Application of 11-o-acetylcyathatriol in preparing medicine for preventing and/or treating gastric ulcer

A kind of technology of oxyacetyl bird and niacin triol, applied in the field of medicine, can solve the problems such as no report of anti-stomach ulcer effect and the like

Active Publication Date: 2014-11-19
INST OF MICROBIOLOGY - CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

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  • Application of 11-o-acetylcyathatriol in preparing medicine for preventing and/or treating gastric ulcer
  • Application of 11-o-acetylcyathatriol in preparing medicine for preventing and/or treating gastric ulcer
  • Application of 11-o-acetylcyathatriol in preparing medicine for preventing and/or treating gastric ulcer

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1、1

[0022] The drug efficacy experiment of embodiment 1, 11-oxoacetyl guanine triol (11-O-acetylcyathatriol)

[0023] (1) Effect of 11-oxoacetyl guanidetriol on ethanol-type gastric ulcer in rats

[0024] Select 60 SD rats with a body weight of 160-200g, half male and half female, and randomly divide them into 6 groups: blank control group, model control group, positive drug control group (famotidine group, 50mg / kg), 11-oxoacetyl bird's nest Alkanetriol dose group I (5 mg / kg), 11-oxyacetyl guanide triol dose group II (10 mg / kg) and 11-oxyacetyl guanide triol dose group III (20 mg / kg). Gastrointestinal administration once a day (the blank control group and the model group were given equal volumes of distilled water) for 5 consecutive days. After 2 hours of the last administration, the rats were given absolute ethanol 1ml / 200g by intragastric administration, and the rats were killed after 1 hour. mouse. Laparotomy was performed, the cardia and pylorus were ligated, and 10ml of 4% ...

Embodiment 2、11

[0042] The toxicity test of embodiment 2, 11-oxoacetyl guanine triol

[0043] A 90-day long-term toxicity experiment was carried out with 6-week-old SD rats with half male and half male. The purchased rats were fed for one week, and 160 rats with behavioral characteristics, no abnormal appearance, healthy and lively, and a body weight of 100±10 g were selected for the experiment. Animals were randomly divided into control group and 11-oxoacetyl guanide triol administration group (dose of 5 mg / kg, 10 mg / kg, 20 mg / kg), 40 animals in each group, half of male and female were housed in separate cages. The laboratory is well ventilated, with constant temperature and humidity.

[0044] 11-Oxyacetyl guanine triol was formulated with normal saline to make 5, 10, 20 mg / ml, administered by intragastric administration of 0.1 ml, the control group was given the same dose of normal saline, administered at 9:00 every morning, and weighed once every 15 days body weight and food intake, and ...

Embodiment 3、11

[0052] The preparation of embodiment 3, 11-oxyacetyl guanine triol tablet

[0053] 11-Oxyacetylcyathatriol tablets are composed of the following components: 11-O-acetylcyathatriol (11-O-acetylcyathatriol) 0.5g; excipients stearyl alcohol, magnesium stearate and hydroxypropyl methyl Base cellulose is 49.5g in total.

[0054] Preparation: fully mix the main ingredient and stearyl alcohol, pass through a 100-mesh sieve, add hydroxypropyl methylcellulose (binder) to make a soft material, pass through a 16-mesh sieve, granulate, dry at 40°C, and granulate . Add magnesium stearate to make lubricant, after mixing, tabletting, make 100 altogether, each 0.5g.

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Abstract

The invention provides a novel application of a medicine of 11-o-acetylcyathatriol as shown in the formula I, and in particular relates to an application of 11-o-acetylcyathatriol as shown in the formula I for preparing a medicine for preventing and/or treating gastric ulcer. The experiment shows that 11-o-acetylcyathatriol has a remarkable medicine effect on a mouse ethanol induced gastric ulcer model, a pylorus ligation induced gastric ulcer model and an acetic acid induced gastric ulcer model when the dosage is 20mg/kg; and moreover, the toxicity experiment shows that 11-o-acetylcyathatriol as shown in the formula I is safe and free of toxic or side effect.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to the application of cyathane-type diterpene compound 11-oxyacetylcyathatriol (11-O-acetylcyathatriol) in the preparation of drugs for preventing and / or treating gastric ulcer. Background technique [0002] Gastric ulcer is a chronic ulcer disease that occurs between the cardia and the pylorus. It is a common clinical disease and frequently-occurring disease. According to statistics, about 11% of people have suffered from this disease. If the disease is not treated in time, gastric perforation, gastric bleeding, obstruction and gastric ulcer canceration are prone to occur, which will bring great pain to the patient physically and mentally. Modern drugs used to treat gastric ulcer mainly use proton pump inhibitors and histamine H2 receptor antagonists to inhibit gastric acid secretion, but many adverse reactions have been reported clinically. Therefore, it is urgent to...

Claims

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Application Information

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IPC IPC(8): A61K31/22A61P1/04
Inventor 刘宏伟韩俊杰赵烽宝丽
Owner INST OF MICROBIOLOGY - CHINESE ACAD OF SCI
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