scholarly journals Research of physico-chemical and technological properties of thioctic acid

2018 ◽  
pp. 71-78
Author(s):  
I. V. Kovalevska ◽  
O. A. Ruban
Keyword(s):  
Compression Ratio ◽  
Dosage Form ◽  
Solid Dispersions ◽  
Slope Angle ◽  
Chemical Properties ◽  
Thioctic Acid ◽  
Technological Properties ◽  
Solid Dosage ◽  
Physico Chemical ◽  
Solubility Determination

Characteristics and relevance of article topic. Analysis of the literature data shows that the thioctic acid preparations are widely used in the treatment of various diseases. At it’s parenteral application inter- and intraindividual level at the plasma can vary significantly. Therefore, the bioavailability of thioctic acid according to the results of clinical researches is only 30% and efficacy largely dependent on the technological features of the dosage form manufacturing process. The goal of paper was researches of the thioctic acid physico-chemical properties for development of composition and technology of solid dosage form with improved bioavailability. Thioctic acid was the object of the study. The complex of physical, chemical and technological tests were used during researches: microscopic, thermal analyzes studies of bulk density, flowability, compression ratio, hygroscopicity, dissolution. Conclusions. According to thermal analysis, thermal stability of thioctic acid sample has been established within 20–180 °C. The results can be used for explanation the temperature regime in the preparation of solid dispersions of thioctic acid by the melting method. Solubility determination according to SP of Ukraine II-ed. and microscopic method showed that the substance is readily soluble in 96% ethanol, which leads to the conclusion about the possibility of preparation thioctic acid solid dispersions by dissolution method. During researches were established physico-chemical and technological properties of the thioctic acid substance, produced by Shanghai modern pharmaceutical Co., LTD (China). Were established that the substance is hygroscopic as evidenced by the change in appearance and weight. It was determined that the substance does not have a satisfactory yield (Carr index – 1,39, slope angle – 60°), compression ratio is 0,495, which is indicative of the lack of sample strength after the removal of pressure. The results of the studies suggest that the physicochemical properties of the substance needed modifications in the manufacture of solid dosage forms with thioctic acid.

scholarly journals SELECTION OF A FILLER FOR TABLETS MANUFACTURED WITH DIRECT COMPRESSION METHOD CONTAINING DRY GINGER EXTRACT

2019 ◽  
Vol 3 ◽  
pp. 26-34 ◽  
Author(s):  
Оlena Ruban ◽  
Malek Alkhalaf ◽  
Nataliia Gerbina
Keyword(s):  
Dosage Form ◽  
Moisture Absorption ◽  
Angle Of Repose ◽  
Direct Compression ◽  
Technological Properties ◽  
Ginger Extract ◽  
Dry Extract ◽  
Solid Dosage Form ◽  
Solid Dosage ◽  
Physico Chemical

The preliminary studies of physico-chemical and pharmaco-technological properties of the dry extract of ginger have determined the need for introduction of different groups of excipients for developing a solid dosage form for the treatment of type II diabetes mellitus. Aim. To choose the rational filler in the composition of tablets with ginger obtained by direct compression. Materials and methods. The study object was the dry extract of ginger (DEG) (producer “Megaprom”, Dnepr,Ukraine) and modern excipients for the production of tablets by direct compression: GalenIQ 721 (BENEO-Palatinit Gmb), Flowlac 100 (Meggle Co.), Tablettose 80 (Meggle Co.), Farmaxx (Merck), Microcelac 100 (Meggle Co.), Vivapur 112 and 102 (JRS Pharm), Prosolv HD 90, Prosolv SMCC 50 (JRS Pharm) manufactured in Germany. Pharmaco-technological and physico-chemical properties of the samples were studied according to conventional methods of the State Pharmacopoeia of Ukraine. Results and discussion. According to the results of the crystallographic analysis, the ability to the moisture absorption, resistance to crushing, disintegration time, fluidity indicators, angle of repose and bulk volume the effect of modern excipients on physicochemical and pharmaco-technological properties of the dry extract of ginger has been studied. Conclusions. According to the results of microscopic analysis, it has been found, that the rational fillers are GalenIQ 721, Prosolv HD 90, Prosolv SMCC 50, Vivapur 102 and Vivapur 112, as they provide a uniform system and the necessary resistance to destruction. The study of the kinetics of the moisture absorption has shown that addition of the fillers significantly reduces the increase in moisture compared to the dry extract. The mixture with GalenIQ 721 has the lowest parameters of moisture absorption at a relative air humidity of 45 %, 75 % and 100 %. In accordance with the results of the pharmaco-technological studies, it has been found that addition of GalenIQ 721 leads to improved flowability, disintegration, settling qualities; it indicates the feasibility of its inclusion into the composition of the solid dosage form.

