Fluconazole Oral Suspension Research Articles

Evaluation of Physical-Chemical and Microbiological Stability of Fluconazole Oral Suspensions for Hospital Use

Fluconazole is an important drug in the treatment of cutaneous and systemic mycoses. The Hospital de Clínicas de Porto Alegre performs a derivation of fluconazole capsules to obtain an oral liquid formulation that is easily administered and whose dose can be adjusted. In order to replace the derivation for a formulation produced from an active pharmaceutical ingredient, this study sought to develop a liquid oral formulation, evaluate its physical chemical and microbiological stability and demonstrate suitability of the analytical method for the formulation assay. Seven different formulations of pharmaceutical suspension form were produced and evaluated for pH, viscosity, sedimentation volume and assay. The analytical method by High Performance Liquid Chromatography was demonstrated. Two most promising formulations were manipulated in the Farmácia Semi-Industrial do Hospital de Clínicas de Porto Alegre and stored in amber PET bottles under three different conditions: room temperature, under refrigeration (2 to 8 ºC) and in an oven (40 ° C). Samples were collected after 0, 7 and 14 days to evaluate physical-chemical stability, assay, pH and macroscopic aspects. Samples were collected after 0 and 21 days to evaluate microbiological stability. It was possible to demonstrate stability for one of the formulations for a 14-day period. Throughout the study, the chosen formulation presented adequate quantification of fluconazole, constant pH, no organoleptic changes and no microbial growth. The results suggest the incorporation of a new formulation for fluconazole to the Farmacia Semi-Industrial portfolio).

FUSOGENIC LIPOSOME FOR THE TREATMENT OF FUNGAL MENINGITIS: AN OVERVIEW

Fungal meningitis is an infection which is caused by fungus which spreads through the blood to the spinal cord. People with weakened immunity get this disease easily like persons with AIDs, etc. To make sure the disease is fungal meningitis, a sample is taken from the cerebrospinal fluid and it is sent to the laboratory. Usually, fungal meningitis is not mediated from person to person, but it is caused when a fungi are inhaled from the surrounding and spread into the blood to the central nervous system. Normally medications such as vaccines, IV, and oral suspensions are given to the people for curing fungal meningitis. Commonly used drugs are Amphotericin B and fluconazole oral suspension. Amphotericin B is an antifungal, antiprotozoal, and hydrophobic drug. However, these drugs cannot give a directly as medication therapy for the patients, because it offers toxic effect and side effects, absorption rate is slower, and crossing the blood–brain barrier (BBB) is getting difficult. Adverse effects can be minimized with the application of nanotechnology. Therefore, in human medical services, the availability of molecular nanotechnology will provide rapid progress. Nanoparticle (NP) systems help to improve the solubility of poorly water-soluble drugs which has been explained using Noyes–Whitney equations. Nanoparticles offers several advantages as a drug delivery system, such as better drug bioavailability, reduction of dosing frequency enables them for the betterment of diseases, can cross the BBB, and it is very cost-effective. Types of NP include polymeric NP, carbon nanotubes, metallic structures, nanocrystals, and fusogenic liposomes. Fusogenic liposomes are a peculiar class of phospholipid vesicles. The fusogenic liposomes can deliver encapsulated NP into the targeted sites and also can cross the BBB. On comparing with cationic liposomes, fusogenic liposomes are more effective as well as rapid in the drug delivery.

Current treatment of oral candidiasis: A literature review.

Candidiasis or oral candidosis is one of the most common human opportunistic fungal infections of the oral cavity. This pathology has a wide variety of treatment which has been studied until these days. The present study offers a literature review on the treatment of oral candidiasis, with the purpose of establish which treatment is the most suitable in each case. Searching the 24 latest articles about treatment of candidiasis it concluded that the incidence depends on the type of the candidiasis and the virulence of the infection. Although nystatin and amphotericin b were the most drugs used locally, fluconazole oral suspension is proving to be a very effective drug in the treatment of oral candidiasis. Fluconazole was found to be the drug of choice as a systemic treatment of oral candidiasis. Due to its good antifungal properties, its high acceptance of the patient and its efficacy compared with other antifungal drugs. But this drug is not always effective, so we need to evaluate and distinguish others like itraconazole or ketoconazole, in that cases when Candida strains resist to fluconazole. Key words:Candidiasis, treatment, miconazole, fluconazole, nystatin.

