Hebei Nengqian Chemical Import and Export Co., LTD
Assessed Supplier Enterprise Certification
- Assessed
Supplier - 4th
years
Assessed Supplier Enterprise Certification
Product Certification&
Enterprise Certification
Country: 
China (Mainland)
Business Type:Trading Company
Tel: +86 18732968538
Mobile: +86 18732968538
Tel: +86 18732968538
Fax: 4001020630
URL: https://www.nengqianchemical.com/
Province/state: Hebei
City: Handan
Street: No.1722, Block C, Yangguang Xinzhuo Plaza, 256 Renmin West Road, Fuxing District, Handan City, Hebei Province
MaxCard:
Ms.AnnaCAS NO.119356-77-3
Pharmaceutical grade(1-50)KilogramPharmaceutical grade(51-99)Kilogram
Our Advantage
Rich Experience
Our products are sold all over Europe,North&South America, Sino-East, Asia and pacific area as well as Africa,we establish long term.
Quality service
Company cooperates with research institutes. We strictly control the process of raw materials up to finished product.
24 hour service
Quick and clear response to customers questions. Warm after sale service, we will help to solve the problems in your usage.
High quality
Dedicated to serving customers first, we provide reasonable prices, high quality products.
1) Standard:BP/USP/EP/Enterprise standard
2) All Purity≥99%
3) We are manufacturer and can provide high quality products with factory price.
2, Fast and safe delivery
1) Parcel can be sent out in 24 hours after payment.Tracking number available
2) Secure and discreet shipment.Various transportation methods for your choice.
3) Customs pass rate ≥99%
4) We have our own agent/remailer/distributor who can help us ship our products very fast and safe,
and we have stock in there for transferring.
| Brief Introduction | Premature ejaculation (PE) is the most common male sexual dysfunction. Dapoxetine hydrochloride,marketed as Priligy and Westoxetin, is a class of PE treatment drugs known as selective serotonin reuptake inhibitors (SSRI) , was the first drug originally approved for the on-demand treatment of men 18–64 years old with PE. Dapoxetine works by inhibiting the serotonin transporter, increasing serotonin's action at the post synaptic cleft, and as a result promoting ejaculatory delay. Dapoxetine was initially developed as an antidepressant. However, unlike other SSRIs, dapoxetine is absorbed and eliminated rapidly in the body. Its fast acting property makes it suitable for the treatment of PE but not as an antidepressant. Used for the treatment of premature ejaculation and erectile dysfunction. Over 98% of men taking this drug will naturally gain a improved erection quality with prolonged time and more frequencies. |
| Physical and chemical properties | White crystal powder with sweet taste and no odor, hygroscopic and soluble in water. It has a stable chemical property with the melting point at 175~177℃. |
| PE treatment | Premature ejaculation (PE) is a common problem worldwide and has significant impact not only on the sufferer but on the partner in terms of self-esteem, interpersonal distress and sexual satisfaction. Tricyclic antidepressants and clomipramine are the most widely used drugs for the treatment of premature ejaculation . Randomized, double blind, placebo-controlled trials have confirmed the efficacy of dapoxetine for the treatment of PE. Different dosage has different impacts on different type of PE. Dapoxetine 60 mg significantly improves the mean intravaginal ejaculation latency time (IELT) compared to that of dapoxetine 30 mg in men with lifelong PE, but there is no difference in men with acquired PE. Dapoxetine, giving 1–3 hours before sexual episode, prolongs IELT, increases the sense of control and sexual satisfaction in men of 18 to 64 years of age with PE. Since PE is associated with personal distress, interrelationship difficulty, dapoxetine provides help for men with PE to overcome this condition. Because lack of specific approval treatment for PE in the US and some other countries, other SSRIs such as fluoxetine, paroxetine, sertraline, fluvoxamine, and citalopram have been used as off label drugs to treat PE. Waldinger's meta