Suppliers with verified business licenses
Audited Supplier
| Repaglinide Chemical Properties |
| Melting point | 129-130.2 °C |
| alpha | D20 +6.97° (c = 0.975 in meth anol); D20 +7.45° (c = 1.06 in metha nol) |
| Boiling point | 672.9±55.0 °C(Predicted) |
| density | 1.137±0.06 g/cm3(Predicted) |
| storage temp. | 2-8°C |
| solubility | DMSO: 34 mg/mL |
| form | solid |
| pka | 4.19±0.10(Predicted) |
| color | white |
| Water Solubility | 89.99mg/L(25 ºC) |
| Merck | 14,8136 |
| InChIKey | FAEKWTJYAYMJKF-QHCPKHFHSA-N |
| CAS DataBase Reference | 135062-02-1(CAS DataBase Reference) |
| Safety Information |
| WGK Germany | 2 |
| RTECS | 000000033825 |
| HS Code | 2933399090 |
| Toxicity | LD50 orally in rats: >1 g/kg (Grell) |
| Repaglinide Usage And Synthesis |
| Diabetes Treatment | Repaglinide, a type of medicines for treating diabetes, is insu linotropic agent which belongs to the non-sulfonylurea. It was developed by Boehringer Ingelheim from Germany, and won approval by FDA from the United States in December 1997. In 1998, it was successively listed in the United States and European countries, with commodity name as NovoNorm. Mainly used in the clinical treatment of typediabetes (non-i nsulin-dependent) patients whose hyperglycemia can't be effectively controlled via diet, weight loss and exercise. In 2008, FDA from the United States approved it going public for Novo Nordisk of replaglinide + metformin HCl, PrandiMet, for treatment of type 2 diabetes. From the point of chemical structure, repaglinide derives from carbamyl methyl benzoic acid, and is a prandial glucose regulator which promots ins ulin secretion rapidly within short time. The functional mechanism is mainly by closing the potassium channels on the β cell membrane, causing calcium influx, and then intracellular calcium concentration increases, thereby stimulating insu lin secretion. But with different acceptor sites of sulfonylurea reaction, the drug does not enter into the β cells, and it neither inhibits protein synthesis nor directly causes ins ulin action. With rapid absorption and metabolism, peak and half-life of this drug are approximately 1 hour. After taking the drug, the plasma insul in concentration rapidly increases, resulting in a significant decrease in blood glucose. Therefore, this product should be taken during the meal, not to eat not to take, which is the so-called "prandial glucose regulator ". Each dose is 0.25g and 2g. Flexible medication can reduce hypoglycemia caused by missing meals or delayed meal. After half a year medication, it can reduce postprandial blood sugar 6mmol/L, fasting blood-glucose 4mmol/L and HbAlc2%; when compared with placebo, it can better improve blood glucose control. Repaglinide is as effective as metformin on obese patients with type 2 diabetes blood glucose; effect of combined use with metformin is better than when it is used alone. Safety studies showed no severe hypoglycemia and liver damage, few drug interactions, and patients were well tolerated. Treatment of diabetic drug repaglinide clinical evaluation, adverse reactions, precautions was edited by Tongtong from Chemicalbook. |
| Chemical properties | White crystalline powder, odorless. Crystallization from ethanol-water (2:1), melting point 126-128ºC. Crystallization from neutral water, melting point 130~131ºC. [α]D20+6.97ºC (C=0.975, meth anol); [α]D20+7.45°(C=1.06, methan ol). Acute toxicity LD50. Rat (g/kg): > 1 oral. |
| Pharmacokinetics | (1) After oral administration, this medicine would be absorbed rapidly; when fed in 2mg to vein at constant speed for 15min, distribution volumes of steady state and clearance phase were respectively 24.37L and 28.89L. Healthy people taking different doses of this product, cmax and AUC showed a dose-dependent increase, but their cmax is similar; a single dose of 2mg, cmax is 15.2~15.5 mg/ml and t1/2 is 0.6 to 0.7h. 98% of this product is metabolized by liver cytochrome P4503A, with 90% of the metabolic products excreted by the bile via feces, and the rest 8% of the metabolites excreted by the kidney. The plasma protein binding rate was 97%, which had no significant accumulation. (2) In intravenous injection, its clearance half-life is 0.6 (1.4~0.5) h, plasma clearance rate is 33 (57~15) L h-1 and the apparent distribution volume is 28.9L. Oral administration of repaglinide has a rapid and complete absorption, either in fasting or eating, it would be well absorbed. Plasma peak achieved after 30~60min, and the half-life was approximately 1h. It would be almost metabolized and eliminated in 4h, and the apparent distribution volume of the steady-state is 0.4L•kg-1. The absolute bioavailability is 63%. The main metabolites are dicarboxylic acid derivative (M1) and glycuronic acid (M7), both are non-hypoglycemic activity. Studies have shown that healthy subjects at different ages (18 to 40 year old adults and elderly people over the age of 65) taking 2.0mg single dose repaglinide or repeatedly after medication, the AUC, cmax, tmax and t1/2 would have no significant difference. Its incidence of tolerance and hypoglycemia are