The release of isoconazole nitrate from different suppository bases: in-vitro dissolution, physicochemical and microbiological studies.

Abstract

The influence of the suppository base on the in-vitro release of isoconazole nitrate was studied by dissolution, physicochemical diffusion and microbiological disk-diffusion methods. Vaginal suppository formulations containing 25 mg isoconazole nitrate for local treatment of vaginitis were prepared by a fusion method, using different hydrophilic and lypophilic suppository bases (PEG 6000, PEG 4000, PEG 1500, Witepsol H15, Novata BD and Cremao). In-vitro release rates were examined by dissolution, physicochemical diffusion and microbiological disk-diffusion methods. In the physicochemical investigations the pH indicators (pH 1-14) erythrosin B, thymol blue, bromocresol green, chlorophenol red, phenol red, and alkali blue were added to agar gels. The discs were placed onto the agar gels and 21 h later, the coloured zone diameters were measured. In the microbiological investigations, the discs were put on the inoculated plates with the suspension of Candida albicans (Institute Pasteur 628). The inoculated plates were incubated at 37 degrees C for 3 days, then the diameters of inhibition zones were measured. In the dissolution investigations release rates were in the order PEG 6000 > PEG 4000 > PEG 1500 > > Witepsol H15 > Cremao > Novata BD. The diffusion distance of isoconazole nitrate in the physicochemical investigation was in the order polyethylene glycols > Witepsol H15 > Novata BD. In the microbiological studies release rates were found with polyethylene glycols > Witepsol H15 > Novata BD > Cremao. The findings in the in-vitro studies suggested that polyethylene glycols are suitable bases for vaginal suppositories.

• Authors: M Asikoglu, G Ertan, G Cosar
• Journal: The Journal of pharmacy and pharmacology (J Pharm Pharmacol) Vol. 47 Issue 9 Pg. 713-6 (Sep 1995) ISSN: 0022-3573 [Print] England
• PMID: 8583380 (Publication Type: Journal Article)

Chemical References

• Antifungal Agents
• Delayed-Action Preparations
• Pharmaceutical Vehicles
• Triglycerides
• witepsol
• Polyethylene Glycols
• Miconazole
• isoconazole

Topics

• Antifungal Agents (pharmacokinetics)
• Calorimetry, Differential Scanning
• Candida albicans (drug effects)
• Delayed-Action Preparations
• Diffusion
• In Vitro Techniques
• Miconazole (analogs & derivatives, pharmacokinetics)
• Molecular Weight
• Pessaries
• Pharmaceutical Vehicles
• Polyethylene Glycols (chemistry, metabolism)
• Solubility
• Triglycerides (chemistry, metabolism)