Optimization, Characterisation and Pharmacokinetic Studies of Mucoadhesive Oral Multiple Unit Systems of Ornidazole

The objective of the present study was to investigate the applicability of matrix type mucoadhesive oral multiple unit systems (MUS) for sustaining the release of ornidazole in the gastrointestinal tract (GIT). The MUS were prepared by ionotropic gelation method using chitosan and hydroxypropyl methyl cellulose K4M (HPMC K4M) according to 32 factorial designs and were evaluated in vitro and in vivo. The particle size length ranged from 0.78 to 1.30 mm and breadth from 0.76 to 1.30 mm, respectively. The entrapment efficiency was in range of 80 to 96%. The rapid wash-off test was observed faster at intestinal pH 6.8 as compared to acidic pH 1.2. The fluoroscopic study revealed the retention of MUS in GIT for more than 5 hours. The pharmacokinetic parameters Cmax, Tmax, mean residence time (MRT) and area under curve (AUC) of developed MUS were found to be improved significantly (p<0.05) when compared with marketed immediate release tablets each containing 500 mg of drug. This study demonstrates that the MUS could be a good alternative to immediate release tablets to deliver ornidazole and expected to be less irritant to gastric and intestinal mucosa

Preparation and pharmacokinetic studies of mucoadhesive oral multiple unit systems of metronidazole

The objective of the present study was to investigate the applicability of matrix type chitosan treated alginate multiple unit systems (MUS) for sustained release of metronidazole prepared by ionotropic gelation method. Spherical MUS with 0.64 ± 0.95 to 0.75 ± 0.38 mm length and 0.63 ± 0.34 to 0.74 ± 0.28 mm breadth and 71.60 ± 0.42 to 82.15 ± 0.35 % entrapment efficiency were produced. The fluoroscopic study reveals that the MUS was retained in gastrointestinal tract (GIT) for more than 5 h and found to be distributed throughout the GIT. The in vivo evaluation in healthy human volunteers of the MUS and that of Flagyl® IR tablets each containing 400 mg drug revealed that the MUS showed improved pharmacokinetic parameters to Flagyl® producing a significantly different (p < 0.05) AUC. This study demonstrates that the MUS could be a good alternative to immediate release tablets to deliver metronidazole and expected to be less irritant to gastric and intestinal mucosa.Colegio de Farmacéuticos de la Provincia de Buenos Aire

Formulation and gastrointestinal transit evaluation of mucoadhesive oral Multiple Unit Systems of Furazolidone

The objective of present study was to improve gastric residence time of furazolidone by preparing mucoadhesive Multiple Unit Systems (MUS) with chitosan, Hydroxypropyl methyl cellulose K4M and sodium carboxymethyl cellulose by employing ionotropic gelation method. The resultant MUS were evaluated in vitro and in vivo. The particle size length ranged between 0.76 ± 0.25 to 0.89 ± 0.23mm, while the breadth was 0.76 ± 0.15 to 0.89 ± 0.06 mm, respectively. Encapsulation efficiency was in range of 82 to 90 %. MUS exhibited good mucoadhesive property in in vitro wash-off test. Stability studies showed no significant change in dissolution profiles (P < 0.05). The Gastrointestinal transit time was determined by fluoroscopic study which revealed that, the MUS retained in gastrointestinal tract for more than 5 hours and distributed throughout GIT. Based upon these results, prepared mucoadhesive MUS can be a good alternative to single unit systems to deliver Furazolidone with improved gastric residence time to treat intestinal amoebiasis.Colegio de Farmacéuticos de la Provincia de Buenos Aire