the same, and its pharmacokinetics and pharmacodynamics are quite similar. Amount-effect relationship of single or multiple medication for healthy subjects and patients with typediabetes shows that repaglinide plasma cmax is dose dependent. After single or multiple dosing, for patients with typediabetes and healthy subjects, the pharmacokinetic parameters are consistent. No significant difference between different ethnic groups. For patients with severe renal impairment, after 7d taking 2.0 mg single dose repaglinide, the clearance rate constant decreases. But compared with healthy subjects, after administration of a single dose or multiple doses of repaglinide, the AUC significantly increased, without significant difference to Cmax and Tmax. Hemodialysis has no significant effect on clearance of repaglinide. |
| Uses | 1. Anti-diabetic medicine. Oral non-sulfonylurea hypoglycemic agent, for the treatment of typediabetes. 2. Used as hypolycemic agent. |
| Production method | Convert the compounds () to their N-acetyl derivatives, with L-glutamate to get salt and then get (S) shaped optical isomer; react with the compounds () to form amide () and then hydrolyzed to obtain the product. |
| Dosage and administration | Tablet: 0.5mg, 1.0mg and 2.0mg. Repaglinide (trade name: NovoNorm) should be taken before main meals (i.e. medicine taken before meals). It would start to promote ins ulin secretion after 30 minutes of oral administration. Generally speaking the medicine should be taken within 15 minutes before the meal, and the time can also be mastered within 0 to 30 minutes before the meal. Please take repaglinide as directed. Doses vary from person to person and depend on their blood glucose. The recommended starting dose is 0.5mg, which can be adjusted every week or every two weeks as necessary. Patients under treatment of other oral hypoglycemic medicines can be directly transferred to repaglinide treatment, and the recommended starting dose is 1mg. The maximum recommended dose for a single dose is 4mg, taking with meals. But the maximum daily dose should not exceed 16mg. For patients with debilitating and malnutrition, the dose should be carefully adjusted. If combined with metformin, repaglinide dose should be reduced. Although repaglinide is mainly by biliary excretion, renal insufficiency patients still should use with caution. |
| Clinical assessment | |
| Adverse reaction | Same as other hypoglycemic drugs, taking repaglinide may occur following adverse reactions: 1. Hypoglycemia: these reactions are usually mild, and to be easily corrected by giving sugar. If it is more severe, glucose can be transfused. 2. Anomalopia: It has been known that changes in blood glucose levels can lead to transient anomalopia, especially at the beginning of treatment. Only a few cases reported above mentioned anomalopia occured at the beginning treatment of repaglinide, but in clinical trials there is no case stopped using repaglinide due to this reason. 3. Gastrointestinal tract: clinical trials have reported gastrointestinal reactions, such as abdominal pain, diarrhea, nausea, vomiting and constipation. Compared with other oral hypoglycemic agents, the frequency and severity of these symptoms were not different. 4. Liver enzyme system: there were rare cases reported elevated liver enzyme index during repaglinide treatment. Most cases were mild and transient, and very few patients discontinued repaglinide treatment due to increased liver enzyme index. 5. Anaphylactic reaction: can occur in the skin allergic reactions, such as itching, redness, urticaria, etc. Because of the different chemical structure, there is no reason to suspect the possibility of cross allergic reaction with sulfonylureas. Studies have not been carried out in pregnant or lactating women, so the pregnancy and lactation women are prohibited to use this product. |
| Attentions | 1. Like most other oral hypoglycemic drugs promoting ins ulin secretion, repaglinide can cause hypoglycemia. When used in combination with metformin, it may increase the risk of hypoglycemia. If after the treatment of combined medication it still sustained high blood glucose, oral hypoglycemic drugs can no longer be used to control blood sugar, and ins ulin treatment is needed. In the event of stress reaction, such as having a fever, trauma, infection or surgery, it may appear hyperglycemia. 2. As with other oral hypoglycemic agents, patients must use it with caution, to avoid hypoglycemia while driving. 3. Medication overdose may cause hypoglycemia, such as dizziness, sweating, tremor, headache, etc. In response to these reactions, effective measures should be taken to correct hypoglycemia, such as oral sugars. More severe hypoglycemia associated with epilepsy, loss of consciousness or coma, should be intravenous infusion of glucose. 4. Hypoglycemic effect of repaglinide will due to enhanced when in combined use with monoamine oxidase inhibitor (MAOI), non-selective β blockers, angiotensin converting enzyme inhibitor (ACEI), non-steroidal anti-inflammatory drugs, salicylate, octreotide, ethanol and hormones that promote the synthesis of metabolism. 5. It will weaken the hypoglycemic effect when in combination use of oral contraceptives, thiazide drug, corticosteroids, d anazol, thyroid hormone and sympathomimetic drug. |
