Design, Optimization And Evaluation Of Empagliflozin Orodispersible Tablets Using Different Superdisintegrants

Objective: The objective of this study was to formulate orodispersible tablets containing empagliflozin by direct compression method with sufficient hardness and rapid disintegration time and to study the effect of functionality differences of super-disintegrants on the tablet properties. Methods: A two factor three level factorial design (32) was used for the formulation optimization of orodispersible tablets of Empagliflozin and experimental trials were performed on all possible formulations, in which the amount of β-cyclodextrin, crospovidone and croscarmellose sodium were selected as independent variables (factor) varied at three different levels: low (-1), medium (0), and high (+1) levels. The drug release and disintegration time were used as dependent variables (response). All formulations were characterized for parameters such as diameter, hardness, weight, thickness, friability, disintegration time, drug release. Results: Formulation FD6 having 30 sec disintegration time, 98.84% drug release after 30 min, 2.8 kg/cm2 hardness and 0.292% friability was found best among all formulations and selected as an optimized formulation with rapid onset of action and enhanced bioavailability (more than 98% drug release within 30 min.) as compared to the oral empagliflozin tablet. Conclusion: Empagliflozin orodispersible tablets with different superdisintegrants were successfully prepared and formulation containing highest percentage of crospovidone was found best among all other formulations in terms of bioavailability and rapid onset of action.

Effect of synthetic super disintegrants and natural polymers in the preparation of donepezil hydrochloride fast disintegration films.

The main aim of the present research was to develop a fast dissolving oral polymeric film with good mechanical properties, faster disintegration and dissolution when placed on tongue. Donepezil hydrochloride (DPH) is prescribed in the treatment of mild to moderate Alzheimer’s disease (AD). The polymers selected for preparing films were sodium alginate (SA), poly vinyl alcohol (PVA) and guar gum (GG). Three batches of films were prepared by solvent casting method with sodium alginate, sodium alginate & PVA and with the combination of sodium alginate & guar gum. From these three batches, three optimized film formulations S3, SP7 and SG8 were selected based on disintegration time. To these three selected film formulations, superdisintegrants sodium starch glycolate (SSG), cross carmellose sodium (CCS) and cross povidone (CP) were added at a concentration of 4% w/w of polymer to improve the disintegration time. The films prepared with or without superdisintegrants were compared for fast releasing properties. Based on DT and in vitro dissolution data, S3CP was selected as the best formulation among the all formulations.

Effect of superdisintegrants and their mode of incorporation on disintegration time and release profile of carbamazepine from immediate release tablet.

In this experiment the effect of mode of incorporation of some superdisintegrants such as sodium starch glycolate, croscarmellose sodium, crospovidone (kollidon CL), ludiflash and Xanthan gum (XG) on dissolution profile and disintegration time of carbamazepine (CBZ), apoorly water soluble drug was studied. The superdisintegrants were incorporated by extragranularly, intragranularly and in direct compression method. Different amount of superdisintegrants (1%, 3% and 6%) was incorporated in different formulations whereas all the other excipients as well as the active drug remained same. The results indicated that sodium starch glycolate, when incorporated extragranularly in wet granulation method significantly enhanced the release profile of CBZ. Kollidon CL was the most effective superdisintegrant in decreasing disintegration time of different tablet formulations (1.95 minutes when extragranularly incorporated). On the other hand, tablets prepared with SSG were found most effective in % drug release irrespective of its mode of incorporation (99.99% when extragranularly incorporated and 99.75 when intragranularly incorporated within one hour). Tablets prepared by direct compression method also showed similar drug release with other methods but tablet hardness was found lower. So addition of superdisintegrants in tablet formulation may be an effective technique to comply compendial drug release.

Effect of synthetic super disintegrants and natural polymers in the preparation of donepezil hydrochloride fast disintegration films.

The main aim of the present research was to develop a fast dissolving oral polymeric film with good mechanical properties, faster disintegration and dissolution when placed on tongue. Donepezil hydrochloride (DPH) is prescribed in the treatment of mild to moderate Alzheimer’s disease (AD). The polymers selected for preparing films were sodium alginate (SA), poly vinyl alcohol (PVA) and guar gum (GG). Three batches of films were prepared by solvent casting method with sodium alginate, sodium alginate & PVA and with the combination of sodium alginate & guar gum. From these three batches, three optimized film formulations S3, SP7 and SG8 were selected based on disintegration time. To these three selected film formulations, superdisintegrants sodium starch glycolate (SSG), cross carmellose sodium (CCS) and cross povidone (CP) were added at a concentration of 4% w/w of polymer to improve the disintegration time. The films prepared with or without superdisintegrants were compared for fast releasing properties. Based on DT and in vitro dissolution data, S3CP was selected as the best formulation among the all formulations.

Design and development of levofloxacin hemihydrate fast dissolving tablets using fenugreek powder.

Levofloxacin hemihydrate is an antibiotic used for bacterial infections. It belongs to flouroquinolones class. Fast dissolving tablets gaining popularity over conventional tablets due to their convenience in administration and suitability for patients like geriatrics and pediatric patients because of their swallowing difficulties. The half-life of the drug is 6-8 hrs and it is rapidly and completely absorbed after oral use for that levofloxacin prepared as fast dissolving tablets. Tablets were prepared by direct compression technique by using MCC as binder. Super disintegrants used are SSG(2%,3%,4% and 5%),CCS(AC-DI-SOL) (2%,3%,4%and 5%), CP(2%,3%,4%and5%)and FGP(2%,3%,4%and 5%),.Among these 4 super disintegrants, Fenugreek powder (FGP) was show best results in the evaluation tests.

Enteric coated tablets of novel proton pump inhibitor with super disintegrants design, in-vitro evaluation and stability studies.

The current work evaluate directly compressible esomeprazole magnesium trihydrate enteric coated tablets were prepared to deliver drug in upper GIT. Different tablets were prepared with super disintegrants like Ac-Di-Sol, Crospovidone, sodium starch glycolate and diluents like Pharmatose DCL11, Mannogem EZ. Tablets were enteric coated using Acryl-EZE. The tablets were evaluated for hardness, disintegration time and in vitro drug release. The powder bed showed good rheological properties and enteric coated tablets showed acid uptake value <5 indicates significant protection of acid liable drug. The compressional parameters were within the limits, the drug content in all formulations was found to be uniform and consistent. In vitro dissolution studies indicated there is no drug loss during gastric phase. The tablets with Pharmatose DCL11 released higher than Mannogem EZ which colud be due to its hydrophilicity and due to swelling of the super disintegrant. Stability studies indicated that the prepared formulations were stable for a period of four months of all formulations showed comparable dissolution profiles with similarity factor more than fifty at p<0.05. From the above findings it can conclude that an Esomeprazole magnesium trihydrate enteric coated tablet could be developed to deliver the drug in to proximal small intestine.