Stability of Reconstituted Fluconazole Oral Suspension in Plastic Bottles and Oral Syringes

Fluconazole for oral suspension is a dry powder with a beyond-use date of 14 days after being reconstituted. Dispensing fluconazole liquid in the inpatient setting would be much more efficient if prefilled oral syringes containing standard doses were readily available. In addition, if the beyond-use date could be extended, the resulting decreased waste would be economically beneficial. To determine the stability of reconstituted fluconazole oral suspension using high-performance liquid chromatography (HPLC). Diflucan lyophilized powder was reconstituted to fluconazole 40 mg/mL using Sterile Water for Irrigation, USP. Samples were stored at room temperature in both the original Diflucan plastic bottles and in amber polyethylene oral syringes with silicon elastomer plunger tips that were sealed with high-density polyethylene caps. Samples were analyzed immediately and at 14, 28, 42, 56, and 70 days. Fluconazole concentrations were measured using a modified stability-indicating HPLC method. At each test interval, the density of the suspension was determined gravimetrically and then used to calculate the exact volume of sample used for each analysis. Excessive degradation was defined as greater than 10% loss of the initial concentration. The stock internal standard was stable for at least 77 days when stored in the dark at room temperature. The stock and working fluconazole standard solutions were prepared fresh at each test interval. Reconstituted oral suspension retained more than 90% of the initial fluconazole concentration for at least 70 days at 22-25 degrees C. No changes in color, odor, or visible microbiological growth were observed in any sample. The pH of the suspension was initially 4.2 and remained essentially unchanged throughout the study. Reconstituted fluconazole oral suspension is stable in both the product's original plastic bottles and in amber polyethylene oral syringes for at least 70 days when stored at 22-25 degrees C.

A Multicenter Randomized Trial Evaluating Posaconazole versus Fluconazole for the Treatment of Oropharyngeal Candidiasis in Subjects with HIV/AIDS

Oropharyngeal candidiasis is the most common opportunistic infection among persons infected with human immunodeficiency virus (HIV). Use of some agents is hampered by lack of efficacy, emergence of resistance, adverse events, and need for intravenous administration. Posaconazole is an extended-spectrum triazole with potent in vitro activity against Candida species, including Candida albicans, Candida glabrata, and Candida krusei (including fluconazole-resistant strains). This multicenter, randomized, evaluator-blinded study of subjects with HIV infection and oropharyngeal candidiasis compared efficacy of posaconazole with that of fluconazole. Subjects received either 200 mg of posaconazole or fluconazole oral suspension on day 1, followed by 100 mg/day for 13 days. The primary study end point--clinical success (cure or improvement) on day 14--was evaluated for 329 subjects. Durability of clinical success was evaluated on day 42. Three hundred fifty subjects received posaconazole (n = 178) or fluconazole (n = 172). Clinical success occurred in 155 (91.7%) of 169 posaconazole recipients and in 148 (92.5%) of 160 fluconazole recipients (95% confidence interval, -6.61% to 5.04%), indicating that posaconazole was not inferior to fluconazole. On day 14, mycological success was 68% in both arms, but by day 42, significantly more posaconazole recipients than fluconazole recipients continued to have mycological success (40.6% vs. 26.4%; P=.038). Fewer posaconazole recipients than fluconazole recipients experienced clinical relapse (31.5% vs. 38.2%). Adverse events were similar between treatment arms. Results demonstrate that posaconazole was as effective as fluconazole in producing a successful clinical outcome. However, posaconazole was more effective in sustaining clinical success after treatment was stopped.

A comparative study of the efficacy and safety of fluconazole oral suspension and amphotericin B oral suspension in cancer patients with mucositis

This randomized study compared the efficacy and safety of fluconazole suspension with that of amphotericin B suspension in patients with head and neck cancer who were suffering from candidiasis during cancer treatment with radiotherapy and/or chemotherapy. A total of 123 evaluable patients received 50 mg fluconazole once daily and 120 evaluable patients received 0.5 g amphotericin B thrice daily for 7–14 days depending on clinical response. A positive culture result was obtained in 121 of 264 (46%) patients; Candida albicans was most common. At the end of treatment, fluconazole and amphotericin B were equivalent (CI 90 of −10.7 to +14.9) in terms of clinical cure and improvement, but the rate of mycologic cure was higher for fluconazole (48%) than amphotericin B (35%). The incidence of adverse events was 39% for fluconazole and 44% for amphotericin B. Fluconazole suspension appeared effective and safe.