None listed
Conditions
Interventions
Intervention1: Ursodiol injection 625 mg/25 mL (25 mg/mL): In cohort I, six subjects will receive Ursodiol injection 625mg/25ml (25mg/ml)
Dose: 600 mg. In cohort II, six subjects will receive Ursodiol
dose 900 mg orally.
Sponsors
Shilpa Medicare Limited
Eligibility
Inclusion criteria
Inclusion criteria: 1. Healthy human subjects between 18-45 years of age (including both) and weight = 50 Kg (BMI 18.00- 25.00 kg/m²). 2. Acceptable findings during registration and screening including, detailed medical history, full physical examination, medical examination, laboratory evaluations, 12- lead ECG and Chest X-Ray (postero-anterior view). 3. Values within Normal Ranges of Laboratory Parameters upon evaluation by the Investigator or Physician. 4. Subjects able to communicate effectively. 5. Subjects willing to give written informed consent and adhere to all the requirements of this protocol. 6. Subject willing to abstain from all kinds of alcoholic beverages, smoking, and caffeine/xanthine containing foods or beverages from 96.00 hours before admission till the last blood sample in study period. 7. Male Subjects: Subjects willing to follow approved birth control methods (a double barrier method) for the duration of the study as judged by the investigator(s), such as (a double barrier method) Condom with spermicide, Condom with diaphragm, or abstinence, Subjects should also not donate sperm during this time. 8. Female subjects: Postmenopausal for at least 1 year or Surgically sterile (bilateral tubal ligation, bilateral oophorectomy or hysterectomy has been performed on the subject)
Exclusion criteria
Exclusion criteria: 1. Volunteers having history of contraindication or hypersensitivity (e.g., anaphylaxis) to ursodeoxycholic acid or other related drugs, or related group of drugs. 2. A history or presence of significant asthma, urticaria, or other allergic-type reactions after taking aspirin or other NSAIDs. Severe, rarely fatal, anaphylacticlike reactions to NSAIDs, seizures, diabetes, migraine, hypertension, cardiovascular, pulmonary, neurological or psychiatric disease/disorder, dermatological, endocrine, eye disorders, immunological, renal, hematopoietic, gastrointestinal, ongoing infectious diseases, or any other significant abnormality as evidenced by medical history and physical examination or according to the opinion of the physician. 3. History or presence of gastrointestinal (GI) inflammation, bleeding, ulceration, and perforation of the stomach, small intestine, or large intestine. 4. History or presence of hepatic, thyroid, or renal dysfunction. 5. History or presence of bronchial asthma. 6. History or evidence of exfoliative dermatitis, Stevens - Johnson syndrome (SJS), and toxic epidermal necrolysis (TEN). 7. Any known enzyme inducing or inhibiting drug taken within 30 days before the study. 8. A depot injection or implant of any drug within 3 months prior to the dose of study medication. 9. Use of CYP enzyme inhibitors or inducers within 30 days prior to the dose of study medication 10. Participation in a drug research study within 90 days prior to dosing of this study. 11. Blood loss or whole blood donation within 90 days prior to drug administration. 12. Current use or anticipated need for drugs with known or suspected interactions with ursodeoxycholic acid. 13. Subjects with hypertension or cardiovascular risk factors. 14. Consumption of high caffeine (more than 5 cups of coffee or tea/day). 15. Smokers who smoke 10 or more cigarettes per day or 20 or more biddies per day or those who cannot refrain from smoking during the study period. 16. History of addiction to any recreational drug or drug dependence. 17. An unusual or abnormal diet, for whatever reason within 96.00 hours prior to admission of study period, e.g. fasting due to religious reasons. 18. History of dehydration from diarrhea, vomiting or any other reason within a period of 96.00 hours prior to study admission of study period. 19. Positive results for drugs of abuse (benzodiazepines, cocaine, opioids, amphetamines, cannabinoids and barbiturates) in urine during the study admission of study period. 20. Positive results for alcohol consumption tests during the study admission. 21. History of pre-existing bleeding disorder. 22. Difficulty with donating blood. 23. Systolic blood pressure less than 100 mm Hg or more than 140 mm Hg. 24. Diastolic blood pressure less than 60 mm Hg or more than 90 mm Hg. 25. Pulse rate less than 60 beats/minute or more than 100 beats/minute. 26. Use of any prescribed medication or OTC medicinal products and herbal medicines during last two weeks preceding the first dosing. 27. Female volunteer who is pregnant, currently breast-feeding. 28. Female subjects demonstrating a positive pregnancy test. 29. Female vo
Design outcomes
Primary
| Measure | Time frame |
|---|---|
| 1. To evaluate safety and tolerability of single ascending doses of Ursodiol injection 625mg/25ml (25mg/ml) (600 mg, 900 mg, 1800 mg & 3500 mg) as intravenous infusion over one hour in healthy adult human subjects. 2. To determine the maximum tolerated dose (MTD)Timepoint: Tolerability of Test product dose will be assessed after each cohort (15 days) | — |
Secondary
| Measure | Time frame |
|---|---|
| To determine single dose pharmacokinetics of Ursodiol injection 625mg/25ml (25mg/ml) as IV infusion. To assess the dose proportionality of ascending doses of Ursodiol injection 625 mg/25 ml (25mg/ml) as IV infusion up to 3500 mg. To compare the pharmacokinetics of ursodeoxycholic acid administered as IV infusion with orally administered Ursodiol CapsulesTimepoint: Blood samples (6.0 mL each) will be collected at -48.00, -42.00, - 36.00, -30.00, -24.00, -18.00, -12.00, -06.00, pre-dose (00.00) hours prior to dosing and at 0.25 (15 minutes after start of infusion), 00.50 (30 minute after start of infusion), 00.75, 00.91 (5 minutes prior to end of infusion), 01.00, 01.17, 01.50, 0l .75, 02.00, 02.50, 03.00, 04.00, 05.00, 06.00, 08.00, 10.00, 12.00, 16.00, 20.00, 24.00, 36.00, 48.00, 96.00, 144.00,216.00,288.00 and 360.00 hours post dose. | — |
Countries
India
Contacts
Public ContactP Veerendra Kumar
Jeevan Scientific Technology Ltd.
Outcome results
None listed