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SODIUM RISEDRONATE

Sodium risedronate

CAS: 115436-72-1

Molecular Formula: C7H12NNaO7P2

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SODIUM RISEDRONATE - Names and Identifiers

Name Sodium risedronate
Synonyms RISEDRONATE NA
Risedronate sodium
SODIUM RISEDRONATE
RISEDRONATE SODIUM
RISEDREMATE SODIUM
Sodium risedronate
RISEDRONIC ACID, SODIUM SALT
(1-hydroxy-2-(3-pyridinyl)ethylidene)bis-phosphonicacimonosodiumsalt
sodium hydrogen [1-hydroxy-1-phosphono-2-(pyridin-3-yl)ethyl]phosphonate
[1-hydroxy-2-(3-pyridinyl)ethylidene]-bis[phosphonic acid] monosodium salt
phosphonic acid, [1-hydroxy-2-(3-pyridinyl)ethylidene]bis-, monosodium salt
CAS 115436-72-1
EINECS 1806241-263-5
InChI InChI=1/C7H11NO7P2.Na/c9-7(16(10,11)12,17(13,14)15)4-6-2-1-3-8-5-6;/h1-3,5,9H,4H2,(H2,10,11,12)(H2,13,14,15)

SODIUM RISEDRONATE - Physico-chemical Properties

Molecular FormulaC7H12NNaO7P2
Molar Mass307.11
Melting Point252-262°C
Boling Point692.3°C at 760 mmHg
Flash Point372.5°C
Solubility DMSO <1 mg/mL Water 2 mg/mL Ethanol <1 mg/mL
Vapor Presure4.03E-20mmHg at 25°C
AppearanceFine white to off-white crystalline powder
Colorwhite to beige
Storage Conditionroom temp
MDLMFCD01706268
UseIs a total synthesis of anti-osteoporosis drugs

SODIUM RISEDRONATE - Risk and Safety

Risk CodesR62 - Possible risk of impaired fertility
R64 - May cause harm to breast-fed babies
Safety DescriptionS20 - When using, do not eat or drink.
S22 - Do not breathe dust.
S36/37 - Wear suitable protective clothing and gloves.
WGK Germany3
RTECSSZ8567500
HS Code29333990

SODIUM RISEDRONATE - Reference Information

bone resorption inhibitor bisphosphonate (bisphosphonates) is a leading osteoporosis (OP) drug developed in the past 30 years and is currently the most important anti-bone resorption inhibitor. Its structure is similar to the endogenous bone metabolism regulator pyrophosphate. It replaces the P-O-P bond in pyrophosphate that is easily hydrolyzed or deactivated by pyrophosphatase in an acidic environment with a P-C-P structure, and its properties are stable in vivo. Diphosphonate is easily deposited in bone tissue, combined with calcium phosphonate in it, and then inhibits the dissolution, absorption, formation and growth of hydroxyapatite crystals and their amorphous precursors, and inhibits its absorption than inhibits its formation And the dose required for growth is lower, that is, at a low dose, it is enough to play the role of anti-bone resorption. According to the chemical structure, bisphosphonate drugs are divided into three generations. The representative drug of the first-generation bisphosphonates is etidronate; the second-generation bisphosphonates introduce nitrogen atoms in their side chains, and the representative drugs include clodronate and pamidronate; The third generation has a cyclic side chain, and the representative drugs are alendronate and risedronate. Risedronate sodium, as the third-generation bisphosphonate drug for anti-osteoporosis, was first developed by Procter & Gamble (Procter & Gamble, P & G) and Hoechst Marion Roussrl. It is a pyridine diphosphonate. Bone absorption inhibitor, chemical name: 1-hydroxy-2-(3-pyridyl) ethylene-diphosphonic acid monosodium salt. It was first marketed in the United States in 1998 and is clinically used to treat osteitis deforming. Risedronate sodium tablets were approved in Sweden in October 1999 and approved by FDA in 2004 for the prevention and treatment of osteoporosis in postmenopausal women.
pharmacokinetics absorption: oral absorption is relatively fast (Tmax ~ 1 hour), the absorption process occurs in the whole digestive tract, the absorbed dose has nothing to do with the dose (from single dose 2.5~30mg, multiple doses 2.5~5mg), the drug is administered every day to reach steady state in 57 days, the average absolute bioavailability of oral 30mg tablets is 0.63%(90% Cl:0.54% ~ 0.75%). Taking risedronate sodium 0.5 hours before breakfast or 2 hours after dinner has the same absorption effect; risedronate sodium must be effective at least 30 minutes before breakfast. Distribution: The average steady-state distribution volume of human is 6.3L Kg-1, and the binding rate of human plasma protein is 24%. Preclinical studies in mice have shown that 14C-labeled risedronate sodium is administered in a single dose, the 60% is distributed to the bone, and the rest of the drug is excreted from the urine. Elimination: Nearly half of the absorbed dose is excreted in the urine within 24 hours, administered intravenously, and returned to normal in the urine on 28 days. The average renal clearance rate was 105ml · min-1(RSD = 34%) and the average total clearance rate was 122 ml · min-1(RSD = 19%). The renal clearance rate was not concentration-dependent, and there was a linear relationship between renal clearance and creatinine clearance rate. The unabsorbed drug is excreted from feces as a prototype. Once absorbed, the serum concentration-time graph is multiphase, with a half-life of 1.5 hours at the beginning. The terminal half-life is 480 hours, and the terminal half-life is believed to be the separation of risedronate sodium from the bone surface.
Synthetic route Using nicotinic acid as raw material, risedronate sodium is obtained through esterification, Claisen condensation, Willgerodt-Kindler reaction, hydrolysis, acidification, etc. Fig. 1 shows the synthetic route of risedronate sodium
indications for the treatment and prevention of osteoporosis in postmenopausal women; glucocorticoid-induced osteoporosis; osteitis deforming. (2016-03-18)
contraindications hypocalcemia; Patients who are highly allergic to any component of this product; Patients who cannot maintain upright position for more than 30 minutes after administration.
precautions risedronate sodium is easy to cause digestive tract dysfunction, such as dysphagia, digestive tract ulcer, etc. You must take the medicine 30 minutes before breakfast, take the medicine with a large amount of water, and do not lie down within 30 minutes after administration. If the food lacks calcium and vitamin D, calcium and vitamin D must be supplemented at the same time. Calcium, aluminum, magnesium and food can interfere with the absorption of risedronate sodium, so it must be administered at different times of the day. Use with caution in patients with severe renal insufficiency. When combined with glucocorticoid administration, the hormone level in the patient must be determined and appropriate replacement methods must be considered.
use treatment of osteoporosis
is a fully synthetic anti-osteoporosis drug
anti-osteoporosis
Last Update:2024-04-09 21:32:03
SODIUM RISEDRONATE
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Email: sales@tnjchem.com
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Mobile: 0086 189 4982 3763
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SODIUM RISEDRONATE
Ertapenem Side-Chain
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