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Long-acting injection dosage form of ketamine pamoate

A technology of ketamine pamoate and pamoate, which is applied in the fields of analgesia or treatment of anti-inflammatory and central nervous system diseases, anesthesia, and sustained-release pharmaceutical compositions of R-ketamine pamoate, and can Addresses issues such as feeling drunk, elevated blood pressure, and sluggishness

Pending Publication Date: 2022-04-12
ALAR PHARMA INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Second, adverse events such as dissociation, dizziness, nausea, sedation, vertigo, hypoesthesia, anxiety, lethargy, increased blood pressure, vomiting, and feeling drunk may occur after administration of ketamine preparations

Method used

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  • Long-acting injection dosage form of ketamine pamoate
  • Long-acting injection dosage form of ketamine pamoate
  • Long-acting injection dosage form of ketamine pamoate

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0103] Embodiment 1: R, the preparation of S-ketamine free base (1)

[0104] 10 g of R,S-ketamine hydrochloride was dissolved in 100 mL of water, and then 150 mL of saturated aqueous sodium bicarbonate solution was added with stirring. The reaction mixture was extracted with dichloromethane (100 mL x 2). The separated organic layers were combined and distilled under reduced pressure to obtain R,S-ketamine free base (1).

Embodiment 2

[0105] Example 2: Preparation of (-)-O, O'-di-p-toluoyl-L-tartrate (2) of R-ketamine

[0106] Dip-toluoyl-L-tartaric acid (13 g, 33.6 mmol) and R,S-ketamine free base (8 g, 33.6 mmol) were dissolved in ethanol (160 mL) and stirred for 5 minutes. To this solution was added dropwise 10 mL of water at room temperature, followed by stirring for 1 hour to obtain a precipitate. The filtrate solution was collected after suction filtration and dried in vacuo. The residue was dissolved in 100 mL of 60% ethanol solution (i.e., EtOH:H 2 O=3:2), and cooled to room temperature for 1 hour to obtain a solid, which was then dried under vacuum. The obtained powders were analyzed by high performance liquid chromatography (HPLC), differential scanning calorimetry (DSC), optical rotation, nuclear magnetic resonance (NMR) spectroscopy and literature information. The (-)-O,O'-di-p-toluoyl-L-tartrate salt (2) of R-ketamine was characterized by specific rotation, melting point (m.p.) and chiral pu...

Embodiment 3

[0108] Example 3: Preparation of (-)-O, O'-di-p-toluoyl-L-tartrate (3) of S-ketamine

[0109] The precipitate from Example 2 was dried under reduced pressure. The solid was dissolved in 100 mL of 40% ethanol solution (i.e., EtOH:H 2 O=2:3), and cooled to room temperature for 1 hour to obtain a solid, which was then dried under vacuum. The powder obtained was analyzed by HPLC, DSC, optical rotation, NMR spectroscopy and literature information. The (-)-O,O'-di-p-toluoyl-L-tartrate salt (3) of S-ketamine was characterized by specific optical rotation, melting point and chiral purity by HPLC as follows:

[0110] c = 1.0, dimethylformamide, chiral purity = 100%. 1 H-NMR (DMSO-d 6 ):7.87(d,4H,J=7.6Hz),7.67(d,1H,J=7.6Hz),7.44(m,3H),7.36(d,4H,J=8.0Hz),5.74(s,2H ), 2.64-2.31(m,2H), 2.39(s,6H), 2.03(s,3H), 1.91-1.59(m,6H).

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Abstract

The present disclosure provides a sustained release pharmaceutical composition comprising ketamine pamoate and a pharmaceutically acceptable carrier thereof. The compositions include aqueous suspensions, solutions, and matrix delivery systems that can provide sustained release for anesthesia, analgesia, or treatment of central nervous system and anti-inflammatory diseases.

Description

technical field [0001] The present disclosure relates generally to dosage forms of ketamine pamoate, and more particularly to sustained release pharmaceutical combinations comprising R,S-ketamine pamoate, S-ketamine pamoate, or R-ketamine pamoate Drugs, and their use in anesthesia, analgesia or treatment of anti-inflammatory and central nervous system diseases. Background technique [0002] Ketamine, namely (2-(2-chlorophenyl)-2-(methylamino)cyclohexan-1-one, is an arylcyclohexylamine derivative and contains equal amounts of S-ketamine and R-ketamine The racemic mixture of ketamine. The molecular weight (MW) of ketamine is 237.73, while the molecular weight of ketamine hydrochloride (HCl) is 274.19. According to human clinical studies, the initial The half-life of the distribution phase is 7 to 11 minutes, and the half-life of the elimination phase is 2 to 3 hours (Way et al., 1982). Ketamine distributes rapidly and has a short duration of action. Therefore, ketamine is usu...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/52A61K9/66A61K31/135A61P25/24
CPCA61K31/135A61P25/24A61K9/0019A61K47/10A61K47/26A61K47/34A61K47/02A61K47/38A61K9/10A61K47/20A61P25/00A61P29/00A61K9/1641
Inventor 林东和文永顺陈嘉宪刘映廷侯睿智吴致榕
Owner ALAR PHARMA INC
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