건강한 한국인 피험자에서 베실산베포타스틴의 약동학 특성에 대한 연구 (Pharmacokinetic Characteristics of Bepotastine Besilate in Healthy Subjects)

서지정보

· 발행기관 : 대한임상약리학회
· 수록지 정보 : Translational and Clinical Pharmacology / 15권 / 1호 / 37 ~ 45페이지
· 저자명 : 김보형, 정재용, 김정렬, 임경수, 임형석, 유경상, 장인진, 신상구

초록

Background: Bepotastine besilate is a non-sedating, second-generation H1-antagonist. It is known to be rapidly absorbed after oral administration and negligibly distributed to the brain. This study aimed to assess pharmacokinetic (PK) characteristics and safety of bepotastine besilate after oral administration in Korean healthy subjects.
Methods: An open, single dose, parallel group, dose-escalation study was performed in sixteen healthy subjects. Two groups of eight subjects received either 10 or 20 mg dosage, respectively. Blood samples for PK assessments were collected till 24 hours after oral administration of bepotastine besilate. For safety assessments, clinical laboratory tests, vital signs, physical examinations, and 12-lead ECGs (electrocardiographies) were measured.
Results: The average area under the concentration-time curves from time zero to infinity (AUC) were 397.12 ± 28.56 (Mean ± SD) μg‧h/L for the 10 mg group, and 776.80 ± 88.48 μg‧h/L for the 20 mg group. The values of average Cmax were 97.19 ± 22.72 μg/L and 188.79 ± 30.39 μg/L in the 10 mg and 20 mg group, respectively. AUC and Cmax appeared to increase proportionally with the dose, and dose-normalized AUC and Cmax were similar between 10 mg and 20 mg dosing groups (t-test, P=0.647 647 and 0.777, respectively). Only one adverse event (hordeolum) was reported during this trial. No clinically significant abnormalities were observed in laboratory tests, vital signs or ECG measurements.
Conclusions: Bepotastine besilate Cmax and AUC values proportionally increased with increasing dose.
Bepotastine besilate was generally safe and well tolerated with only a mild adverse event.

영어초록

Background: Bepotastine besilate is a non-sedating, second-generation H1-antagonist. It is known to be rapidly absorbed after oral administration and negligibly distributed to the brain. This study aimed to assess pharmacokinetic (PK) characteristics and safety of bepotastine besilate after oral administration in Korean healthy subjects.
Methods: An open, single dose, parallel group, dose-escalation study was performed in sixteen healthy subjects. Two groups of eight subjects received either 10 or 20 mg dosage, respectively. Blood samples for PK assessments were collected till 24 hours after oral administration of bepotastine besilate. For safety assessments, clinical laboratory tests, vital signs, physical examinations, and 12-lead ECGs (electrocardiographies) were measured.
Results: The average area under the concentration-time curves from time zero to infinity (AUC) were 397.12 ± 28.56 (Mean ± SD) μg‧h/L for the 10 mg group, and 776.80 ± 88.48 μg‧h/L for the 20 mg group. The values of average Cmax were 97.19 ± 22.72 μg/L and 188.79 ± 30.39 μg/L in the 10 mg and 20 mg group, respectively. AUC and Cmax appeared to increase proportionally with the dose, and dose-normalized AUC and Cmax were similar between 10 mg and 20 mg dosing groups (t-test, P=0.647 647 and 0.777, respectively). Only one adverse event (hordeolum) was reported during this trial. No clinically significant abnormalities were observed in laboratory tests, vital signs or ECG measurements.
Conclusions: Bepotastine besilate Cmax and AUC values proportionally increased with increasing dose.
Bepotastine besilate was generally safe and well tolerated with only a mild adverse event.

참고자료

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