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Co-crystal of tapentadol hydrochloride and celecoxib, composition and preparation method thereof

A technology of tapentadol hydrochloride and celecoxib, which is applied in the treatment of pain medicine, the co-crystal of tapentadol hydrochloride and celecoxib and its pharmaceutical composition and preparation field can solve the problem of different concentration Changes in expectations, patient compliance and impairment of treatment benefit, dosing errors, etc.

Active Publication Date: 2016-09-28
ANHUI HEALSTAR PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the need for frequent dosing can lead to dosing errors and undesired changes in the plasma concentration of the compound, which can be detrimental to patient compliance and therapeutic benefit, especially when treating chronic pain conditions in this way

Method used

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  • Co-crystal of tapentadol hydrochloride and celecoxib, composition and preparation method thereof
  • Co-crystal of tapentadol hydrochloride and celecoxib, composition and preparation method thereof
  • Co-crystal of tapentadol hydrochloride and celecoxib, composition and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] Example 1 Preparation of Tapentadol Hydrochloride and Celecoxib Cocrystal

[0038] Weigh 2.57g of tapentadol hydrochloride and place it in a 100ml round bottom flask, add 10ml of absolute ethanol, stir to dissolve, then add 3.81g of celecoxib, heat to reflux, the solution is clear and transparent, reflux for 2 hours, distill about 5ml Ethanol, cooled to room temperature, let stand for 5 hours, then precipitated co-crystals, filtered, and dried the solid in vacuum at 60-65°C for 6 hours to obtain 6.3 g of tapentadol hydrochloride and celecoxib co-crystals, with a yield of 98.7%.

Embodiment 2

[0039] Example 2 Physical and Chemical Properties Test of Tapentadol Hydrochloride and Celecoxib Cocrystal

[0040] 1. Melting point

[0041] The co-crystals of tapentadol hydrochloride and celecoxib were taken and determined according to the law (Appendix VI C of Part Two of the Chinese Pharmacopoeia 2010 Edition). The melting point of the sample was determined to be 270.4-273.0°C.

[0042] Determined by the same method, the melting point of tapentadol hydrochloride is: 210.5-213.7°C; the melting point of celecoxib is: 161.3-165.1°C

[0043] 2. Hygroscopicity

[0044] Take about 1 g of tapentadol hydrochloride and celecoxib eutectic raw materials, spread it into a flat weighing bottle with constant weight to form a thin layer (thickness is about 5 mm), weigh it accurately, and then place it in air, filled with saturated Place it in a closed container of sodium chloride solution (RH75%) and a closed container filled with saturated potassium nitrate solution (RH92.5%) for 10 da...

Embodiment 3

[0051] Example 3 Structural Characterization of Tapentadol Hydrochloride and Celecoxib Cocrystal

[0052] 1. XRPD characterization

[0053] The XRPD characterization of the co-crystal of tapentadol hydrochloride and celecoxib is listed in the following table:

[0054]

[0055] The entire list of peaks or a subset thereof may be sufficient to characterize the co-crystal. For example, the co-crystal can be characterized by at least 3 peaks selected from the peaks at 16.022, 18.212, 19.631, 21.550, 22.418, 25.393, 29.394 and an XRPD pattern substantially similar to that of Figure 1 .

[0056] 2. DSC characterization

[0057] DSC of the co-crystals of tapentadol hydrochloride and celecoxib showed that the co-crystals had a broad endothermic peak around 271°C.

[0058] 3. TG characterization

[0059] The co-crystal TG of tapentadol hydrochloride and celecoxib showed that the co-crystal lost weight significantly at 238°C to 280°C.

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Abstract

The invention relates to a novel eutectic crystal of tapentadol hydrochloride and celecoxib, a method for preparing the eutectic crystal, a pharmaceutical composition containing the eutectic crystal and application of the eutectic crystal in drugs for treating pains, including acute pain, chronic pain, neuropathic pain, nocuous pain, mild and severe pain degradation, hyperalgesia, pain related to central sensitization, abnormal pain and cancer pain.

Description

technical field [0001] The invention belongs to the technical field of chemical pharmacy, and in particular relates to a co-crystal of tapentadol hydrochloride and celecoxib, a pharmaceutical composition, a preparation method thereof and an application in medicine for treating pain. Background technique [0002] Pain is a clinical symptom of many diseases and a protective response of the body to noxious stimuli. Analgesics are divided into two categories, narcotic analgesics acting on the central nervous system and non-steroidal anti-inflammatory analgesics acting on the peripheral system. Central analgesics have a strong analgesic effect, but because of Large side effects, especially the addictive nature, limit its application. Non-steroidal anti-inflammatory analgesics are a class of drugs with antipyretic, analgesic and anti-inflammatory effects. They are basic drugs for pain treatment. The analgesic effect is weaker than the former, but the side effects are relatively s...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07C215/54C07C213/10C07D231/12A61K31/635A61P29/00A61P25/00A61P37/08A61P35/00A61P3/10A61P19/02A61P19/08A61P21/00A61K31/137
Inventor 徐奎刘丽刘经星
Owner ANHUI HEALSTAR PHARM CO LTD
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