scholarly journals RESEARCH ON THE SELECTION OF EXCIPIENTS AS THE RATIONALE FOR THE COMPOSITION OF THE TABLETS WITH DRY EXTRACT OF SANGUISORBA OFFICINALIS

2020 ◽  
Vol 2 ◽  
pp. 66-75
Author(s):  
Lyudmila Shulga ◽  
Kateryna Bezkrovna ◽  
Nina Domar

The aim. The aim of the research was to study the effect of different groups of excipients on the pharmaco-technological propertiesof the powder mass for tabletting in the development of the composition of the tablets with dry extract of Sanguisorba officinalis for complex therapy of the gastrointestinal tract diseases. Materials and methods. Objects of study - dry extract Sanguisorba officinalis, 25 excipients used in the production of tablets by the method of direct compression, grouped into five groups of factors (fillers based on sugars and microcrystalline cellulose, disintegrants, glidants and lubricants), samples of powder masses. Studies on the determination of pharmaco-technological properties (fluidity, bulk density, bulk density after shrinkage, degree of compressibility, Hausner ratio, and angle of repose) of the obtained powder masses were carried out according to the methods of the State Pharmacopoeia of Ukraine, Second edition. The method of mathematical planning of the experiment was used in the work, the obtained results were subjected to variance analysis, and the ranked series of advantages were placed, in which the excipients were placed in the sequence of their influence on the studied pharmaco-tecnological parameters. Results and discussion. The influence of excipients (factors) on the pharmaco-technological properties (responses) of the powdered tablet masses with the construction of ranked benefits was studied using a five-factor experiment, a hyper-Graeco-Latin square. The results of the analysis of variance showed that glidants have the greatest influence on the fluidity, the bulk density and the bulk density after shrinkage. Neusilin US 2 significantly affects the fluidity of the powder masses and Hausner ratio, the talc having the greatest effect on the bulk density and the bulk density after shrinkage of the powder masses. The representative of the disintegrants group – Sodium starch glycolate most influences the compressibility index, the sugar-based filler – Pearlitol 500 DC – on the angle of repose. Conclusions. The effect of 25 excipients on the pharmaco-technological characteristics of the powdered tablet masses with dry extract of Sanguisorba officinalis was studied. It was found that among the sugars-based fillers equally good results were shown in the powder masses with Compri sugar, Tablettose 80 and Pearlitol 500 DC; among the microcrystalline cellulose based fillers is Prosolv 90; among glidants – Neusilin US 2; no comparison was made of the disintegrants and lubricant excipients from the studied list of leader substances. The results of the studies indicate the possibility of obtaining tablets by the direct compression method, and further study of their pharmaco-technological characteristics will allow to establish the optimal composition of excipients.

2019 ◽  
Vol 3 ◽  
pp. 26-34 ◽  
Author(s):  
Оlena Ruban ◽  
Malek Alkhalaf ◽  
Nataliia Gerbina

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.


2019 ◽  
Vol 11 (02) ◽  
pp. 37-42
Author(s):  
Desy Nawangsari

Avicel® PH is branded name from microcrystalline cellulose that is generally used in pharmaceutical preparations. Avicel® PH are being used as filler or binder in dosage formulas in tablets especially for direct compression because having a good flowing rate and a good compressibility. This study aims to compare the influence of the use Avicel® PH 101 and Avicel® PH 102 as a filler on of preparations a tablet of ascorbic acid. A method of the research was conducted by making granule of ascorbic acid tablet with the variation filler, then the granule was evaluate in .The results showed Avicel® PH 102 as a filler produce granule which better seen from the flowability, static angle of repose, carr’s index and hausner ratio .  


2020 ◽  
pp. 18-21
Author(s):  
E. Blynskaya ◽  
S. Tishkov ◽  
V. Bueva ◽  
K. Alekseev ◽  
V. Alekseev ◽  
...  

