Dipen R. Bhimani

The main objective of present research work was to design, development and characterization of glutathione lyophilized injection. Component excipients were selected based on the preliminary studies. Solubility trials were done to determine the solubility of Glutathione in water with different concentration of sodium bicarbonate. Then glutathione injection was formulated and lyophilized by setting the lyophilization cycle parameters. But, when glutathione was lyophilized alone the cake collapse was observed. So, in order to overcome this problem lyoprotectants (mannitol, lactose, trehalose and sucrose) were added in different concentration i.e. 5% and 10%. The lyophilization cycle was developed for these formulations by changing the process parameter. After formulation development, lyophilization cycle was optimized by reducing the total cycle time. Cycle time reduced at the initial stage of primary drying till the formulation remained stable. First stage of primary drying was reduced to 2520 minutes where the cake remains elegant. The batch L1 developed by FD cycle 11 with 5% trehalose having total lyophilization cycle time 59.75 hours was considered as optimized formulation because it exhibited a good cake formation and pH, moisture content, reconstitution time and assay was found within the range of desired product profile. Short term stability studies were conducted for the optimized formulation as per ICH guidelines for a period of 30 days which revealed that the formulation is stable. It was conclude that the lyophilization technique proves to be an advantage for development of stable injectable dosage form of Glutathione. Keywords: Glutathione, Lyophilized Injection, Injectable Dosage Form.

The main objective of the current research work was to formulate and evaluate taste masked effervescent tablet. Dicyclomine HCl is very bitter in taste. The purpose of this research was to reduce the bitterness of Dicyclomine HCl using Hydroxyl Propyl Betacyclodextrin by inclusion complex method and formulate effervescent tablet with sufficient mechanical integrity and to achieve faster disintegration in the water.: Components excipients and Dicyclomine HCl HP- Betacyclodextrin inclusion complex were selected based on preliminary studies. A comparative evaluation of the taste masking was carried out for developed formulation. Citric acid, tartaric acid, sodium bicarbonate was used in 1:2:3.44 ratio for effervescent mixture. 32full factorial design was applied. Ratio of citric acid and hardness were taken as independent variables dissolution of Paracetamol and Dicyclomine HCl at 5 minutes, disintegration time, and friability were taken as dependent variables. Optimized formulation was then evaluated for general tablet evaluation and dissolution. Short term accelerated stability studies were performed for tablets prepared using optimized formulation. Optimized batch composition had ratio of Paracetamol: citric acid and hardness at concentration of 1:0.45 (mg) and 8 (kg/cm2) respectively. All the evaluation parameters of the optimized batch met the acceptance criteria. The taste masked effervescent tablet of Paracetamol and Dicyclomine HCl was formulated successfully by wet granulation method. Keywords: Paracetamol, Dicyclomine HCl, Taste masking, Effervescent tablet, Wet granulation.

The main objective of the present investigation was to formulate and evaluate chronomodulated pulsatile drug delivery system of Trimetazidine Hydrochloride which was aimed to release the drug after lag time (6 hrs) in order to mimic circardian rhythm of Angina Pectoris.Preformulation studies and compatibility studies were carried out for drug and excipients. Core tablet was prepared by direct compression using sodium starch glycolate as superdisintegrant and press coated with different polymer & varying its ratio. Further prepared tablets were optimized using 32 full factorial design. Nine batches were prepared varying the amount of polymer and ratio of polumer (HPMC K4M: EC) and they were evaluated for precompressional and postcompressional tests. Optimized batch was derived statistically using desirability function (Minitab 17).The Model was validated by formulating the check point batch. Accerelated stabilitiy study was carried out of optimized batch. Preformulation and compatibility studies was carried out using FTIR , DSC which shows satisfactory results, no interaction was found between drug and excipients. Press coating of core tablet with the combination of HPMC K4M and EC was found to be providing the desired release. Results of precompressional and postcompressional was found to be within the limits. Varying  the amount of coating and ratio of polymer have significant effect on lag time(Y1) as well as on time required for 90% drug release (Y2).Optimized batch shows lag time of 6 hrs followed by complete release within 1 hrs which is desiered in case of pulsatile delivery. No significant bias was found between predicted and observed value of check point batch.The data of stability study revealed that the optimized formulation is stable. Pulsatile drug delivery system of Trimetazidine Hydrochloride for chronomodulated therapy can be prepared by press coating technique using 200 mg of coating and HPMC K4M:EC(10:90) ratio of polymer which will provide lag time of 6hrs and complete release within 1 hrs.

A major problem in ocular therapeutics is the attainment of optimal drug concentration at the site of action, which is compromised mainly due to precorneal loss resulting in only a small fraction of the drug being ocularly absorbed. Brimonidine tartrate is an antiglaucomic agent which shows rapid precorneal exclusion and reduced ocular bioavailability when given in form of conventional ophthalmic formulations. The poor bioavailability and therapeutic response exhibited by conventional ophthalmic solutions may be overcome by the use of in-situ gel forming ophthalmic systems that are instilled as drops into the eye and undergo a sol–gel transition in the cul-de-sac. In the present study, environmentally responsive ophthalmic drug delivery system composed of two gelling polymers with different phase transition mechanisms was developed. Combination of polyacrylic acid (carbopol 934P) and xanthan gum was investigated as ophthalmic vehicle. Different ratios of these polymers were used to prepare environmentally responsive ophthalmic drug delivery system by simple mixing procedure. Developed formulation was assessed for various evaluation parameters such as appearance/clarity, pH, gelation, drug content, rheological measurement, in-vitro release, and sterility testing and stability study. Prepared formulation showed agreeable appearance/clarity, acceptable pH and good gelation property. In-vitro studies demonstrated adequate drug content, desired rheological behaviour and reasonable in-vitro drug release property. Formulation was stable over one month period. In conclusion, the optimum concentration of polymers results in minimized drug loss and sustained drug release. On the basis of these findings, prepared in-situ gel may be considered as a viable alternative to conventional brimonidine tartrate eye drops.