SYNTHESIS, CHARACTERIZATION AND EVALUATION OF STARCH XANTHATE AS A SUPERDISINTEGRANT IN THE FORMULATION OF FAST DISSOLVING TABLETS Original Article (original) (raw)
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International Journal of Applied Pharmaceutics, 2017
Objective: To evaluate starch xanthate as a super disintegrant in the formulation of fast dissolving tablets of poorly soluble drugs employing 2 3 factorial design. Methods: Starch xanthate was synthesized by gelatinization process. The synthesized starch xanthate was subjected to physical and micromeritic evaluation. To establish as starch xanthate as a super disintegrant, fast dissolving tablet of ibuprofen was prepared employing starch xanthate in different proportions in each case by direct compression method employing 2 3 factorial design. All fast dissolving tablets prepared were evaluated for 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. Fourier transform infrared spectra (FTIR) and Differential scanning calorimetry (DSC) study indicated the absence of interaction between Ibuprofen and starch xanthate. All the fast dissolving tablets formulated employing starch xanthate were of good quality with regard to drug content(100±5%), hardness (3.6-4 kg/sq. cm), and friability (0.12-0.15%). The disintegration time of all the formulated tablets was found to be in the range of 13±0. 02 to 108±0.02s. The optimised formulation FL7 has the least disintegration time i.e., 13±0. 02s. The In vitro wetting time of the formulated tablets was found to be in the range of 90±0.15 to 369±0.17s. The In-Vitro wetting time was less (i.e., 90s) in optimized formulation FL7. The water absorption ratio of the formulated tablets was found to be in the range of 94±0.16 to 192±0.15%. The cumulative drug dissolved in the optimized formulation FL7 was found to be 99.63±0.24% in 5 min. Conclusion: Starch xanthate was found to be a super disintegrant which enhanced the dissolution efficiency when combined with sodium starch glycolate, croscarmellose sodium, with the ibuprofen and hence it could be used in the formulation of fast dissolving tablets to provide immediate release of the contained drug within 5 min.
International Journal of Applied Pharmaceutics
Objective: To synthesize, characterize and evaluate starch xanthate as a superdisintegrant in the formulation of fast dissolving tablets by employing 23 factorial design.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 23 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) were used in the evaluation of prepared fast dissolving tablets.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 ...
The aim of the present investigation was to develop fast dissolving tablets of Ibuprofen, an NSAID drug used for the treatment of arthritis. Due to its low solubility, gastric irritation and its short biological half-life of 2 hours, fast dissolving tablets of Ibuprofen were prepared using superdisintegrants in order to improve the dissolution rate, thereby the absorption and to reduce gastric irritation. The influence of concentration of the sodium starch glycolate was studied by a set of four formulations (F1, F2, F3, F4) with concentrations of sodium starch glycolate viz, 2%, 3%, 4% & 5%w/w respectively. Also the influence of various superdisintegrants was studied by a set of three formulations (F4, F5 and F6) with three superdisintegrants viz, Sodium starch glycolate(5%), Croscarmellose sodium(5%), Crospovidone (5%) respectively. The formulation prepared with 5%w/w of sodium starch glycolate was offered relatively rapid release of Ibuprofen when compared with other concentrations of Sodium Starch glycolate. The formulation prepared with Crospovidone was offered relatively rapid release of Ibuprofen when compared with other superdisintegrants. So, we can conclude that nature and concentration of the superdisintegrant showed influence on the rate of dissolution. The dissolution rate was found to follow first order kinetics.
