Antimicrobial activity assessment of time-dependent release bilayer tablets of amoxicillin trihydrate

Abstract

The aim of present study was the assessment of antimicrobial activity of prepared time-dependent release bilayer tablets of amoxicillin trihydrate and in vitro evaluation of drug release by antimicrobial assay using agar plate diffusion method. The bilayer tablets comprised of a delayed and sustained release layer. Direct compression method was used for the preparation of bilayer tablets containing Eudragit-L100 D55 as delayed release polymer, and HPMCK4M and HPMCK15 as sustained release polymers. The prepared bilayer tablets containing amoxicillin trihydrate were evaluated for hardness, thickness, friability, weight variation and drug content. Further, in vitro drug release was assessed by antimicrobial assay using S. aureus and E. coli as test microorganisms. The aliquot samples of in vitro drug release study were found to be effective against both microorganisms for 16 hours due to sustained action. The in vitro drug release study and antimicrobial assay showed that bilayer tablets have sustained release profile of drug delivery with time-dependent burst release after a lag-time of 2 hours. The lower MIC value (2 µg/mL) of prepared bilayer tablets vis-à-vis marketed preparation (5 µg/mL) represented its good antimicrobial activity. Uniterms:Chronotherapeutics. Time-dependent release. In vitro dissolution. Minimum inhibitory concentration. Zone of inhibition.O objetivo do presente estudo foi avaliar a atividade antimicrobiana de formulações de comprimidos de dupla camada contendo amoxicilina triidratada para liberação tempo dependente e avaliação da liberação in vitro do fármaco pelo ensaio de atividade antimicrobiana utilizando o método de difusão em placa de ágar. Os comprimidos de dupla camada consistem em uma camada para liberação retardada e outra sustentada. O método de compressão direta foi usado para a preparação dos comprimidos de dupla camada contendo Eudragit-L 100 D55 como polímero para liberação retardada e HPMCK4M ou HPMCK15 como polímeros para liberação sustentada. As formulações de comprimidos de dupla camada contendo amoxicilina triidratada foram avaliadas quanto a dureza, espessura, friabilidade, variação de peso e conteúdo de fármaco. Além disso, a liberação do fármaco in vitro foi avaliada por ensaio de atividade antimicrobiana usando S. aureus e E. coli como microrganismos teste. A alíquota das amostras do estudo de liberação do fármaco in vitro demonstrou ser efetiva contra ambos os microrganismos por um período de 16 horas devido à ação sustentada. O estudo de liberação do fármaco in vitro e o ensaio de atividade antimicrobiana mostraram que os comprimidos de dupla camada tiveram um perfil de liberação sustentada do fármaco com um pico de liberação após 2 horas de ensaio. O menor valor de MIC (2 ug/mL) dos comprimidos de dupla camada quando comparados à formulação comercial (5 ug/ mL) representa uma boa atividade antimicrobiana. Unitermos:Cromoterapia. Liberação tempo-dependente. Dissolução in vitro. Concentração inibitória mínima. Zona de inibição.

Comparison between the dissolution profiles of prolonged-release ciprofloxacin tablets available in the Colombian market

“…The release of an active pharmaceutical ingredient (API) from solid oral formulations is a prerequisite for its absorption, bioavailability, and subsequent clinical response, and it depends on the physicochemical characteristics of the API, on the excipients used, and on the product technology (Qiu et al, 2016). Differences in the formulation among this kind of products can affect their release characteristics, and for MR formulations of antibiotics, it has been shown that changes in the composition affecting the release profile of the drug can also cause variations in the minimum inhibitory concentration and the emergence of bacterial resistance, which is currently a major public health problem (Beg et al, 2012). Considering that the difference between generic and reference drugs is precisely in the composition of the formulation, it would be possible to find variations in the release profiles among MR antibiotics from different manufacturers, early through in vitro dissolution studies, before the in vivo evaluation of bioequivalence (Anderson et al, 1998).…”

Biological Evaluation and Theoretical Study of Bi-dentate Ligand for Amoxicillin Derivative with Some Metal Ions

“…Schiff bases have distinction in medicinal and pharmaceutical arenas due to their expansive spectrum of biological activity such as antibacterial, antifungal (2,3), anticancer (4) and herbicidal activities (5). Amoxicillin (C 16 H 19 N 3 O 5 S) is a semi synthetic penicillin type antibiotic which has little effect toward gram-negative bacteria and high effect toward gram-positive bacteria (6). It is used in human medicine as well as in veterinary practice.…”

<p>Mini-Tablets versus Nanoparticles for Controlling the Release of Amoxicillin: In vitro/In vivo Study</p>

“…21 Amoxicillin is included in all current therapeutic regimens for H. pylori eradication. [22][23][24] The most reported causes of eradication failure of H.…”