Formulation Development and Evaluation of Diltiazem Hydrochloride Gastro Retentive Floating Tablets

Abstract

The investigation was concerned with design and characterization of oral sustained release gastro retentive floating tablets of DiltiazemHCl in order to improve efficacy and better patient compliance. Present investigation was to formulate, evaluate and optimize gastro retentive tablet of DiltiazemHCl. This tablets released drug till 24 hrs due to floating mechanism of polymer s. Gastro retentive floating tablets were prepared by direct compression method using various proportions of polymersHPMC K4M, HPMC K100M,Carbopol 934, Ethyl cellulose, Xanthan gum along with Sodium bicarbonatethe sustained release behaviour of the fabricated tablets was investigated. Tablets were prepared by directcompretiontechnique.Formulation was optimized on the basis of acceptable tablet properties and in vitro drug release. The resulting formulation produced robust tablets with optimum hardness, consistent weight uniformity and low friability. All tablets but one exhibited gradual and nearcomplete sustained release for DiltiazemHCl (90-100%) at the end of 24 h. The results of dissolution studies indicated that formulation Dtz15 was found to be most successful as it exhibits drug release pattern very close to theoretical releas e profile. A decrease in release kinetics of the drug was observed on increasing polymer ratio.

Quality aspects in the development of pelletized dosage forms

“…The most preferable processing can be done at temperature above the M.P. of semi-crystalline polymers or [ 50 , 51 , 52 , 53 , 54 , 55 , 56 , 57 , 58 , 59 , 60 , 61 , 62 , 63 , 64 , 65 , 66 , 67 , 68 , 69 , 70 , 71 , 72 , 73 , 74 , 75 , 76 , 77 , 78 , 79 , 80 , 81 , 82 , 83 , 84 , 85 , 86 , 87 , 88 , 89 , 90 , 91 , 92 , 93 , 94 , 95 , 96 , 97 , 98 , 99 , 100 ] °C above the glass transition temperature Tg of amorphous polymers, but below the M. P. of the crystalline API [ 80 , 81 ].…”

“…The pellets produced, exhibited a smooth surface and low porosity by the use of triacetin and diethyl phthalate as plasticizers [ 98 ]. The sustained release tablet were also explored from the pellets prepared using cheaper excipients and exhibited marginal difference in the performance [ 99 ].…”

“…The pellets produced, exhibited a smooth surface and low porosity by the use of triacetin and diethyl phthalate as plasticizers(98). The sustained release tablet were also explored from the pellets prepared using cheaper excipients and exhibited marginal difference in the performance(99) Kleinebudde & Reitz, 2009 developed sustained release matrix spheres by solvent-free spheronization process. A binary lipid mixture with different amounts of Witocan 42/44®, Dynasan 114® and theophylline as model drug were used to produce extrudates.…”