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Strontium ranelate

Strontium ranelate 구조식 이미지
카스 번호:
135459-87-9
상품명:
Strontium ranelate
동의어(영문):
Protos;S 12911;Protelos;S 12911-2;TrontiuMranelate;StrontiuM Ranelic;Srtontiumranelate;STRONTIUM RANELATE;Ranelate StrontiuM;StronitiuM ranelate
CBNumber:
CB1838150
분자식:
C12H6N2O8SSr2
포뮬러 무게:
513.491
MOL 파일:
135459-87-9.mol

Strontium ranelate 속성

녹는점
>310°C (dec.)
저장 조건
-20°C Freezer
용해도
H2O: soluble1mg/mL, clear (warmed)
물리적 상태
powder
색상
white to beige
CAS 데이터베이스
135459-87-9

안전

위험품 표기 Xn
위험 카페고리 넘버 20/21/22
안전지침서 36/37
유엔번호(UN No.) 3077
WGK 독일 3
RTECS 번호 XM7581000
HS 번호 29349990

Strontium ranelate C화학적 특성, 용도, 생산

개요

Strontium ranelate, a divalent strontium salt of ranelic acid, has been developed and launched for the treatment of osteoporosis. As early as 1910, investigations suggested that strontium stimulates the formation of osteoid tissues while simultaneously repressing the resorptive process in bones. Specifically, strontium enhances pre-osteoblastic cell replication, inhibits pre-osteoclast differentiation, and suppresses the bone-resorbng activity of osteoclasts. From the evaluation of 26 strontium salts, ranelic acid was selected as the ideal strontium carrier due to its physicochemical and pharmacokinetic properties. The thiophene core of ranelic acid is constructed by the condensation of dialkyl 3-oxoglutarate, malononitrile, and sulfur in a suitable alcohol in the presence of morpholine or diethylamine. The resultant diester of 5-amino-3-carboxymethyl-4-cyano-2-thiophenecarboxylic acid is subsequently dialkylated with an alkyl bromoacetate to provide the tetraester precursor to strontium ranelate. Strontium ranelate is supplied in a 2 g sachet, and the drug is evenly suspended in water prior to consumption. Since the simultaneous ingestion of either calcium or food has a negative influence on the bioavailability of strontium ranelate, it is recommended that strontium ranelate be administered once a day at bedtime. Following this regimen, the absolute bioavailability of strontium is 27% while that of ranelic acid is 2.5%. Because strontium ranelate dissociates after intake, and ranelic acid has negligible absorption, the effects of the drug on bone metabolism are dependent on the pharmacokinetics of strontium. In postmenopausal women, the half-life of strontium is 6.3±2.3 days, and renal clearance accounts for 57%of the total clearance of 12mL/min. After a 25-day treatment, the maximum plasma concentration of strontium is 20±2.3 mg/L. In addition, not only is perfect stability of strontium plasma concentration achieved within 3 to 24 months of chronic administration so is stabilization of strontium incorporation into bones. Strontium is incorporated into bone by two mechanisms. The predominant mode involves the rapid, saturable surface exchange with calcium. A slower mechanism embodies the incorporation of strontium into the crystal lattice of the bone mineral; however, only a small amount of calcium in the apatite is substituted by strontium at pharmacological doses. A phase II clinical trial assessed the effect of various strontium ranelate doses in postmenopausal women with established osteoporosis. The primary efficacy endpoint for this double-blind, randomized, placebo- controlled trial was the measure of mean lumbar bone mineral density (BMD) by dual-energy X-ray absorptiometry. A statistically significant dose-dependent increase in lumbar BMD was observed; increases of 1.3, 5.9, 8.3, and 13.6% were recorded for placebo, 500-, 1000-, and 2000-mg doses of strontium ranelate, respectively. In a phase III trial encompassing 1,649 osteoporotic postmenopausal women from 12 countries, the efficacy of a 2 g/day dose in preventing new vertebral fractures was evaluated. The mean lumbar BMD was 0.73 g/cm2 while the mean age at baseline was 70 years. All of the enrolled patients had at least one prior vertebral fracture. The primary end point for this study was a reduction in the incidence of patients experiencing fractures. While 222 women in the placebo group experienced a new vertebral fracture, only 139 patients treated with strontium ranelate presented with new fractures. Furthermore, the risk of fracture was reduced by 51% in the third year alone, implicating the sustained efficacy of the drug. For both the phase II and phase III studies, strontium ranelate was well tolerated with most of the adverse events being mild-to-moderate in severity. The most commonly reported events in all treatment groups were musculoskeletal disorders (back pain, arthralgia, and lumbar pain). As for laboratory measurements, only creatine phosphokinase, the musculoskeletal isoenzyme, was significantly elevated in the 1000-mg and 2000-mg strontium ranelate groups; however, this did not translate into any particular clinical or biological abnormality. Without relevant data regarding bone safety in patients with renal impairment, strontium ranelate is currently contraindicated in patients with creatine clearance below 30mL/min.

화학적 성질

Crystalline Solid

Originator

Fujisawa (Japan)

용도

Bone metabolism modulator; inhibits bone resorption while maintaining bone formation. Antiosteoporotic

용도

Strontium ranelate (Protelos) is a strontium(II) salt of ranelic acid for (-)-desmethoxyverapamil binding to calcium channel with IC50 of 0.5 mM.

상표명

Protelos

Strontium ranelate 준비 용품 및 원자재

원자재

준비 용품


Strontium ranelate 공급 업체

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