ABSTRACT
Ketoconazole is photolabile antifungal drug. Photochemical reactions may decrease its therapeutic effect or induce toxic compounds. The aim of this study was to prepare ketoconazole loaded microemulsion containing H. suaveolens oil with antifungal and antioxidant powers in order to obtain effective antifungal formulation. The release study, antifungal activity and photostability test, were then evaluated. The results showed that optimized Hyptis suaveolens microemulsion for ketoconazole loading was selected through construction of pseudo-ternary phase diagrams. It consisted of 12.5% H. suaveolens oil, 12.5% capryol, 25% tween 80, 25% ethanol and 25% water. Mean globule size was 153 nm, as analyzed by photon correlation spectroscopy. Ketoconazole-loaded Hyptis suaveolens microemulsion and Hyptis suaveolens microemulsion had antifungal activity against Candida albican, Microsporum gypseum and Trichophyton mentagrophyte, showing inhibition zone ranged from 28-37 mm and 23-32 mm, respectively. Ketoconazole was released from Hyptis suaveolens microemulsion more than 90% within 5 days. In the results of photostability test, ketoconazole-loaded Hyptis suaveolens microemulsion gave significantly higher remaining ketoconazole than ketoconazole solution. This study demonstrated that Hyptis suaveolens microemulsion could be used to improve the photoprotection of photolabile drug
ABSTRACT
The main purposes of this study are to prepare cross-linked carboxymethyl jackfruit starch [CL-CMJF] and to evaluate its pharmaceutical property as a tablet disintegrant. CL-CMJF was prepared by a dual carboxymethyl-crosslinking reaction in a flask containing jackfruit seed starch [JFS], chloroacetic acid [CAA], sodium hydroxide [NaOH] and sodium trimetaphosphate [STMP]. The reaction was carried out using methanol as a solvent for 60 min at 70°C and at JFS:CAA:NaOH:STMP ratio of 1.0:0.29:0.28:0.07. The obtained CL-CMJF, with degree of substitution and degree of crosslinking calculated to be 0.34 and 0.06, respectively, was insoluble but swellable in water. Rheological study revealed a decreased in solution viscosity compared to the non-crosslinked CMJF. The water uptake of CL-CMJF was 23 times higher than that of native starch and was comparable to that of a commercial superdisintegrant, sodium starch glycolate [SSG]. The swelling ability of CL-CMRS was similar to that of crosscarmellose sodium [CCS], another commercial superdisintegrant. Disintegration test of aspirin tablets containing 2%w/w of JFS, CL-CMJF, SSG and CCS showed disintegration times in the order of SSG < CCS CL-CMJF <<< JFS. The results suggested that CL-CMJF could be developed as a tablet disintegrant