Variation concentration effect of propyleneglycol, glycerin, and polyethyleneglycol 400 to physical properties and dissolution rate of loratadine liquisolid tablet

2021 ◽  
Vol 32 (4) ◽  
pp. 583-587
Author(s):  
Mikhania Christiningtyas Eryani ◽  
Esti Hendradi ◽  
Siswandono

Abstract Objectives This study aimed to evaluate the variation concentration effect of propyleneglycol, glycerin, and polyethyleneglycol 400 as a nonvolatile solvent on the physical properties and dissolution rate of the loratadine liquisolid tablet. Methods The tablet was formulated into 10 formulas, where nine were liquisolid and one was conventional (CT). The concentration of propyleneglycol, glycerin, and polyethyleneglycol used in liquisolid tablets were 14, 15, and 16%. Furthermore, the mixture was evaluated based on flow properties and compressibility index. The tablet was evaluated based on hardness, friability, disintegration time, and dissolution, and the data obtained was evaluated with ANOVA or Kruskal–Wallis statistic program. Results The result showed that flow properties, disintegration time, and dissolution have a significant value less than 0.05. The tablet friability for all concentration solvents, hardness at 14 and 15% solvent concentration, and compressibility index at 15 and 16% have significant value more than 0.05. The 16% propyleneglycol type solvent concentration tablet has the physical properties and contains the best solution Conclusions From the result, it is reasonable to conclude that F7 is the tablet with all the physical properties and the best dissolution.

Author(s):  
Ganesh kumar Gudas ◽  
Manasa B ◽  
Senthil Kumaran K ◽  
Rajesham V V ◽  
Kiran Kumar S ◽  
...  

Promethazine.HCl is a potent anti-emetic. The central antimuscarinic actions of antihistamines are probably responsible for their anti-emetic effects. Promethazine is also believed to inhibit the medullary chemoreceptor trigger zone, and antagonize apomorphine -induced vomiting. Fast dissolving tablets of Promethazine.HCl were prepared using five superdisintegrants viz; sodium starch glycolate, crospovidone, croscarmellose, L-HPC and pregelatinised starch. The precompression blend was tested for angle of repose, bulk density, tapped density, compressibility index and Hausner’s ratio. The tablets were evaluated for weight variation, hardness, friability, disintegration time (1 min), dissolution rate, content uniformity, and were found to be within standard limit. It was concluded that the fast dissolving tablets with proper hardness, rapidly disintegrating with enhanced dissolution can be made using selected superdisintegrants. Among the different formulations of Promethazine.HCl was prepared and studied and the formulation S2 containing crospovidone, mannitol and microcrystalline cellulose combination was found to be the fast dissolving formulation. In the present study an attempt has been made to prepare fast dissolving tablets of Promethazine.HCl, by using different superdisintegrants with enhanced disintegration and dissolution rate. 


2020 ◽  
Vol 5 (2) ◽  
pp. 220-229
Author(s):  
Dyera Forestryana ◽  
◽  
Yunitha Hestiarini ◽  
Aristha Novyra Putri

Water pumpkin (Lagenaria siceraria) is a vegetable that contains secondary metabolites that are beneficial to health. Its use as a vegetable is less attractive to the people so that to increase its utilization, dosage forms are made that can attract public interest, one of which is effervescent granules. Effervescent granules are the most popular dosage form because they can serve in fresh drinks. This study aims to determine the effect of variations in the concentration of acids (citric acid-tartaric acid) and base (sodium bicarbonate) on the physical properties of the formula. The water pumpkin effervescent granules made with various ratios of citric acid, tartaric acid, and sodium bicarbonate consisting of FI (2: 1: 2.5); F II (1: 2: 2,5); F III (2: 1: 3,52); F IV (1: 2: 3,44). The granule made by the wet granulation method. The physical properties of the formula included organoleptic, moisture content, flow properties, compressibility index, pH, solubility time, and acceptability test. Based on the results of the evaluation of physical properties, the granule formula of the water pumpkin effervescent meets the standard requirements with a moisture content of 1.26% -2.26%, flow properties from 6.33 to 7.0 seconds, angle of repose 31.14˚-33.69 ˚, compressibility index 13.61% -17.08%, pH 6.1-7.1 and dissolving time 191-223.33 seconds. Variations of citric acid-tartaric acid and sodium bicarbonate affect the physical properties and taste of the effervescent granules. Based on the acceptability test showed that the panelists liked the water pumpkin effervescent granules in FII.


2017 ◽  
Vol 9 (6) ◽  
pp. 39
Author(s):  
Zainab E. Jassim

Objective: The purpose of this study was to enhance the dissolution pattern of the practically water-insoluble diuretic drug, furosemide through its formulation into liquisolid tablets.Methods: A mathematical model was used to formulate four liquisolid powder systems using polyethylene glycol 400 as a non-volatile water miscible liquid vehicle. The liquid loading factors of the vehicle were used to calculate the optimum quantities of carrier (Avicel PH 102) and coating materials (Aerosil 200) needed to prepare acceptably flowing and compactible powder mixtures and (R) ratio used was 25. The liquisolid tablets were evaluated for weight variation, percent friability, hardness, content uniformity, disintegration time and in vitro drug release profile. Drug and the prepared systems were characterized by fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC) and powder x-ray diffraction (PXRD) studies.Results: The enhanced dissolution rate due to the increased wetting properties and the large available surface areas for dissolution were obtained in case of the liquisolid tablets. The selected optimal formulation (F2) of 50% drug concentration released 90% of its content during the first 10 min compared to 65% of DCT. FTIR studies revealed that there was no interaction between drug and polymers. DSC and PXRD indicated conversion of crystalline to amorphous form of furosemide. Conclusion: The dissolution rate of furosemide can be enhanced to a great extent by liquisolid technique.


