Single-dose Pharmacokinetic Study of Deferiprone Extended Release Tablets Versus Ferriprox Immediate Release Tablets Under Fasting and Fed Conditions in Healthy Volunteers
试验速览
- 阶段
- 1 期
- 状态
- 已完成
- 发起方
- ApoPharma
- 入组人数
- 20
- 试验地点
- 1
- 主要终点
- Cmax for Serum Deferiprone
研究概览
简要总结
The purpose of this study is to look at the pharmacokinetics of a new formulation of deferiprone (deferiprone extended release tablets) under fed and fasting conditions.
详细描述
This is a single-center, open-label, randomized, 5-period, 5-sequence study of the pharmacokinetics of a new formulation of deferiprone, extended release tablets, in twenty healthy volunteers. In each study period, blood samples for pharmacokinetics assessment will be collected pre-dose and over 24 hours post-dose. Safety will be assessed throughout the study.
研究设计
- 研究类型
- Interventional
- 分配方式
- Randomized
- 干预模型
- Crossover
- 盲法
- None
入排标准
- 年龄范围
- 18 Years 至 49 Years（Adult）
- 性别
- All
- 接受健康志愿者
- 是
入选标准
- •Male or female aged ≥18 to <50 years
- •A female volunteer of childbearing potential must agree to use an accepted contraceptive regimen from at least 28 days prior to the first administration of the study drug until at least 30 days after the last dose of the study drug
- •A sexually active male must agree that he and/or his female partner will use a medically acceptable method of contraception throughout the study and for at least 30 days following drug administration
- •Body mass index (BMI) greater than or equal to 18.5 kg/m^2 and below 30.0 kg/m^2
- •Body weight of at least 60 kg
- •Non- or ex smoker
- •Clinical laboratory values within the laboratory's stated normal range; if not within this range, an abnormal value must be without any clinical significance
- •Have no clinically significant diseases captured in the medical history, or evidence of clinically significant findings on physical examination and/or clinical laboratory evaluations (hematology, general biochemistry, coagulation, ECG, and urinalysis)
排除标准
- •Pregnant or breastfeeding
- •Absolute neutrophil count (ANC) < 1.8 x 109/L at screening (no repeat can be performed)
- •History of significant hypersensitivity to deferiprone or any related products (including excipients of the formulations) as well as severe hypersensitivity reactions (such as angioedema) to any drugs
- •History or presence of gastrointestinal, liver or kidney disease, or any other conditions known to interfere with the absorption, distribution, metabolism, or excretion of drugs or known to potentiate or predispose to undesired effects
- •Presence of significant cardiovascular, pulmonary, hematologic, neurological, psychiatric, endocrine, immunologic or dermatologic disease
- •Suicidal tendency, history of seizures, history of head trauma with coma or craniotomy/trepanation, state of confusion, or clinically relevant psychiatric diseases
- •Presence of out-of-range cardiac interval (PR < 110 msec, PR > 220 msec, QRS < 60 msec, QRS >119 msec and QTcF > 450 msec for males and > 460 msec for females) on the screening ECG or other clinically significant ECG abnormalities
- •Maintenance therapy with any drug or significant history of drug dependency or alcohol abuse (> 3 units of alcohol per day, intake of excessive alcohol, acute or chronic)
- •Any clinically significant illness in the previous 28 days before Day 1 of this study
- •Use of any enzyme-modifying drugs, including strong inhibitors of cytochrome P450 (CYP) enzymes (such as cimetidine, fluoxetine, quinidine, erythromycin, ciprofloxacin, fluconazole, ketoconazole, diltiazem and HIV antivirals) and strong inducers of CYP enzymes (such as barbiturates, carbamazepine, glucocorticoids, phenytoin, rifampin and St John's Wort), in the previous 28 days before Day 1 of this study
- •Any history of tuberculosis and/or prophylaxis for tuberculosis
- •Serum ferritin value below the normal limit of the reference laboratory at screening
- •Positive urine screening of alcohol and/or drugs of abuse
- •Positive results on HIV Ag/Ab Combo, Hepatitis B surface Antigen (HBsAG (B) (hepatitis B)) or anti-Hepatitis C Virus (HCV (C)) tests
- •Positive result on a serum pregnancy test
- •Receipt of an investigational product in another clinical trial in the previous 28 days before Day 1 of this study
- •Donation of 50 mL or more of blood in the previous 28 days before Day 1 of this study or donation of 500 mL or more of blood (Canadian Blood Services, Hema-Quebec, clinical studies, etc.) in the previous 56 days before Day 1 of this study
研究组 & 干预措施
ER, fasting conditions
A single 1000 mg dose of deferiprone extended release tablet formulation administered under fasting conditions
干预措施: Deferiprone extended release (Drug)
ER, fed conditions
A single 1000 mg dose of deferiprone extended release tablet formulation administered under fed conditions
干预措施: Deferiprone extended release (Drug)
ER half-tablets, fed conditions
A single 1000 mg dose of deferiprone extended release tablet formulation (one 1000 mg tablet divided in two) administered under fed conditions
干预措施: Deferiprone extended release (Drug)
IR, fasting conditions
A single 1000 mg dose of deferiprone immediate release tablet formulation administered under fasting conditions
干预措施: Deferiprone immediate release (Drug)
IR, fed conditions
A single 1000 mg dose of deferiprone immediate release tablet formulation administered under fed conditions
干预措施: Deferiprone immediate release (Drug)
结局指标
主要结局
Cmax for Serum Deferiprone
时间窗: Samples were collected pre-dose and at 0.25, 0.5, 0.75, 1.0, 1.33, 1.66, 2.0, 2.5, 3.0, 3.5, 4.0, 4.5, 5.0, 6.0, 8.0, 12.0, 16.0, and 24.0 hours post-dose.
Maximum measured serum concentration. Blood samples will be collected pre-dose and over a 24-hour interval post-dose
Tmax for Serum Deferiprone
时间窗: Samples were collected pre-dose and at 0.25, 0.5, 0.75, 1.0, 1.33, 1.66, 2.0, 2.5, 3.0, 3.5, 4.0, 4.5, 5.0, 6.0, 8.0, 12.0, 16.0, and 24.0 hours post-dose.
Time of maximum observed serum concentration. Blood samples will be collected pre-dose and over a 24-hour interval post-dose
AUC0-∞for Serum Deferiprone
时间窗: Samples were collected pre-dose and at 0.25, 0.5, 0.75, 1.0, 1.33, 1.66, 2.0, 2.5, 3.0, 3.5, 4.0, 4.5, 5.0, 6.0, 8.0, 12.0, 16.0, and 24.0 hours post-dose.
Area under the serum concentration time curve extrapolated to infinity. Blood samples will be collected pre-dose and over a 24-hour interval post-dose.
次要结局
- Number of Subjects With Adverse Events (AEs)(Throughout the trial, from the time of the first dose until the last study visit (Day 36 or early termination))