Synthesis of rutin derivatives to enhance lipid solubility and development of topical formulation with a validated analytical method

2021 ◽  
Vol 19 ◽  
Author(s):  
Murad Abualhasan ◽  
Mohyeddin Assali ◽  
Abeer Mahmoud ◽  
Abdel Naser Zaid ◽  
Numan Malkieh
Keyword(s):  
Analytical Method ◽  
Raw Materials ◽  
Varicose Veins ◽  
Lipid Solubility ◽  
Synthetic Approach ◽  
Topical Formulation ◽  
Lipophilic Compounds ◽  
Internal Bleeding ◽  
Ester Prodrug ◽  
Low Solubility

Background: Rutin is available on the market as a topical formulation for the treatment of several conditions, such as internal bleeding, hemorrhoids, and varicose veins. However, these gels have low solubility and limited bioavailability due to their decreased lipid solubility. Objective: In this study, we aimed to synthesize potentially novel lipophilic rutin prodrugs. The suggested library of these rutin prodrugs includes changing the solubility profile to facilitate rutin transport across biological barriers, thereby improving drug delivery through topical application. Methods: Six rutin derivatives were synthesized based on the ester prodrug strategy. The synthesized compounds were formulated as topical ointments, and their permeability via Franz diffusion was measured. An ultraviolet (UV) analytical method was developed in our laboratories to quantify rutin derivatives both as raw materials and in final dosage forms. The analytical method was then validated. Result: The results of Franz diffusion analyses showed that transdermal permeability increased by 10_Fo.jpgl height=""d for decaacetylated rutin compared to the other esterified rutins. A simple analytical method for the analysis of the formulated rutin ester was developed and validated. Moreover, the formulated ointment of decaacetylated rutin in our research laboratory was found to be stable under stability accelerated conditions. Synthesis of potentially more lipophilic compounds would yield novel rutin prodrugs suitable for topical formulation. Conclusion: This project provides a synthetic approach for many similar natural products. The research idea and strategy followed in this research project could be adapted by pharmaceutical and herbal establishments.

The certification of the aflatoxin mass fractions in peanut butter

2008 ◽  
Vol 1 (3) ◽  
pp. 283-289
Author(s):  
G. Buttinger ◽  
S. Harbeck ◽  
R. Josephs
Keyword(s):  
Analytical Method ◽  
Raw Materials ◽  
Peanut Butter ◽  
The European Union ◽  
Method Performance ◽  
Mass Fractions ◽  
Food And Feed ◽  
Combined Uncertainty ◽  
Aflatoxin B ◽  
Certified Values

In the context of control activities contamination of food and feed with aflatoxins is a frequently observed non compliance. Pistachios, peanuts and products thereof are particularly affected. The Institute for Reference Materials and Measurements has therefore produced a peanut butter material certified for its aflatoxin mass fractions. This certified reference material (CRM) allows for the evaluation of analytical method performance and the assessment of the comparability of results from different laboratories. The CRM was produced using naturally contaminated raw materials to ensure equivalent behaviour compared to samples routinely encountered. The homogeneity and stability of the CRM were thoroughly tested and certified values were determined in an inter-laboratory study. Furthermore, uncertainties of the certified values were assessed including contributions of the homogeneity, stability and certification studies to the combined uncertainty. This newly prepared CRM allows an assessment of trueness of the analytical method at a concentration level corresponding to the legal limits enforced in the European Union. The material has the following certified properties: aflatoxin B1 1.77±0.29 µg/kg, aflatoxin B2 0.48±0.07 µg/kg, aflatoxin G1 0.9±0.4 µg/kg, aflatoxin G2 0.31±0.12 µg/kg and total aflatoxins, as sum of aflatoxins B1, B2, G1 and G2, 3.5±0.5 µg/kg.

scholarly journals ANALISIS DIFFERENTIAL COST DAN OPPORTUNITY COST DALAM PENGAMBILAN KEPUTUSAN MEMBELI ATAU MEMPRODUKSI SENDIRI PADA INDUSTRI RUMAH PANGGUNG WOLOAN

2015 ◽  
Vol 13 (03) ◽  
Author(s):  
Romeo Fersi Mongdong ◽  
Jenny Morasa ◽  
Heince Wokas
Keyword(s):  
Cost Analysis ◽  
Analytical Method ◽  
Opportunity Cost ◽  
Raw Materials ◽  
Quantitative Result ◽  
Opportunity Costs ◽  
Business World ◽  
Differential Costs ◽  
The Right ◽  
The Cost

