Abstract

Objective: This study aimed to analyze the pharmacokinetic (PK) characteristics, safety, and bioequivalence (BE) of a test (T) preparation of a nifedipine controlled-release tablet and the reference (R) drug (Adalat GTIS) in Chinese study participants in the context of fasting and postprandial states.
Materials and methods: An open-label, single-center, randomized, single-dose, two-period study was designed including two separate arms, one with administration under fasting conditions and one with administration under postprandial conditions (high-fat, high-calorie breakfast). After oral administration, the nifedipine concentrations in plasma were quantitatively analyzed using liquid chromatography-tandem mass spectrometry (LC-MS/MS) at regular intervals. Primary PK parameters, including the area under the concentration curve from 0 to infinity (AUC_0–∞), the area under the concentration profile from 0 to the last measurable concentration time (AUC_0–t), and maximal measured plasma concentration (C_max) were log-transformed with BE limits of 80 – 125% to evaluate BE. All adverse events (AEs) were wholly supervised.
Results: The PK profiles of the T and R formulations were comparable to each other under both fasting and postprandial conditions. The 90% confidence intervals (CIs) of the AUC_0–∞, AUC_0–t, and C_max were 92.69 – 106.06%, 93.32 – 107.05%, and 99.53 – 116.71%, respectively, under the fasting state. The 90% CIs of the AUC_0–∞, AUC_0–t, and C_max were 105.05 – 117.40%, 105.43 – 117.82%, and 102.66 – 116.30%, respectively, in the postprandial arm. 47 cases of drug-associated AEs were noted in the entire research.
Conclusion: Under both the fasting and postprandial states, the two nifedipine controlled-release formulations were bioequivalent and safe in healthy Chinese subjects.

Author Details

Authors

• Huan Lu¹
• Fei Zhou¹
• Cuijie Rui²
• Hen You²
• Wenhao Zhang³
• Yaxin Zhang^{1, 6}
• Juefang Ding⁴
• Shunbo Zhao⁵
• Qiang Wu^{1, 6}

Departments

• ¹ Phase I Clinical Trial Ward, Second Affiliated Hospital, Bengbu Medical University, Bengbu, Anhui,
• ² Qingdao Huanghai Pharmaceutical Co., Ltd., Nanjing,
• ³ Department of Clinical Medical, First Clinical Medical College, Anhui Medical University, Hefei,
• ⁴ Nanjing Jining Pharmaceutical Technology Co., Ltd.,
• ⁵ Nanjing Kelitai Pharmaceutical Technology Co., Ltd., Nanjing, and
• ⁶ Bengbu Medical University, Bengbu, Anhui, China

Address

Qiang Wu
Phase I Clinical Trial Ward
Second Affiliated Hospital
Bengbu Medical University
Bengbu, 233080, China
Email: [email protected]

Citation