Objective: The study aimed to design and evaluate a dispersible tablet of flavonoid PGAL isolated from Saraca asoca leaves for antidepressant activity. Methods: The phytoconstituent was isolated from a methanolic extract of Saraca asoca leaves using silica gel column (60-120 mesh) chromatography. The dispersible tablets were prepared by direct compression and then evaluated for various tablet evaluation parameters and antidepressant activity, performing Tail Suspension Test (TST), Forced Swim Test (FST), Locomotion activity, Brain glutamate level and brain nitrite level. Results: Hardness of 2.85±0.13 kg/cm2 to 3.25±0.15 kg/cm2 and friability of 0.35% to 0.48% indicate that the prepared tablets were mechanically sound. Test for weight variation was also within tolerance limits, i.e. 2.04% to 4.25% difference in weight of the tablet from the average weight of 10 tablets. The tablets also passed the test for drug content uniformity, 97.35% to 100.35%, i.e. always within the prescribed limits of 95% to 105%. Disintegration time, 2 min to 2.75 min, and dispersion time, 3.25 min to 3.75 min, were also exemplary. The antidepressant activity was displayed by the optimized formulation as indicated by a significant decrease (p<0.05) in immobility time in TST as well as FST; a significant decrease (p<0.05) in the level of brain tissue glutamate as well as nitrite in PGAL formulation treated mice when compared with negative control, as did by standard drug fluoxetine. Conclusion: The formulation has been optimized based on dispersion time. The formulation with minimum dispersion time, i.e. F1, has been considered an optimized formulation. The prepared optimized formulation was found to comply with all physical parameters and antidepressant activity.

Background The main objective of the present study was to develop and optimize an effervescent tablet of levetiracetam, an antiepileptic drug, using central composite design with response surface methodology (RSM).The present investigation helps to overcome the problem associated with levetiracetam tablets and liquid dosage forms with children and elderly people like bad taste and swallowing difficulties. It also facilitates as an alternative manufacturing process for advanced patented technology like 3D printing process employed in SPRITAM® tablet. Levetiracetam effervescent tablets were prepared by dry granulation (roll compaction) method using water-soluble excipients and optimized by central composite rotatable design (CCRD) using two variables (citric acid and effersoda) at two levels (high and low). Overall, fourteen formulation trials were generated through statistical software Minitab 17.3.0 placing 6 center points, 4 cube points, and 4 axial points. All formulations were subjected to compression using single punch machine. Results Quality attributes of compressed tablets were evaluated using various compendial and non-compendial tests. RSM was used to observe the responses like effervescent time, hardness, and friability of the prepared tablet batches for different levels of all the variables. Polynomial equations were developed, and model plots (contour plot and 3-dimensional model surface plots) were generated to study the impact of acid-base couple on the responses. Finally, the optimized formulation was selected on the basis of desired effervescent time, hardness, friability, percent drug release, and drug content. From the studied RSM design, it was observed that small changes in the independent variables (citric acid and effersoda) correlate with shifts in the dependent variables, i.e., the desired responses. The study reveals that all the independent variables (citric acid and effersoda) and dependent variables (effervescent time, hardness, and friability) have a good correlation as indicated by good linear regression coefficient of 0.9808, 0.9939, and 0.9892 for effervescent time, hardness, and friability respectively. Conclusion Levetiracetam effervescent tablets are satisfactorily prepared by dry granulation (roll compaction) approach. All desired critical quality attributes were found to be satisfactory. The applicability of RSM with desirability function in optimizing the levetiracetam formulation has made it possible to identify the impact of various independent variables and explore their effect on required responses.

Available online on:15.01.2018@http://ijrdpl.co m http://dx.doi.org/10.21276/ IJRDPL. 2278-0238.2018.7(1).2924-2930 ABSTRACT: Background: Studies suggested that fever may have a beneficial for safe drug delivery. The use of paracetamol in therapeutic doses generally is safe, although hepatotoxicity has occurred with recommended dosages in children. Material and Method: home storage conditions at a temperature ranging from (2-8 °C) representing refrigerator and accelerated condition. Prepare a solvent mixture consisting of 0.4 volumes of formic acid, 15 volumes of methanol and 85 volumes of water. Result: Evaluated prepared 4 formulations the physical description (Color, odor, and taste) were found colorless, none and sweet. The pH of F1, F2, F3, and F4 was found 5.39,5.16,5.09 and 5.04. In these four formulations, we were selected F1 on the behalf of best pH. The F1 formulation weight per ml was found 1.0312 gm/ml. the assay of paracetamol syrup F1 formulation was found 99.88%. The stability of four formulations was found 5.36,5.16,5.08 and 5.03 Conclusion: It was concluded that F1 formulation was good and stabilized formulation. Like syrup formulations made by use of a combination of physiologically compatible mixed solubilizes. The proposed mixed solubilizes are known to be safe; hence, toxicities/safety related issues may not raise concern, suggesting the adaptability for large-scale manufacturing i.e. industrial feasibility.

Objectives: In the present investigation a novel oral drug delivery system was developed by combining two different techniques floating and mucoadhesive system so called floatadhesive, in order to obtain a controlled system that could remain in the stomach for prolonged period and release the drug in a controlled manner. Materials and Methods: Microspheres containing Famotidine were prepared by ionic gelation method using Mimosa pudica seed mucilage as a natural mucoadhesive polymer. Sodium alginate (SA) and chitosan (CS) were incorporated as drug release modifier. The microspheres were characterized by scanning electron microscopy and evaluated by employing shape and particle size, % drug entrapment efficiency, in vitro floating ability, in vitro mucoadhesion and in vitro drug release pattern. Results: The prepared microspheres were acceptably spherical with a mean particle size in the range of 334 ± 1.18 µm to 498 ± 1.12 µm. Drug entrapment efficiency was observed in the range of 72.82 ± 1.10% to 92.38 ± 1.20%. Formulations containing a combination of both mucilage and chitosan showed increased in vitro mucoadhesion and buoyancy as compared to formulations containing chitosan alone. In vitro drug release for all the formulations in 0.1N HCl was diffusion controlled gradually throughout 12 h and followed Higuchi's and Korsmeyer Peppas kinetics. The mechanism of in vitro drug release was non-fickian type controlled by swelling and relaxation of the polymer. Conclusion: The developed microspheres have dual advantages of being floating and mucoadhesive to increase oral bioavailability and releasing drug in a controlled manner, to reduce the required frequency of administration thereby promoting patient compliance.

An approach was used to enhance the solubility of BCS Class II drug, Gliclazide. The objective of this study was to formulate liposomal drug delivery system and to show the potential of Soya lecithin, tween 80 in enhancing the solubility and bioavailability of Gliclazide. Initial preparations were done by mixing the drug and carrier. Formulations were prepared by heat fusion method as it is considered as the mechanism for the enhancement of solubility and dissolution of the drug. The in-vitro releases of the different formulations were studied based on the effect of surfactant and oil including their thermodynamic stability. Formulated drug and adjuvants were characterized by spectrophotometry (UV, FTIR and photon correlation). Dissolution studies showed that F3 had the smallest particle size of 127.6 nm, with values for other formulations ranging from 176.8-248.8 nm. The cumulative percentage release for all formulations ranged from 21.20 ± 1.68% to 80.92 ± 3.82%; with F3 having the highest value of 80.92 ± 3.82%. Soya lecithin, soybean oil and tween 80 showed no significant influence on formulation's stability. These results confirm that the potential of liposomal drug delivery containing oil and surfactants as an adjuvant are expected to increase the oral bioavailability as confirmed by the increased in-vitro release.