Medicated chewing gum is a convenient dosage form that allows to expand the range of medicines, ensure adherence of patients to the treatment and extend patent protection for well-known names of medicines. This article describes the technological properties of the Health in Gum® chewing gum base, which provides medicinal chewing gums with minimal addition of excipients by direct compression.


2019 ◽  
Vol 7 (22) ◽  
pp. 3729-3732
Author(s):  
Urip Harahap ◽  
Marianne Marianne ◽  
Yuandani Yuandani ◽  
Lia Laila

BACKGROUND: Pugun tano extract had been studied for its effect as hepatoprotector. However, the usage of the plant in the form of extract has a limitation, especially if the extract is consumed by the people due to the unpleasant taste and odour. Then, the extract needs to be transformed into a particular dosage form, such as a capsule. But before the capsule can be produced, a preformulation study of pugun tano extract into a granule mass in capsule need to be evaluated. AIM: The study aimed to formulate the ethanolic extract of pugun tano (Curanga fel-terrae (Lour.) Merr) as granule mass in the capsule dosage form. METHODS: The pugun tano ethanolic extract was formulated in several steps included preparation of dry extract using coating method with polyvinylpyrrolidone (PVP) and granule mass production. The excipients used for the granule mass were lactose granules (made with tapioca starch using wet granulation), corn starch (made with 3 concentrations of 5% (F1), 7.5% (F2) and 10% (F3)), talcum, magnesium stearate, methylparaben, and propylparaben. The granule mass was evaluated for the bulk density, tapped density, inter-particle porosity, Carr’s index, Hausner ratio, angle of repose, and flowability. RESULTS: The results showed that all of the formulae passed the requirement of the preformulation test. The bulk density of the granule mass was 0.79 – 0.86 g/ml; the tapped density was 0.88 – 0.90 g/ml; the inter-particle porosity was 0.03 – 0.14; the Carr’s index was 2.71 – 11.94%; the Hausner ratio was 1.09-1.12; the angle of repose was 26.10 – 28.90°; and the flowing time was 5.97 – 6.63 seconds. All of the formulae showed good flowability and free-flowing properties. CONCLUSION: It is concluded that the obtained formula


2020 ◽  
Vol 19 (8) ◽  
pp. 1569-1576
Author(s):  
Hamad S. Alyami ◽  
Samer S. Abu-Alrub ◽  
Mater H. Mahnashi ◽  
Mohammad H. Alyami ◽  
Osaid T. Al Meanazel

Purpose: To investigate the influence of two often-used excipients (starch and microcrystalline cellulose) on the physical properties of powder blends and tablets that contain mannitol as diluent.Methods: Powder and powder mixtures of three commonly used excipients (starch, mannitol and microcrystalline cellulose) were thoroughly examined using the angle of repose for flowability, particle size analyzer to determine the diameter of the particles, scanning electron microscopy (SEM) for morphological assessment, and x-ray diffraction to determine crystalline/amorphous characteristics. Tablets were prepared by direct compression technique and were evaluated for mechanical strength and disintegration behavior as part of quality control test.Results: The results showed that increase in MCC concentration of the mixture leads to significantly enhanced flowability (p < 0.05) when compared to starch. The angle of repose for mannitol/MCC powder mixture with 70 % w/w MCC was approximately 29°, indicating good flow properties of thepowder mix. Moreover, starch tablets containing MCC exhibited better mechanical strength and longer disintegration time, while, at 1:1 ratio of MCC and mannitol, tablet disintegration was faster (33.0 ± 5.2s)Conclusion: MCC (at 30 %w/w in the blend) produces optimal flow of the powder blend and superior mechanical strength, Keywords: Tablet disintegration, Flowability, Starch, Hardness, Mechanical strength


2021 ◽  
pp. 73-81
Author(s):  
Svitlana Chernetska ◽  
Natalia Beley ◽  
Mariana Demchuk

