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A single intravenous drip of voriconazole for injection developed by Qilu Pharmaceutical (Hainan) Co., Ltd. and the original product "vfend" was given to healthy subjects , The pharmacokinetic differences and tolerance of the two preparations were evaluated at the doses of 4mg / kg and 6mg / kg.
Low dose group: 24 healthy adult subjects are planned to be enrolled. Intravenous drip Voriconazole (T) for injection or reference preparation vfend ® (R) in fasting state per cycle. The dosage was 4 mg / kg for 80 min;After a 7-day cleaning period, the second cycle of cross administration.
High dose group: 24 healthy adult subjects are planned to be enrolled. Intravenous drip Voriconazole (T) for injection or reference preparation vfend ® (R) in fasting state per cycle. The dosage was 6 mg / kg for 120 min;After a 7-day cleaning period, the second cycle of cross administration.
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| Label | Type | Description | Intervention Names |
|---|---|---|---|
| Voriconazole (R) | Active Comparator |
| |
| Voriconazole (T) | Experimental |
|
| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| 4 mg/kg Voriconazole | Drug | Low dose group: 24 healthy adult subjects are planned to be enrolled. Intravenous drip Voriconazole for injection in fasting state per cycle. The dosage was 4 mg / kg for 80 min. |
| Measure | Description | Time Frame |
|---|---|---|
| AUC0-t | 17 tubes (3ml / tube) of venous blood were collected in the low dose group. 3ml of venous blood was collected from the contralateral upper arm at 0:00 (within 1 hour before administration) and 0.50h, 1.0h, 1.33h (80min, at the end of administration), 1.42h (85min), 1.5h, 1.75h, 2.0h, 2.5h, 3.0h, 4.0h, 6.0h, 8.0h, 12.0h, 24.0h, 36.0h and 48.0h after administration. 18 tubes (3ml / tube) of venous blood were collected in the high-dose group. 3ml of venous blood was collected from the contralateral upper arm at 0:00 (within 1 hour before administration) and 0.50h, 1.0h, 1.5h, 1.75h, 2.0h (at the end of administration), 2.08h (125min), 2.17h (130min), 2.33h (140min), 2.5h, 3.0h, 4.0h, 6.0h, 8.0h, 12.0h, 24.0h, 36.0h and 48.0h after administration. The plasma concentration of voriconazole was determined by LC-MS / MS. Winnonlin ® 6.4 calculate the pharmacokinetic parameters. | ± 1 minute within 4 hours. ± 3 minutes for 4-12 hours. ± 5 minutes for more than 12 hours. |
| AUC0-∞ | 17 tubes (3ml / tube) of venous blood were collected in the low dose group. 3ml of venous blood was collected from the contralateral upper arm at 0:00 (within 1 hour before administration) and 0.50h, 1.0h, 1.33h (80min, at the end of administration), 1.42h (85min), 1.5h, 1.75h, 2.0h, 2.5h, 3.0h, 4.0h, 6.0h, 8.0h, 12.0h, 24.0h, 36.0h and 48.0h after administration. 18 tubes (3ml / tube) of venous blood were collected in the high-dose group. 3ml of venous blood was collected from the contralateral upper arm at 0:00 (within 1 hour before administration) and 0.50h, 1.0h, 1.5h, 1.75h, 2.0h (at the end of administration), 2.08h (125min), 2.17h (130min), 2.33h (140min), 2.5h, 3.0h, 4.0h, 6.0h, 8.0h, 12.0h, 24.0h, 36.0h and 48.0h after administration. The plasma concentration of voriconazole was determined by LC-MS / MS. Winnonlin ® 6.4 calculate the pharmacokinetic parameters. | ± 1 minute within 4 hours. ± 3 minutes for 4-12 hours. ± 5 minutes for more than 12 hours. |
