VERSATILE RP-HPLC METHOD DEVELOPMENT FOR QUANTITATIVE ESTIMATION OF TELMISARTAN AND RAMIPRIL IN ANIMAL PLASMA

Objective: A fast, specific, and sensitive high-performance liquid chromatographic method has been developed and validated for the quantitative determination of unchanged Ramipril (RAM) and Telmisartan (TEL) in animal plasma.Methods: Analytes were extracted from animal plasma, 250 µl of animal plasma sample were mixed with internal working standard (25 ngmL-1) with the further addition of chloroform (HPLC Grade, Merck). The clear organic layer was separated and reconstituted to 1 ml in mobile phase and analysed by HPLC. The method was validated and evaluated in terms of linearity, accuracy, precision, specificity, limit of detection and limit of quantitation.Results: Absorption maxima of TEL and RAM was found to be 270 and 273 nm respectively. TEL and RAM with their respective internal standards (I. S.) were found to be well separated from the co-eluted components and there were no interferences from the endogenous material. The limit of detection (LOD) and limit of quantitation (LOQ) were found to be 2.01±.05; 4.88±0.10 and 0.11 and 0.25 for TEL and RAM respectively on the basis of a signal to noise ratio. The ruggedness of the method at various parameters was found to be±1.94% and±1.02% for TEL and RAM respectively. The low values of %RSD (<2.0) for each of the drug proposed that during all deliberate variations, middle-quality control (MQC) was not affected and it was in accordance with that of actual.Conclusion: Thus developed High-Performance Liquid Chromatography (HPLC) method was found to be more accurate, precise, sensitive, selective and reproducible

Extended release promethazine HCl using acrylic polymers by freeze-drying and spray-drying techniques: formulation considerations

The present study investigated a novel extended release system of promethazine hydrochloride (PHC) with acrylic polymers Eudragit RL100 and Eudragit S100 in different weight ratios (1:1 and 1: 5), and in combination (0.5+1.5), using freeze-drying and spray-drying techniques. Solid dispersions were characterized by Fourier-transformed infrared spectroscopy (FT-IR), differential scanning calorimetry (DSC), Powder X-ray diffractometry (PXRD), Nuclear magnetic resonance (NMR), Scanning electron microscopy (SEM), as well as solubility and in vitro dissolution studies in 0.1 N HCl (pH 1.2), double-distilled water and phosphate buffer (pH 7.4). Adsorption tests from drug solution to solid polymers were also performed. A selected solid dispersion system was developed into capsule dosage form and evaluated for in vitro dissolution studies. The progressive disappearance of drug peaks in thermotropic profiles of spray-dried dispersions were related to increasing amount of polymers, while SEM studies suggested homogenous dispersion of drug in polymer. Eudragit RL100 had a greater adsorptive capacity than Eudragit S100, and thus its combination in (0.5+1.5) for S100 and RL 100 exhibited a higher dissolution rate with 97.14% drug release for twelve hours. Among different formulations, capsules prepared by combination of acrylic polymers using spray-drying (1:0.5 + 1.5) displayed extended release of drug for twelve hours with 96.87% release followed by zero order kinetics (r²= 0.9986).O presente trabalho compreendeu estudo de um novo sistema de liberação prolongada de cloridrato de prometazina (PHC) com polímeros acrílicos Eudragit RL100 e Eudragit S100 em diferentes proporções em massa (1:1 e 1:5) e em combinação (0,5+1,5), utilizando técnicas de liofilização e de secagem por aspersão As dispersões sólidas foram caracterizadas por espectrofotometria no infravermelho por transformada de Fourier (FT-IR), calorimetria diferencial de varredura (DSC), difratometria de raios X (PXRD), Ressonância Magnética Nuclear (RMN), microscopia eletrônica de varredura (SEM) e, também, por estudos de solubilidade e de dissolução in vitro em HCl 0,1 N (pH 1,2), água bidestilada e tampão fosfato (pH 7,4). Realizaram-se, também, testes de adsorção da solução do fármaco nos polímeros sólidos. Desenvolveu-se sistema de dispersão sólida exclusiva dentro das cápsulas, que foi avaliado por meio de estudos de dissolução in vitro. Relacionou-se o desaparecimento progressivo de picos do fármaco em perfis termotrópicos de dispersões secas por spray à quantidade aumentada de polímero, enquanto os estudos de SEM sugeriram dispersão homogênea do fármaco no polímero. O Eudragit RL100 apresentou maior capacidade de adsorção do que o Eudragit S100 e, dessa forma, a combinação de (0,5+1,5) para S100 e para RL100 mostrou taxa de dissolução maior, com liberação de 94,17% de fármaco em 12 horas. Entre as várias formulações, as cápsulas preparadas pela combinação de polímeros acrílicos utilizando secagem por aspersão (0,5+1,5) apresentou liberação prolongada do fármaco em 12 horas, com 96,78% de liberação, seguindo cinética de ordem zero (r² = 0,9986

