Effect of the mode of super disintegrant incorporation on dissolution in wet granulated tablets (original) (raw)
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2015
The purpose of the study was to formulate immediate release tablets using various types of disintegrants (crospovidone, sodium starch glycolate and sodium carboxymethylcellulose), in order to investigate the effect of mode of incorporation of disintegrants on release mechanism from tablets. Acetaminophen, a poor soluble drug was used as a model drug to evaluate its release characteristics from different formulations. The USP paddle method was selected to perform the dissolution profiles carried out by USP apparatus 2 (paddle) at 50 rpm in 900 ml phosphate buffer pH 5.8. Successive dissolution time, time required for 25%, 50 % and 80 % of the drug release (T25%, T50%, T80%) was used to compare the dissolution results. A One way analysis of variance (ANOVA) was used to interpret the result. Statistically significant differences were found among the drug release profile from all the formulations except mode of addition of crosspovidone. At a fixed amount of disintegrants, extragranular...
2011
The objective of the present investigation was to study the influence of Superdisintegrants like sodium starch glycolate (SSG), croscarmelose sodium (CCS), crospovidone (CP), Physical mixture of Superdisintegrants and Co process superdisintegrants as dissolution enhancer on in-vitro dissolution in a model formulation and their different mode of incorporation like intragranular, extra granular and equal distribution between these two. Among the superdisintegrant croscarmelose sodium showed comparatively faster disintegrations time than sodium starch glycolate and crospovidone.The results indicated that Coprocess superdisintegrant was effective in improving the dissolution of the drugs used in the study and generally intragranular mode of addition seemed to be the best mode of incorporation.
International Journal of Applied Pharmaceutics, 2021
Objective: To synthesize, characterize and evaluate starch crotonate as a superdisintegrant in the formulation of Piroxicam fast dissolving tablets by employing 2 3 factorial design. Methods: Starch crotonate was synthesized and its physical and micromeritic properties were performed to evaluate it. The fast dissolving tablet of Piroxicam were prepared by employing starch crotonate as a superdisintegrant in different proportions in each case by direct compression method using 2 3 factorial design. Results: The starch chrotonate prepared was found to be fine, free flowing and amorphous. Starch crotonate exhibited good swelling in water with swelling index (50%). The study of starch crotonate was shown by fourier transform infrared spectra (FTIR). The drug content (100±5%), hardness (3.6-4 kg/sq. cm), and friability (<0.15%) have been effective with regard to all the formulated fast dissolving tablets employing starch crotonate. The disintegration time of all the formulated tablets was found to be in the range of 18±03 to 66±03 sec. The optimized formulation F8 had the least disintegration time i.e., 18±03 sec. The wetting time of the tablets was found to be in the range of 49.92±0.11 to 140±0.18s. The In vitro wetting time was less (i.e., 74±0.37s) in optimized formulation F8. The water absorption ratio of the formulated tablets was found to be in the range of 27.58±0.01 to 123.07±0.33%. The percent drug dissolved in the optimized formulation F8 was found to be 99.83% in 10 min. Conclusion: Starch crotonate, when combined with sodium starch glycolate, croscarmellose sodium, with Piroxicam was found to be an effective super disintegrant which improved the dissolution efficiency and could therefore be used in the formulation of quick dissolvi ng tablets to provide immediate release of the contained drug within 10 min.
International Journal of Pharmaceutical Sciences, 2024
This work looks into how to improve the oral dissolving qualities of fast disintegrating tablets (FDTs) by formulating and testing them using cutting-edge super disintegrants. Modern super disintegrants have the ability to dissolve and disintegrate quickly in FDTs, which could be advantageous for patient convenience and compliance. To maximize tablet disintegration times, a variety of super disintegrants were used, such as sodium starch glycolate, crospovidone, and croscarmellose sodium. Excipients such binders, diluents, and sweeteners were carefully chosen to ensure compatibility and maintain the overall integrity of the tablet matrix. Hardness, friability, and disintegration time—three physicochemical characteristics of FDTs—were methodically assessed in order to determine how various super disintegrants affected the quality of the tablets. To evaluate the drug release characteristics of FDTs, in vitro dissolution assays were carried out utilizing recognized dissolution media. When the results were compared to those of conventional tablets, the dissolution kinetics showed the enhanced performance ascribed to the addition of super disintegrants. Evaluations of stability under both fast and extended storage settings were carried out to guarantee the long-term resilience of the developed FDTs. A thorough examination looked into how the environment might affect the tablets' chemical and physical stability.
International Journal of Applied Pharmaceutics, 2018
Objective: To synthesize, characterize and evaluate starch xanthate as a superdisintegrant in the formulation of fast dissolving tablets by employing 2 3 Methods: Starch xanthate was synthesized by gelatinization process. The physical and micromeritic properties were performed to evaluate the synthesized starch xanthate. The fast dissolving tablet of ibuprofen was prepared by employing starch xanthate as a superdisintegrant in different proportions in each case by direct compression method using 2 factorial design. 3 factorial design. The drug content, hardness, friability, disintegration time and other dissolution characteristics like percent dissolved in 5 min (PD5), dissolution efficiency in 5 min (DE5%) and first order rate constant (K1 Results: The starch xanthate prepared was found to be fine, free flowing slightly crystalline powder. Starch xanthate exhibited good swelling in water. The study between ibuprofen and starch xanthate was shown the absence of interaction by fourier transform infrared spectra (FTIR) and differential scanning calorimetry (DSC). The drug content (100±5%), hardness (3.6-4 kg/sq. cm), and friability (0.12-0.15%) has been effective with regard to all the formulated fast dissolving tablets employing starch xanthate. The disintegration time of all the formulated tablets was found to be in the range of 12±0.01 to 312±0.02s. The optimized formulation F5 has the least disintegration time i.e., 12±0.01s. The In vitro wetting time of the formulated tablets was found to be in the range of 76±0.21 to 217±0.17s. The In vitro wetting time was less (i.e., 90s) in optimized formulation F5. The water absorption ratio of the formulated tablets was found to be in the range of 16±0.16 to 174±0.21%. The cumulative drug dissolved in the optimized formulation F5 was found to be 99.83±0.56% in 5 min.) were used in the evaluation of prepared fast dissolving tablets. Conclusion: The dissolution efficiency of ibuprofen was enhanced when starch xanthate was found to be a superdisintegrant when combined with sodium starch glycolate, croscarmellose sodium and, hence it could be used in the formulation of fast dissolving tablets to provide immediate release of the contained drug within 5 min.