| Chemical Properties | White to Off-White Solid |
| Originator | Boehringer Ingelheim (Germany) |
| Uses | Non-sulfonylurea oral hypoglycemic agent. Used as an antidiabetic |
| Uses | The R-enantiomer showed only weak hypoglycemic activity. Repaglinide impurity |
| Uses | antineoplastic |
| Uses | A KIR6 (KATP) channel blocker |
| Brand name | Prandin (Novo Nordisk). |
| General Description | Repaglinide is 2-ethoxy-4-[2-[[(1S)-3-methyl-1-[2-(1-piperidinyl)phenyl]butyl]amino]-2-oxoethyl]benzoic acid(Prandin); approvals for generics are pending. Combinationsare available with metformin in the United States(Prandimet), and the drug may also be coprescribed with oneof the thiazolidinediones (typically pioglitazone or rosiglitazone;see previous discussion). To establish the most clinicallyvaluable dose, the patient is titrated while monitoringblood glucose levels and hemoglobin glycosylation (HbA1c)as an index of longer-term overall control. |
| General Description | Repaglinide, (+)-2-ethoxy-4-[N-[3-methyl-1(S)-[2-(1-piperidinyl) phenyl]butyl]carbamoyl-methyl]benzoicacid (Prandin), represents a new class of nonsulfonylureaoral hypoglycemic agents. With a fast onset and ashort duration of action, the medication should be taken withmeals. It is oxidized by CYP 3A4, and the carboxylic acidmay be conjugated to inactive compounds. Less than 0.2%is excreted unchanged by the kidney, which may be an advantagefor elderly patients who are renally impaired. Themost common side effect involves hypoglycemia, resultingin shakiness, headache, cold sweats, anxiety, and changes inmental state. |
| Biological Activity | K ATP channel blocker that binds with high affinity for SUR1 when co-expressed with Kir6.2 (K d = 0.42 nM). Antidiabetic glucose regulator with hypoglycaemic effect in vivo . |
| Clinical Use | Repaglinide is a nonsulfonylurea in sulin secretagogue that was introduced in the United States in 1998 for type 2 diabetes. |
Hubei Marvel Biopharmaceutical Co., Ltd. is located in Wuhan, Hubei Province, which is a water, land, and air transportation hub. It is a company dedicated to the development and sales of fine chemicals, pesticide raw materials, and other products.
The company is committed to developing into a powerful brand company with independent import and export management rights. Its innovative and breakthrough products not only make Marvel Pharmaceutical a leader in the industry domestically, but also enjoy a high reputation internationally. Always adhere to the business philosophy of "customer satisfaction and enterprise development", build a bridge with customers with the spirit of integrity and dedication, and serve customers better, faster, and more accurately.
The company has independent import and export management rights and an excellent sales team. With the diligent efforts of all employees, we have opened up a vast market for the company. The company's products sell well throughout the country and are exported to countries and regions such as Europe, America, Southeast Asia, and Africa. The number of customers served each year is over 2000, winning unanimous recognition and praise from our customers.
Q1: May I get one sample before placing order?
Re: Yes, Sample are available. For normal products, samples are for free and you just need to bear the freight; For those high value products, you just need to freight and certain product cost. When we both cooperate for some times or when you are our VIP customer, free sample will be offered when you need.
Q2: Which payment is available for your company?
Re: T/T, L/C or Alibaba trade insurance. You can choose the one which is convenient for you.
Q3: How and when can I get my goods after payment?
Re: For small quantity products, they will be delivered to you by international courier(DHL, FedEx, TNT etc.)
or by air. Usually it will cost 3-5days that you can get the goods after delivery.For large quantity products,
shipping by see is worthwhile.It will cost days to weeks to come to your destination port, which depends on
where the port is.
Q4: Is there any possible to use my appointed label or package?
Re: Yes. If needed, we'd like to use label or package according to your requirement.
Q5: How can you guarantee the goods you offer is qualified?
Re: We always believe honesty and responsibility are basis of one company, so whatever products we provide for you all are qualified. We will have goods tested and provide COA before delivery for sure.
Advantages:
1. Faster delivery: Sample order in stock and 3-7 days for bulk production.
2. We have strong cooperation with DHL, TNT, UPS, FEDEX, EMS. Or you also can choose your own shipping forwarder.
3. After-Sale Service:
1)International Authorized Third-Party Test For The Products You Demand.
2)60 Days Warranty of quality of goods.
Suppliers with verified business licenses
Audited Supplier 
){kind=link}
){kind=link}