scholarly journals Preparation of 2-phenyl-9-diethylaminoethylimidazo[1,2-α]benzimidazole dinitrate tablets and development of quality control methods

2021 ◽  
Vol 10 (2) ◽  
pp. 62-67
Author(s):  
A. M. Domanina ◽  
M. V. Chernikov ◽  
I. P. Remezova ◽  
E. F. Stepanova ◽  
A. M. Shevchenko ◽  
...  
Keyword(s):  
Quality Control ◽  
Dosage Form ◽  
Chemical Properties ◽  
Antimicrobial Effect ◽  
Film Coating ◽  
Technological Properties ◽  
Physico Chemical ◽  
The Stability ◽  
Object Of Study

Introduction. Currently, for the treatment of gastric ulcer, drugs with a combined effect are used. To eliminate possible side effects of the drugs used, the search for new molecules to create more effective and safe histamine H2 receptors continues. As a possible solution to these problems, we investigated the substance dinitrate of 2-phenyl-9-diethylaminoethylimidazo[1,2-α] benzimidazole (DFDB).Aim. The aim of this study was to obtain 2-phenyl-9-diethylaminoethylimidazo[1,2-α]benzimidazole dinitrate tablets and develop methods for quality control.Materials and methods. The object of study was tablets based on the substance DF DB. The physicochemical and technological properties of the tablet dosage form were studied. Pharmaco-technological and physico-chemical indicators were determined according to the methods of the State Pharmacopoeia of the XIV edition. Identification and quantitative determination of DFDB in tablets was performed by HPLC.Results and discussion. Based on the physico-chemical properties and determination of the main technological indicators of DFDB, an optimal tableting technology has been developed. The optimal composition of tablets has been developed. Identification of tablets is proposed to be carried out using HPLC in comparison with the standard sample of DFDB. Related impurities, according to the data obtained, do not exceed 0.1 %. We found that the tablets do not have an antimicrobial effect. The analyzed tablets correspond to category 3A. The content of DFDB should be from 95 to 105 % of the declared amount in one tablet. During the analysis, we conducted biopharmaceutical and technological studies of the finished dosage form during storage under the conditions of long-term stability testing in polymer cans with screw-on lids. It is shown that the selected composition of excipients and the production technology ensure the stability of the finished dosage form for two years of storage under the observed conditions. To select the tableting technology, the main technological properties of the DFDB substance are analyzed. The choice of excipients and the composition of the film coating was carried out.Conclusion. The technology is developed and standardization of tablets based on the substance DFDB is proposed.

Amorphous and Crystalline Particulates: Challenges and Perspectives in Drug Delivery

2017 ◽  
Vol 23 (3) ◽  
pp. 350-361 ◽  
Author(s):  
Hisham Al-Obaidi ◽  
Mridul Majumder ◽  
Fiza Bari
Keyword(s):  
Crystal Engineering ◽  
Drug Carrier ◽  
Solid Dispersions ◽  
Chemical Properties ◽  
Pharmaceutical Product ◽  
Water Soluble ◽  
Amorphous Form ◽  
Physico Chemical ◽  
Water Soluble Drugs ◽  
Amorphous Drug

Crystalline and amorphous dispersions have been the focus of academic and industrial research due to their potential role in formulating poorly water-soluble drugs. This review looks at the progress made starting with crystalline carriers in the form of eutectics moving towards more complex crystalline mixtures. It also covers using glassy polymers to maintain the drug as amorphous exhibiting higher energy and entropy. However, the amorphous form tends to recrystallize on storage, which limits the benefits of this approach. Specific interactions between the drug and the polymer may retard this spontaneous conversion of the amorphous drug. Some studies have shown that it is possible to maintain the drug in the amorphous form for extended periods of time. For the drug and the polymer to form a stable mixture they have to be miscible on a molecular basis. Another form of solid dispersions is pharmaceutical co-crystals, for which research has focused on understanding the chemistry, crystal engineering and physico-chemical properties. USFDA has issued a guidance in April 2013 suggesting that the co-crystals as a pharmaceutical product may be a reality; but just not yet! While some of the research is still oriented towards application of these carriers, understanding the mechanism by which drug-carrier miscibility occurs is also covered. Within this context is the use of thermodynamic models such as Flory-Huggins model with some examples of studies used to predict miscibility.

scholarly journals Comparative Plasma Exposure of Albendazole after Administration of Rapidly Disintegrating Tablets in Dogs

