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Treatment medicament for resisting infectious diseases, and preparation method and application thereof

A technology for infectious diseases and therapeutic drugs, applied in the field of medicine, can solve the problems such as the preparation method and use of crystalline hydrate that have not been reported

Active Publication Date: 2011-08-17
刘力
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

For example, the following literatures elaborate on it from different aspects: Peng Jingqi, Observation of the curative effect of new houttuyfonate sodium in the treatment of 28 cases of progressive psoriasis, Practical General Medicine, 2005, 5: 439-40; Qiu Cuiqin, etc., New Medicine, 1979, 12: 601-602; Du Aifang et al., Study on the treatment of clinical mastitis of cows with synthetic houttuyniatin, Journal of Zhejiang Agricultural Sciences, 1997, 3: 165-8; Observation on the curative effect of new houttuyn sodium in treating common acute infectious diseases in children , Chinese Journal of Traditional Chinese and Western Medicine, 2005, 11:76; Zhao Zhigang et al., In Vitro Antibacterial Activities of Berberine Hydrochloride, Houttuyfonate Sodium and Allicin, Chinese Journal of Clinical Pharmacology, 2005, 3:119-121; Yuan Lujiang , et al., Research on the relationship between surface activity and antibacterial ability of houttuyniatin homologues, Journal of Traditional Chinese Medicine; 2004, 6: 7-9; Chinese Proprietary Medicine, 2006, 6:895-6; HPLC Determination of the Content of New Houttuyniatin Raw Materials, Chinese Medicinal Materials, 2001, 8:595-6; Research on the inhibitory effect of liver cancer, Journal of Zhongshan Medical College, 1984, 2: 35-39; however, their crystalline hydrates and their preparation methods and uses have not been reported yet

Method used

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  • Treatment medicament for resisting infectious diseases, and preparation method and application thereof
  • Treatment medicament for resisting infectious diseases, and preparation method and application thereof
  • Treatment medicament for resisting infectious diseases, and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0061] Example 1: Sodium caproyl acetaldehyde sulfite monohydrate C 10 h 20 C(O)CH 2 CH(OH)SO 3 Na·H 2 O) Preparation

[0062] Put 28 grams of decanoyl acetaldehyde in a 250ml eggplant-shaped flask, stir to dissolve, add 30g of saturated aqueous solution of sodium bisulfite, control the temperature between 20-60°C, stir and react for 1-4 hours, cool down, place, The residue was crystallized with 500ml of ethanol, 100ml of water, and 20ml of methanol, cooled to below 15°C, and placed until the solid was fully separated out, filtered with suction, washed with water and ethyl acetate, filtered with suction, dried, and the solid was washed with ethanol / water (volume Ratio about 0.5:1) about 400-600ml and about 5ml of 1,4-dioxane for recrystallization, cooling to below 15°C, standing until the solid is fully separated, suction filtering, drying to obtain a solid, solid 42 After drying at about ℃ for about 6 hours, 22 g of off-white crystals were obtained, melting point: decomp...

Embodiment 2

[0075] Embodiment 2: caproyl acetaldehyde sodium sulfite 1 hydrate (C 12 h 23 NaO 5 S·H 2 O) Preparation

[0076] Put 22g of methyl nonyl ketone into a 500ml eggplant-shaped bottle, add 30ml of anhydrous ether, 16ml of absolute ethanol, and 80ml of benzene, add 3.6g of sodium metal under stirring, heat, stir to dissolve, and control the temperature 20-60 Between ℃, add 19ml of dry ethyl formate, stir for 4 hours, add acetic acid to make it acidic, separate the water layer, then extract with ether and benzene, combine the organic layer, evaporate the organic layer under reduced pressure, add hydrogen sulfite dropwise Saturated aqueous solution of 20 g of sodium, stirred for 1 h, cooled the reactant to below 15°C, left to stand until the solid was fully separated out, filtered with suction, washed with water and ethyl acetate, filtered with suction, and the solid was washed with ethanol / water (volume ratio 4:1 ) about 400-600ml and about 5ml of 1,4-dioxane for recrystallizat...

example 1

[0089] Reference Example 1: Preparation of Houttuyfonate Sodium Anhydrate

[0090] Take a small amount of the solid product of Example 2 and dry it in vacuum at about 82°C in the presence of phosphorus pentoxide for more than 12 hours, let it cool, and place it for 12 hours to obtain houttuyfonate sodium anhydrous.

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PUM

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Abstract

The invention relates to a treatment medicament for resisting infectious diseases, and a preparation method and application thereof, in particular to an alkyl acyl acetaldehyde sulfite derivative and a preparation method and application thereof. The derivative has the high storage stability, and is suitable for preparing medicaments for treating or preventing respiratory tract infection of human or animals, urogenital system infection, gastrointestinal tract bacterial infection, the infection of enterocoelia, pelvic cavity, biliary tract and typhia, injection of bones and joints, skin soft tissue infection, septicemia, cervicitis, sinusitis, tympanitis, blepharitis, conjunctivitis and psoriasis which are caused by Gram-positive or negative bacterial sensitive bacteria, virus, chlamydia, mycoplasma and fungi and liver cancers and enhancing immunity.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a therapeutic drug for anti-infective diseases, that is, crystalline hydrate of alkyl acetaldehyde sulfite and its preparation method and application. Background technique [0002] So far, the published literature has only reported capricoylglyoxal sodium sulfite (sodium houttuyfonate, sodiumhouttuyfonate, C 12 h 23 NaO 5 S, molecular weight: 302.36) and sodium lauryl acetaldehyde sulfite (sodium neohouttuydine, Sodium lauroyl-α-hydroxyethyl sulfonate, C 14 h 27 NaO 5 S. Molecular weight: 330.42), etc. For example, the following literatures elaborate on it from different aspects: Peng Jingqi, Observation of the curative effect of new houttuyfonate sodium in the treatment of 28 cases of progressive psoriasis, Practical General Medicine, 2005, 5: 439-40; Qiu Cuiqin, etc., New Medicine, 1979, 12: 601-602; Du Aifang et al., Study on the treatment of clinical mastitis of cows w...

Claims

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Application Information

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IPC IPC(8): C07C309/08C07C303/32A61K31/185A61P31/04A61P31/12A61P31/10A61P31/00A61P37/02A61P35/00A61P1/16
CPCA61K31/185C07C309/08A61K9/0019A61P1/16A61P31/00A61P31/04A61P31/10A61P31/12A61P35/00A61P37/02A61P37/04A61P43/00
Inventor 刘力
Owner 刘力
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