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首页> 外文期刊>European journal of gastroenterology and hepatology >Gut delivery of budesonide, a locally active corticosteroid, from plain and controlled-release capsules.
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Gut delivery of budesonide, a locally active corticosteroid, from plain and controlled-release capsules.

机译：从普通和控释胶囊中肠胃吸收布地奈德，一种局部活性的皮质类固醇。

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OBJECTIVE: To compare the pharmacokinetics and site of uptake of budesonide from a controlled-release formulation and a deuterium-labelled standard formulation given before and after a meal. METHODS: Six healthy volunteers were randomized into an open, crossover study. They received 4.5 mg controlled-release budesonide (mixed with In pellets to trace gastrointestinal transit) and 4.8 mg 2H8-budesonide simultaneously at each of two visits: one visit before a standardized breakfast and the other after breakfast. Plasma concentrations of budesonide were followed over 24 h. The transit of the (111)In pellets through the gastrointestinal tract was followed for 36 h. Data on the site of absorption were calculated from transit times and absorption curves. RESULTS: The time to peak plasma concentration was significantly increased with controlled-release budesonide when compared with the deuterium-labelled standard formulation (before breakfast, 4.5 h vs 1.8 h; after breakfast, 5.2 h vs 2.9 h). When given afterbreakfast, the controlled-release formulation was associated with a mean residence time 1.6 h longer than that seen with the standard formulation. However, the areas under the plasma concentration curves were similar with the two formulations, regardless of when the treatments were given (before breakfast, 18.0 +/- 3.8 nmol/l vs 18.0 +/- 6.0 nmol/l; after breakfast, 16.9 +/- 7.0 nmol/l vs 18.5 +/- 9.0 nmol/l). Over 60% of the total budesonide absorbed from controlled-release capsules was delivered and absorbed in the ileum and colon. The corresponding proportion for the standard formulation was approximately 33%. CONCLUSIONS: Controlled-release budesonide effectively delivers most of the budesonide dose to the ileum and colon, the regions that are most often affected by inflammatory bowel disease. In addition, the time of food intake has little effect on the site of absorption or the bioavailability of the controlled-release formulation. Delivery to the colon and ileum was independent of whether the drug was given before or after breakfast.
机译：目的：比较餐前和餐后从控释制剂和氘代标准制剂中布地奈德的药代动力学和摄取部位。方法：将六名健康志愿者随机分为一个开放式交叉研究。他们在两次就诊中分别接受一次4.5毫克控释布地奈德（与In颗粒混合以追踪胃肠道转运）和4.8毫克2H8-布地奈德，一次是在标准早餐前，一次是在早餐后。在24小时内跟踪布地奈德的血浆浓度。跟踪（111）In颗粒通过胃肠道的转运时间为36小时。根据传输时间和吸收曲线计算吸收位点的数据。结果：与氘标记的标准制剂相比，布地奈德控释血浆血浆浓度达到峰值的时间显着增加（早餐前4.5 h比1.8 h;早餐后5.2 h vs 2.9 h）。给予早餐后，控释制剂的平均停留时间比标准制剂长1.6小时。但是，无论何时给予治疗，血浆浓度曲线下的面积均与两种配方相似（早餐前为18.0 +/- 3.8 nmol / l，而早餐前为18.0 +/- 6.0 nmol / l;早餐后为16.9 + +/- 7.0 nmol / l对18.5 +/- 9.0 nmol / l）。从控释胶囊中吸收的布地奈德总量的60％以上被递送并吸收到回肠和结肠中。标准配方的相应比例约为33％。结论：布地奈德控释有效地将大部分布地奈德剂量输送至回肠和结肠，回肠和结肠是最常受炎症性肠病影响的区域。此外，进食时间对控释制剂的吸收部位或生物利用度影响很小。送至结肠和回肠的时间与早餐之前或之后是否服用药物无关。

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