Entrega liposomal de 5 fluorouracilo y tretinoína: un aspecto del tratamiento tópico de las verrugas cutáneas

Background: Tretinoin and 5-fluorouracil are indicated for treatment of various skin disorders and actinic keratosis respectively. Objective: Present study was focused to design liposomes containing 5- fluorouracil and tretinoin. Design was further optimized by 32 full factorial design. Methods: Liposomes were prepared by ethanol injection method and evaluated by Transmission Electron Microscopy, percentage entrapment efficiency, zeta potential and in vitro drug release. Optimized formulation was subjected to histopathological and stability studies at 4ºC, 25ºC and 60ºC temperatures. Results: No drug crystals were visible in transmission electron microscopy, regardless of the preparation technique or the loaded drug. Formulation F9 showed maximum drug entrapment of 72.86% and 69.70% for 5-fluorouraciland tretinoin respectively. When phospholipid concentration was increased from 40 to 60 mg/ml, encapsulation efficiencies of formulation increased. Zeta potential and particle size were maintained within range of -19.14 to -25.61 and 100 to 200 nm respectively which facilitated good stability and penetration of liposomes. Dissolution profiles of formulations F1 to F6 showed high amount of drug release (30.6 to 67.42%) at 2 h. Liposomes were not stable at high temperature but formulations were most stable when stored at lower temperature i.e. 4oC. Conclusion: So, in liposomes both 5-fluorouracil and tretinoin were successfully incorporated and it can be further used for formulation development. Objetivo: El presente estudio se centró en el diseño de liposomas que contenían 5-fluorouracilo y tretinoína. El diseño fue optimizado por 32 diseño factorial completo. Metodos: Los liposomas se prepararon mediante el método de inyección de etanol y se evaluaron mediante Microscopía Electrónica de Transmisión, % de eficiencia de encapsulación, potencial zeta y liberación de fármaco in vitro. La formulación optimizada se sometió a estudios histopatológicos y de estabilidad a temperaturas de 4ºC, 25ºC y 60ºC. Resultados: Ningún cristal de los fármacos era visibles en el Microscopía Electrónica de Transmisión, sin importar la técnica de la preparación o el fármaco cargado. La formulación F9 demostró el atrapamiento máximo del fármaco del 72,86% y del 69,70% para 5-fluorouracilo y tretinoína respectivamente. Cuando la concentración del fosfolípido fue aumentada a partir de 40 a 60 mg/ml, las eficiencias de encapsulación de la formulación aumentaron. El potencial de zeta y el tamaño de partícula fueron mantenidos dentro de la gama de-19,14 a -25,61 y 100 a 200 nanómetros respectivamente, que facilitó la buena estabilidad y la penetración de liposomas. Los perfiles de disolución de las formulaciones F1 a F6 mostraron una alta cantidad de liberación de fármaco (30,6 a 67,42%) a las 2h. Los liposomas no eran estables a alta temperatura, pero las formulaciones eran más estables cuando se almacenaban a una temperatura más baja, es decir, 4 ºC. Concusiones: Así, en los liposomas, tanto los fármacos 5-fluorouracilo como los tretinoína se incorporaron con éxito y se pueden utilizar para el desarrollo de la formulación

Enteric coated HPMC capsules plugged with 5-FU loaded microsponges: a potential approach for treatment of colon cancer