The business world today is characterized by increasing competition among existing companies. Competition occurs in all sectors of the economy both industry, trade, and services. One of the decisions that must be taken in planning at every alternative is to buy or produce itself a component of raw materials. Differential cost are related to the opportunity cost, which is the differential cost incurred costs as a result of certain decisions while the opportunity cost is the cost incurred when choosing a decision. The purpose of this study to analyze the differential costs and opportunity costs in the decision to buy or produce their own on Industri Rumah Panggung Woloan. The analytical method used is descreptive quantitative. Result of the differential cost analysis showed that the right decisions can be taken by the management company the manufactures its own because getting a hihgter differential gain, compared to buying from outside. While the opportunity cost of the buying raw materials from outside is more profitable, thus producing itself becomes more expensive. Should the leadership Industri Rumah Panggung Woloan produce their own wood from the outside becauseit would be more adventageous, compared to taking wood there are kept alone.

scholarly journals The effect of N-alkyl modification on the antimalarial activity of 3- hydroxypyridin-4-one oral iron chelators

Blood ◽  
1991 ◽  
Vol 77 (3) ◽  
pp. 637-643 ◽  
Author(s):  
C Hershko ◽  
EN Theanacho ◽  
DT Spira ◽  
HH Peter ◽  
P Dobbin ◽  
...  
Keyword(s):  
Antimalarial Activity ◽  
Iron Chelators ◽  
Lipid Solubility ◽  
Lipophilic Compounds ◽  
Labile Iron Pool ◽  
Ring Nitrogen ◽  
Iron Pool ◽  
Chelating Compounds

Abstract The antimalaria effect of iron chelators is attributed to their interaction with a labile iron pool within parasitised erythrocytes, and it was postulated that increased affinity to iron as well as increased lipophilicity may improve antimalarial activity. In the present study we have examined the antimalarial effect of 3- hydroxypyridin-4-ones, a family of bidentate orally effective iron chelators whose lipophilicity may be modified by altering the length of the R2 substituent on the ring nitrogen. A significant dose-related suppression of Plasmodium falciparum cultures was observed with all drugs tested in vitro at concentrations of 5 mumol/L or higher. In contrast, there was a clear segregation of the in vivo effect on P berghei in rats (300 mg/kg/d subcutaneous) into two categories: compounds CP20, 38, and 40 failed to suppress malaria, whereas CP51, 94, and 96 had a strong antimalarial effect, similar or better than deferoxamine. There was a close linear correlation between the suppression of peak parasite counts and the reduction in hepatic nonheme iron induced by the various drugs tested (r = .9837). The most lipophilic compounds were also the most effective in suppressing malaria and in depleting hepatic iron stores. These data indicate that 3-hydroxypyrydin-4-ones are able to suppress malaria in vivo and in vitro. Because lipid solubility is an important determinant of antimalarial action, our study provides useful information regarding the selection of orally effective iron-chelating compounds that may be suitable for clinical application as antimalarial agents.

scholarly journals Fruit Seeds as Sources of Bioactive Compounds: Sustainable Production of High Value-Added Ingredients from By-Products within Circular Economy

Molecules ◽  
2019 ◽  
Vol 24 (21) ◽  
pp. 3854 ◽  
Author(s):  
Fidelis ◽  
Moura ◽  
Kabbas Junior ◽  
Pap ◽  
Mattila ◽  
...  
Keyword(s):  
Chemical Composition ◽  
Circular Economy ◽  
Raw Materials ◽  
Scale Up ◽  
Sustainable Use ◽  
Value Added ◽  
Water Soluble ◽  
Lipophilic Compounds

The circular economy is an umbrella concept that applies different mechanisms aiming to minimize waste generation, thus decoupling economic growth from natural resources. Each year, an estimated one-third of all food produced is wasted; this is equivalent to 1.3 billion tons of food, which is worth around US$1 trillion or even $2.6 trillion when social and economic costs are included. In the fruit and vegetable sector, 45% of the total produced amount is lost in the production (post-harvest, processing, and distribution) and consumption chains. Therefore, it is necessary to find new technological and environmentally friendly solutions to utilize fruit wastes as new raw materials to develop and scale up the production of high value-added products and ingredients. Considering that the production and consumption of fruits has increased in the last years and following the need to find the sustainable use of different fruit side streams, this work aimed to describe the chemical composition and bioactivity of different fruit seeds consumed worldwide. A comprehensive focus is given on the extraction techniques of water-soluble and lipophilic compounds and in vitro/in vivo functionalities, and the link between chemical composition and observed activity is holistically explained.

