Ibandronate sodium monohydrate

Описание

Ibandronate Sodium Monohydrate is a highly potent nitrogen-containing bisphosphonate used for the treatment of osteoporosis.
Ibandronate Sodium Monohydrate inhibits bone resorption as a sodium salt and complexed with technetium Tc 99m for bone imaging. The monophosphonates are not active and the biphosphonates are used in disorders affecting the skeleton such as metastatic disease, asteoporosis and Paget's. Ibandronate Sodium Monohydrate is an inhibitor of FDPS.

Химические свойства

[1-Hydroxy-3-(methylpentylamino)-propylidene]bisphosphonic acid sodium salt is White Crystalline Powder

Использование

Inhibits bone resorption as a sodium salt and complexed with technetium Tc 99m for bone imaging. The monophosphonates are not active. Biphosphonates are used in disorders affecting the skeleton such as asteoporosis, metastatic disease, and Paget d

Механизм действия

The action of ibandronate on bone tissue is based on its affinity for hydroxyapatite, which is part of the mineral matrix of bone. Ibandronate inhibits osteoclast activity and reduces bone resorption and turnover. In postmenopausal women, it reduces the elevated rate of bone turnover, leading to, on average, a net gain in bone mass.

Фармакокине?тика

Absorption
The absorption of oral ibandronate occurs in the upper gastrointestinal tract. Plasma concentrations increase in a dose-linear manner up to 50 mg oral intake and increases nonlinearly above this dose.
Following oral dosing, the time to maximum observed plasma ibandronate concentrations ranged from 0.5 to 2 hours (median 1 hour) in fasted healthy postmenopausal women. The mean oral bioavailability of 2.5 mg ibandronate was about 0.6% compared to intravenous dosing. The extent of absorption is impaired by food or beverages (other than plain water). The oral bioavailability of ibandronate is reduced by about 90% when BONIVA is administered concomitantly with a standard breakfast in comparison with bioavailability observed in fasted subjects. There is no meaningful reduction in bioavailability when ibandronate is taken at least 60 minutes before a meal. However, both bioavailability and the effect on bone mineral density (BMD) are reduced when food or beverages are taken less than 60 minutes following an ibandronate dose.
Distribution
After absorption, ibandronate either rapidly binds to bone or is excreted into urine. In humans, the apparent terminal volume of distribution is at least 90 L, and the amount of dose removed from the circulation via the bone is estimated to be 40% to 50% of the circulating dose. In vitro protein binding in human serum was 99.5% to 90.9% over an ibandronate concentration range of 2 to 10 ng/mL in one study and approximately 85.7% over a concentration range of 0.5 to 10 ng/mL in another study.
Metabolism
There is no evidence that ibandronate is metabolized in humans.
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