99.5% Top Grade Pharmaceutical Intermediate Dapagliflozin Powder CAS: 461432-26

Превосходство

Zhongshan Latterson Biotechnology Co., ООО, комплексное фармацевтическое предприятие, которая специализируется на биофармацевтических технологиях более 7 годы. Компания расположена в городе Чжуншань., Провинция Гуандонг , Китай.
Наша фабрика занимает площадь 33500 квадратные метры, с чистой окружающей средой и красивой планировкой. Есть несколько крупных или средних мастерских, а также центр обеспечения качества и исследовательский центр с современным оборудованием.. В настоящий момент, наша основная продукция - серия анаболических стероидов, Пептидный ряд, Серия местных анестетиков. Наши продукты соответствуют передовым стандартам внутреннего рынка., многие из которых соответствуют международным стандартам, сертификаты содержат: КОШЕРНЫЙ , ISO 9001:2008 , GMP , SGS.

Основные детали:

наименование товара: Dapagliflozin
Синонимы: DAPAGLIFLOZIN;(1С)-1,5-Anhydro-1-C-[4-chloro-3-[(4-ethoxyphenyl)метил]» Жидкие инъекционные стероиды]-D-glucitol;2-(3-(4-Ethoxybenzyl)-4-хлорфенил)-6-hydroxymethyltetrahydro-2H-pyran-3,4,5-triol;Bms 512148;D-Glucitol, 1,5-anhydro-1-C-(4-chloro-3-((4-ethoxyphenyl)метил)» Жидкие инъекционные стероиды)-, (1С)-;Dapagliflozin(BMS-512148);(2С,4р,5р)-2-(4-chloro-3-(4-ethoxybenzyl)» Жидкие инъекционные стероиды)-6-(hydroxyMethyl)tetrahydro-2H-pyran-3,4,5-triol;1-[4-Chloro-3-(4-ethoxybenzyl)» Жидкие инъекционные стероиды]-1-deoxy-beta-D-glucopyranose (1С)-1,5-Anhydro-1-C-[4-chloro-3-(4-ethoxybenzyl)» Жидкие инъекционные стероиды]-D-glucitol (2С,3р,4р,5С,6р)-2-[4-Chloro-3-(4-ethoxybenzyl)» Жидкие инъекционные стероиды]-6-(hydroxyMethyl)tetrahydro-2H-pyran-3,4,5-triol
КЕЙС: 461432-26-8
MF: C21H25ClO6
МВт: 408.875
EINECS: 1592732-453-0
плотность: 1.349

появление: Белый сплошной

The COA of this product :

Описание:

