Investigation of the Permeability of Antiretroviral Drugs Lamivudine and Valganciclovir via Single-Pass Intestinal Perfusion (SPIP) Method

Senem Şanlı, Mustafa Sinan Kaynak, Nurullah Sanli, Emine Ertürk Balta
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Abstract

Introduction: Antiretroviral medications are widely used to treat HIV infections. Lamivudine (3TC) is prescribed for HIV-1 infection management in adults and pediatrics, while valganciclovir (VGC) is a prodrug of ganciclovir derived from valine. Method: The Biopharmaceutics Classification System (BCS) estimates the contributions of intestinal permeability, dissolution, and solubility in oral drug absorption. Intestinal permeability refers to a substance's capacity to pass through the protective layer of cells in the intestine. The intestinal permeability of 3TC and VGC was analyzed and categorized using the single-pass intestinal perfusion technique according to the BCS in male Sprague Dawley rats, and a reversed- phase HPLC method was validated for precise and accurate measurement. objective: Intestinal permeability refers to a substance's capacity to pass through the protective layer of cells in the intestine. Result: According to the BCS, 3TC and VGC have been classified as having low permeability when compared to metoprolol tartrate, which is classified as Class I with good permeability and resolution. Conclusion: The permeability values derived from this work can be valuable in exposure assessment models.
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通过单通道肠道灌注(SPIP)法研究抗逆转录病毒药物拉米夫定和缬更昔洛韦的渗透性
导言:抗逆转录病毒药物被广泛用于治疗艾滋病毒感染。拉米夫定(3TC)是成人和儿童治疗 HIV-1 感染的处方药,而缬更昔洛韦(VGC)是从缬氨酸中提取的更昔洛韦原药。方法:生物制药分类系统(BCS)估算了口服药物吸收过程中肠道渗透性、溶解性和可溶性的贡献。肠道渗透性是指物质通过肠道细胞保护层的能力。根据 BCS,采用单通道肠道灌注技术对雄性 Sprague Dawley 大鼠的 3TC 和 VGC 的肠道渗透性进行了分析和分类,并验证了反相 HPLC 方法的精确性和准确性:肠道渗透性是指物质通过肠道细胞保护层的能力。结果:根据 BCS,3TC 和 VGC 被归类为低渗透性,而酒石酸美托洛尔被归类为 I 级,具有良好的渗透性和分辨率。结论这项工作得出的渗透性值可用于暴露评估模型。
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