analysis shows that the use of these conventional antidepressants increasing IELT from two to ninefold above base line in comparison of three to eightfold when dapoxetine is used. However, these SSRIs must be taken daily in order to achieve meaningful efficacy, and the long half-life increases the risk of the drug accumulation and as a consequence increased of adverse effects such as decreasing sexual libido and causing erectile dysfunction. Dapoxetine, on the other hand, is a fast-acting SSRI. It is rapidly absorbed and eliminated from the body within a few hours. This favorable pharmacokinetics minimizes the risk of the drug's accumulation in the body, and therefore reducing side effects. |
| Mechanism of Actions | The mechanism through which dapoxetine affects premature ejaculation is still unclear. However, it is presumed that dapoxetine works by inhibiting serotonin transporter and subsequently increasing serotonin's action at pre and postsynaptic receptors. Human ejaculation is regulated by various areas in the central nervous system (CNS). The ejaculatory pathway originates from spinal reflex at the thoracolumbar and lumbosacral level of spinal cord activated by stimuli from male genital. These signals are relayed to the brain stem, which then is influenced by a number of nuclei in the brain such as medial preoptic and paraventricular nulcei. Clement's study performed on anaesthetized male rats showed that acute administration of dapoxetine inhibits ejaculatory expulsion reflex at supraspinal level by modulating activity of lateral paragigantocellular nucleus (LPGi) neurons. These effects cause an increase in pudendal motoneuron reflex discharge (PMRD) latency. However, it is unclear whether dapoxetine acts directly on LPGi or on the descending pathway in which LPGi located. |
| Development in Marketing internationally | Originally developed by Eli Lilly pharmaceutical company, dapoxetine was sold to Johnson & Johnson in 2003 and submitted as a New Drug Application to the Food and Drug Administration (FDA) for the treatment of PE in 2004.Dapoxetine is sold in some European and Asian countries, and in Mexico. In the US, dapoxetine has been in phase III development since 2003. However, it was rejected by FDA last year. In 2012, Menarini acquired the rights to sell Dapoxetine in Europe, most of Asia, Africa, Latin America and the Middle East. |
| Synthesis | There are many ways to synthesize dapoxetine, which can be divided into two categories. The first category is achiral synthesis where pure S-configuration dapoxetine is obtained from the resolution of racemic dapoxetine or its intermediate. The other is the methods of asymmetric synthesis, where S-configuration dapoxetin is directly obtained through metal catalysis or enzyme catalysis without resolution .
(2) Synthesis of dapoxetine from 1-naphthol as raw material The reaction between 1-naphthol and 3-phenylpropyl bromide is followed by bromination on the benzyl radical, the substitution of dimethylamine and the resolution of the obtained racemic products. The starting material of this route, 3-phenylpropyl bromide is rather expensive, and the bromination yield is low. 3-phenylpropyl bromide can also be replaced by 3-phenylpropyl chloride obtained by the reaction of phenylpropanol with dichlorofuran. (3) Synthesis of dapoxetine from (s)-3-chlorophenyl propanol as raw material the etherification between (S)-3-chlorophenyl propanol and 1-naphthol is followed by the one-pot reaction of methanesulfonyl chloride and dimethylamine to get S configuration of dapoxetine. This route has relatively less step and no need for resolution but the raw material (S)-3-chloropropenal alcohol is expensive and often unavailable and the reaction conditions are demanding. (4) Synthesis of dapoxetine from 3-chlorophenylacetone as raw material Through the reduction, condensation and N-methylation of 3-chlorophenylacetone as the starting material, the racemic dapoxetine is obtained and then its S-configuration is obtained. But the expensive 3-chlorophenyl acetone causes high production costs.