The work was aimed at developing novel enteric coated HPMC capsules (ECHC) plugged with 5 Florouracil (5-FU) loaded Microsponges in combination with calcium pectinate beads. Modified quasi-emulsion solvent diffusion method was used to formulate microsponges based on 32 factorial design and the effects of independent variables (volume of organic solvent and Eudragit RS100 content) on the dependent variables (Particle size, %EE & % CDR) were determined. The optimized microsponges (F4) were characterized by SEM, PXRD, TGA and were plugged along with calcium pectinate beads in HPMC capsules and the HPMC capsules were further coated with enteric polymer Eudragit L 100 (Ed-L100) and/ or Eudrgit S 100 (Ed-S 100) in different proportions. In vitro release study of ECHC was performed in various release media sequentially SGF for 2 h, followed by SIF for the next 6 h and then in SCF (in the presence and absence of pectinase enzyme for further 16 h). Drug release was retarded on coating with EdS-100 in comparison to blend of EdS-100: EdL-100 coating. The percentage of 5-FU released at the end of 24 h from ECHC 3 was 97.83 ± 0.12% in the presence of pectinase whereas in control study it was 40.08 ± 0.02% drug. The optimized formulation was subjected to in vivo Roentgenographic studies in New Zealand white rabbits to analyze the in vivo behavior of the developed colon targeted capsules. Pharmacokinetic studies in New Zealand white rabbits were conducted to determine the extent of systemic exposure provided by the developed formulation in comparison to 5-FU aqueous solutions. Thus, enteric coated HPMC capsules plugged with 5-FU loaded microsponges and calcium pectinate beads proved to be promising dosage form for colon targeted drug delivery to treat colorectal cancer.O trabalho teve como objetivo o desenvolvimento de novas cápsulas com revestimento entérico HPMC (ECHC) conectadas com microesponjas carregadas com fluoruracila (5-FU) em combinação com grânuos de pectinato de cálcio. O método de difusão de solvente modificado quasi-emulsão foi usado para formular microesponjas com base no planejamento fatorial 32 e determinaram-se os efeitos das variáveis independentes (volume de solvente orgânico e conteúdo Eudragit RS100) sobre as variáveis dependentes (tamanho de partícula, EE% e % CDR). As microesponjas otimizadas (F4) foram caracterizadas por SEM, PXRD, TGA e ligadas aos grânulos de pectinato de cálcio em cápsulas de HPMC e estas foram, ainda, revestidas com polímero entérico Eudragit L 100 (Ed-L100) e/ou Eudrgit S 100 (Ed S 100) em diferentes proporções. No estudo de liberação in vitro de ECHC foi realizada em vários meios de liberação sequencial SGF durante 2 h, seguido de SIF para as próximas 6 h, e, em seguida, em SCF (na presença e na ausência de enzima pectinase por mais 16 h). A liberação do fármaco foi retardada em revestimento com a EDS-100, em comparação com mistura de EDS-100: EDL-100, de revestimento. O percentual de 5-FU liberado de ECHC 3 ao final de 24 h foi 97,83 ± 0,12% em presença de pectinase, enquanto que para o controle foi de 40,08 ± 0,02% do fármaco. A formulação otimizada foi submetida a estudos Roentgenográficos in vivo, em coelhos brancos Nova Zelândia, para analisar o comportamento das cápsulas desenvolvidas direcionadas ao cólon. Os estudos de farmacocinética em coelhos brancos da Nova Zelândia foram conduzidos para determinar a extensão da exposição sistêmica propiciada pela formulação desenvolvida, em comparação com solução aquosa de 5-FU. Assim, cápsulas entéricas de HPMC revestidas e conectadas com microesponjas carregadas com 5-FU e grânulos de pectinato de cálcio se mostraram promissoras como formulação para liberação do fármaco no cólon no tratamento do câncer colorretal

Primary and novel approaches for colon targeted drug delivery – A review

The colon is a site where both local and systemic delivery of drugs can take place. Local delivery could, for example, allow topical treatment of inflammatory bowel disease. Treatment could be made more effective if it were possible for drugs to be targeted directly on the colon. Systemic side effects could also be reduced. Colon specific systems might also allow oral administration of peptide and protein drugs, which are normally inactivated in the upper parts of the gastrointestinal tract. Primary approaches for CDDS (Colon Specific Drug Delivery), which includes prodrugs, pH and time dependent systems and microbially triggered drug delivery system achieved limited success and having limitations. Newly developed CDDS, which includes pressure controlled colonic delivery capsules (PCDCS), CODESTM and osmotic controlled drug delivery are unique in terms of achieving in vivo site specificity and feasibility of manufacturing process. This review also focuses on evaluations of CDDS in general.Keywords: Colon drug delivery systems; Primary approaches; Newly developed approaches; evaluation of colon targeted drug delivery system

Assessing the Environmental and Economic Sustainability of Functional Food Ingredient Production Process

Development and application of novel technologies in food processing is vital for ensuring the availability of adequate, safe, and convenient food with the desired quality and functional properties. Environmental and economic sustainability of technologies is essential prior to their application in the food processing sector. The objective of this research is to determine the environmental and economic feasibility of ultrasound-assisted extraction (UAE) for recovering functional food ingredients from seaweed. Experimental data is used to conduct a life cycle assessment (LCA) to investigate the environmental performance with a functional unit (FU) of obtaining 1 g of extracted polyphenols, measured as gallic acid equivalents (mg GAE)/g seaweed. A life cycle impact assessment is performed with ReCiPe 2016 at midpoint. The cost of manufacturing (COM) of phenolic-rich extracts (as functional ingredient, bioactive, or nutraceutical) is estimated using time-driven activity-based costing (TDABC). The environmental profile findings show that across all categories, the UAE has considerably lower impacts than the conventional method, with electricity as the most important impact contributor, followed by solvent production. An economic assessment estimates the COM over a one-year period at a large scale using the UAE to be EUR 1,200,304, EUR 2,368,440, and EUR 4,623,290 for extraction vessel capacities of 0.05, 0.1, and 0.15 m3, respectively. Raw materials (including the type of raw material) and operational labour costs are the primary contributors to the COM. The findings thus present evidence to support the adoption of an environmentally and economically viable technology for functional ingredient production

