Formulation and evaluation of sulfadimidine and trimethoprim tablets using wet granulation technique
DOI:
https://doi.org/10.12923/j.2084-980X/25.2/a.21Keywords:
dissolution, tablet excipients, sulphadimidine, trimethoprim, wet granulation, superdisintegrantAbstract
The objective of this study was to develop tablet formulations of sulphadimidine sodium (SDD-Na) and trimethoprim (TMP), evaluate and compare the efficiency of some excipients such as: superdisintegrant - croscarmellose sodium (Ac-Di-Sol), silicon dioxide (Aerosil), lactose and microcrystalline cellulose (Avicel pH-101) as base excipients for physical tablets properties and increasing the dissolution rate of SDD-Na and TMP. All tablet formulations were prepared by wet granulation process. Dissolution properties such as DP 30,45,60 (percent of drug dissolved at 30, 45 and 60 minutes), and dissolution rate constant value (K) were considered for comparing the dissolution results. The dissolution of SDD-Na and TMP from all examined tablet formulations followed Higuchi model kinetics with correlation coefficient (R) values from 0.984 to 0.995. The physical properties and in vitro drug release study revealed that tablets disintegration efficiency and drug dissolution depend on the amount of added disintegrant, the amount and presence of microcrystalline cellulose (Avicel) and lactose. Tablet formulation without addition of microcrystalline cellulose showed faster dissolution rate and shorter disintegration time as compared with that of tablets of formulations with microcrystalline cellulose. The results reveal that besides the type of diluents, the way of using superdisintegrant plays a major role in controlling disintegration of tablets. The portion of Ac-Di-Sol used as an intragranulary in the wet granulation process, is not as effective as that of the process of extragranulary addition. Tablets formulations F4 and F5 exhibited satisfactory friability, acceptable hardness, fulfilled the requirement for disintegration time for compressed tablets, and met the acceptable specifications with regard to drug release properties.
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