| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ADME/Pharmacokinetics |
Absorption, Distribution and Excretion
Oral ibandronate is 0.63% bioavailable. In a study of healthy males, a 10mg oral dose had a Tmax of 1.1±0.6h and a Cmax of 4.1±2.6ng/mL. The Tmax is approximately 1 hour, while Cmax varies depending on dose. A 2mg intravenous dose of ibandronate has an AUC of 316ng\*h/mL, a 4mg intravenous dose of ibandronate has an AUC of 581ng\*h/mL, and a 6mg intravenous dose of ibandronate has an AUC of 908ng\*h/mL. Ibandronate is predominantly eliminated in the urine and the unabsorbed drug is eliminated unchanged in the feces. The apparent terminal volume of distribution of ibandronate is 90-368L in headlthy subjects and 103L in postmenopausal women with osteopenia. The total clearance of ibandronate is 84-160mL/min. Metabolism / Metabolites Ibanronate is not metabolized in humans. No evidence of ibandronate being metabolized in humans. Route of Elimination: Ibandronate is eliminated by renal excretion. Unabsorbed ibandronate is eliminated unchanged in the feces. Half Life: 10-60 hours Biological Half-Life The half life of ibandronate in postmenopausal women ranges from 37-157 hours. |
|---|---|
| Toxicity/Toxicokinetics |
Toxicity Summary
The action of ibandronate on bone tissue is based partly on its affinity for hydroxyapatite, which is part of the mineral matrix of bone. Nitrogen-containing bisphosphonates (such as pamidronate, alendronate, risedronate, ibandronate and zoledronate) appear to act as analogues of isoprenoid diphosphate lipids, thereby inhibiting farnesyl pyrophosphate (FPP) synthase, an enzyme in the mevalonate pathway. Inhibition of this enzyme in osteoclasts prevents the biosynthesis of isoprenoid lipids (FPP and GGPP) that are essential for the post-translational farnesylation and geranylgeranylation of small GTPase signalling proteins. This activity 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. Effects During Pregnancy and Lactation ◉ Summary of Use during Lactation Ibandronate is poorly absorbed orally (average in adults 6% on an empty stomach, negligible with food), so absorption of ibandronate by a breastfed infant is unlikely. However, since no information is available on the use of ibandronate during breastfeeding, an alternate drug may be preferred, especially while nursing a newborn or preterm infant. ◉ Effects in Breastfed Infants Relevant published information was not found as of the revision date. ◉ Effects on Lactation and Breastmilk Relevant published information was not found as of the revision date. Protein Binding Ibandronate's protein binding in serum varies from 85.7-99.5% over a concentration of 0.5-10ng/mL, but is generally 86% across a concentration range of 20-2000ng/mL. Toxicity Data LD50 = 811 mg/kg (rat, oral) |
| References |
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| Additional Infomation |
Pharmacodynamics
Ibandronate is a nitrogen containing bisphosphonate used to treat and prevent osteoporosis in postmenopausal women. The therapeutic index is wide as overdoses are not especially toxic, and the duration of action is long as the half life can be up to 157 hours. Patients should be counselled regarding the risk of upper GI adverse reactions, hypocalcemia, musculoskeletal pain, osteonecrosis of the jaw, atypical fractures of the femur, and severe renal impairment. |
| Molecular Formula |
C9H23NO7P2
|
|---|---|
| Molecular Weight |
319.22902
|
| Exact Mass |
319.094
|
| CAS # |
114084-78-5
|
| Related CAS # |
Ibandronate Sodium Monohydrate;138926-19-9;Ibandronic Acid-d3 sodium;1329834-28-7;Ibandronic acid-d3;1130899-41-0;Ibandronate Sodium;138844-81-2
|
| PubChem CID |
60852
|
| Appearance |
Typically exists as solid at room temperature
|
| Density |
1.5±0.1 g/cm3
|
| Boiling Point |
587.8±60.0 °C at 760 mmHg
|
| Melting Point |
113-115ºC
|
| Flash Point |
309.3±32.9 °C
|
| Vapour Pressure |
0.0±3.7 mmHg at 25°C
|
| Index of Refraction |
1.538
|
| LogP |
-0.65
|
| Hydrogen Bond Donor Count |
5
|
| Hydrogen Bond Acceptor Count |
8
|
| Rotatable Bond Count |
9
|
| Heavy Atom Count |
19
|
| Complexity |
342
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
OC(P(O)(O)=O)(P(O)(O)=O)CCN(C)CCCCC
|
| InChi Key |
MPBVHIBUJCELCL-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C9H23NO7P2/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)
|
| Chemical Name |
[1-hydroxy-3-[methyl(pentyl)amino]-1-phosphonopropyl]phosphonic acid
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
|
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.1325 mL | 15.6627 mL | 31.3254 mL | |
| 5 mM | 0.6265 mL | 3.1325 mL | 6.2651 mL | |
| 10 mM | 0.3133 mL | 1.5663 mL | 3.1325 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Efficacy of Oral Ibandronate in Osteoporosis
CTID: NCT03186131
Phase: Phase 2 Status: Recruiting
Date: 2021-09-21
Products are for research use only; We do not sell to patients
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