Archaic semisedentary foragers and analytical nodule analysis: The Aught-Six site of Northwestern Colorado

2018 ◽  
Vol 39 (3) ◽  
pp. 171-197
Author(s):  
Matthew J Landt ◽  
Justin P Williams
Keyword(s):  
Analytical Method ◽  
Raw Materials ◽  
Primary Objective ◽  
Stone Tool ◽  
Piceance Basin ◽  
Technological Systems ◽  
Projectile Point ◽  
Lithic Assemblage

Nodule analysis is designed to highlight the ways in which different lithic sources were utilized and incorporated into the stone tool industries of past societies. In 2008 and 2009, excavations in the Piceance Basin of Northwestern Colorado, an area with local chert and quartzite quarries, provided an opportunity to use a nodule analyses for a Section 106-driven project. The Aught-Six site lithic assemblage suggests that Archaic tool kits in Northwestern Colorado are likely to be heavily reliant on a variety of raw materials found across the region, though Bridger chert nodules were the primary objective pieces for the new tools during the basin house occupation. The results of the analyses not only highlight specific areas of projectile point production, but they also indicate that nodule analysis remains a powerful analytical method for understanding how raw materials are incorporated into the technological systems of semisedentary Archaic foragers.

scholarly journals Surface Modification of SnO2with Phosphonic Acids

2017 ◽  
Vol 2017 ◽  
pp. 1-7 ◽  
Author(s):  
Ramona Gheonea ◽  
Carmen Mak ◽  
Eleonora Cornelia Crasmareanu ◽  
Vasile Simulescu ◽  
Nicoleta Plesu ◽  
...  
Keyword(s):  
Surface Modification ◽  
Phosphonic Acid ◽  
Raw Materials ◽  
Optical Quality ◽  
Synthetic Approach ◽  
Phosphonic Acids ◽  
Molar Ratios ◽  
Long Time ◽  
Ft Ir ◽  
Synthesized Materials

The aim of the present work was the study of phosphonic acids grafting on the surface of SnO2at different molar ratios. In this paper we describe the functionalization of SnO2surfaces with phosphonic acids RPO(OH)2. The surface modification process was achieved by using phenyl-phosphonic acid (PPA) and vinyl-phosphonic acid (VPA). The synthesized materials were investigated by using FT-IR, TGA (in air and in nitrogen), EDX, ESEM, and TEM methods. This synthetic approach has many advantages: films with optical quality and controlled thickness can be obtained using low temperatures and cheap raw materials, by using “green chemistry” synthetic routes. The hybrid materials have structures diversity and fascinating applications, attracting attention for a long time, due to their potential.

scholarly journals Comparison of the Robustness of Spectrophotometric Method and High-Performance Liquid Chromatographic Method for the Determination of Pioglitazone in Solid Dosage Form

2021 ◽  
pp. 37-45
Author(s):  
Sara Zahid ◽  
Fatima Zahid ◽  
Asma Ahmed ◽  
Waqas Safir
Keyword(s):  
Spectrophotometric Method ◽  
Analytical Method ◽  
High Performance ◽  
Dosage Form ◽  
Raw Materials ◽  
High Performance Liquid Chromatographic ◽  
Hplc Method ◽  
The Body ◽  
Solid Dosage Form ◽  
Solid Dosage

Pioglitazone is a drug that reduces the amount of glucose (sugar) in the blood. It is included in the class of anti-diabetic drugs called “thiazolidinedione” that are used in the treatment of type II diabetes. It attaches to the peroxisomes proliferated- activated receptor gamma (PPARϒ) on tissues throughout the body and causes the cells to become more sensitive to insulin. As a result, more glucose is removed from the blood.The aim of the study is more precisely to find out the better analytical method for the quantitative measurement of the content of pioglitazone in commercially available drugs using two analytical methods i-e Spectrophotometric method and HPLC method.The analytical method for the pioglitazone hydrochloride was developed by HPLC, and then validated the method according to compendial requirements. Pioglitazone in various Dowglit and Gliden tablets was determined by this developed methodPrecision, Accuracy and stability of Pioglitazone was checked which came out to be100.40% and 100.19% respectively. The analysis of pioglitazone hydrochloride in solid dosage form using the HPLC method shows the results are more sensitive, accurate, validated and economical and can be easily applied to raw materials and finished goods compared to the Spectrophotometer method.