Asian Journal of Pharmaceutical and Clinical Research, 2021
Objective: The main aim is to design, optimize, and evaluate ibuprofen fast-dissolving tablets by employing starch valerate-A novel super disintegrant. Methods: The fast-dissolving tablet of ibuprofen was prepared by employing starch valerate as super disintegrant in different proportions in each case by direct compression method using 23 factorial design, sodium starch glycolate, and crospovidone used as super disintegrants. In the 2 3 factorial design, these super disintegrants were applied to investigate the interaction effects of three variables, that is, (a) starch valerate, (b) sodium starch glycolate, and (c) crospovidone. The drug content, hardness, friability, disintegration time, and other dissolution characteristics were determined. Results: The starch valerate prepared was found to be fine, free-flowing, slightly crystalline powder. Starch xanthate exhibited good swelling in water with 125.2%. All the fast-dissolving tablets formulated employing starch valerate were of good quality with regard to drug content (100±5%), hardness (3.6-3.8 kg/sq. cm), and friability (0.11-0.12%). The disintegration time of all the formulated tablets was found to be in the range of 12±0.02 to 30±0.02s. The optimized formulation FL8 has the least disintegration time, that is, 12±0. 02s. The in vitro wetting time of the formulated tablets was found to be in the range of 21±0.09 to 44±0.10s. The in-vitro wetting time was less (i.e., 90s) in optimized formulation FL8. The water absorption ratio of the formulated tablets was found to be in the range of 30±0.12 to 100±0.09%. Conclusion: Starch valerate was found to be a super disintegrant which enhanced the dissolution efficiency when combined with sodium starch glycolate, crospovidone, with the ibuprofen.
SBT Journals Formulation and Evaluation of Fast Dissolving Tablet of Ibuprofen by Sublimation Method
2015
The aim of the proposed work was to formulate and characterize fast dissolving tablets of Ibuprofen for rapid dissolution, which may produce rapid onset of action. In this work, fast dissolving tablets of Ibuprofen were prepared by sublimation method with a view to enhance patient compliance. Sodium starch glycolate in different concentration was used as super-disintegrant, and Ammonium carbonate (20-30 % w/w) was used as subliming agent. The prepared batches of tablets were evaluated for Physico-chemical properties, wetting time, in-vitro disintegration and in-vitro drug release. Among the prepared formulations, the formulation (F4) containing 4% w/w of sodium starch glycolate and 25% w/w of ammonium carbonate as a subliming agent was found to be promising with disintegration time of 28 seconds, wetting time of 18 seconds and percentage of drug release of 99.5% for 30 mins. So we can conclude F4 is the best formulation when compared to all other formulations.
Asian Journal of Pharmaceutical and Clinical Research
Objective: The main aim of the present work is to enhance the solubility and bioavailability of the ibuprofen by formulating it into fast-dissolving tablets employing starch glutamate as a novel superdisintegrant. Materials and Methods: Starch glutamate was prepared from native potato starch and glutamic acid by the esterification process. Drug-excipient compatibility studies were performed between the starch glutamate and ibuprofen with the help of Fourier transform infrared spectroscopy, and differential scanning calorimetry techniques. Ibuprofen fast dissolving tablets were formulated employing different superdisintegrants along with the starch glutamate (a novel superdisintegrant) by the direct compression method. The prepared ibuprofen fast-dissolving tablets were evaluated for various pre- and post-compression parameters along with the in vitro and in vivo release characteristics. Optimized formulation stability studies were performed at accelerated conditions for 6 months as ...
Indonesian Journal of Pharmaceutics, 2019
The dissolution of tablets is one of a drug absorption determinant. Disintegrant agent has play an important role on determining the dissolution of tablets. In this experiment, the dissolution behaviours of Acetaminophen and Ibuprofen Tablet was studied using various disintegrant agent such as Low substituted – Hydroxypropyl Cellulose (L–HPC) 21, L–HPC 22 and Sodium Starch Glycolate (SSG) as comparator. Those disintegrant agents were used at three concentration (6%, 7% and 8%) for every tablets formula. Tablets were made by wet granulation method and pressed using single punch 13 mm flat E. Korsch machine. Evaluation of each tablets quality were conducted include for uniformity of weight and size (diameter and thickness), hardness, friability, disintegration time and dissolution. Physically standards from tablets were in good condition, the standards of the weight and thickness uniformity, hardness and friability met the requirement. The dissolution profile on Acetaminophen Tablets ...