| Cmax | 17 tubes (3ml / tube) of venous blood were collected in the low dose group. 3ml of venous blood was collected from the contralateral upper arm at 0:00 (within 1 hour before administration) and 0.50h, 1.0h, 1.33h (80min, at the end of administration), 1.42h (85min), 1.5h, 1.75h, 2.0h, 2.5h, 3.0h, 4.0h, 6.0h, 8.0h, 12.0h, 24.0h, 36.0h and 48.0h after administration. 18 tubes (3ml / tube) of venous blood were collected in the high-dose group. 3ml of venous blood was collected from the contralateral upper arm at 0:00 (within 1 hour before administration) and 0.50h, 1.0h, 1.5h, 1.75h, 2.0h (at the end of administration), 2.08h (125min), 2.17h (130min), 2.33h (140min), 2.5h, 3.0h, 4.0h, 6.0h, 8.0h, 12.0h, 24.0h, 36.0h and 48.0h after administration. The plasma concentration of voriconazole was determined by LC-MS / MS. Winnonlin ® 6.4 calculate the pharmacokinetic parameters. |
| Measure | Description | Time Frame |
|---|---|---|
| Adverse event | All adverse events (clinical symptoms, signs or diseases) occurring during the test (including cleaning period) shall be recorded in the source file. The signs and symptoms, occurrence date and time, duration, end date and time, measures taken and follow-up of adverse events shall also be recorded. | Up to two years. |
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Inclusion Criteria:
Exclusion Criteria:
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| Name | Affiliation | Role |
|---|---|---|
| Yu Cao, Doctor | National Medical Products Administration | Principal Investigator |
| Facility | Status | City | State | ZIP | Country | Contacts |
|---|---|---|---|---|---|---|
| Phase I Clinical Research Center | Qingdao | Shanndong | 266003 | China |
| PubMed Identifier | Type | Citation | Retractions |
|---|---|---|---|
| 36869387 | Derived | Li X, Wang C, Shi P, Liu Y, Tao Y, Lin P, Li T, Hu H, Sun F, Liu S, Fu Y, Cao Y. Pharmacokinetics and safety of two Voriconazole formulations after intravenous infusion in two doses in healthy Chinese subjects. BMC Pharmacol Toxicol. 2023 Mar 3;24(1):14. doi: 10.1186/s40360-023-00652-3. |
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| ID | Term |
|---|---|
| D065819 | Voriconazole |
| ID | Term |
|---|---|
| D014230 | Triazoles |
| D001393 | Azoles |
| D006573 | Heterocyclic Compounds, 1-Ring |
| D006571 | Heterocyclic Compounds |
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A total of 48 healthy adult subjects were enrolled; Intravenous drip Voriconazole (T) for injection or reference preparation vfend ® (R)in fasting state per cycle; After a 7-day cleaning period, the second cycle of cross administration.
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| 6 mg/kg Voriconazole | Drug | High dose group: 24 healthy adult subjects are planned to be enrolled. Intravenous drip Voriconazole for injection in fasting state per cycle. The dosage was 6 mg / kg for 120 min. |
|
| ± 1 minute within 4 hours. ± 3 minutes for 4-12 hours. ± 5 minutes for more than 12 hours. |
| Tmax | 17 tubes (3ml / tube) of venous blood were collected in the low dose group. 3ml of venous blood was collected from the contralateral upper arm at 0:00 (within 1 hour before administration) and 0.50h, 1.0h, 1.33h (80min, at the end of administration), 1.42h (85min), 1.5h, 1.75h, 2.0h, 2.5h, 3.0h, 4.0h, 6.0h, 8.0h, 12.0h, 24.0h, 36.0h and 48.0h after administration. 18 tubes (3ml / tube) of venous blood were collected in the high-dose group. 3ml of venous blood was collected from the contralateral upper arm at 0:00 (within 1 hour before administration) and 0.50h, 1.0h, 1.5h, 1.75h, 2.0h (at the end of administration), 2.08h (125min), 2.17h (130min), 2.33h (140min), 2.5h, 3.0h, 4.0h, 6.0h, 8.0h, 12.0h, 24.0h, 36.0h and 48.0h after administration. The plasma concentration of voriconazole was determined by LC-MS / MS. Winnonlin ® 6.4 calculate the pharmacokinetic parameters. | ± 1 minute within 4 hours. ± 3 minutes for 4-12 hours. ± 5 minutes for more than 12 hours. |
| female pregnancy test |
Urine pregnancy examination was performed during the screening period. Blood pregnancy tests were performed at the end of the study or early termination of the trial. |
| Day 16 after administration. |