2013 ◽  
Vol 2013 ◽  
pp. 1-7 ◽  
Author(s):  
Silvina G. Castro ◽  
Alicia Dib ◽  
Gonzalo Suarez ◽  
Daniel Allemandi ◽  
Carlos Lanusse ◽  
...  
Keyword(s):  
Dosage Form ◽  
Solid Dispersions ◽  
Plasma Exposure ◽  
Solid Dosage Form ◽  
Solid Dosage ◽  
Drug Plasma ◽  
Key Factor

The main objectives of this study were (a) to evaluate thein vitroperformance of the rapid disintegration tablets as a way to improve the solid dispersions and (b) to study thein vivopharmacokinetics of the albendazole modified formulation in dogs. Rapid disintegration of tablets seems to be a key factor for efficiency of solid dispersions with regard to improvement of the albendazole bioavailability. Thein vivoassays performed on dogs showed a marked increase in drug plasma exposure when albendazole was given in solid dispersions incorporated into rapid disintegration tablets compared with conventional solid dosage form.

scholarly journals The pharmaco-technological studies of the tablet solid dosage form for the treatment of otolarynological diseases

2020 ◽  
pp. 51-60
Author(s):  
М. К. Гулзода ◽  
A. У. Рахмонов ◽  
К. С. Махсудов ◽  
Р. С. Мусоєв ◽  
С. M. Мусозода ◽  
...  
Keyword(s):  
Dosage Form ◽  
Raw Materials ◽  
Biologically Active Substances ◽  
Biologically Active ◽  
Technological Properties ◽  
Medicinal Products ◽  
Solid Dosage Form ◽  
Plant Raw Materials ◽  
Solid Dosage ◽  
Active Substances

The prevalence of acute respiratory diseases, the particular severity of their course, as well as the frequent relapses and complications require constant search for new, more effective and safe medicines for their prevention and treatment and introduction of these drugs into clinical practice. Generally, most of the medications used in the treatment of acute respiratory viral infections have a number of side effects. Currently, one of the promising areas of pharmacy is the study of biologically active substances, the medicinal plant raw material, and production of extracts and herbal medicines based on them. Objective – pharmaceutical development of a scientifically based composition, technology for obtaining anti-inflammatory and antimicrobial tablets developed on the basis of a selected and standardized plant substance-a thick extract of the leaves of sage nutmeg, which grows in Tajikistan.  When solving the task used the methods of evaluating the technological properties of LRS, physico-chemical properties of plant extracts, physical and technological properties of the mass for tabletting, pharmaco-technological tests of the developed tabletsa study of quantitative content of biologically active substances was determined by Pharmacopoeia methods. The developed solid dosage form with thick extract of sage leaves can be registered as a medicinal product, and the developed technology of tablets with thick extract of sage leaves can be of interest to manufacturers of medicinal products from plant raw materials. The developed methods can be used in laboratories for the detection and quantitative determination of BAS in plant raw materials of Clary sage leaves and medicinal products from this LRS. Thus, based on the results of pharmacological and technological research, we have developed a technology for obtaining a thick extract of sage nutmeg and tablets based on it for the treatment of otolaryngological diseases, which in turn is of interest for further research of the developed drug and its introduction into production.

PHYSICO CHEMICAL EVALUATION OF AVIPATTIKARA CHURNA AND ITS DEVELOPED FORM OF SYRUP

INDIAN DRUGS ◽  
2015 ◽  
Vol 52 (06) ◽  
pp. 38-42
Author(s):  
G.G. Gadad ◽  
◽  
K. S. Gudaganatti ◽  
V.S. Mannur
Keyword(s):  
Dosage Form ◽  
Oral Route ◽  
Physicochemical Analysis ◽  
Dosage Forms ◽  
Solid Dosage ◽  
Chemical Evaluation ◽  
Physico Chemical ◽  
Limit Test ◽  
Loss Of Appetite ◽  
Liquid Dosage Form

Development and modification of Ayurvedic classical formulations into widely acceptable dosage forms is an important area to be focused in the present era. The designing of liquid dosage form has generally been emphasized on the basis of ease of administration to those individuals who have difficulty in swallowing solid dosage forms, specially in pediatric and geriatric group. Churna (powders) are the preferentially administered Ayurvedic formulations by oral route. Most of these powders are hygroscopic, bitter to taste and should be administered with suitable vehicle. Avipattikara Churna is one of the unique formulation widely practiced in the management of common ailments like Amlapitta (hyperacidity), Vibandha (constipation), Agnimandya (loss of appetite), Arsha (hemorrhoids). Modification of the classical Churna (solid dosage form) into a more acceptable and convenient syrup (liquid dosage form) with modern pharmaceutical methods and its physico-chemical analysis is the main aim of the study. In the present study Avipattikara syrup was developed with 66.7 % w/V of Khandasharkara (sugar candy powder) without any pharmaceutical additives. Physicochemical analysis, microbial limit test, and physical quality tests for Avipattikara Churna and syrup were carried out respectively. Results suggest that, the developed syrup had a quality of ideal syrup.