AAPS PharmSciTech, 2005
The purpose of this study was to investigate the efficiency of superdisintegrants in promoting tablet disintegration and drug dissolution under varied media pH. Significant reductions in the rate and extent of water uptake and swelling were observed for both sodium starch glycolate (Primojel) and croscarmellose sodium (Ac-Di-Sol) in an acidic medium (0.1 N HCl) but not for crospovidone NF (Polyplasdone XL10), a nonionic polymer. When Primojel and Ac-Di-Sol were incorporated in model formulations, a significant increase in tablet disintegration time was observed for slowly disintegrating tablets (lactose-based tablets) but not for the rapidly disintegrating tablets (dicalcium phosphate-based tablets). The dissolution rate of the model drug, hydrochlorothiazide, was found highly dependent on both tablet disintegration efficiency and the solubility of base material(s) in the testing medium. A laser diffraction particle size analyzer proved to be an effective tool for determining the intrinsic swelling of disintegrant particles in different media. Water uptake and swelling were confirmed as 2 important functions of superdisintegrants. The reduced water uptake and swelling capacity of disintegrants containing ionizable substituents in an acidic medium can potentially jeopardize their efficiency in promoting tablet disintegration and the drug dissolution rate.
Journal of Young Pharmacists, 2012
to their in vivo performance. ODT technologies used range from lyophilization to tablet compression resulting in ODTs with differing characteristics. Lyophilized tablets and ODTs formulated by moulding at low pressure disintegrate rapidly due to their porous structure. This high porosity contributes to their weak mechanical strength, an undesirable quality requiring special packaging. The ideal property of ODTs is rapid buccal disintegration with sufficient mechanical strength to allow for handling and shipment without recourse to specialized packaging.
Effect of drug-carrier interaction on the dissolution behavior of solid dispersion tablets
Pharmaceutical Development and Technology, 2010
The objective of this study was to compare the dissolution behavior of tablets prepared from solid dispersions with and without drug-carrier interactions. Diazepam and nifedipine were used as model drugs. Two types of carriers were used; polyvinylpyrrolidone (PVP K12, K30 and K60) and saccharides (inulin 1.8 kDa, 4 kDa and 6.5 kDa). Solid dispersions with various drug loads were prepared by lyophilization. It was found that the drug solubility in aqueous PVP solutions was significantly increased indicating the presence of drug-carrier interaction while the drug solubility was not affected by the saccharides indicating absence of drug-carrier interaction. X-ray powder diffraction and modulated differential scanning calorimetry revealed that all solid dispersions were fully amorphous. Dissolution behavior of solid dispersion tablets based on either the PVPs or saccharides was governed by both dissolution of the carrier and drug load. It was shown that a fast drug dissolution of solid dispersions with a high drug load could be obtained with carrier that showed interaction with the drug.
Water-sorption properties of tablet disintegrants
Journal of Pharmaceutical Sciences, 1975
The water-sorption properties of four tablet disintegrants, starch, sodium carboxymethylcellulose, sodium starch glycolate, and a cation-exchange resin, were examined in the form of powders and in compressed tablets prepared from calcium phosphate dibasic dihydrate. Dissolution properties of the tablets compare well to the water-sorption properties. The effect of storage in the presence of water vapor upon tablets containing the various disintegrants was evaluated in terms of tablet hardness and disintegration time. Differences in the effects produced in the various tablet formulations can be related to the differing mechanisms whereby the disintegrants effect tablet rupture. Photomicrographic data support the conclusions drawn from the water-sorption, disintegration, and dissolution studies. Sodium starch glycolate and the cation-exchange resin merit careful consideration by formulators using calcium phosphate dibasic dihydrate or similar direct compression matrixes.
Objective: The aim of the present study was to formulate the oro dispersible tablets (ODTs) of Orlistat (OST) by direct compression technique using melt granulation method. Methods: Super disintegrants were used for the preparation of ODTs namely Crospovidone (CP), Croscarmellose sodium (CCS), Sodium starch glycolate (SSG). The powder mixture was subjected to pre compression evaluation like FTIR, Micromeritic, solubility studies and post-compression evaluation like friability, hardness, wetting time, dispersion time, disintegration time and in vitro dissolution rate. Results: FTIR studies confirmed that there was no chemical interaction between the drug and excipients. Micromeritic studies revealed that the powder blend has good flow ability. The results of hardness and friability complied with the official standards. The solid dispersions (SDs) prepared in OST to PEG 6000 ratio of 1:2 were showed good solubility than other SDs and it was selected for formulation development. It was evident from the results that the increase in super disintegrants concentration decreases the wetting, dispersion and disintegration times and CP showed the best results than other super disintegrating agents. Conclusion: The F4 formulation showed optimum drug release of 98.99 % at the end of 15 min when compared to the other formulations; it might be due to the presence of CP.