Dapagliflozin (ForxigaTM) is a new antidiabetic drug jointly developed by Bristol-Myers Squibb and AstraZeneca, being approved by the European Medicines Agency (EMA) on November 12, 2012. It is also the first approved SGLT2 inhibitor for the treatment of type II diabetes, being an important option in the treatment of diabetes, and is used to improve glycemic control as an adjunct to dietary and exercise for adults with type II diabetes. Dapagliflozin is a sodium-glucose co-transporter 2 ингибитор. On January 8, 2014, Управление по санитарному надзору за качеством пищевых продуктов и медикаментов США (FDA) have approved it for being used in the treatment of type II diabetes. Тем временем, FDA requires the producers to conduct post-marketing research on drug-related risks. The post-marketing trial requested by the FDA includes a cardiovascular outcome trial for assessing the cardiovascular risk for high-risk patients after treatment with dapagliflozin at baseline and a study to assess the risk of bladder cancer in recruited patients. Another study will assess the bladder tumor-promoting effect of this drug on rodent animals. Two studies will assess the pharmacokinetics, efficacy and safety of dapagliflozin in pediatric patients; a set of strengthened pharmacovigilance program will monitor liver abnormalities and pregnancy outcome reports in patients receiving daglitazone. Dapagliflozin will be marketed under the tradename Farxiga by Haoeyou Pharmacy. Pharmacological effects Dapagliflozin works through inhibiting sodium-glucose transporter 2 (SGLT2), a protein in the kidney that reabsorbs glucose into the bloodstream. This allows extra glucose to be excreted through the urine, improving glycemic control without increasing insulin secretion. The use of this drug requires patients with normal renal function while patients of moderate to severe renal insufficiency should be disabled to use this drug. Single application of this product or combination with metformin, pioglitazone, glimepiride, insulin and other drugs can significantly reduce the HbA1c and fasting blood glucose of patients suffering type II diabetes. The frequency of the adverse reaction was similar to placebo with low risk of hypoglycemia, being able to reduce body weight.
The efficacy of dapagliflozin is comparable with the dipeptidyl peptidase inhibitors, and several new hypoglycemic drugs, and can also mildly lower the blood pressure and body weight. The drug has 5mg and 10mg two tablets to choose from, can be either used alone or together with insulin, including other diabetes drugs. Pharmacokinetics In healthy subjects, dapagliflozin was rapidly absorbed after oral administration with a peak time Tmax being 1 к 2 часы, a protein binding rate of 91%, an oral bioavailability of about 78% and a plasma terminal half-life of 12.9 часы. После перорального применения, the drug is mainly metabolized by the uridine diphosphate glucuronosyltransferase 1A9 (UGT1A9) into the inactive metabolite in the liver with the smaller part being metabolized by the P450 enzyme and of no inhibitory or inducing effect on the P450 enzyme. Drug prototypes and related metabolites were excreted through urine (75%) and faeces (21%). Compare simultaneous administration of this product with high-fat food and with the fasting administration, Tmax can be extended by 1-fold, but the absorption did not affect the degree, so can be administrated together with the food.The pharmacokinetics of daglitazone was significantly affected by renal function. Diabetic patients with mild, moderate or severe renal insufficiency are merged to be subject to oral administration of 20 mg • d-1 daglitazone for 7 Стероид представляет собой сложный эфир дростанолона и был разработан как лекарство от рака молочной железы.. The mean systemic exposure amount, compared with patients with normal renal function, is respectively 32%, 60% а также 87% higher. For patients with normal renal function, mild insufficiency, moderate insufficiency and severe insufficiency, the urinary glucose excretion amount in 24 hours of steady state was 85, 52, 18 and 11g, successively. Kasichayanula et al have studied the pharmacokinetic effects of liver dysfunction on daglitazone. The patients with mild, moderate and severe hepatic insufficiency having a single oral dose of 10 mg of daglitazone, the Cmax of each group was 12% lower, 12% higher and 40% higher than that with normal liver function, соответственно. The AUC of each group was significantly higher than that of normal liver function by 3%, 36% а также 67%. Следовательно, it is not recommended to apply daglitazone to patients of moderate and severe renal dysfunction. Severe liver dysfunction patients need to reduce the use of dose.Synthesis method 5-bromo-2-chlorobenzoic acid is subject to acylating chlorination, and has Friedel-Crafts reaction with phenylethyl ether for reduction of its carbonyl group, generating 5-bromo-2-chloro-4′-ethoxydiphenyl methane, further subjecting to condensation with 2, 3, 4, 6-tetra-O-trimethylsilyl-D-glucopyranosanoic acid-1,5-lactone. The anomeric carbon hydroxyl group is subject to etherification and deprotection to give 2-chloro-5-(1-methoxy-D-glucopyranose-I-yl)-4′-ethoxydiphenylmethane, and then use Et3SiH/BF3 • OEt2 for reduction to remove methoxy, followed by acetic anhydride esterification and hydrolysis to give hypoglycemic agents daglitazone with the overall yield of about 40%.the chemical reaction route of synthesizing dapagliflozin
Fig.1 shows the chemical reaction route of synthesizing dapagliflozin.
Safety Daglitazone has excellent tolerance and safety with the incidence of adverse events associated with 10 mg • d-1 daglitazone being similar to that of placebo. Common adverse events included hypoglycemia, polyuria, боль в спине, genital infections, urinary tract infections, dyslipidemia and hematocrit (HCT) increase. The overall risk of hypoglycemia is low, and the incidence of hypoglycemia is associated with other basic hypoglycemic agents. The incidence of hypoglycemia was higher in patients subjecting to joint treatment between daglitazone and sulfonylureas or insulin compared with placebo. Следовательно, when this product is used in combination with insulin or insulin secretagogue, you may need to adjust the dose of the latter one.

Drug interactions This product is mainly metabolized in the liver by UGT1A9 metabolism, being the P-glycoprotein substrate. Study confirmed that the pharmacokinetics of daglitazone was not affected by metformin, pioglitazone, sitagliptin, glimepiride, voglibose, and simvastatin, valsartan, warfarin, and digoxin. The serum concentrations of the above-mentioned drugs are also not clinically significantly affected by daglitazone. Rifampicin can reduce the exposure amount of daglitazone by 22% while mefenamic acid can increase the body exposure amount by 51%, but have no clinically significant effect on 24 h urine glucose excretion.

