Madhusudan Rao Y

Single unit floating effervescent matrix tablets of Dipyridamole were successfully prepared with hydrophilic polymers like HPMC K4M , HPMC K15M and HPMC K100M with 10% NaHCO3 by Simple direct compression method with drug: polymer ratio of 1:1.5,1:2,1:2.5:1.3. FT-IR studies were conducted between drug, polymer and various excipients used in the formulations. Evaluation parameters of powder blend like Hausner’s ratio, Compressibility index, Angle of repose were carried out and results showed that the powder has good flow properties. Formulated tablets gave satisfactory results for various evaluation parameters like tablet hardness (5-6 Kg/cm2), weight variation (±10%), Friability (

The purpose of the present study was to design, characterize and evaluate extended release coated tablets of Metoprolol Succinate (MS) to reduce its dosing frequency. Core tablets were prepared using various matrix forming agents like HPMC, HPC, and HEC, and further subjected for coating using blend of aqueous dispersion of a hydrophobic and hydrophilic polymer, (Surelease®: HPMC E15) to control the drug release of the highly water soluble drug Metoprolol Succinate. Varying the matrix forming agent concentrations in the core tablets and percentage coating build up on core tablets showed range of drug release patterns in phosphate buffer pH 6.8. The present study dealt with the suitable grade of cellulose polymer and optimized coating composition which can modify the drug release to match up with the USP dissolution specifications and marketed product for the MS. The optimized formulation containing Metolose 90 SH 100000 and 3% coating with plasticized Surelease: hydroxypropyl methylcellulose (HPMC E15) showed extended drug release up to 24hrs and the drug release pattern was similar with the specifications. The in-vitro dissolution studies revealed that the release rate is inversely proportional to the concentration of matrix former in the core tablet and percent of coating thickness. The kinetic treatment illustrate that the optimized formulation HMC5 followed zero order kinetics with diffusion mediated drug release which is evidenced from n value of (0.73) Peppas equation. FT-IR and DSC studies indicated no interaction between the drug and excipients and prepared formulations showed good stability as per ICH guidelines. Key words: Metoprolol Succinate, Extended Release, HPMC E15, Surelease, Coated Tablet

  Promethazine Hydrochloride (PMZ), a low bioavailabe drug, used for the management of emesis. The purpose of the present investigation was to develop buccoadhesive tablets for PMZ and to evaluate for their physicochemical, in vitro, ex vivo and in vivo parameters. Ex vivo drug permeation through porcine buccal membrane from the drug solution was conducted to know the permeation characteristics of the PMZ. The controlled-release PMZ tablets were produced by direct compression method using Sodium CMC and Carbopol 934P as mucoadhesive polymers and evaluated for in vitro drug release, in vitro bioadhesion, in vivo residence time, swelling and erosion studies, surface pH, ex vivo drug permeation through porcine buccal membrane from the optimized buccal tablet (F10) and stability studies. Formulation F10 showed maximum drug release (96.3 %) in 6 h, with the Higuchi model release profile and permeated 49.8 % of the drug with flux 1.45 mg h–1cm–2 through porcine buccal membrane. The optimized formulation showed peak detachment force (1.64 N), work of adhesion (0.36 mJ), in vivo residence time (287 min), swelling index (204%), erosion (53.1%) and surface pH (6.92). In vivo mucoadhesive behaviour of the optimized formulations was studied in healthy human volunteers and subjective parameters were evaluated. The stability of the optimized formulation was studied and no significant changes were detected in drug content and in vitro release after 6 months. PMZ mucoadhesive tablets for buccal delivery could be prepared with required permeation, bioadhesive and in vivo residence properties.