Enhancement of Solubility and Dissolution Characteristics of Ibuprofen by Solid Dispersion Technique
In this study solid dispersions (SDs) of ibuprofen were prepared by melt dispersion technique using macrogol 4000 and macrogol 6000 as carrier. Physical mixtures (PMs) of ibuprofen were also prepared with the same carrier and in the same drug-carrier ratio (1:0.5, 1:1 and 1:1.5) to compare the dissolution profile. The solid dispersions and physical mixtures were investigated for drug loading, saturation solubility and dissolution behavior. Saturation solubility study was carried out in phosphate buffer (pH 7.2), 0.1 N HCl solution and distilled water. Solid dispersions were found effective to enhance the solubility of ibuprofen significantly in all the media. Dissolution test was carried out in two different media, phosphate buffer (pH 7.2) and 0.1 N HCl. Solid dispersion containing macrogol 6000 at the ratio of 1:1.5 (drug: carrier) showed faster and higher drug release and was found to be most effective among all the solid dispersions. Drug carrier interactions were studied by comparing Fourier Transform Infrared Spectroscopy (FT-IR) of solid dispersions with pure drug which revealed that the SDs were stable. So, solid dispersion may be an effective technique to enhance dissolution rate of ibuprofen.
Preparation and Evaluation of Fast Dissolving Ibuprofen-Polyethylene Glycol 6000 Solid Dispersions
Drug Delivery, 2008
To improve its oral absorption, rapidly dissolving ibuprofen solid dispersions (SD) were prepared in a relatively easy, simple, quick, inexpensive, and reproducible manner, characterized by scanning electron microscopy (SEM), differential scanning calorimetry (DSC), and Fourier transform infrared spectroscopy (FTIR). They were evaluated for solubility, in vitro release, and oral bioavailability of ibuprofen in rats. Loss of individual surface properties during melting and resolidification as revealed by SEM indicated the formation of effective SDs. Absence or shifting toward the lower melting temperature of the drug peak in SDs and physical mixtures in DSC study indicated the possibilities of drug-polymer interactions. However, no such interactions in the solid state were confirmed by FTIR spectra that showed the presence of drug crystalline in SDs. Quicker release of ibuprofen from SDs in rat intestine resulted in a significant increase in AUC and C max , and a significant decrease in T max over pure ibuprofen. Preliminary results from this study suggested that the preparation of fast-dissolving ibuprofen SDs by low temperature melting method using PEG 6000 as a meltable hydrophilic polymer carrier could be a promising approach to improve solubility, dissolution, and absorption rate of ibuprofen.
Iran J Pharm Sci, 2007
Ibuprofen solid dispersions were prepared by the solvent and fusion-solvent methods using polyethylene glycol (PEG), polyvinylpyrrolidone (PVP), eudragit RS PO, eudragit RL PO and hydroxypropylmethylcellulose (HPMC) as carriers to improve physicochemical characteristics of ibuprofen. The prepared solid dispersions were evaluated for the flowability, solubility characteristics and dissolution behavior. Flowability studies of powders showed that solid dispersion technique improve flow properties compared with the physical mixtures. Solid dispersion technique found to be effective in increasing the aqueous solubility of ibuprofen. The dissolution of ibuprofen and polymers (PVP, HPMC, eudruagit and PEG-6000) were investigated using UV spectroscopy. Dissolution was carried out in phosphate buffer (pH 6.8) using a standard USP II dissolution apparatus. In vitro dissolution studies showed that in the dispersion systems containing eudragit or HPMC, dissolution of ibuprofen was retarded, which attributed to ionic interaction and gel forming, respectively. But solid dispersion containing PEG, as a carrier, gave faster dissolution rates than the physical mixtures. Finally, solid dispersion of ibuprofen:PEG 6000 prepared in 1:1.5 ratio showed excellent physicochemical characteristics and was found to be described by the zero order kinetic, and was selected as the best formulation in this study.