Phytochemicals & Pharmacological activity of Xanthium strumarium: An Updated Review

Therapeutic plants are of extraordinary worth in the field of treatment and fix of infections. Throughout the long term, logical examination has extended our insight into the compound constituents of the therapeutic plants, which decide the restorative properties. The purpose of this paper is to summarize the progress of modern research, and provide a systematic review on the traditional usages, phytochemistry, pharmacology of the X. strumarium. Plant parts like leaves, organic product, bark and seed have been accounted for having antidiabetic, antiulcer, calming, invulnerable modulator and pain- relieving movement. This survey tends to the tentatively validated realities and furthermore proposes the requirement for research on substance and pharmacological properties of Xanthium strumarium

Patterns of injuries in homicidal cases

Death, an inevitable part of life, prompts an exploration into the manner and method by which it occurs. This study aims to analyze the patterns of injuries in homicidal cases brought for postmortem examination. In 2019, a total of 28,918 murder cases were registered in India, showing a slight decrease of 0.3% in comparison to 2018 (29,017 cases). The study aims to understand the different injury patterns in homicide. At the Department of Forensic Medicine, Gandhi Medical College, Bhopal, India, a total of 62 males and 12 females, along with one unknown gender person, where submitted to postmortem examination. The majority of cases belonged to urban, with leading causes of death being shock and hemorrhage followed by craniocerebral damage. This study concludes that sharp edges and deep cuts were the primary injury patterns in homicide cases. Morte, uma inevitável parte da vida, incita uma exploração a respeito da maneira e do método de sua ocorrência. Este estudo tem por objetivo analisar os padrões de lesões em casos de homicídios verificados em exames post-mortem. Em 2019, registrou-se um total de 28.918 casos de assassinato na India, mostrando um leve decréscimo de 0,3% em comparação com 2018 (29.017 casos). Este estudo objetiva entender os diferentes padrões de lesão em homicídios. No Departamento de Medicina Forense da Gandhi Medical College, em Bhopal, India, um total de 62 homens, 12 mulheres e uma pessoa de gênero não identificado, foram submetidas à análise post mortem. A maioria dos casos pertencia a áreas urbanas, com principal causa de morte sendo choque e hemorragia seguida de dano crânio cerebral. Este estudo conclui que arestas afiadas e cortes profundos foram os principais padrões de lesões em casos de homicídio. 

Virtual Voting System

India's voting system plays an important role in Indian Democracy. The existing system is offline and has certain weaknesses. In recent years, the spread of covid19, inefficient rural voters, people far from their place of birth, paper waste affecting nature, budgets that should be used for development, invisible fraud, waste of human labor, have been recorded and can be avoided by the virtual voting system. The research aims to supply an easy and secure electoral system in India. The method used descriptive qualitative. The results indicate that a virtual voting system is environmentally friendly and is considered a resource-saving way for the election. It is because minimizes errors and increases voter participation through convenient virtual voting. In conclusion, a virtual voting system can develop anAadhar based advanced Electronic Voting Machine (EVM), which helps in a free and fair way of conducting election

A Review on Phyto-Pharmacological Aspects of Apamarg (Achyranthes aspera Linn.)

Achyranthes aspera is very important ayurvedic medicinal plant. It is known as Apamarg Sanskrit name, prickly chaff flower in English and Naayuruvi in Tamil. It belongs to the family Amaranthaceae. This medicinal plant found as a weed thrrought India up to 900 m. Though almost all of its parts are used in traditional system of medicines, seeds, roots, and shoots are the most important parts, which are used medicinally. The major phytoconstituents are carbohydrate, protein, glycosides, alkaloids, tannins, flavonoids, and lignin. It also contains the phytochemicals like oleanolic acid, Saponin A and saponin B. A large number of phytochemical constituents have been isolated from the plant which possesses several pharmacological activities like diuretic, purgative, laxative, antiasthmatic, hepatoprotective, anti-allergic, hepatitis, renal disorders, dermatological disorders, gynecological disorders, gonorrhea, malaria, fever, cough, diabetes. The juice of the plant is used in the treatment of boils, diarrhea, dysentery, hemorrhoids, rheumatic pains, itches and skin eruption