Formulation development and in vitro Evaluation of sustained release matrix tablets of Cefpodoxime proxetil

The present focus is on the development of sustained release formulations due to its inherent boons. There are several advantages of sustained release drug delivery over conventional dosage forms like improved patient compliance, reduction in fluctuation and increased safety margin of potent drug. The present study was aimed to prepare a sustained drug delivery system to design a controlled release oral dosage form of Cefpodoxime proxetil. The sustained release matrix tablets of Cefpodoxime proxetil were prepared by wet granulation and evaluated for different parameters such as weight variation, drug content, thickness, hardness, friability and In vitro release studies. The in vitro dissolution study was carried out for 12 hours using USP (Type- II) paddle apparatus in hydrochloride (0.1N) as dissolution media for first 2 hours and phosphate buffer (pH 6.8) for next 10 hours. Based on the in vitro dissolution data, formulation F8 was selected as the best formulation from Cefpodoxime proxetil formulations (F1 – F9) as the drug release was retarded up to 12 hours with 96.29 % and followed zero order release kinetics & drug release mechanism was diffusion.

Physical characterization and In Vitro evaluation of dissolution rate from Cefpodoxime proxetil loaded Self solidifying Solid SNEDDS

Background: Cefpodoxime proxetil (CPD) is a broad-spectrum cephalosporin indicated in respiratory and urinary tract infections. CPD is a BCS class IV drug with pH-dependent solubility and has poor bioavailability. This study investigated the challenges of developing ternary components based on solid SNEDDS of CPD for in vitro dissolution rate enhancement and self-solidifying behaviour. Method: Tween 80, Transcutol and PEG6000 were employed as surfactant, solvent & solidifying a base of ternary components to develop self-solidifying solid SNEDDS, respectively. Ternary phase diagrams were used to characterize solidifying behaviour of ternary components in different proportions. S-SNEDDS formulations were drawn on the solidification areas available in the phase diagram and characterized for IR, XRD, DSC and in-vitro drug release in various pH media. Results : Ternary components for the preparation of self solidifying solid SNEDDS were selected based on drug solubility. FTIR and DSC characterization studies ruled out any drug interaction between CPD and components chosen to prepare S-SNEDDS. CPD was transformed from a crystalline into an amorphous state in ternary dispersions as revealed from XRD data. Optimized formulation (S-S 1) demonstrated more than 95% of drug release irrespective of the pH environments of the medium. Calculation of dissolution efficiency and similarity factors indicate that S SNEDDS resulted in a higher drug dissolution rate over binary dispersion (p<0.01). The stability studies showed that the S SNEDDS were stable in performances and CPD assay. Conclusion: Present investigation provides an alternative approach for enhancing the CPD dissolution rate using self-solidifying solid SNEDDS exhibited solidification behaviour at ambient temperature conditions and drug loading. Which could be exploited over conventional dosage form.

Formulation and Characterization of Dispersible Tablets of Cefpodoxime Proxetil: A Cephalosporin Antibiotic

The objective was to formulate rapid dispersible tablets of Cefpodoxime Proxetil using various types of superdisintegrants viz., Croscarmellose sodium (CCS), Sodium starch glycolate (SSG) and Crospovidone (CP) in varied concentrations (1-5%). The model drug for current investigation, Cefpodoxime Proxetil, a broad spectrum third generation Cephalosporin antibiotic belongs to BCS class IV. The preformulation studies were accomplished by determining the compatibility of model drug with respective excipients by FTIR studies. These studies, revealed no chemical interaction of excipients with the model drug. The formulation development was achieved in phases comprising of preliminary screening, pre-optimization and optimization studies. The bitter taste of model drug was masked by addition of flavors and sweeteners to make it pleasant for pediatric patients upon oral administration. The formulations (F1-F6) were prepared by direct compression method. The percent released from all formulations showed release of more than 90% of drug within 30 min with drug content of more than 95%. The study showed that formulation containing CCS as superdisintegrants furnished best results. Formulation F5 showed maximum (99.6%) drug release within 30 minutes which is prerequisite for dispersible tablets. It also possessed a rapid release of drug from the formulation. The F5 formulation showed comparative dissolution profile vis-a-vis a commercialized formulation. The study concluded that dispersible tablets of Cefpodoxime Proxetil can be an alternative to conventional dosage form for the treatment of urinary tract infection, skin infection, and upper respiratory tract infections.