Improvement of fluconazole flowability and its effect on dissolution from tablets and capsules

Abstract

The aim of this work was to improve fluconazole flowability by wet granulation and to study the effect of granulation on drug dissolution from tablets and capsules. Fluconazole was submitted to a process of wet granulation in a high-speed granulator using Plasdone Ò K29/32 or K90. Flow properties of granules and dissolution profiles for tablets and capsules produced with them were determined. Fluconazole granules demonstrated better flowability, calculated by angle of repose and compressibility index data, compared with powder. Additionally, it was observed that the granulation process improved the dissolution efficiency (ED) of fluconazole from tablets and capsules, which could also suggest an increase in bioavailability. Higher dissolution efficiencies were achieved with Plasdone ® K29/32.Uniterms: Fluconazole/flowability. Tablets/dissolution. Capsules/dissolution. Plasdone Ò O objetivo deste trabalho foi melhorar as características de fluxo do fluconazol com o emprego da granulação úmida e estudar o efeito desse processo na dissolução do fármaco em cápsulas e comprimidos. O fluconazol foi submetido ao processo de granulação úmida num granulador de alta velocidade empregando Plasdone Ò K29/32 e K90. Foram determinadas as propriedades de fluxo dos grânulos e obtidos os perfis de dissolução de cápsulas e comprimidos obtidos com os granulados em estudo. Os grânulos de fluconazol apresentaram melhores características de fluxo após o processamento, demonstradas por meio das determinações do ângulo de repouso e do índice de compressibilidade, comparativamente à matéria-prima. Adicionalmente, observou-se que o processo de granulação melhorou a eficiência de dissolução (ED) do fluconazol nos comprimidos e cápsulas.

Use of Box–Behnken design for optimization of compounded medication: acyclovir capsules report

“…The dissolution efficiencies (DE%) were determined for the ratio among the area under the dissolution curves, between the times zero and 60 minutes (AUC0-60) calculated applying the trapezoidal method, and the total area of the rectangle (AUCTR) defined for the ordinate (100% of dissolution) and for the abscissa (t=60 minutes) (15). The statistical analysis of variance (ANOVA) followed Tukey's post-hoc test, using Statistica 12.5 software, was performed considering as significant the values of p < 0.05.…”

“…Percentages of acyclovir dissolved for the developed formulations(1)(2)(3)(4)(5)(6)(7)(8)(9)(10)(11)(12)(13)(14)(15).…”

Fluconazole-tartaric acid co-crystal formation and its mechanical properties

“…The drug is given orally in capsule or tablet dosage form (Charoo et al, 2014). However, FLU has poor flowability, so this drug has limitations in the manufacture of tablets by direct compression (Consiglieri et al, 2010). Several fluconazole co-crystals have been made, but they are generally made to increase their solubility, including fluconazole cocrystals with malic acid, maleic acid, fumaric acid (Kastelic et al, 2010), dipicolinic acid, and adipic acid (Dayo Owoyemi et al, 2019).…”

Calcium alginate microparticles containing anti-TB drugs

“…Следовательно, существует необходимость в лекарственных препара-тах, содержащих флуконазол, которые обеспечивают стабильное высвобождение его invitro, а также бы-строе и стабильное всасывание invivo [11]. В связи с этим, в данной работе были проведены исследования по созданию полимерных терапевтических систем на основе микрочастиц альгината кальция с пролонгированным высвобождением флуконазола и рифампицина.…”