Author(s):  
Rishi Thakkar ◽  
Yu Zhang ◽  
Jiaxiang Zhang ◽  
Mohammed Maniruzzaman

AbstractThis study demonstrated the first case of combining novel continuous granulation with powder-based pharmaceutical 3-dimensional (3D) printing processes to enhance the dissolution rate and physical properties of a poorly water-soluble drug. Powder bed fusion (PBF) and binder jetting 3D printing processes have gained much attention in pharmaceutical dosage form manufacturing in recent times. Although powder bed-based 3D printing platforms have been known to face printing and uniformity problems due to the inherent poor flow properties of the pharmaceutical physical mixtures (feedstock). Moreover, techniques such as binder jetting currently do not provide any solubility benefits to active pharmaceutical ingredients (APIs) with poor aqueous solubility (>40% of marketed drugs). For this study, a hot-melt extrusion-based versatile granulation process equipped with UV-Vis process analytical technology (PAT) tools for the in-line monitoring of critical quality attributes (i.e., solid-state) of indomethacin was developed. The collected granules with enhanced flow properties were mixed with vinylpyrrolidone-vinyl acetate copolymer and a conductive excipient for efficient sintering. These mixtures were further characterized for their bulk properties observing an excellent flow and later subjected to a PBF-3D printing process. The physical mixtures, processed granules, and printed tablets were characterized using conventional as well as advanced solid-state characterization. These characterizations revealed the amorphous nature of the drug in the processed granules and printed tablets. Further, the in vitro release testing of the tablets with produced granules as a reference standard depicted a notable solubility advantage (100% drug released in 5 minutes at >pH 6.8) over the pure drug and the physical mixture. Our developed system known as DosePlus combines innovative continuous granulation and PBF-3D printing process which can potentially improve the physical properties of the bulk drug and formulations in comparison to when used in isolation. This process can further find application in continuous manufacturing of granules and additive manufacturing of pharmaceuticals to produce dosage forms with excellent uniformity and solubility advantage.Abstract Figure


2021 ◽  
Vol 16 (2) ◽  
pp. 111-117
Author(s):  
B.B. Mohammed ◽  
E.J. John ◽  
G.T. Abdulsalam ◽  
K.P. Bahago

Background: Tablets must be able to release the active drug in the gastrointestinal tract for absorption. The release profile of solid pharmaceutical dosage formulations can be quantified by assessing the disintegration and dissolution times tests. Binders are adhesives either from sugar or polymeric material that are added to tablet formulations to provide the cohesiveness required for the bonding together of the granules under compaction to form tablets.Objective: The objective of the study was to formulate and assess ibuprofen tablets using different concentrations of binders (Acacia and Gelatin).Methods: The granules were prepared using wet granulation method and analysed for flow properties based on USP/NF protocols. After granule compression, the tablets release profiles were thereafter assessed via the tablet dissolution and disintegration tests.Results: Weight variation, thickness and diameter were within the acceptable values for all batches indicative of a uniform flow. Batches with binder concentrations of 10 % and 20 % failed disintegration test due to a disintegration time above 15 min while the release rate for batches 1 and 4 was about 88 % in 60 min as against the other batches whose release rate was less than 50 % in 60 min as a result of increasing their binder concentrations.Conclusion: The study concluded that increasing the concentration of acacia and gelatin above 5% led to a decrease in percentage of drug released and an increase in disintegration time above 30 mins because 5% batches gave the best release profiles.


2015 ◽  
Vol 26 (1) ◽  
pp. 40-44

The preparation suppositories contain 250 mg of paracetamol on different bases using Novata BD, Novata BCF and composition of Novata BCF/BD (1:1). Suppositories were prepared by the fusion method. The prepared formulations with or without surfactants (Tween 80, Span 60) at concentrations of 2% and 4% (w/w) were tested for hardness, to tal time of de for ma tion, disintegration time, content uniformity and release of the drug. The release of the drug was carried in the apparatus with the stirrer shade in phosphate buffer (pH 7.2) at 100 rpm. The physical properties of the prepared suppositories were according with the requirement of Polish Pharmacopoeia 9th edition. Addition of 4 % Tween 80 to suppository bases significantly increased the drug release from all the investigated formulations. However, incorporation of Span 60 did not result in improvement of the drug release significantly.


Author(s):  
Setyawan D. ◽  
Siswandono Siswandono ◽  
Winantari A. N. ◽  
Zu’aimah K.

Objective : Acyclovir (ACV) is well-known antiviral agent that has absorption problem, mainly due to its poor solubility in water and oral bioavailability. To improve acyclovir physical properties, especially dissolution properties, acyclovirnicotinamide(NCT) cocrystal was formed. Methods : ACV-NCT cocrystal was prepared using slurry method using ethanol as solvent with different concentration. The ACV-NCT cocrystal from each sample groups was characterized using powder X-ray diffraction (PXRD), and then dissolution properties evaluated. Results : Each ACV-NCT cocrystals prepared from slurry method with different ethanol concentrations have different PXRD profile. Dissolution analysis (ED15) showed that ACV-NCT cocrystallization using slurry methods with 10,0 ml/g as ethanol concentration significantly increase ED15 values compared to acyclovir and acyclovir-nicotinamide physical mixture (α=0,05). Conclusion : ACV-NCT cocrystal successfully formed using slurry method with 10,0 ml/g as optimal ethanol concentration.


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