The optimization of the composition of fertilizers based on milled phosphorites

2019 ◽  
Vol 60 (12) ◽  
pp. 133-139
Author(s):  
Nadezhda V. Syrchina ◽  
◽  
Tamara Ya. Ashikhmina ◽  
Nadezhda N. Bogatyreva ◽  
Grigory Ya. Kantor ◽  
...  
Keyword(s):  
Crop Production ◽  
Raw Materials ◽  
Mineral Fertilizer ◽  
Hydrodynamic Cavitation ◽  
Small Enterprises ◽  
Organic Mineral ◽  
Phosphate Mines ◽  
Comparison Object ◽  
Low Solubility ◽  
New Jobs

The phosphorites of many domestic deposits can be used as cheap natural phosphorus fertilizers of regional importance. The limitation of their use is due to the low solubility and, consequently, low agrochemical effectiveness. To increase the solubility of phosphorites (activation), it is proposed to use the method of granulation of phosphorite flour (PF) with an organomineral additive containing milled sulfur, glauconite and highly decomposed peat, dispersed by hydrodynamic cavitation. Phosphate activation is ensured by acids formed in the process of microbiological oxidation of sulfur in soils (convert insoluble phosphates to more soluble hydrophosphates), glauconite (promotes adsorption and ion exchange binding of cations that form insoluble phosphates, activates soil microbiota) and humic acid peat (oxides into stable complexes, stimulate the activity of soil microorganisms). In laboratory conditions, samples of the corresponding organic-mineral fertilizer were obtained. As phosphate raw materials, the PF of the Vyatka-Kama deposit (Russia) and the Khneifis deposit (Syria) were used. The study of the effect of fertilizer on the chemical composition of soils was carried out in a laboratory experiment. As a comparison object, simple superphosphate was used. Fertilizers were applied to the soil in an amount of 0.1 g per 1 kg of air-dried soil. It was revealed that already 7 days after fertilizing, the mobility of phosphorus increases by 31-45%, while the pH of the soil solution does not change. The sulfate content in soils increased by an average of 33%. In all variants of the experiment, the application of activated PF in the soil led to the same result as the application of simple superphosphate. Based on PF and an activating organomineral additive, a granular form of phosphorus fertilizer with sulfur and humic substances can be obtained that is not inferior in effectiveness to simple superphosphate. The production of appropriate fertilizer can be arranged at small enterprises and directly at phosphate mines, which will create new jobs and provide regional crop production with relatively cheap and fairly effective forms of phosphate fertilizers that comply with the principles of green chemistry. The composition and technology of fertilizer production make it possible to position it as a natural organic-mineral fertilizer for organic farming.

Effect of Diluent Polarity on Extraction Equilibria of Acrylic Acid from its Aqueous Solutions by Tri-n-Octylaime

2013 ◽  
Vol 807-809 ◽  
pp. 2801-2804 ◽  
Author(s):  
Yeon Ki Hong ◽  
Hyoung Wook Lee ◽  
Sung Min Bae
Keyword(s):  
Acrylic Acid ◽  
Aqueous Solutions ◽  
Extraction Efficiency ◽  
Raw Materials ◽  
Dilute Aqueous Solutions ◽  
Amine Complex ◽  
Increasing Demand ◽  
Low Solubility ◽  
Extraction Equilibria ◽  
Active Diluents

Acrylic acid and its derivatives are raw materials for polymeric, paint additives, adhesive, textile and leather treating products. The increasing demand of acrylic acid is great attention for its recovery from dilute aqueous solutions. With this aim, the amine based extraction of acrylic acid from its aqueous solutions in polar diluents was investigated. In the extraction, the tri-n-octylamine in polar diluents was found to provide higher extraction efficiency than that in nonpolar diluents. It was presumed that the acid-amine complex formation is difficult and the low solubility of acid-amine complex is low in nonpolar diluents. Higher extraction efficiency for acrylic acid was obtained with the polarity of active diluents due to higher solubility for acid-amine complex with polarity of diluents.

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