) prepared from Penaeus monodon (Fabricius, 1798) shell waste. On contrary to the most recognizable adsorption studies using chitin, this is the first study using unique nanoparticles of ⩽50 nm used for the dye adsorption process. The results showed that the adsorption process increased with increase in the concentration of CNP, contact time and temperature with the dyestuff, whereas the adsorption process decreased with increase in the initial dye concentration and strong acidic pH. The results from Fourier transform infrared (FTIR) spectroscopy confirmed that the interaction between dyestuff and CNP involved physical adsorption. The adsorption process obeys Langmuir isotherm (R2 values were 0.992, 0.999 and 0.992 for MB, BPB and CBB, and RL value lies between 0 and 1 for all the three dyes) and pseudo second order kinetics (R2 values were 0.996, 0.999 and 0.996 for MB, BPB and CBB) more effectively. The isotherm and kinetic models confirmed that CNP can be used as a suitable adsorbent material for the removal of dyestuff from effluents

Formulación y evaluación de sistema de liberación osmotica de ibuprofeno

Aim: The present work was aimed to formulate and evaluate osmotic pump delivery system of Ibuprofen to provide a uniform concentration of drug at the absorption site and thereby maintain the plasma concentration within therapeutic range, which minimizes side effects and reduces the frequency of administration.Material and Methods: In the present work, 5 formulations (F1 to F5)of Ibuprofen osmotic drug delivery systems(ODDS) were prepared using two osmogens (NaCl and KCL) in two concentrations and a control F6 (without osmogens) by wet granulation technique. The excipients used in this study did not alter physicochemical properties of the drug, as tested by FTIR. Prior to compression, the prepared granules were evaluated for flow and compression characteristics. After compression, the tablets were evaluated for hardness, thickness, weight variation, friability, percentage of weight gain, drug content, in vitro release and stability studies.Results: The results revealed that the pre-compression and post-compression parameters are within the limits. Among all the formulations, F3 showed a controlled drug release of 63.54% at the end of 10th hour. The results of optimized formulation (F3) subjected to stability studies for 60 days at 27º±2ºC/60 ± 5% RH and 50º±2ºC/75 ± 5% RH showed that there was no significant change in the drug content and percentage drug release and the product was stable even after 2 months.Conclusions: From the study, it was concluded that Ibuprofen osmotic pump tablet prepared with potassium chloride (10%) as osmogent and cellulose acetate as coating polymer may be considered as a suitable alternative to currently available formulations of Ibuprofen.Objetivos: El objetivo del presente trabajo ha sido formular y evaluar el sistema de suministro de ibuprofeno mediante bomba osmótica para proporcionar una concentración uniforme de fármaco en el sitio de absorción y por lo tanto mantener la concentración plasmática dentro del intervalo terapéutico, lo que minimiza los efectos secundarios y reduce la frecuencia de administración.Material y Métodos: En el presente trabajo, 5 formulaciones (F1 a F5) de sistemas de administración de ibuprofeno osmótico (odds) se prepararon utilizando dos osmoagentes (NaCl y KCl) en dos concentraciones y un control (F6) (sin osmoagentes) por la técnica de granulación en húmedo. Los excipientes utilizados en este estudio no alteran las propiedades fisicoquímicas del fármaco, según lo testado por FTIR. Antes de la compresión, los gránulos preparados se evaluaron para la fluidez y la compresión. Después de la compresión, los comprimidos se evaluaron para la dureza, espesor, variación de peso, la friabilidad, el porcentaje de ganancia de peso, contenido de fármaco, la liberación in vitro y estudios de estabilidad.Resultados: Los resultados revelaron que los parámetros pre y post-compresión están dentro de los límites. Entre todas las formulaciones, F3 mostró una liberación controlada de fármacos de 63,54% al final de la décima hora. Los resultados de formulación optimizada (F3) sometido a estudios de estabilidad durante 60 días a 27º ± 2 °C/60 ± 5% HR y 50±2 °C/75 ± 5% HR mostraron que no hubo ningún cambio significativo en el contenido de fármaco y el porcentaje de liberación del fármaco y el producto fue estable incluso después de 2 meses.Conclusiones: En el estudio, se llegó a la conclusión de que la tableta de bomba osmótica ibuprofeno preparado con cloruro de potasio (10%) como osmoagente y acetato de celulosa como el polímero de revestimiento puede ser considerado como una alternativa adecuada actualmente disponibles para la formulaciones de ibuprofeno

Screening and Regulation Mechanism of Key Transcription Factors of <i>Penicillium expansum</i> Infecting Postharvest Pears by ATAC-Seq Analysis

Transcription factors play a key role in Penicillium expansum infection process. Although the crucial characteristics of some transcription factors of pathogenic fungi have been found, many transcription factors involved in P. expansum infections have not been explored and studied. This study aimed to screen the transcription factors of P. expansum involved in postharvest pear infections by ATAC-seq analysis and to analyze the differentially expressed peak-related genes by GO enrichment and KEGG pathway analysis. Our results found the up-regulation of differentially expressed peak-related genes involved in the MAPK signaling pathway, pentose phosphate pathway, starch and sucrose metabolism, and pentose and glucuronate interconversions. Our study especially confirmed the differential regulation of transcription factors MCM1, Ste12 and gene WSC in the MAPK signaling pathway and PG1, RPE1 in the pentose and glucuronate interconversions pathway. These transcription factors and related genes might play an essential role in pear fruit infection by P. expansum. RT-qPCR validation of twelve expressed peak-related genes in P. expansum showed that the expression levels of these twelve genes were compatible with the ATAC-Seq. Our findings might shed some light on the regulatory molecular networks consisting of transcription factors that engaged in P. expansum invasion and infection of pear fruits

Microclimatic parameters affect Cladosporium rot development and berry quality in table grapes

Cladosporium cladosporioides is an emerging pathogenic fungus that causes Cladosporium rot in postharvest table grapes (Vitis vinifera). However, studies investigating the infection process of C. cladosporioides are lacking. Therefore, this study aimed to elucidate the infection process by investigating the influence of microclimatic parameters (temperature, wetness and fungal age) in C. cladosporioides pathogenesis, activities of grape defense-related enzymes and grape quality during the infection. C. cladosporioides effectively infects grapes by developing distinct colonies on the artificial wounds and berry surfaces, completing its life cycle within 48 h. The C. cladosporioides disease incidence optimally occurred at 20 °C and 25 °C. Wetness played an influential role in the infectivity of C. cladosporioides and 7-day-old C. cladosporioides resulted in the most serious disease incidence of table grapes. As a result of infection, the quality of grapes was affected, including berry weight, pH, titratable acidity (TA), total soluble solids (TSS), and ascorbic acid level. This infection also induced defense-related enzymes, including polyphenoloxidase (PPO), peroxidase (POD), phenylalanine ammonialyase (PAL), and catalase (CAT), at certain times. The findings of this study demonstrated that Cladosporium rot development depended on the microclimatic parameters of grapes, significantly affected the grape quality and induced grape's defense-related enzymes