安娜·瑪麗亞·蓋利迪烏
介紹：
進行了一項研究以評估三氯苯達唑亞砜的藥物動力學。三氯苯達唑的活性代謝物為6-氯-5-(2,3-二氯苯氧基)-2-甲硫基苯並咪唑，並考察了兩種含三氯苯達唑50 mg /ml的口服混懸液方案在36隻健康羊體內的生物等效性。三氯苯達唑，商品名Egaten，用於治療片形吸蟲病及肺吸蟲病。它對於這兩種情況都非常可行。它是驅蟲藥苯並咪唑類的個體。苯並咪唑類藥物具有典型的原子結構，但三氯苯達唑具有氯化苯環，但沒有氨基甲酸酯聚集。苯並咪唑，例如三氯苯達唑，通常被認為是與β-微管蛋白結合，阻止微管的聚合。
方法：
為了確定測試項目相對於參考項目的總體生物利用度，研究被計劃為一項隨機、混合檢查，在兩個研究時間範圍的每一個的禁食條件下組織單獨的部分。為了確保三氯苯達唑亞砜羊血漿固定，創建並批准了一種快速、特異的優質流體色譜與質譜聯用 (LC-MS/MS) 技術。
Fluid chromatography–mass spectrometry (LC-MS) is a scientific science strategy that consolidates the physical division capacities of fluid chromatography (or HPLC) with the mass investigation abilities of mass spectrometry (MS). Coupled chromatography - MS frameworks are famous in substance investigation in light of the fact that the individual abilities of every strategy are improved synergistically. While fluid chromatography isolates blends with numerous parts, mass spectrometry gives auxiliary personality of the individual segments with high sub-atomic particularity and discovery affectability. This couple strategy can be utilized to break down biochemical, natural, and inorganic mixes ordinarily found in complex examples of ecological and organic beginning. LC-MS framework contains an interface that productively moves the isolated parts from the LC section into the MS particle source. The interface is essential in light of the fact that the LC and MS gadgets are in a general sense incongruent. The versatile stage in a Liquid Chromatography framework is a pressurized fluid, the MS analyzers generally work under high vacuum. In this way, it is beyond the realm of imagination to straightforwardly siphon the eluate from the LC section into the MS source. In general, the interface is a precisely straightforward piece of the LC-MS framework that moves the greatest measure of analyte, expels a critical bit of the versatile stage utilized in LC and jelly the synthetic personality of the chromatography items (synthetically idle). As a necessity, the interface ought not meddle with the ionizing productivity and vacuum states of the MS framework. These days, most broadly applied LC-MS interfaces depend on barometrical weight ionization (API) systems like electrospray ionization (ESI), environmental weight synthetic ionization (APCI), and climatic weight photograph ionization (APPI).These interfaces opened up during the 1990s following a multi decade long innovative work process.
The interface between a fluid stage method (HPLC) with a consistently streaming eluate, and a gas eliminate strategy conveyed in a vacuum was hard for quite a while. The approach of electrospray ionization changed this. As of now, the most widely recognized LC-MS interfaces are electrospray ionization (ESI), environmental weight synthetic ionization (APCI), and barometrical weight photograph ionization (APPI). These are more up to date MS particle sources that encourage the progress from a high weight condition (HPLC) to high vacuum conditions required at the MS analyser. In spite of the fact that these interfaces are depicted independently, they can likewise be economically accessible as double ESI/APCI, ESI/APPI, or APCI/APPI particle sources. Different testimony and drying methods were utilized previously (e.g., moving belts) yet the most widely recognized of these was the disconnected MALDI affidavit. Another methodology still a work in progress called direct-EI LC-MS interface, couples a nano HPLC framework and an electron ionization prepared mass spectrometer.
LC-MS is generally utilized in the field of bioanalysis and is uncommonly engaged with pharmacokinetic investigations of pharmaceuticals. Pharmacokinetic examines are expected to decide how rapidly a medication will be cleared from the body organs and the hepatic blood stream. MS analyzers are valuable in these examinations on account of their shorter investigation time, and higher affectability and particularity contrasted with UV identifiers generally joined to HPLC frameworks. One significant favorable position is the utilization of couple MS-MS, where the indicator might be modified to choose certain particles to section. The deliberate amount is the aggregate of atom sections picked by the administrator. For whatever length of time that there are no obstructions or particle concealment, the LC partition can be very brisk. LC-MS is much of the time utilized in tranquilize advancement since it permits speedy atomic weight affirmation and structure recognizable proof. These highlights accelerate the way toward creating, testing, and approving a disclosure beginning from an immense range of items with potential application. LC-MS applications for medicate advancement are profoundly mechanized techniques utilized for peptide mapping, glycoprotein mapping, lipodomics, normal items dereplication, bioaffinity screening, in vivo sedate screening, metabolic soundness screening, metabolite distinguishing proof, pollution recognizable proof, quantitative bioanalysis, and quality control.
The deliberate plasma groupings of triclabendazole sulfoxide were utilized for the assurance of bioequivalence between the test item concerning the reference item. Non compartmental examination of the pharmacokinetic information of triclabendazole sulphoxide demonstrated likeness between first-request energy of the test and reference item.
Results and Discussion:
確定了相關的藥物動力學參數，如 Cmax、AUClast、AUCtot。測試品的 Cmax 平均值為 56.0 (17.1) µg/ml，參考產品的 Cmax 平均值為 54.4 (20.1) µg/ml。測試品的 AUClast 平均值為 1655.6 (443.9) µg/ml xh，參考產物的 AUClast 平均值為 1803.3 (750.6) µg/ml xh。試驗品的 AUCtot 平均值為 1702.4 (445.9) µg/ml xh，參考產物的 AUCtot 平均值為 1847.7 (755.6) µg/ml xh。 Cmax 和 AUClast 的平均生物等值平均值測試與參考比分別為 1.05119 和 0.969058。三氯苯達唑亞砜試驗與參考平均值之比的 90% 信賴區間，Cmax 和 AUClast 分別為 98.28-112.44% 和 87.97-106.75%，位於 80-125% 的常規生物等效性範圍內。對於測試產品和參考產品的 Tmax（Friedman 和 Kruskal Wallis 測試），平均值之間的差異不具有統計顯著性。
結論：
因此，就三氯苯達唑亞砜的藥物動力學速率和程度而言，供試品與參考品生物等效
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