Bioavailability augmentation of silymarin using natural bioenhancers: An in vivo pharmacokinetic study

Abstract Pharmacokinetic studies were carried out in male and female rats to quantify silymarin as silybin (A+B) after the oral administration of various silymarin formulations combined with three bioenhancers, namely, lysergol, piperine, and fulvic acid, and compared with plain silymarin formulation (control). A non-compartmental analysis, model independent analysis, was utilized, and various pharmacokinetic parameters (C max, T max, and AUC 0-t) were calculated individually for each treatment group, and the values were expressed as mean ± SEM (n = 6). Plasma samples obtained from the rats were analyzed for the concentration of silymarin through a validated RP-HPLC method and on the basis of data generated from the pharmacokinetic studies. Results indicated that the bioenhancers augmented pharmacokinetic parameters and bioavailability increased 2.4-14.5-fold in all the formulations compared with the control. The current work envisages the development of an industrially viable product that can be further subjected to clinical trials and scientifically supports the development of silymarin as a contemporary therapeutic agent with enhanced bioavailability and medicinal values.

Silimarina / Silymarin

Introduction: Silymarin is a plant known for decades and with varied medicinal properties targeted to the liver.Objective: To investigate evidence of the use of silymarin in alcoholic liver disease and on hepatitis B and C.Methods: Review of the literature through electronic search, including studies of good methodological quality assessing the effects of silymarin on liver.Results: A systematic review of 13 studies and only 3 of them with good methodological quality showed unsatisfactory results in chronic liver diseases most common evolutionary disease as alcoholic and viral hepatitis B and C. Were demonstrated statistically significant changes in the decrease of transaminases and gamma-GT (gamma-glutamyl transpeptidase) in alcoholic liver disease, but did not change the mortality and other clinical and biochemical parameters in both alcoholic liver disease and in liver viral.Conclusion: Experimental studies have shown beneficial effects of silymarin in the liver by various drugs. However, there is insufficient evidence of its efficacy and safety in the treatment of chronic alcoholic liver disease and viral in its outcome greater mortality.

Introdução: A silimarina é uma planta conhecida há décadas e com propriedades medicinais variadas direcionadas para o fígado.Objetivo: Verificar evidências do uso da silimarina na doença alcóolica do fígado e nas hepatites B e C.Métodos: Revisão sistematizada da literatura por meio de busca eletrônica, incluindo estudos com boa qualidade metodológica que avaliem os efeitos da silimarina em hepatopatias.Resultados: Uma revisão sistemática com 13 estudos e somente 3 deles com boa qualidade metodológica mostraram resultados não satisfatórios nas hepatopatias crônicas evolutivas mais comuns como por doença alcóolica e hepatites virais B e C. Foram demonstradas alterações estatisticamente significantes na diminuição das transaminases e gama-GT (gama-glutamil transpeptidase) na doença hepática alcoólica, porém, sem alterar a mortalidade e outros parâmetros clínicos e bioquímicos tanto na hepatopatia alcoólica como nas hepatopatias virais.Conclusão: Estudos experimentais mostraram efeitos benéficos da silimarina nas hepatopatias por diversas drogas. No entanto, não há evidências suficientes de sua eficácia e segurança no tratamento de hepatopatias crônicas alcoólicas e virais no seu desfecho maior, a mortalidade.

Dissolution test for silymarin tablets and capsules.

Silybine (SBN), isosilybine (ISBN), silycristine (SCN), silydianine (SDN), and taxifoline (TXF) are the main active flavonoids commonly found in the dried fruits of Silybum marianum, Gaertner (Compositae). Concentrations of these compounds, except TXF, are usually expressed together as silymarin content. This paper describes a simple dissolution test developed to estimate silymarin (Sl) in pharmaceutical formulations. Five commercial products were tested using this new method (including tablets, sugar tablets, and capsules): two from Argentina, one from Brazil, one from Spain, and one from Italy. Results demonstrated that, provided the dosage form disintegrates, amounts dissolved range from 50 to 90% of the labeled value. Products were analyzed by high performance liquid chromatography (HPLC) and UV spectrophotometry.