Abstract. Fungal keratitis is a serious corneal disease that may result in loss of vision. There are limited treatment options available in Iraqi eye hospitals which might be the main reason behind the poor prognosis of many cases. The purpose of this study was to prepare and pharmaceutically evaluate clotrimazole-β-cyclodextrin (CTZ-β-CD) eyedrops then clinically assess its therapeutic efficacy on fungal keratitis compared with extemporaneous amphotericin B eyedrops (0.5% w/v). A CTZ-β-CD ophthalmic solution was prepared and evaluated by various physicochemical, microbiological, and biological tests. The prepared formula was stable in 0.05 M phosphate buffer pH 7.0 at 40±2°C and 75±5% RH for a period of 6 months. Light has no significant effect on the formula's stability. The CTZ-β-CD eyedrops efficiently complied with the isotonicity, sterility, and antimicrobiological preservative effectiveness tests. Results of the clinical study revealed that 20 (80%) patients showed a favorable response to the CTZ-β-CD eyedrops, while 16 patients (64%) exhibited a favorable response to amphotericin B (P>0.05). The mean course of treatment was significantly (P<0.05) less in the CTZ treatment group than in the amphotericin group (21.5±5.2 vs. 28.3±6.4 days, respectively). The CTZ formulation was significantly (P<0.05) more effective in the management of severe cases and also against Candida sp. than amphotericin B. There was no significant difference (P<0.05) between both therapies against filamentous fungi. The CTZ-β-CD formulation can be used alternatively to other ophthalmic antimycotic treatment options in developing countries where stability, cost, or efficacy is a limiting factor.
Azithromycin is the drug of choice in the treatment of several bacterial infections, most often those causing middle ear infection, bronchitis, pneumonia, typhoid and sinusitis. It’s also effective against certain urinary tract infections and venereal diseases. This study was carried out to prepare an acceptable suspension either as dry physical mixture powder or granules to be reconstituted, through studying the effect of various type and concentration of suspending agent (xanthan gum, hydroxypropyl methylcellulose (HPMC), either alone or in combination) on the release profile of the drug. The best prepared suspension formulas (H& III) were selected depending on the dissolution profile of each formulas and then compared with the reference suspensions (Zithromax and Azi-once).The viscosity, sedimentation volume, Resuspendability and expiration date were evaluated for the chosen formulas (H&III) and compared with references ZithromaxÒ and Azi-onceÒ.The result indicated that the chosen formula – H had better dissolution rate compared with references suspensions, Also it was less viscous than them.While other chosen formula – III had lower dissolution rate compared with ZithromaxÒ and higher dissolution rate than AZi – once, also it was less viscous than both references.It was found that the dry physically mixed powder (formula – H) was more stable than the granular suspension (Formula III) since the expiration date for formula H and formula III were 3.24 and 2.7 years respectively. Key words: Azithromycin, suspending agent, suspension.
A new model aqueous micro fine suspension of tinidazole (TND) was developed on the basis of the combination with chlorhexidine gluconate to be useful in treatment of ungal corneal infection or ulcer (fungal keratitis). In vitro clinical study for TND - chlorhexidine gluconate showed a significant antifungal activity against certain species of fungi isolated from patients with corneal ulcer . Propylene glycol (PG) was chosen because it is known as a good solubilizer , it could be used as a tonicity adjustment agent in appropriate concentration & it is nontoxic . An enhancement in the solubility of TND was achieved also by interaction with a non-ionic surfactant polysorbate 80 (Tween80) and PG. . The models prepared by using PG were showed some practical advantages over the models containing a combination of PG and non –ionic surfactant polysorbate 80 (Tween 80) , by enhancement the in vitro dissolution & releasing of TND suspension .Previous histological studies have shown that these additives used not cause eye irritation. The prepared models showed high physiological tolerance onrabbit eye. Moreover high molecular weight methylcellulose (MC) was effective to create appropriate viscosity that was maintained unchanged after heatsterilization.
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