R&D Department, Lo.Li. Pharma, Rome, Italy.
Eur Rev Med Pharmacol Sci. 2017 Jun;21(2 Suppl):83-88.
Broadening clinical evidence has markedly designated inositol(s) as a common and effective therapeutic approach for PCOS and infertility. Although considerable research has been focused on the use in clinical practice of myo-inositol (myo-ins) and D-chiro-inositol (D-chiro-ins), the two major inositol stereoisomers, less attention has been paid to their bioavailability. Therefore, the aim of this paper is to gather and analyze information on inositol(s) bioavailability, to better delineate its optimal concentration for scientific and clinical purposes. Throughout the search in PubMed, Google Scholar, and ResearchGate we identified only two studies that investigated the pharmacokinetic (PK) profile of different myo-ins administrations. This analysis found no advantage in terms of PK for single 4 g dosing of myo-ins compared to 2 g twice a day, which allowed to get a 24-hour coverage, contrary to the singular dose. Indeed, the differences regarding the area under the curve (AUC) between the two PK profiles are linked only to the maximum concentration (Cmax) but not to the time variable. In conclusion, splitting the therapeutic dosage of 4 g myo-ins in two distinct administrations seems to be the best approach for a full-day coverage.
广泛的临床证据显著表明,肌醇(inositol(s))是多囊卵巢综合征(PCOS)和不孕的一种通用且有效的治疗方法。尽管大量研究集中在肌醇(myo-ins)和 D-手性肌醇(D-chiro-ins)这两种主要的肌醇立体异构体在临床实践中的应用上,但对它们的生物利用度关注较少。因此,本文的目的是收集和分析有关肌醇(inositol(s))生物利用度的信息,以便更好地确定其用于科学和临床目的的最佳浓度。在 PubMed、Google Scholar 和 ResearchGate 上进行搜索后,我们仅确定了两项研究调查了不同肌醇给药的药代动力学(PK)特征。这项分析发现,与每天两次服用 2 克相比,单次服用 4 克肌醇在 PK 方面没有优势,因为后者可以实现 24 小时覆盖,而不是单次给药。实际上,两种 PK 曲线下面积(AUC)之间的差异仅与最大浓度(Cmax)有关,而与时间变量无关。总之,将 4 克肌醇的治疗剂量分为两次服用似乎是全天覆盖的最佳方法。