Potassium sodium dehydroandrographolide succinate enteric-coated preparation and preparation method

A technology of Yanhuning intestinal and enteric-coated preparations, which is applied in antiviral agents, pharmaceutical formulas, medical preparations of non-active ingredients, etc., and can solve allergic reactions or pyrogen-like reactions, patients' psychological and physiological resistance, and production process requirements High-level problems, to achieve the effect of protecting active ingredients, increasing the difficulty of quality control, and reducing allergic reactions

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

However, as a traditional Chinese medicine extract, Yanhuning failed to completely remove the tannins and other biomacromolecules in the extraction process, and these macromolecules directly enter the blood circulation after injection, which may easily cause allergic reactions or pyrogens. reaction; at the same time, the residual pyridine in the process of synthesis and refining is also easy to cause side effects
Moreover, compared with oral administration, injection administration is extremely painful, and it is easy to cause psychological and physical resistance of patients, and the medication compliance is poor, which also limits the use of Yanhuning to a certain extent.
[0005] At present, although there are some attempts to make Yanhuning into enteric-coated preparations, because Yanhuning is a neutral drug, it is easy to dissolve in water and unstable under weak acidic conditions. Destruction, resulting in incomplete drug absorption and low bioavailability
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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  • Potassium sodium dehydroandrographolide succinate enteric-coated preparation and preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Example 1: Preparation of refined Yanhuning

[0035] Use the commercially available Chuanhuning, after lipidation reaction with sodium sulfite, then directly synthesize Yanhuning with one of sodium bicarbonate and potassium bicarbonate or according to a specific ratio, so as to reduce repeated drying, dissolving, heating and other processes. The specific preparation method is as follows: taking Chuanhuning as raw material, adding anhydrous sodium sulfite and 90% ethanol into an extraction tank, simultaneously passing nitrogen protection, stirring and mixing, heating in a water bath, and controlling the temperature at 60°C. After the raw materials are dissolved, stop heating and slowly add 19% KHCO 3 and 10% Na 2 CO 3 Mix solution (mixed according to mass ratio 1:1), produce CO 2 gas, crystals are precipitated in the reaction solution, and the CO 2 After the production is completed, heat it in a water bath at a temperature of about 60°C until it dissolves, then add a...

Embodiment 2

[0036] Embodiment 2: preferred isolation layer material

[0037] (1) The composition of Yanhuning enteric-coated preparation is shown in Table 1.

[0038] Table 1 The composition of Yanhuning enteric-coated preparation

[0039]

[0040] When preparing the mixture of lactose and microcrystalline cellulose, the mass ratio of 2:1 is prepared at one time, so for the convenience of operation, the ratio of 2:1 is selected throughout the text. In practice, lactose: microcrystalline cellulose = 1:1 to 3:1 is acceptable. If this ratio is exceeded and the lactose is too high, it may cause difficulty in forming pills and tablets in the later stage.

[0041] (2) Based on the mass fractions of the prescriptions in Table 1, respectively select Yanhuning with different precisions, and different materials and different mass ratios of the isolation layer materials, and carry out the screening of Yanhuning and isolation layer materials. The specific selection is as follows: Table 2 shows....

Embodiment 3

[0056] Example 3: Recipe and preparation method of Yanhuning enteric-coated preparation

[0057] (1) The composition of Yanhuning enteric-coated preparation is shown in Table 4.

[0058] Table 4 The composition of Yanhuning enteric-coated preparation

[0059]

[0060]

[0061] (2) The refined Yanhuning was prepared according to the method of Example 1, and the precision was 99.5%.

[0062] (3) Isolation layer coating. With purified water or 80% ethanol aqueous solution, the isolation layer material is mixed, and it is prepared as a solution with a solid content of 5%, and then the antioxidant cysteine ​​is added to form a solution with a solid content of 5% (in order to control product quality, The solid content needs to be controlled at 3%~15%), stir evenly with an air pump mixer. Pass Yanhuning, lactose, microcrystalline cellulose, and micropowder silica gel through a 200-mesh sieve, and put them into a high-speed centrifugal granulator coating machine to directly c...

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Abstract

The invention belongs to the field of medicine processing, and particularly relates to a potassium sodium dehydroandrographolide succinate enteric-coated preparation and a preparation method. The preparation method comprises the specific steps of forming a specific formula based on the effective component potassium sodium dehydroandrographolide succinate and auxiliary materials acceptable in pharmaceutical science, coating an isolation layer and coating an enteric-coated layer through a specific processing technology, then adding suitable auxiliary materials so as to prepare an enteric-coatedcapsule, enteric-coated particles and enteric-coated dry suspension. The refinement method for potassium sodium dehydroandrographolide succinate greatly reduces impurities and lowers occurrence rate of side effects; the special preparation process and parameter for producing the potassium sodium dehydroandrographolide succinate enteric-coated preparation can effectively protect active components of potassium sodium dehydroandrographolide succinate, thereby guaranteeing the medicine effect of the finished product and improving the bioavailability of oral potassium sodium dehydroandrographolidesuccinate. The preparation method has easy steps, is easy to operate and is suitable for industrial production.

Description

technical field [0001] The invention belongs to the field of pharmaceutical processing, and in particular relates to a Yanhuning enteric-coated preparation and a preparation method thereof. Background technique [0002] Yanhuning (potassium sodium dehydroandrographolide succinate, PSDS) is the sodium salt of potassium half-ester succinate of andrographolide, known as "Chinese medicine antibiotics", with heat-clearing, detoxifying and antiviral effects, mainly used for viral pneumonia and viral infections Respiratory tract infection, can inhibit early capillary permeability increase and inflammatory exudation and edema; has specific excitatory pituitary-adrenal cortex function, can promote the release of ACTH, and increase the biosynthesis of ACTH in the anterior pituitary; The effect of various viruses such as viruses, influenza viruses, respiratory viruses, etc. [0003] However, the general preparation process of Yanhuning used in medicine is as follows: extract andrograp...

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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