Name | Tapentadol Hydrochloride |
Synonyms | Tapentadol HCl Tapentadol hcl Tapentadol Hydrochloride Tapentadol hydrochloride solution 3-[(1R,2R)-3-(DiMethylaMino)-1-ethyl-2-Methylpro 3-[(1R,2R)-3-(dimethylamino)-1-ethyl-2-methylpropyl]phenol 3-((2R,3R)-1-(diMethylaMino)-2-Methylpentan-3-yl)phenol hydrochloride 3-[(1R,2R)-3-(Dimethylamino)-1-ethyl-2-methylpropyl]phenol Hydrochloride Phenol, 3-[(1R,2R)-3-(diMethylaMino)-1-ethyl-2-Methylpropyl]-, (HCl salt) |
CAS | 175591-09-0 |
EINECS | 687-970-4 |
InChI | InChI=1/C14H23NO/c1-5-14(11(2)10-15(3)4)12-7-6-8-13(16)9-12/h6-9,11,14,16H,5,10H2,1-4H3/t11-,14+/m0/s1 |
Molecular Formula | C14H24ClNO |
Molar Mass | 257.81 |
Density | 0.97g/cm3 |
Melting Point | 178-194°C |
Boling Point | 323.493°C at 760 mmHg |
Flash Point | 9℃ |
Vapor Presure | 0mmHg at 25°C |
Storage Condition | -20°C Freezer, Under Inert Atmosphere |
Refractive Index | 1.518 |
Risk Codes | R11 - Highly Flammable R23/24/25 - Toxic by inhalation, in contact with skin and if swallowed. R39/23/24/25 - |
Safety Description | S7 - Keep container tightly closed. S16 - Keep away from sources of ignition. S36/37 - Wear suitable protective clothing and gloves. S45 - In case of accident or if you feel unwell, seek medical advice immediately (show the label whenever possible.) |
UN IDs | UN1230 - class 3 - PG 2 - Methanol, solution |
WGK Germany | 1 |
Overview | since, the president of the American Pain Society, jamescampbel, first proposed that pain is the fifth most important vital sign, and now, world Health Organization (WHO), pain has been identified as the "fifth vital sign" after blood pressure, respiration, pulse, and body temperature, and the study of pain has been paid more and more attention. At present, the most commonly used analgesics are non-steroidal anti-inflammatory drugs (NSAIDs) and opioids. Although they have achieved good clinical efficacy, due to the limitations of the mechanism, NSAIDs have varying degrees of adverse reactions, such as gastrointestinal reactions, gastric ulcer, gastric bleeding and allergies; Opioids are due to potential abuse, tolerance and withdrawal reactions, their clinical application has been greatly limited. In 2003, the German company Gruenenthal successfully developed a new molecular compound tapentadol, which has improved side effects compared with other opioids and NSAIDs, improving the safety and tolerability of opioids. Currently, immediate and sustained release formulations of tapentadol have been developed and marketed in several countries for the relief of moderate to severe acute or chronic pain in the adult central nervous system, there is no imported preparation of the drug in China. |
research progress | at present, only oral liquid and tablets (immediate release tablets and sustained release tablets) of tapentadol hydrochloride are available, both are developed by Johnson & Johnson, Inc., USA, for the relief of moderate to severe acute or chronic pain in adults. 1) multi-Immediate Release Tablets of tapetat hydrochloride: the multi-Immediate Release Tablets of tapetat hydrochloride were approved by FDA in November 2008, and the trade name was Nucynta, it is clinically used to relieve moderate to severe acute pain in the central nervous system of adults, and its prescription uses cross-linked sodium carboxymethyl cellulose as a disintegrant to achieve rapid release and effectively relieve acute pain. The immediate release formulations of tapentadol are available in strengths of 50,75 and 100mg with a maximum daily dose of 600mg. 2) tapentadol hydrochloride sustained-release tablets: For patients with chronic pain, sustained-release preparations have incomparable advantages over ordinary tablets. In order to relieve chronic pain, tapentadol hydrochloride sustained-release tablets were developed and approved by FDA in August 2011. At present, hydrophilic gel matrix tablets are widely used in sustained-release preparations, accounting for 60% ~ 70% of the listed skeleton type varieties. Tapentadol sustained-release tablets are hydroxypropyl methyl cellulose (HPMC) as the skeleton material, the release rate of the drug was adjusted by the pore forming agent, and the hydrophilic gel matrix tablet was prepared for 12H slow release. Its sustained-release tablets have several specifications, Including 50,100,150,200 and 250mg, only 2 times a day, can obtain 24H stable blood concentration and continuous analgesic effect, greatly improving the curative effect. 3) tapentadol hydrochloride oral solution: tapentadol hydrochloride oral solution was approved by FDA in September 2012, which is colorless and clear liquid, specification is 20g · L-1 (equivalent to 23g · L-1 tapentadol hydrochloride), there are and packaging, for the treatment of adult moderate to severe acute pain, the initial dose is 2.5mL (equivalent to 50mg tapentadol), taken once every 4~6h, the main non-active ingredients are a hydrated citric acid, sucralose, sodium hydroxide and so on. |