None listed
Conditions
Interventions
Ia0 Group (The positive control group in subcutaneous injection):Subcutaneous injection: 4mL of Levobupivacaine hydrochloride injection at concentration of 0.325% and 0.5%
Ia Group (The placebo group in subcutaneous injection):Subcutaneous injection: 4mL of 0.9% sodium chloride injection
Ia-1 Group :Subcutaneous injection: 4mL of 0.13%/0.033% levobupivacaine and 2-hydroxyethyl lidocaine aminium bromide injection (LL10)
Ia-2 Group:Subcutaneous injection: 4mL of 0.25%/0.065% LL10
Ia-3 Group:Subcutaneous injection: 4mL of 0.44%/0.113% LL10
Ia-4 Group:Subcutaneous injection: 4mL of 0.63%/0.163% LL10
Ia-5 Group:Subcutaneous injection: 4mL of 0.88%/0.227% LL10
Ia-6 Group:Subcutaneous injection: 4mL of 1.07%/0.276% LL10
Ia-7 Group:Subcutaneous injection: 4mL of 1.26%/0.325% LL10
Ib Group (The placebo group in subcutaneous injection) (not conducted):Subcutaneous injection: 0.9% sodium chloride injection (10, 15, 20, 25, 30, 35mL, one participant for each volume )
Ib-1 Group (not conducted):Subcutaneous injection: 10mL of C% LL-10 (C, the concentration of LL10 in the Ib study, was chosen according to the findings of the Ia study)
Ib-2 Group (not conducted):Subcutaneous injection: 15mL of C% LL10
Ib-3 Group (not conducted):Subcutaneous injection: 20mL of C% LL10
Ib-4 Group (not conducted):Subcutaneous injection: 25mL of C% LL10
Ib-5 Group (not conducted):Subcutaneous injection: 30mL of C% LL10
Ib-6 Goup (not conducted):Subcutaneous injection: 35mL of C% LL10
Ic0 Group (The positive control group in femoral nerve block):Femoral nerve block:20mL of 0.325% Levobupivacaine hydrochloride injection
Ic Group (The placebo group in femoral nerve block):Femoral nerve block: 20mL of 0.9% sodium chloride injection
Ic-1 Group:Femoral nerve block: 20mL of 0.13%/0.033% LL10
Ic-2 Group:Femoral
Sponsors
West China Hospital, Sichuan University
Eligibility
Sex/Gender
All
Age
18 Years to 55 Years
Inclusion criteria
Inclusion criteria: 1. Healthy subjects aged 18-55 years with full capacity for civil conduct, no gender limit; 2. Body weight >=50.0kg and body mass index between 19.0 and 26.0kg/m^2 [Body mass index (BMI) = weight (kg)/height ^2 (m^2)], including the critical value; 3. Subjects with normal vital signs: systolic blood pressure >=90 and =60 and =50 and =95% during air inhalation; Respiratory rate >=10 and <=25 times/min; Body temperature <=37.3?; 4. Laboratory tests (blood routine, blood biochemistry, coagulation function, urine routine), 12-lead electrocardiogram, positive and lateral chest radiograph were normal or abnormal but had no clinical significance, in which ALT or AST <=1.2xULN, creatinine <=1.2xULN; 5. Able to fully understand the procedures and methods of the study, willing to strictly follow the clinical trial protocol to complete the study, and sign the informed consent.
Exclusion criteria
Exclusion criteria: 1. People with a history of severe allergy to narcotic drugs, allergic constitution, or known history of allergy to any component of this product and its excipients; 2. There are important viscera of primary diseases such as heart, liver, kidney or blood metabolism, such as history, has a history of head trauma, disease or surgery, a history of mental nerve disease, a history of epilepsy, has a history of anesthesia accident of clinical significance, has the family history of genetic diseases such as malignant hyperthermia, has a history of peripheral nerve disease, a history of mental derangement pain, history of glucose-6-phosphate dehydrogenase deficiency, porphyria; 3. Severe infection, trauma or major surgery within 4 weeks prior to screening; Or acute illness of clinical significance (as determined by the investigator), such as gastrointestinal disease, infection (respiratory or central nervous system infection, etc.), occurring within 2 weeks prior to screening; 4. Those who have a history of drug abuse or have tested positive for drug abuse; 5. Skin damage, scar, infection, abnormal color or pigmentation at the intended administration site; Sensory and motor abnormalities at the intended administration site (or innervation area); 6. Smokers who smoked more than 5 cigarettes a day in the 3 months before screening; 7. Positive breath test for alcohol or alcohol abuse in the last 3 months (drinking more than 14 units of alcohol per week: 1 unit = about 285mL for beer, or about 25mL for spirits, or about 100mL for wine); 8. People have participated in clinical trials of any drug or medical device within 3 months prior to screening, or have participated in clinical trials of any drug for 3 or more times in the past year; 9. People who consumed excessive amounts of tea, coffee or caffeinated beverages in the preceding 3 months (more than 8 cups per day, 1 cup =250mL), or consumed any food or beverage containing caffeine (such as coffee, strong tea, chocolate, cola, etc.) in the 48h prior to the first dosed study; 10. Use of prescription or over-the-counter drugs (vitamins, dietary supplements, traditional Chinese medicines, etc.) within 2 weeks or less than 5 half-lives (whichever is older) prior to screening; 11. There is no guarantee that strenuous physical activity will be avoided on the day of administration and for the following 2 days; 12. Hepatitis B surface antigen (HBsAg), hepatitis C antibody (HCV antibody), treponema pallidum antibody or HIV antibody positive for any index screening; 13. People who are expected to be prone to surgery or hospitalization during the trial; 14. People whose total blood loss exceeds 200mL in the 3 months before screening due to blood donation or other reasons (except blood loss during menstrual period for women); 15. Pregnant or lactating people; Male people (or their partners) or female peoples who had a pregnancy plan, sperm donation plan or egg donation plan during the 2 weeks prior to screening and 3 months after the end of the trial, and who did not wish to use a medically approved non-drug contraceptive method (e.g., condoms, complete abstinence, contraceptive rings, etc.) during the trial; 16. People with any other factors deemed unsuitable for participation in this study by the investigator.
Design outcomes
Primary
| Measure | Time frame |
|---|---|
| Safety and tolerability indicators––Adverse event(The incidence and severity of AE and SAE);Safety and tolerability indicators –– Vital signs;Safety and tolerability indicators –– 12-lead electrocardiogram;Safety and tolerability indicators –– Laboratory tests (including complete blood count, blood biochemistry, coagulation function, and urine routine);Safety and tolerability indicators –– Physical examination; | — |
Secondary
| Measure | Time frame |
|---|---|
| Plasma drug concentration of hydroxyethyl bromide (QX-OH) and levobupivacaine (Levo-BUP) (PK parameters, including Cmax, AUC0-t, AUC0-8, Tmax, t1/2z, Vz, CLz, and MRT0-8, were calculated using a non-compartmental analysis method);Mass balance (The content of QX-OH, Levo-BUP, and metabolites in feces and urine);Clinical effects ( including mechanical pain threshold,pinprick test,transcutaneous electrical nerve stimulation,and assessment of lower limb muscle strength); | — |
Countries
China
Contacts
Public ContactZhang Wensheng
West China Hospital, Sichuan University
Outcome results
None listed