Ali Al-Montaser Bellah H, Abdel-Aal Fatma A M, Rageh Azza H, Mohamed Abdel-Maaboud I
Department of Pharmaceutical Analytical Chemistry, Faculty of Pharmacy, Assiut University, Assiut, Egypt.
J Sep Sci. 2022 Dec;45(23):4187-4197. doi: 10.1002/jssc.202200531. Epub 2022 Oct 18.
Diabetes is a known risk factor for sexual dysfunction in men; diabetic men have an increased risk of erectile dysfunction compared to non-diabetic men. Canagliflozin is one of the common antidiabetic drugs that is readily used in the treatment of type-2 diabetes. Concomitantly phosphodiesterase 5 inhibitors, such as tadalafil, can be given to the patient to alleviate erectile dysfunction. Canagliflozin is reported to be one of the cytochrome P450 3A4 enzyme inhibitors, that might seriously influence blood concentration levels of tadalafil but there is no study till now, discussing this interaction. Therefore, a fast, simple, and sensitive high-performance thin-layer chromatographic method was developed, validated, and applied for the simultaneous determination of tadalafil and canagliflozin in spiked and real human plasma. The limit of detection for tadalafil was 0.14 ng/band and for canagliflozin was 0.16 ng/band. The limit of quantitation value for tadalafil was 0.43 ng/band and for canagliflozin was 0.47 ng/band. Tadalafil and canagliflozin were determined simultaneously in real human plasma using the described procedure and the method was applied for in vivo pharmacokinetic drug interaction study between the studied drugs, which proved significant interaction between them when administered simultaneously.
糖尿病是男性性功能障碍的已知风险因素；与非糖尿病男性相比，糖尿病男性患勃起功能障碍的风险更高。卡格列净是常用于治疗2型糖尿病的常见抗糖尿病药物之一。同时，可以给患者使用磷酸二酯酶5抑制剂，如他达拉非，以缓解勃起功能障碍。据报道，卡格列净是细胞色素P450 3A4酶抑制剂之一，可能会严重影响他达拉非的血药浓度水平，但目前尚无研究讨论这种相互作用。因此，开发、验证了一种快速、简单、灵敏的高效薄层色谱法，并将其应用于加标和实际人血浆中他达拉非和卡格列净的同时测定。他达拉非的检测限为0.14 ng/条带，卡格列净的检测限为0.16 ng/条带。他达拉非的定量限为0.43 ng/条带，卡格列净的定量限为0.47 ng/条带。使用所述方法同时测定实际人血浆中的他达拉非和卡格列净，并将该方法应用于所研究药物之间的体内药代动力学药物相互作用研究，结果证明同时给药时它们之间存在显著相互作用。