In this routine, N-Boc-(R)-phenylglycine 13, the carboxyl group is reduced to hydroxyl and the hydroxy is sulfonylated to produce the intermediate 14. And the addition of sodium cyanide is carried out to extend the carbon chain , And the known compound 10 is obtained after the reduction of the carboxylic acid. Finally, the target product, dapoxetine, was obtained by a two-step reaction. The raw material N-Boc-(R)-phenylglycine is not readily available and its price is high. The use of expensive borane and highly toxic NaCN makes the long synthesis route less welcomed. (2) Synthesis of dapoxetine with (R)-1-phenyl-1,3-propanediol as raw material The primary hydroxyl group in (R)-1-phenyl-1,3-propanediol 15 is selectively protected with p-toluenesulfonyl chloride, etherified, methanesulfonylated and amino-substituted to produce dapocetine. The chiral raw material 15 source is difficult to get with a high price. |
| Usage and Dosage | Oral administration of one pill 20-30 mins before sexual intercourse； it can be taken irregularly; it’s better to take it with an empty stomach; avoid fatty food during administration; no tea before administration. Its effect is significant when the user under sexual stimulus. |
| Adverse effects | The most common effects when taking dapoxetine are nausea, dizziness, dry mouth, headache, diarrhea, and insomnia, which will soon disappear. Discontinuation due to adverse effects is dose related. According to McMahon in recent study in Asia, the rate of discontinuation is 0.3%, 1.7%, and 5.3% of 1067 studied subjects with placebo, dapoxetine 30 mg, and dapoxetine 60 mg respectively. Unlike other SSRIs used to treat depression, which have been associated with high incidences of sexual dysfunction, dapoxetine is associated with low rates of sexual dysfunction. Taken as needed, dapoxetine has very mild adverse effects on loss of libido (<1%) and ED (<4%). |
| Contraindications | A contraindication is a situation in which a drug should not be used, because it may be harmful to the patient. Juveniles, children and pregnant women are not allowed to take dapoxetine. Dapoxetine should not be used in men with moderate to severe hepatic impairment and in those receiving CYP3A4 inhibitors such as ketoconazole, ritonavir, and telithromycine. Dapoxetine can also not be used in patients with heart failure, permanent pacemaker, or other significant ischemic heart disease. Caution is advised in men receiving thioridazine, monoamine oxidase inhibitors, SSRIs, serotonin-norepinephrine reuptake inhibitors, or tricyclic antidepressant. If a patient stops taking one of these drugs, he should wait for 14 days before taking dapoxetine. If a patient stops taking dapoxetine, he should wait for 7 days before receiving these drugs. |
| Interactions |
|
| References | # # |
| Uses | Antidepressant. |
| Uses | Dapoxetine-d7 Hydrochloride is a Labelled Dapoxetine (D185700). A selective serotonin reuptake inhibitor (SSRI). |
| Definition | ChEBI: Dapoxetine is a member of naphthalenes. |
| Clinical Use | Dapoxetine is a selective serotonin re-uptake inhibitor (SSRI) which has been approved in Finland and Sweden for the treatment of premature ejaculation.Dapoxetine was discovered and developed by Lilly and was licensed to Alza, a wholly-owned subsidiary of Johnson & Johnson. |
| Synthesis | Several synthetic routes for the preparation of dapoxetine have been disclosed, all on gram scale. Based on the routes and yields, the most likely process route is described in the scheme 4. Commercially available (R)-(+)-3-chloro-1-phenyl- 1-propanol (19) was reacted with 1-naphthol in the presence of 50% aqueous sodium hydroxide in DMF to give ether 20 in 90% yield. Activation of the secondary alcohol was accomplished through treatment of 20 with methane sulfonyl chloride and triethylamine with catalytic DMAP. Upon complete conversion to the corresponding mesylate, dimethylamine was added to the reaction mixture. The addition of hydrochloric acid in ethyl acetate to the resultant crude product gave dapoxetine hydrochloride (IV) in 67% yield. Purification of this material by re-crystallization from isopropanol provided IV in 86% yield and in 99.6% ee.
|
Product Packaging：
1) 1kg/bag (1kg net weight, 1.1kg gross weight, packed in an aluminum foil bag)
2) 25kg/drum (25kg net weight, 28kg gross weight; Packed in a cardboard-drum with two plastic-bags inside; Drum Size: 510mm high, 360mm diameter)
Storage：
Stored in a cool and dry well-closed container. Keep away from moisture and strong light/heat.
