Andrographolide enteric-coated granule capable of being accurately dissolved out and preparation method

A technology of Yanhuning intestinal and Yanhuning, which is applied in the field of Yanhuning enteric-coated granules and its preparation, can solve the problems of easily causing allergic reactions or pyrogen-like reactions, not being universally applicable, and pyridine easily causing side effects, etc., to achieve Increase the difficulty of quality control, improve the uniformity and reproducibility, and reduce the effect of yield

Active Publication Date: 2018-05-04
HUANGSHAN C KING PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] However, in the prior art, the extracted Yanhuning is administered by injection
As a traditional Chinese medicine extract, Yanhuning failed to completely remove the tannin and other biological macromolecules in the extraction process, and these macromolecules directly enter the blood circulation after injection, which may easily cause allergic reactions or fever. React as it is; at the same time, the residual pyridine in the process of synthesis and refining is also easy to cause side effects
[0004] At present, although there are some attempts to make Yanhuning into enteric-coated granules, because Yanhuning is a neutral drug, it is easy to dissolve in water and unstable under weak acidic conditions. A large amount is released and destroyed in the stomach, and the amount that actually reaches the intestinal tract is very small and the bioavailability is low
At the same time, Yanhuning is very sensitive to water, heat, and light. The pharmaceutical process has high requirements on the production process. Conventional pharmaceutical temperature, time and other parameters are not only not universally applicable to Yanhuning preparations, but may also be due to poor conditions. Appropriate, causing the efficacy to be destroyed, and the effective content in the final product is low

Method used

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  • Andrographolide enteric-coated granule capable of being accurately dissolved out and preparation method
  • Andrographolide enteric-coated granule capable of being accurately dissolved out and preparation method
  • Andrographolide enteric-coated granule capable of being accurately dissolved out and preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Example 1: Preparation of refined Yanhuning

[0028] Commercially available Chuanhuning is used for esterification reaction with sodium sulfite, and then directly synthesized with sodium bicarbonate and potassium bicarbonate or in a specific ratio to reduce repeated drying, dissolution, heating and other processes. The specific preparation method is as follows: using andrographis paniculata as a raw material, adding anhydrous sodium sulfite and 90% ethanol into an extraction tank, while protecting with nitrogen, stirring and mixing, heating in a water bath, and controlling the temperature at 60°C. Stop heating after the raw materials are dissolved, and slowly add 19% KHCO dropwise 3 And 10% Na 2 CO 3 Mixed solution (mixed by mass ratio 1:1) to produce CO 2 Gas, crystals are precipitated in the reaction liquid, wait for CO 2 After the production is completed, heat to dissolve in a water bath at a temperature of about 60°C, and then add an appropriate amount of absolute ethan...

Embodiment 2

[0029] Example 2: Preferable isolation layer material

[0030] (1) The mass fractions of Yanhuning enteric-coated pellets are shown in Table 1.

[0031] Table 1 Yanhuning enteric-coated pellets prescription

[0032]

[0033] As the mixture of lactose and microcrystalline cellulose is prepared at a mass ratio of 2:1, the ratio of 2:1 is selected throughout the text for the convenience of operation. In actual operation, lactose: microcrystalline cellulose=1:1~3:1 can be used. If it exceeds this ratio, the lactose is too high, which may cause difficulties in pelletizing and tableting in the later stage.

[0034] (2) Based on the mass scores of each group in Table 1, select Yanhuning with different precisions and isolation layer materials with different materials and different mass ratios to screen Yanhuning and isolation layer materials. The specific choices are as follows Table 2 shows.

[0035] Table 2 Selection of Yanhuning and isolation layer materials

[0036]

[0037] (3) Coating o...

Embodiment 3

[0049] Example 3: Yanhuning enteric-coated pellets prescription and preparation method

[0050] (1) The formula of Yanhuning enteric-coated pellets is shown in Table 4.

[0051] Table 4 Yanhuning enteric-coated pellets prescription

[0052]

[0053]

[0054] (2) The refined Yanhuning was prepared according to the method of Example 1, with an accuracy of 99.5%.

[0055] (3) Coating of isolation layer. Mix the material of the isolation layer with purified water or 80% ethanol aqueous solution to prepare a solution with a solid content of 5%, and then add the antioxidant cysteine ​​to prepare a solution with a solid content of 5% (in order to control product quality, The solid content needs to be controlled within 3%-15%), and stir evenly with an air pump mixer. Pass Yanhuning, lactose, microcrystalline cellulose, and micro-powdered silica gel through a 200-mesh sieve, and add them to a high-speed centrifugal granulating coating machine to directly coat the isolation layer to reduce th...

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Abstract

The invention belongs to the field of medicine processing, and concretely relates to an andrographolide enteric-coated granule capable of being accurately dissolved out and a preparation method. The preparation method concretely comprises the steps of adopting andrographolide as an effective component, adding pharmacologically acceptable ingredients, forming a specific formula, coating an isolatedlayer and coating an enteric-coated layer through a specific processing technology, and adding appropriate ingredients to prepare into the enteric-coated granule. According to the refined andrographolide preparation method provided by the invention, the generation of impurities is greatly reduced, and the occurrence rate of a side effect is reduced; with a preparation process and parameters special for producing the andrographolide enteric-coated granule, active ingredients of the andrographolide can be effectively protected, a medicine effect of the finished product is ensured, and the andrographolide oral medication bioavailability is improved. The production process provided by the invention is simple in process and easy in operation and industrial production.

Description

Technical field [0001] The invention belongs to the field of medical processing, and specifically relates to a precise dissolution of Yanhuning enteric-coated granules and a preparation method. Background technique [0002] Potassium sodium dehydroandrographolide succinate (PSDS), potassium sodium salt of andrographolide succinate half ester, is known as the "Chinese medicine antibiotic". It has heat-clearing, detoxifying and antiviral effects. It is mainly used for viral pneumonia and viral diseases. Respiratory tract infection, can inhibit early capillary permeability increase and inflammatory exudation and edema; have specific excitement of pituitary-adrenal cortex function, can promote the release of ACTH, increase the biosynthesis of ACTH in the anterior pituitary; it has inactivated glands in vitro The role of viruses, influenza viruses, respiratory viruses and other viruses. [0003] However, in the prior art, the extracted Yanhuning is administered by injection. As a trad...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/50A61K31/365A61K47/38A61K47/10A61P11/00A61P31/12A61P7/10A61P31/14A61P31/16
CPCA61K9/5031A61K9/5047A61K9/5073A61K9/5089A61K31/365
Inventor 司鹏付杰周世文
Owner HUANGSHAN C KING PHARMA
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