Evaluating the effect of spherical crystallization of acetylsalicylic acid crystal and crystal agglomeration of Manihotesculenta starch on direct compression tablet properties

Spherical crystallization and crystal agglomeration have been used to optimize compact crystals and functional properties of powders. The aim of this work is to evaluate the effect of spherical crystallization of acetylsalicylic acid crystals and crystal agglomeration of Manihotesculenta starch on direct compression tablet. Typical spherical crystallization using three solvent system of water–ethanol-carbon tetrachloride was used to produce spherical acetylsalicylic acid. Salting-out agglomeration of gelling in water and salting in ethanol was used to produce starch-xerogel from Manihotesculenta starch. The modified products were qualified using FT-IR analysis. The analysis results showed that modification did not alter chemical nature of the products. Acetylsalicylic acid tablets were formulated using spherical-crystallizedacetylsalicylic acid with 5 and 10% w/w starch-xerogel respectively, and using acetylsalicylic acid with 5 and 10% w/w of starch, and microcrystalline cellulose respectively. The physicochemical properties of the tablets were evaluated. Astatistical 23 factorial design of the tablet properties at 5% level of significance showed that the effects of the variables are different. Theacetylsalicylic acid tablets formulated from direct compression of spherical-crystallizedacetylsalicylic acid with 5 % w/w starch-xerogel produced quality tablets comparable to standard tablets from direct compression of acetylsalicylic acid with10 % w/w microcrystalline cellulose. Spherical crystallization and crystal agglomeration optimized the compact crystals of starch and acetylsalicylic acid, and improved direct compression properties of the crystals, and drug release from tablet.

Development, Feasibility Assessment and in-vitro Evaluation of Diclofenac Potassium Multilayered Tablets

Introduction: Diclofenac potassium has widely been utilized as an analgesic and anti-inflammatory agent. To achieve rapid onset of action with prolonged therapeutic action is an immense need of time. In present project a study was conducted on preparation with physicochemical determination of diclofenac potassium tablets, this unique tablet have duel characteristics like rapid onset of action due to orodispersible coat and extended release of API due to sustained release core. Methodology: As diclofenac potassium is not sensitive to water so wet granulation method was efficiently employed to prepare the granules of sustained release core, while direct compression was done to prepare orodispersible outer coat layer in order to give rapid release. Results and Discussion: In evaluations granules characteristics and tablet properties were studied. Result of both pre compression and post compression studies were coming in pharmacopeia acceptable ranges. The orodispersible layer disintegrated with in 18sec, which gives sufficient amount of API as loading dose, in order to maintain the plasma drug concentration in therapeutic range the core will release drug in sustained manner within 10 hours in gastrointestinal tract (GIT) fluid (pH 6.8). The results of kinetic models were complying with Higuchi model. Conclusion: In present work, a rapid release outer dispersible layer of drug was constructed on a sustained release core. Results of study gives expected outcomes to maintained initial concentration of drug which persist for long time. The combination of sodium starch glycolate, dry starch, and cross povidone exhibited promising super disintegrant efficiency while Hydroxypropylmethyl cellulose K15 showed excellent sustained release properties.

Effect of Different Direct Compaction Grades of Mannitol on the Storage Stability of Tablet Properties Investigated Using a Kohonen Self-Organizing Map and Elastic Net Regression Model

This study tested 15 direct compaction grades to identify the contribution of different grades of mannitol to the storage stability of the resulting tablets. After preparing the model tablets with different values of hardness, they were stored at 25 °C, 75% relative humidity for 1 week. Then, measurement of the tablet properties was conducted on both pre- and post-storage tablets. The tablet properties were tensile strength (TS), friability, and disintegration time (DT). The experimental data were analyzed using a Kohonen self-organizing map (SOM). The SOM analysis successfully classified the test grades into three distinct clusters having different changes in the behavior of the tablet properties accompanying storage. Cluster 1 showed an obvious rise in DT induced by storage, while cluster 3 showed a substantial change in mechanical strength of the tablet including a reduction in the TS and a rise in friability. Furthermore, the data were analyzed using an Elastic net regression technique to investigate the general relationships between the powder properties of mannitol and the change behavior of the tablet properties. Consequently, we succeeded in identifying the crucial powder properties for the storage stability of the resulting tablets. This study provides advanced technical knowledge to characterize the effect of different direct compaction grades of mannitol on the storage stability of tablet properties.