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Preparation method and applications of rabeprazole sodium liposome

A technology of rabeprazole sodium lipid and rabeprazole sodium, which is applied in the field of preparation of rabeprazole sodium liposomes, can solve the problems affecting the safety, effectiveness, moisture absorption and discoloration of preparations, and the lack of light and heat. Stability and other issues, to achieve the effects of long drug action time, inhibition of gastric acid secretion, and protection of gastric mucosa

Inactive Publication Date: 2016-10-19
邓学峰
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Since rabeprazole sodium raw material is sensitive to light, heat and humidity, it is easy to absorb moisture and change color, and it is not stable under light and heat, thus affecting the safety and effectiveness of the final preparation. How to solve this problem in the preparation process becomes the key point of the preparation. Key and Difficulties

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0016] Specific Embodiments Example 1 Weigh lecithin and cholesterol at a molar ratio of 2:1, add rabeprazole sodium composition to 4mL of absolute ethanol in a water bath at 55°C until dissolved, and inject 20mL of pH6. In the hydration medium of 0-8.0 phosphate buffer solution, stir and hydrate for 30 minutes, remove ethanol by rotary evaporation (55°C, vacuum degree 0.1MPa), cool rapidly, and homogenize under ultra-high pressure (pressure 25000PSI, cycle 2-4 times), Then freeze-dry, that is.

Embodiment 2

[0017] Example 2 Rabeprazole sodium tablet 20mg (calculated as rabeprazole sodium) Prescription: 1000 parts of rabeprazole sodium liposome, 500g lactose, 1000g crospovidone, 1000g magnesium stearate, made 1000 pieces.

[0018] Preparation method: Take rabeprazole sodium liposome, lactose, crospovidone, and magnesium stearate according to the prescription amount, mix them evenly, and directly compress them into tablets to obtain tablets.

Embodiment 3

[0019] Example 3 Rabeprazole sodium capsule 20 mg (calculated as rabeprazole sodium) Prescription: 1000 parts of rabeprazole sodium liposome, 2000 g of microcrystalline cellulose, 1000 g of sodium carboxymethyl starch, 1000 g of magnesium stearate , made into 1000 capsules.

[0020] Preparation method: Weigh rabeprazole sodium liposome, microcrystalline cellulose, sodium carboxymethyl starch, and magnesium stearate according to the prescription, mix them evenly, and fill them in a capsule machine to obtain capsules.

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PUM

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Abstract

The invention provides a preparation method and applications of rabeprazole sodium liposome. The preparation method is characterized in that lecithin and cholesterol are adopted as film materials and an ethanol injection method is adopted to encapsulate a rabeprazole sodium composition into the rabeprazole sodium liposome. According to the present invention, the rabeprazole sodium liposome has characteristics of targeting property, slow releasing property, cell affinity, histocompatibility, no toxicity, and drug stability increasing; the obtained preparation has characteristics of high stability, low side effect and long drug acting time, and further has effects of gastric acid secretion inhibiting, gastric mucosa protecting, and Helicobacter pylori killing; and with the application of the ethanol injection method to prepare the rabeprazole sodium liposome, the continuous production can be achieved, and the industrialized requirement can be well met, such that the broad application prospects are provided in the field of medicine.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a preparation method and application of rabeprazole sodium liposome. Background technique [0002] Rabeprazole sodium is a proton pump inhibitor anti-ulcer drug. It is the sodium salt form of rabeprazole. It was first successfully developed by Japan's Eisai company. The trade name is Polite, the role of proton pump inhibitors It is to reduce gastric acid secretion and stabilize the lesion, so as to achieve the effect of curing gastric and duodenal ulcer and gastroesophageal reflux disease. It is mainly used clinically to treat acid-related diseases, such as gastric and duodenal ulcers, peptic ulcers, gastroesophageal reflux disease, and Zoller-Ellison syndrome. [0003] Rabeprazole is a benzimidazole substitute that inhibits gastric acid secretion by binding to the proton pump of gastric lining cells. This product specifically inhibits the action of ATPase, which is a key enzy...

Claims

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Application Information

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IPC IPC(8): A61K33/00A61K9/127A61P1/04A61P31/04A61K31/4439A61K31/4164
Inventor 邓学峰耿华靖刘澎
Owner 邓学峰