Design and Development of Cyclobenzaprine HCl Sustained Release Pellets by Wurster Coating Method

Abstract

Background Cyclobenzaprine is structurally related to the tricyclic antidepressants. Cyclobenzaprine may be slightly different than the other musculoskeletal agents because it is believed to decrease skeletal muscle spasm through atropine-like effects directly on the cerebral motor neurons. Cyclobenzaprine may also have analgesic properties that may add to its therapeutic effects. This research encompasses all oral dosage forms and strengths.Objective Even though Cyclobenzaprine HCl tablets are available in market we can formulate pellets because pellets demonstrate good flow properties in the intestine and require less cost for the production of formulation. The main aim of the present study was to produce the extended-release Cyclobenzaprine HCl capsules of 16 hours release to reduce the dosing frequency as a skeletal muscle relaxant when compared with the innovator drug Amrix. Cyclobenzaprine HCL is a muscle relaxant that works on the central nervous system by altering the signals from the brain causing muscle to tighten.Methodology Cyclobenzaprine hydrochloride sustained release SR pellets were prepared by Wurster coating method using different excipients and polymers to release the drug slowly for an extended period of time. The method of preparation of Cyclobenzaprine hydrochloride SR pellets involves two steps drug coating and polymer coating. In the drug coating process the drug was coated in a suspension form on the dummy pellets dried and sieved. Drug coated pellets were coated with SR polymer to form SR pellets. These SR pellets were dried sieved and sent for quality control.Results After 12th hour the percentage drug release from the formulations were 89.6 87.4 85.8 85.6 83.9 75.1 for the formulation containing EC N14 2.5 5 7.5 and EC N50 10 12.5 and 15 respectively. The dissolution profile was shown and the mean dissolution time of pellets was noted to be 6.19 hrs. Formulation F5 was identified to be the most superior formulation.Conclusion Accordingly it can be concluded that the F5 12.5 ww EC N50 is a robust one and the performance is less likely to be affected by the various factors studied. The formulations were subjected to stability studies according to the International Council for Harmonisation of Technical Requirements for Pharmaceuticals for Human Use ICH guidelines for three months which demonstrated all the tested formulations to be stable.