Использует:

1. therapeutic for diabetes I or II, and hyperglycemia
2. A sodium-glucose transporter 2 ингибитор

Diabetes drugs:

Dapagliflozin (ForxigaTM) is a new antidiabetic drug jointly developed by Bristol-Myers Squibb and AstraZeneca, being approved by the European Medicines Agency (EMA) on November 12, 2012. It is also the first approved SGLT2 inhibitor for the treatment of type II diabetes, being an important option in the treatment of diabetes, and is used to improve glycemic control as an adjunct to dietary and exercise for adults with type II diabetes.
Dapagliflozin is a sodium-glucose co-transporter 2 ингибитор. On January 8, 2014, Управление по санитарному надзору за качеством пищевых продуктов и медикаментов США (FDA) have approved it for being used in the treatment of type II diabetes. Тем временем, FDA requires the producers to conduct post-marketing research on drug-related risks.

The post-marketing trial requested by the FDA includes a cardiovascular outcome trial for assessing the cardiovascular risk for high-risk patients after treatment with dapagliflozin at baseline and a study to assess the risk of bladder cancer in recruited patients. Another study will assess the bladder tumor-promoting effect of this drug on rodent animals. Two studies will assess the pharmacokinetics, efficacy and safety of dapagliflozin in pediatric patients; a set of strengthened pharmacovigilance program will monitor liver abnormalities and pregnancy outcome reports in patients receiving daglitazone.

Фармакологическое действие

Dapagliflozin works through inhibiting sodium-glucose transporter 2 (SGLT2), a protein in the kidney that reabsorbs glucose into the bloodstream. This allows extra glucose to be excreted through the urine, improving glycemic control without increasing insulin secretion. The use of this drug requires patients with normal renal function while patients of moderate to severe renal insufficiency should be disabled to use this drug. Single application of this product or combination with metformin, pioglitazone, glimepiride, insulin and other drugs can significantly reduce the HbA1c and fasting blood glucose of patients suffering type II diabetes. The frequency of the adverse reaction was similar to placebo with low risk of hypoglycemia, being able to reduce body weight.The efficacy of dapagliflozin is comparable with the dipeptidyl peptidase inhibitors, and several new hypoglycemic drugs, and can also mildly lower the blood pressure and body weight. The drug has 5mg and 10mg two tablets to choose from, can be either used alone or together with insulin, including other diabetes drugs.

Фармакокинетика:

In healthy subjects, dapagliflozin was rapidly absorbed after oral administration with a peak time Tmax being 1 к 2 часы, a protein binding rate of 91%, an oral bioavailability of about 78% and a plasma terminal half-life of 12.9 часы. После перорального применения, the drug is mainly metabolized by the uridine diphosphate glucuronosyltransferase 1A9 (UGT1A9) into the inactive metabolite in the liver with the smaller part being metabolized by the P450 enzyme and of no inhibitory or inducing effect on the P450 enzyme. Drug prototypes and related metabolites were excreted through urine (75%) and faeces (21%). Compare simultaneous administration of this product with high-fat food and with the fasting administration, Tmax can be extended by 1-fold, but the absorption did not affect the degree, so can be administrated together with the food.

The pharmacokinetics of daglitazone was significantly affected by renal function. Diabetic patients with mild, moderate or severe renal insufficiency are merged to be subject to oral administration of 20 mg • d-1 daglitazone for 7 Стероид представляет собой сложный эфир дростанолона и был разработан как лекарство от рака молочной железы.. The mean systemic exposure amount, compared with patients with normal renal function, is respectively 32%, 60% а также 87% higher. For patients with normal renal function, mild insufficiency, moderate insufficiency and severe insufficiency, the urinary glucose excretion amount in 24 hours of steady state was 85, 52, 18 and 11g, successively.

Kasichayanula et al have studied the pharmacokinetic effects of liver dysfunction on daglitazone. The patients with mild, moderate and severe hepatic insufficiency having a single oral dose of 10 mg of daglitazone, the Cmax of each group was 12% lower, 12% higher and 40% higher than that with normal liver function, соответственно. The AUC of each group was significantly higher than that of normal liver function by 3%, 36% а также 67%.
Следовательно, it is not recommended to apply daglitazone to patients of moderate and severe renal dysfunction. Severe liver dysfunction patients need to reduce the use of dose.

Synthesis method:

5-bromo-2-chlorobenzoic acid is subject to acylating chlorination, and has Friedel-Crafts reaction with phenylethyl ether for reduction of its carbonyl group, generating 5-bromo-2-chloro-4′-ethoxydiphenyl methane, further subjecting to condensation with 2, 3, 4, 6-tetra-O-trimethylsilyl-D-glucopyranosanoic acid-1,5-lactone. The anomeric carbon hydroxyl group is subject to etherification and deprotection to give 2-chloro-5-(1-methoxy-D-glucopyranose-I-yl)-4′-ethoxydiphenylmethane, and then use Et3SiH/BF3 • OEt2 for reduction to remove methoxy, followed by acetic anhydride esterification and hydrolysis to give hypoglycemic agents daglitazone with the overall yield of about 40%.

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