Delivery：
Usually within3-5 working days after full payment.
transport：
EMS,DHL, TNT, UPS ,FEDEX, BY AIR, BY SEA
DHL Express, FedEx and EMS for quantity less than 50KG, usually called as DDU service;
Sea shipping for quantity over 500KG; And air shipping is available for 50KG above;
For high value products, please select air shipping and DHL express for safe;
Our Service:
1. Fast Delivery: We can delivery within 24 hours upon receipt of your payment.
2. Quality can be promised. Hot sell to Worldwide.
3. Payment Terms: T/T,, t/t
4. Free Sample available at any time.
5. Tracking your order at any time. Inform your order's further new situation at any time.
6. Package: Professional packing with professional materials.
Packing:
1. Inner double plastic bags----25kg/Fiber drum (35*35*45cm, GW: 28kg, NW: 25kg);
2. Inner double plastic bags----5kg/Aluminum foil bag (GW: 6.5kg, NW: 5kg).
3. Inner double plastic bags----1kg/Aluminum foil bag (GW: 1.5kg, NW: 1kg).
P.S.: we accept packaging customization.
Delivery:
1. Stock products are normally shipping within 3 working days.
2. For rush delivery, please contact our sales team for particular arrangement.
Shipping Details:
1. We ship goods via DHL, Fedex, UPS, TNT, China post, NL Post and other couriers, weight from 10g to 1000kg or even bulker.
2. Shipping details & shipping documents will be provided and sent by email.
3. We keep tracking the shippment until clients well received.
4. After years export shipping experience, with professional and experienced cooperated forwarders, we ensure that goods can be delivered in multiple ways safetly and efficiently.
About us
Our company specializes in processing and selling chemical raw materials, chemical products, pharmaceutical intermediates, veterinary medicine intermediates, dye intermediates, pigments, cosmetics raw materials and chemical reagents,
We have compalete sales and service team , information feedback vertical integration of a sound marketing network, products are sold throughout the country and exported to South Asia, Europe, America, Africa and other more than 20 countries and regions.
Companies adhering to the "pursuit of quality, innovation and development" business philosophy, to serve as a foundation, for the survival by the quality, seek development by science and technology, adhere to quilty comes first,fair price,good sense of customer service and responsibility. in the future hebei Nengqian import and export trade Co.,Ltd will always hold "integrity, innovation" business philosophy, to achieve honesty management, on the way of specialization, internationalization, Keep moving!
FAQ:
1. Are you a trade company or factory
We are a factory with our own trading company.
2.How do you control the quality
Our factory is equipped with professional technicians to control quality, out inspectors take sample for testing every 2 hours to ensure the quality of our production. We also accept BV, SGS or any other Third-party inspection.
3. How long is lead time
We deliver goods within 3 days for small order, 7-10 days for bulk order.
4. Where is your factory located How can I visit the factory
Our factory located in HEBEI, China.
5. Can i get some samples
Yes, we can supply free sample, but the shipping cost be paid by our customers.
6. How to start orders or make payments
Proforma invoice will be sent first after confirmation of order, enclosed our bank information.Payment by T/T,
7. How to confirm the Product Quality before placing orders
You can get free samples for some products,you only need to pay the shipping cost or arrange a courier to us and take the samples.
You can send us your product specifications and requests,we will manufacture the products according to your requests.
8. How long is lead time
We deliver goods within 3 days for small order, 7-10 days for bulk order.
9. How do you treat quality complaint
First of all, our quality control will reduce the quality problem to near zero. If there is a realquality problem caused by us, we will send you free goods for replacement or refund your loss.