The aim. The aim of the research was to study the influence of excipients amount on the technological parameters of the compression mixture and tablets based on dry extract of Origanum vulgare L. herb using the method of random balance. Materials and methods. Objects of the study – Origanum vulgare L. herb dry extract, 8 excipients that have been studied at two quantitative levels. The tablets were prepared by direct compression method. The formulations were designed according to the method of random balance. The technological parameters of the compression mixture and tablets based on Origanum vulgare L. herb dry extract have been studied as a function of quantitative factors: silicon, magnesium carbonate basic, dioxide magnesium aluminometasilicate (Neusilin S1®), isomalt (GalenIQ™720), F-melt® Type C (co-spray dried excipients), sucralose, berry flavor and citric acid. Results and discussion. The increase in the amount of Neusilin S1®, GalenIQ™720 and F-melt®, and the decrease in the amount of magnesium carbonate basic and silicon dioxide improved the flowability expressed by the Hausner ratio. Results of bulk density and tapped density of the compression mixture depended on the quantities of GalenIQ™720 and F-melt®. All formulations of the prepared tablets had the rapid disintegration and ranging from 6 to 15 minutes. Resistance for crushing and friability tablets’ were improved with a decrease in the amount of silicon dioxide and increase in the amount of Neusilin S1®, F-melt® and sucralose. Higher resistance to moisture of tablets based on Origanum vulgare L. dry extract was obtained by using Neusilin S1®, F-melt® and sucralose on the upper levels. Conclusions. The tablets based on Origanum vulgare L. herb dry extract were successfully manufactured by direct compression method. The random balance method enabled us to identify the most significant quantitative factors to optimize their composition in the tablets based on the dry extract of Origanum vulgare L. herb.


Author(s):  
T. A. Butkevych ◽  
М. L. Syatynya ◽  
V. P. Popovych

The aim of the work. To study the pharmaco-technological properties of granulate and tablets based on Flammulina velutipes biomass dry powder, to develop the composition and technology of the medication. Materials and Methods. Research of granules and tablets pharmaco-technological properties (sieve analysis, bulk density, tapped density, compressibility index, Hausner ratio, flowability of tablet mass, average weight, resistance to crushing, friability and disintegration of tablets) was carried out in accordance to the requirements of State Pharmacopoeia of Ukraine 2nd edition. Results and Discussion. The determined pharmaco-technological parameters of the granulate indicate good values ​​of the bulk density, tapped density, compressibility index, Hausner ratio and flowability. An intermediate product undergoes a tabletting process to produce a qualitative finished product of satisfactory appearance (plain, cylindrical tablets with a facet, yellowish-white color with brown inclusions, with a height of 4 mm, and diameter of 10 mm), a constant average mass (1.0 g), and strength (68 N). Conclusions. The pharmaco-technological properties of tablet mass (granulate) and Flammulina velutipes biomass dry powder tablets (sieve analysis, bulk density, tapped density, compressibility index, Hausner ratio, flowability, average weight, resistance to crushing, friability and disintegration) were studied. The composition and technology of Flammulina velutipes biomass dry powder tablets have been developed, pharmaco-technological parameters of their quality have been studied, technological block diagram of industrial production has been developed.


Author(s):  
María de J. Perea-Flores ◽  
Miriam F. Fabela-Morón ◽  
Adolfo A. Rayas-Amor ◽  
Rigoberto V. Pérez-Ruíz ◽  
Rafael Ruíz-Hernández ◽  
...  

