Ex-vivo evaluation of crab shell chitosan as absorption enhancer in ciprofloxacin tablet formulation

This study was aimed at evaluating crab shell chitosan as absorption enhancer in ciprofloxacin tablet formulation using the ex-vivo model. Six batches of ciprofloxacin tablets containing varying concentrations of crab shell-derived chitosan ranging from 0 to 5% w/w at 1% w/w intervals were produced. Batch CTS-0 containing no chitosan served as the control. The crushing strength, friability, disintegration time, dissolution profile and permeation profile of all the batches were determined. Friability was not significantly affected but the crushing strength and disintegration time of tablets decreased with increase in concentration of chitosan. There was no significant difference in the cumulative percent drug released in 1 h but the cumulative percent drug permeated in 4 h increased with increase in the concentration of chitosan. It increased from 68% (when no chitosan was added) to 81.8% (when 5% w/w chitosan was incorporated). The polymer caused a faster onset of drug release but the eventual total drug released was not significantly influenced. It also improved the permeation of the released drug. This study correlates with in-vivo bioavailability study because the usual oral bioavailability of ciprofloxacin without absorption enhancer is 70%. Hence, crab shell chitosan at concentration of 5% w/w could increase the absorption of ciprofloxacin from 70 to 82%. The study suggests the use of the chitosan at this concentration to improve the absorption of ciprofloxacin.Key words: Crab shell chitosan, ciprofloxacin, dissolution, permeation, absorption

PRELIMINARY INVESTIGATIONS INTO THE PHYSICOCHEMICAL AND COMPACTION CHARACTERISTICS OF MODIFIED STARCH OF DISCOREA ALATA USING DICLOFENAC SODIUM TABLET

Objective: This work focused on evaluating the micromeritic and compressional properties of pregelatinized African water yam (Discorea alata) starch and its modified forms with comparison to pregelatinized corn starch and microcrystalline cellulose.Methods: Two modifications of the water yam starch were prepared; acetone dehydrated pregelatinized form (DSA) and an admixture of DSA and pregelatinized corn starch (CDSA). A third form of starch is the acetone dehydrated pregelatinized corn starch (CSA). These were used to form batches compacted as tablets using diclofenac sodium as the active moiety. Physicochemical and flow characteristics of the starch powders were elucidated, and the drug starch compatibility studies done using the Fourier transform Infra-red (FTIR) technique. Compaction studies were investigated on tablets formed at different compression pressures and Heckel plots were prepared.Results: The slope of the straight line (K) of 0.8959 was greatest for F1 while yield pressure (Py) value of 10.965 was highest for F3. These values from the Heckel plot suggest that while the tablets of control batch of microcrystalline cellulose (F4) and a batch of pregelatinized corn starch (F2) formed harder compacts, less likely deformed plastically, the Discorea alata batch (F1) and the admixed batch (F3) were likely to deform plastically. Also, the binding efficiency of the compact was significantly high (47.81%Kgscm-1) for F4 at 56.5Kpas compaction pressure, higher than that obtainable for any of the other formulations at the compaction pressures under consideration. All starches formed had similar moisture content (of 10%) despite the different sources but the interaction between the water molecule and pregelatinized water yam starch improved as revealed by viscosity(7.18mPas), hydration capacity(3.27%) and swelling index (250%) of CDSA.Conclusion: It could be concluded that pregelatinized water yam starch could be used as a substitute for corn starch or microcrystalline cellulose as a pharmaceutical excipient (binder/filler) in tablets formulation