Light-stabilized pharmaceutical composition, and preparation method and pharmaceutical application thereof

A composition and drug technology, applied in the field of medicine, can solve problems such as easy decomposition

Active Publication Date: 2020-02-28
HUNAN DONGTING PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0011] In addition, it is known that lorazepam is sensitive to light and is easily decomposed when exposed

Method used

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  • Light-stabilized pharmaceutical composition, and preparation method and pharmaceutical application thereof
  • Light-stabilized pharmaceutical composition, and preparation method and pharmaceutical application thereof
  • Light-stabilized pharmaceutical composition, and preparation method and pharmaceutical application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0109] Embodiment 1: Preparation of lorazepam

[0110] Step 1, acetoxylation reaction prepares the acetoxy compound of formula II

[0111] Add 1 mol (305 g) of the ketone base of formula I, 14 mol of glacial acetic acid, 2.5 mol of potassium acetate, 1.8 mol of potassium persulfate, and 2.5 mol of iodine into the reaction flask, stir at 80°C to react for 7 hours, then distill under reduced pressure at 65°C Remove the acid solution; then add ethyl acetate (4 times the amount of the ketone base), 5% sodium thiosulfate solution (6 times the amount of the ketone base) in the reaction flask, stir for 25 minutes, let stand layer; collect the organic layer, extract the aqueous layer twice with ethyl acetate, combine the organic layers, add 1.25 times the volume of saturated sodium chloride solution therein, stir for 25 minutes, let stand to separate the layers, and separate the organic layer; the organic layer Add medicinal charcoal (0.75%), stir and decolorize at 65°C for 25 minu...

Embodiment 2

[0116] Embodiment 2: Preparation of lorazepam

[0117] Step 1, acetoxylation reaction prepares the acetoxy compound of formula II

[0118]Add 1 mol (305 g) of ketones of formula I, 15 mol of glacial acetic acid, 2 mol of potassium acetate, 2 mol of potassium persulfate, and 2 mol of iodine into the reaction flask, stir at 70°C to react for 8 hours, then distill off the acid solution at 70°C under reduced pressure Then add ethyl acetate (3 times of the ketone-based charging capacity), 5% sodium thiosulfate solution (7 times of the ketone-based charging capacity) in the reaction flask, stir for 20 minutes, leave standstill and make layering; collect Extract the organic layer and the aqueous layer twice with ethyl acetate, combine the organic layers, add 1 times the volume of saturated sodium chloride solution to it, stir for 20 minutes, let stand to separate the layers, and separate the organic layer; the organic layer is used for medicinal purposes Charcoal (0.5%), stirred a...

Embodiment 3

[0123] Embodiment 3: Preparation of lorazepam

[0124] Step 1, acetoxylation reaction prepares the acetoxy compound of formula II

[0125] Add 1 mol (305 g) of ketones of formula I to the reaction flask, 12 mol of glacial acetic acid, 3 mol of potassium acetate, 1.5 mol of potassium persulfate, and 3 mol of iodine, stir at 90°C to react for 6 hours, then distill off the acid at 60°C under reduced pressure solution; then add ethyl acetate (5 times of the ketone-based feeding amount), 5% sodium thiosulfate solution (5 times of the ketone-based feeding amount) in the reaction flask, stir for 30 minutes, and let stand to make stratification; Collect the organic layer, extract the aqueous layer twice with ethyl acetate, combine the organic layers, add 1.5 times the volume of saturated sodium chloride solution to it, stir for 30 minutes, let stand to separate the layers, and separate the organic layer; add medicine to the organic layer Use charcoal (1%), stir and decolorize at 60...

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Abstract

The invention relates to a light-stabilized pharmaceutical composition, and a preparation method and pharmaceutical application thereof. Specifically, the pharmaceutical composition comprises a lorazepam crystal and pharmaceutical adjuvants. The lorazepam crystal is radiated by Cu-K alpha. In a powder X-ray diffraction pattern expressed by an angle of 2 theta, there are diffraction peaks at approximately 12.17 degrees, approximately 14.15 degrees, approximately 15.27 degrees, approximately 16.84 degrees, approximately 17.91 degrees and approximately 20.81 degrees. For example, the crystal hasdiffraction peaks at approximately 7.93 degrees, approximately 9.04 degrees, approximately 12.17 degrees, approximately 14.15 degrees, approximately 15.27 degrees, approximately 16.84 degrees, approximately 17.91 degrees, approximately 20.81 degrees, approximately 21.44 degrees and approximately 26.38 degrees. A new crystal form and the pharmaceutical composition, which are used for preparing lorazepam and prepared by the method, exhibit excellent properties as described in the description of the invention.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to a preparation method of benzodiazepine drug lorazepam. It also relates to lorazepam prepared by the method, and its use in drugs with anxiolytic, antiepileptic, anticonvulsant and sedative hypnotic effects. The lorazepam of the present invention presents a new crystal form. Furthermore, the present invention also relates to a light-stabilized lorazepam pharmaceutical composition and its preparation method and pharmaceutical application. Background technique [0002] Loarzepam, molecular formula C15H10Cl2N2O2, molecular weight 321.16, chemical name: 7-chloro-5-(2-chlorophenyl)-1,3-dihydro-3-hydroxy-2H-1,4-benzo Diazepine-2-one, its chemical structural formula is: [0003] [0004] Lorazepam is white or off-white crystalline powder; odorless; lorazepam is slightly soluble in ethanol and almost insoluble in water. [0005] Lorazepam, also known as lorazepam, lorazepam and lora...

Claims

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Application Information

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IPC IPC(8): A61K31/5513C07D243/26C07D243/24A61P25/22A61P25/08A61P25/20
CPCA61K31/5513C07D243/26C07D243/24A61P25/22A61P25/08A61P25/20C07B2200/13
Inventor 王波侯奇伟冯建辉
Owner HUNAN DONGTING PHARMA
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