scholarly journals Electrospun Solid Dispersions of Maraviroc for Rapid Intravaginal Preexposure Prophylaxis of HIV

2014 ◽  
Vol 58 (8) ◽  
pp. 4855-4865 ◽  
Author(s):  
Cameron Ball ◽  
Kim A. Woodrow
Keyword(s):  
Drug Delivery ◽  
Dosage Form ◽  
Drug Loading ◽  
Solid Dispersions ◽  
High Surface ◽  
Aqueous Media ◽  
Volume Ratio ◽  
Water Soluble ◽  
High Drug ◽  
Solid Dosage

ABSTRACTThe development of topical anti-human immunodeficiency virus (HIV) microbicides may provide women with strategies to protect themselves against sexual HIV transmission. Pericoital drug delivery systems intended for use immediately before sex, such as microbicide gels, must deliver high drug doses for maximal effectiveness. The goal of achieving a high antiretroviral dose is complicated by the need to simultaneously retain the dose and quickly release drug compounds into the tissue. For drugs with limited solubility in vaginal gels, increasing the gel volume to increase the dose can result in leakage. While solid dosage forms like films and tablets increase retention, they often require more than 15 min to fully dissolve, potentially increasing the risk of inducing epithelial abrasions during sex. Here, we demonstrate that water-soluble electrospun fibers, with their high surface area-to-volume ratio and ability to disperse antiretrovirals, can serve as an alternative solid dosage form for microbicides requiring both high drug loading and rapid hydration. We formulated maraviroc at up to 28 wt% into electrospun solid dispersions made from either polyvinylpyrrolidone or poly(ethylene oxide) nanofibers or microfibers and investigated the role of drug loading, distribution, and crystallinity in determining drug release rates into aqueous media. We show here that water-soluble electrospun materials can rapidly release maraviroc upon contact with moisture and that drug delivery is faster (less than 6 min under sink conditions) when maraviroc is electrospun in polyvinylpyrrolidone fibers containing an excipient wetting agent. These materials offer an alternative dosage form to current pericoital microbicides.

scholarly journals DEVELOPMENT OF A SOLID DOSAGE FORM WITH ADSORPTION ACTIVITY

2021 ◽  
Vol 8 (4) ◽  
pp. 233-241
Author(s):  
M. V. Chirkova ◽  
D. K. Gulyaev ◽  
M. P. Chugunova ◽  
V. D. Belonogova
Keyword(s):  
Picea Abies ◽  
Dosage Form ◽  
Raw Materials ◽  
Water Soluble ◽  
Technological Properties ◽  
Adsorption Activity ◽  
Polysaccharide Complex ◽  
Solid Dosage Form ◽  
Solid Dosage ◽  
Soluble Polysaccharide

Enterosorbents are produced in various dosage forms – powders, tablets, pastes, etc., some of them are also manufactured in the form of capsules. A water-soluble polysaccharide complex (WSPC) manifesting a pronounced adsorption activity, which determines the prospects for the development of dosage forms of sorbents, was obtained from the cones of European Spruce (Picea abies).The aim of the work is to develop a solid dosage form with an adsorption activity based on a water-soluble polysaccharide complex from the cones of European Spruce (Picea abies).Materials and methods. The samples of European Spruce (Picea abies) cones were collected on the territory of Ilyinsky district of the Perm Krai and used as plant raw materials. A water-soluble polysaccharide complex was obtained from the raw materials. In order to improve the technological properties of the substance, (WSPC) granulates were obtained. The granulates were hand-made by wet granulation. The adsorption activity of the obtained granules was determined by the ability to bind methylene blue.Results. As a result of the experiment it has been established, that the WSPC substance of European Spruce (Picea abies) cones needs to be improved in its technological properties. Granulation of the substance led to an improvement in technological properties and an increase in the adsorption activity in most of the selected compositions. It has also been shown that increased moisture content of granulate decreases its adsorption activity. A direct dependence of the adsorption activity on the concentration of the granulating liquid (with the exception of some granulates) has been revealed, but no significant effect of the size of the granulate particles on the manifestation of the adsorption effect has been reported. According to the results of the study, a dosage form “Capsules” has been proposed for the compositions that showed the best results of the adsorption activity, and their biopharmaceutical evaluation was carried out according to the disintegration test.Conclusion. Thus, a solid dosage form with an adsorption activity has been obtained. The study shows the prospects for further research on the preparation of the drug with an adsorption activity based on the water-soluble polysaccharide complex of European Spruce (Picea abies) cones.

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