Objective: Evaluate the physical-chemical properties and characterize the microstructure of four varieties of traditional Mexican chili (Capsicum annuum L.) powders: “Arbol”, “Guajillo”, “Piquin” and “Mole ranchero” (Ancho chili). Design/methodology/approach: Physical-chemical properties of chili powders were evaluated by means of moisture content, particle size, aerated and tapped bulk density, Carr index, Hausner ratio, angle of repose (flow properties), capsaicin, and carotenoids content. Microstructure of samples was characterized by Confocal Laser Scanning Microscopy and Scanning Electron Microscopy. ANOVA analysis and Tukey test were performed to evaluate the significant statistical difference between samples at 95% of confidence level. Results: “Arbol”, “Guajillo”, “Piquin” and “Mole Ranchero” chili powders presented a cohesive behavior respect to its flow properties related to aerated and tapped bulk density, angle of repose, Carr Index, and Hausner ratio values under moisture content between 6.59-14.48 gH2O/100g d.s. “Arbol” and “Piquin” chili powders presented the higher capsaicin content, while “Guajillo” and “Mole ranchero” showed the higher carotenoids content. FTIR spectra confirmed the presence of secondary amide, phenolic groups, alkanes, and aliphatic chains that belong to capsaicin structure at specific absorption bands. Microstructure of chili powders presented particles with surface imperfections as cracks and dents, and smooth surface that influence physical-chemical and flowability properties. Limitations on study/implications: Hight moisture content affect the physical-chemical properties, flowability and microstructure of traditional Mexican chili powders. Findings/conclusions: Moisture content between 6.59 and 14.48 gH2O/100g d.s. influences the physical-chemical properties, flowability and microstructure of traditional Mexican chili powders. To improve physical-chemical properties and flowability behavior of chili powders is required that moisture content be lower than 6.59 H2O/100g d.s.


Author(s):  
Kusuma P. ◽  
Syukri Y ◽  
Sholehuddin F. ◽  
Fazzri N. ◽  
Romdhonah . ◽  
...  

The most efficient tablet processing method is direct compression. For this method, the filler-binder can be made by coprocessing via spray drying method. The purpose of this study was to investigate the effect of spray dried co-processing on microcrystalline cellulose (MCC) PH 101, lactose and Kollidon® K 30 as well as to define the optimum proportions. Spray dried MCC PH 101, lactose, and Kollidon® K 30 were varied in 13 different mixture design proportions to obtain compact, free-flowing filler-binder co-processed excipients (CPE). Compactibility and flow properties became the key parameters to determine the optimum proportions of CPE that would be compared to their physical mixtures. The result showed that the optimum proportion of CPE had better compactibility and flow properties than the physical mixtures. The optimum CPE, consisting of only MCC PH 101 and Kollidon® K 30 without lactose, that were characterized using infrared spectrophotometer, differential scanning calorimetry (DSC), X-ray diffraction (XRD), and scanning electron microscope (SEM) indicated no chemical change therein. Therefore, this study showed that spray dried MCC PH 101, lactose and Kollidon® K 30 could be one of the filler-binder alternatives for direct compression process.


Bio-Research ◽  
2020 ◽  
Vol 18 (1) ◽  
Author(s):  
BB Mohammed ◽  
EJ John ◽  
NK Ajuji

Tablets at present, remain the most preferred oral dosage form because of many advantages they offer to formulators as well as physicians and patients. The objective of this work was to determine the effect of co-processing on the disintegration and drug-release profile of ibuprofen tablets prepared from a co-processed excipient. The co-processed excipient (CE) containing lactose, gelatin and mucin in the ratio 90:9:1 was prepared using co-fusion. The excipient was evaluated for its physicochemical properties and then used to formulate tablets with the addition of a disintegrant by direct compression. The tablets were evaluated for their tablet properties and compared with tablets prepared with cellactose- 80® (CEL) and spray dried lactose® (SDL) and a physical mix (PM) of the co-processed ingredient. Results from evaluation of CE showed that flow rate, angle of repose, Carr’s index and Hausner’s ratio were 5.28 g/sec, 20.30o, 23.75 % and 1.31, respectively. Tablets prepared with CE had friability (0%), crushing strength (5.25) KgF, disintegration time (3 mins) and T50% (2 mins). For CEL, friability (0.4 %), crushing strength (7.25) KgF, disintegration time (1 min) and T50% (2 mins); SDL, friability (1.57 %), crushing strength (7.50) KgF, disintegration time (4 mins) and T50% (2 mins) and PM, friability (2.38 %), crushing strength (5.00) KgF, disintegration time (1 min) and T50% (2 mins). In conclusion, the disintegration time and drug release profile for CE was not superior but compared favorably with CEL, SDL and PM.  


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