138926-19-9 Usage
Description
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.
Chemical Properties
[1-Hydroxy-3-(methylpentylamino)-propylidene]bisphosphonic acid sodium salt is White Crystalline Powder
Uses
Different sources of media describe the Uses of 138926-19-9 differently. You can refer to the following data:
1. 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
2. bone resorption inhibitor, anthypercalcemic
3. An inhibitor of bone resorption
Mechanism of action
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.
Pharmacokinetics
AbsorptionThe 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.DistributionAfter 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.MetabolismThere is no evidence that ibandronate is metabolized in humans.https://www.accessdata.fda.gov
References
1) Russell (2006), Ibandronate: Pharmacology and preclinical studies; Bone 38 S7
Check Digit Verification of cas no
The CAS Registry Mumber 138926-19-9 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 1,3,8,9,2 and 6 respectively; the second part has 2 digits, 1 and 9 respectively.
Calculate Digit Verification of CAS Registry Number 138926-19:
(8*1)+(7*3)+(6*8)+(5*9)+(4*2)+(3*6)+(2*1)+(1*9)=159
159 % 10 = 9
So 138926-19-9 is a valid CAS Registry Number.
InChI:InChI=1/C9H23NO7P2.Na.H2O/c1-3-4-5-7-10(2)8-6-9(11,18(12,13)14)19(15,16)17;;/h11H,3-8H2,1-2H3,(H2,12,13,14)(H2,15,16,17);;1H2/q;+1;/p-1
138926-19-9Relevant articles and documents
Preparation method of sodium ibandronate
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Paragraph 0019; 0020; 0023; 0024; 0025; 0028; 0029; 0033, (2017/07/04)
Relating to the technical field of pharmaceutical synthesis, the invention provides a preparation method of sodium ibandronate. The preparation method includes: taking 3-methylamino propanenitrile as the raw material to prepare 3-(N-methyl-N-n-amylamine)propionic acid hydrochloride, then reacting the 3-(N-methyl-N-n-amylamine)propionic acid hydrochloride with phosphorous acid and phosphorus trichloride to obtain ibandronic acid, and subjecting the ibandronic acid and sodium hydroxide to salification so as to obtain sodium ibandronate. The preparation method of sodium ibandronate provided by the invention reduces the refining frequency, lowers the refining loss, avoids the defects of low yield and long period brought about by a lot of refining steps, and the great harm to human and environment, and has the advantages of simple operation, good process repeatability and easy industrial production.
PROCESS FOR THE PREPARATION OF 3-(N-METHYL-N-PENTYL)AMINO-1-HYDROXYPROPANE-1,1-DIPHOSPHONIC ACID SALT OR DERIVATIVES THEREOF
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Page/Page column 7-8, (2012/02/02)
The present invention relates to an improved process for the preparation of 3-(N-methyl-N- pentyl)amino-1-hydroxypropane-1,1-diphosphonic acid, monosodium salt, or its derivatives, in substantially pure crystalline form.
PROCESS FOR MAKING 1-HYDROXYALKYLIDENE-1,1-BIPHOSPHONIC ACIDS
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Page/Page column 11, (2011/04/14)
Synthesis of biphosphonate compounds can be carried out using a combination of a halophosphorous compound and water as the phosphonation agent.
