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蔗糖醋酸异丁酸酯(SAIB)作为雌二醇和舒必利的递送载体:对去势雄马内分泌反应及季节性不排卵母马卵巢反应的评估

Sucrose Acetate Isobutyrate (SAIB) as a Delivery Vehicle for Estradiol and Sulpiride: Evaluation of Endocrine Responses in Geldings and Ovarian Response in Seasonally Anovulatory Mares.

作者信息

Oberhaus Erin L, Wilson Kaitlyn M, Camp Caroline M, Sones Jenny L

机构信息

School of Animal Sciences, Louisiana Agricultural Experiment Station, Louisiana State University Agricultural Center, Baton Rouge, LA.

School of Animal Sciences, Louisiana Agricultural Experiment Station, Louisiana State University Agricultural Center, Baton Rouge, LA.

出版信息

J Equine Vet Sci. 2022 May;112:103896. doi: 10.1016/j.jevs.2022.103896. Epub 2022 Feb 10.

Abstract

Sulpiride in vegetable shortening (VS) stimulates prolactin in horses for up to 10 days. Although effective, a pharmaceutical grade vehicle is needed for clinical application of sulpiride in horses. Sucrose acetate isobutyrate (SAIB), a hydrophobic polymer, may be an alternative to VS. Four in vivo experiments assessed the efficacy of SAIB for delivery of sulpiride, estradiol cypionate (ECP), and estradiol benzoate (EB). The first three studies utilized geldings to compare prolactin and luteinizing hormone (LH) concentrations between sulpiride delivered in VS and SAIB, and ECP or EB delivered in SAIB. Sulpiride stimulated (P < .01) prolactin similarly between vehicles. Geldings pretreated with EB had higher (P < .05) prolactin responses to sulpiride compared to ECP-treated geldings on days 5, 6 and 9. Both estradiol-sulpiride treatments stimulated LH with no differences between ECP and EB. Experiment 3 compared a simultaneous injection of EB-sulpiride to a non-simultaneous injection (one day apart) of EB-sulpiride. Prolactin was stimulated (P < .05) in both treatment groups, but the response lasted 2 days longer in geldings treated a day apart. Plasma LH increased (P < .01) in both groups equally for 10 days. Experiment 4 applied simultaneous and non-simultaneous EB-sulpiride treatments to seasonally anovulatory mares to induce ovarian activity. Prolactin and LH were stimulated similarly between treatments; however, non-simultaneously treated mares tended (P = .07) to have an ovarian response earlier. In conclusion, SAIB was a suitable vehicle for administration of estradiol and sulpiride and could be an alternative to VS for sustained-release drug delivery.

摘要

蔬菜起酥油(VS)中的舒必利可刺激马的催乳素分泌长达10天。虽然有效,但舒必利在马临床应用中需要药用级载体。蔗糖乙酸异丁酸酯(SAIB)是一种疏水性聚合物,可能是VS的替代品。四项体内实验评估了SAIB用于递送舒必利、环丙孕酮(ECP)和苯甲酸雌二醇(EB)的效果。前三项研究使用去势雄马比较VS和SAIB中递送的舒必利以及SAIB中递送的ECP或EB之间的催乳素和促黄体生成素(LH)浓度。两种载体中舒必利刺激催乳素的效果相似(P <.01)。与ECP处理的去势雄马相比,在第5、6和9天,用EB预处理的去势雄马对舒必利的催乳素反应更高(P <.05)。两种雌二醇 - 舒必利处理均刺激LH,ECP和EB之间无差异。实验3比较了EB - 舒必利同时注射与非同时注射(间隔一天)的情况。两个治疗组中催乳素均受到刺激(P <.05),但间隔一天治疗的去势雄马中反应持续时间长2天。两组血浆LH均在10天内同等程度增加(P <.01)。实验4对季节性无排卵母马应用同时和非同时的EB - 舒必利处理以诱导卵巢活动。两种处理之间催乳素和LH受到的刺激相似;然而,非同时处理的母马倾向于(P = 0.07)更早出现卵巢反应。总之,SAIB是用于施用雌二醇和舒必利的合适载体,并且可以作为VS用于缓释药物递送的替代品。

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