Moghadamnia Yasaman, Kazemi Sohrab, Rezaee Boshra, Rafati-Rahimzadeh Mehrdad, Ebrahimpour Soheil, Aghapour Fahimeh
Alzahra University, Tehran, Iran.
Cellular and Molecular Biology Research Center, Health Research Institute, Babol University of Medical Sciences, Babol, Iran.
Caspian J Intern Med. 2019 Spring;10(2):150-155. doi: 10.22088/cjim.10.2.150.
Enteric-coated capsules are solid dosage forms which are designed to bypass the stomach and release the drug in the small intestine. This study was done to compare pharmacokinetics of ibuprofen tablet and ibuprofen as enteric-coated capsule using sodium alginate beads.
A crossover randomized study was performed on 12 healthy volunteers receiving a single dose of regular ibuprofen tablet (200 mg) and enteric-coated capsule (200 mg). The washout time between the periods was one month. Pharmacokinetic and pharmacodynamic blood samples were collected for 16 hours following treatment. High-performance liquid chromatography (HPLC) method used the following specifications: C18 column with 4.6 mm diameter & 25 mm length, the fluorescent detector of excitation and emission wavelengths were 224 and 290 nm, respectively.
After a single oral dose of ibuprofen formulations, the median times to maximum concentration were 60 and 240 minutes in ibuprofen tablet (200 mg) and enteric-coated capsule, respectively. The maximum levels for the participants receiving ibuprofen tablet and enteric-coated capsule were 11.71±1.3 and 10.32±4.19 µg/mL, respectively. The pharmacokinetic (PK) modeling data showed the area under curve (AUC) to be 61.51 hours & 86.62 hours for the group receiving the tablet and the capsule, respectively.
According to the results, in is concluded that enteric coating may delay the onset of ibuprofen effect and increases the duration of action. This formulation has advantages over the conventional drug delivery systems as it lengthens the dosing intervals and also increases patient compliance for chronic pain.
肠溶胶囊是一种固体剂型，其设计目的是绕过胃部并在小肠中释放药物。本研究旨在比较布洛芬片剂和使用海藻酸钠珠的布洛芬肠溶胶囊的药代动力学。
对12名健康志愿者进行交叉随机研究，他们分别接受单剂量的常规布洛芬片剂（200毫克）和肠溶胶囊（200毫克）。各阶段之间的洗脱期为一个月。治疗后16小时采集药代动力学和药效学血样。高效液相色谱（HPLC）方法采用以下规格：直径4.6毫米、长度25毫米的C18柱，激发和发射波长的荧光检测器分别为224和290纳米。
单次口服布洛芬制剂后，布洛芬片剂（200毫克）和肠溶胶囊达到最大浓度的中位时间分别为60分钟和240分钟。接受布洛芬片剂和肠溶胶囊的参与者的最大血药浓度分别为11.71±1.3和10.32±4.19微克/毫升。药代动力学（PK）建模数据显示，接受片剂和胶囊的组的曲线下面积（AUC）分别为61.51小时和86.62小时。
根据结果得出结论，肠溶包衣可能会延迟布洛芬起效时间并延长作用持续时间。这种剂型比传统给药系统具有优势，因为它延长了给药间隔，也提高了患者对慢性疼痛的依从性。
