Nimodipine

Nimodipine, a poorly soluble drug, was considered to be fit for solid dispersions to improve its solubility and bioavailability. Our study intended to prepare Nimodipine solid dispersions by solvent evaporation method using various novel polymers. Solubility and dissolution studies indicate that Kolliwax RH 40 and SLS is the most suitable polymer. The solubility studies were corresponded with dissolution data and the formulation SD15 was found to be having highest drug release of about 98.96±5.15% in about 90 minutes. In-vitro release data from several formulations containing XRD and SEM studies indicate no crystallinity in the optimized formulation SD15. FTIR studies suggested good drug excipient compatibility between all components of prepared formulation. From in vivo bioavailability studies, Cmax of the optimized formulation SD15 was 4.34±0.08ng /ml, was significantly higher as compared to pure drug suspension, i.e., 2.78±0.35ng/ml. Tmax of optimized formulation was decreased significantly when compared with pure drug (1.00±0.05hr, 2.00±0.01hr), AUC0-? and AUC0-t for optimized solid dispersion formulation was significantly higher (p<0.05) as compared to pure drug suspension. The present study demonstrated that formulation of Nimodipine solid dispersion by solvent evaporation technique is a highly effective strategy for enhancing the bioavailability of poorly water soluble Nimodipine.

  Nimodipine is an antihypertensive, calcium channel blocker, vasodilator agent and used in the treatment of various cardiovascular disorders such as angina pectoris, cardiac arrhythmia and hypertension. Oral bioavailability of Nimodipine is around 13% and having half life 9 hrs. In present research work an attempt has been made to prepare fast dissolving tablets of Nimodipine by direct compression technique with β-cyclodextrin complexes using various superdisintegrants. The powder blends were subjected for pre-compressional parameters. The prepared tablets were evaluated for post-compressional parameters. The prepared tablets were characterized by DSC and FTIR Studies. No chemical interaction between drug and excipients was confirmed by DSC and IR studies. The values of pre-compression parameters evaluated were within prescribed limits and indicated good free flowing property. All the post-compressional parameter are evaluated were prescribed limits and results were within IP acceptable limits. The tablets were evaluated for the in-vitro disintegration time and it was observed that the time for all the formulations varied from 19.24 to 48.29 sec. The promising formulations CCP4, CCC4 and CSS1 shows the 90 % of drug released within 5-8 min. Among all the formulation CCP4 (15 % crospovidone) were found to be best and showed a disintegration time of 19.24 sec, 50 % of drug released in 0.96 min, and 90 %  of drug released in 4.78 min. The stability study was conducted as per the ICH guidelines and the formulations were found to be stable, with insignificant changes in hardness, drug content and disintegration time. These results revealed that fast dissolving tablets of the poorly soluble drug, Nimodipine, showing enhanced dissolution and, hence, better patient compliance. Key words: Fast dissolving tablets, Nimodipine, sodium starch glycolate, croscarmellose sodium, crospovidone,  β-cyclodextrin.