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Method for modifying bitter taste of berberine, berberine hydrochloride and related compound preparations

A technology of berberine hydrochloride and compound preparations, which is applied in the directions of pharmaceutical formulations, medical preparations without active ingredients, and medical preparations containing active ingredients.

Inactive Publication Date: 2012-12-12
SHANGHAI ZHANGJIANG ENG RES CENT OF MODERN PREPARATION TECH OF TRADITIONAL CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Taste-masking research on (hydrochloric acid) berberine and traditional Chinese medicine compound containing (hydrochloric acid) berberine by ion exchange resin method, has not been reported yet

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0017] Embodiment 1: the bitter taste of berberine covered by ion exchange resin method

[0018] Berberine has significant antibacterial ability, but due to its strong bitter taste, it is mainly used in clinically as conventional tablets and capsules. Its bitter taste hinders the development of new dosage forms of berberine and limits its use in children and elderly patients.

[0019] Adopting the method of the present invention is: get the berberine that purity is 98%, be dissolved in pure water, add IRP88 type cation exchange resin in the berberine aqueous solution, the pH of regulating solution is 5, and the cation exchange resin consumption is berberis 0.6 times the amount of alkali, stirring and dispersing at 25°C for 2.0 h, effectively masked the bitterness of the berberine solution.

[0020] The mouthfeel before and after taste masking was compared by manual evaluation method. The results are shown in Table 1. After taste masking by ion exchange resin, the taste of ber...

Embodiment 2

[0029] Embodiment 2: ion exchange resin method covers the bitter taste of berberine hydrochloride

[0030] Adopting the method of the present invention is: get the berberine hydrochloride that purity is 98%, be dissolved in pure water, add D155 type cation exchange resin in the berberine hydrochloride aqueous solution, the pH of regulating solution is 4.0, and the cation exchange resin consumption is 1.2 times the amount of berberine, stirring and dispersing at 45°C for 0.5 h at a constant temperature effectively masked the bitterness of the berberine hydrochloride solution.

[0031] The mouthfeel before and after taste masking was compared by manual evaluation. The results are shown in Table 3. After taste masking with ion exchange resin, the taste of berberine hydrochloride solution changed from a strong bitter taste, which was immediately spit out, to a taste that just felt bitter, and the taste masking effect was remarkable.

[0032]

[0033] Table 3 The mouthfeel before ...

Embodiment 3

[0040] Embodiment 3: Ion-exchange resin method covers the bitter taste of traditional Chinese medicine compound Xiexin Decoction

[0041] Coptis chinensis is the dried rhizome of Coptis chinensis and Coptidis triangularis in Ranunculaceae. Berberine is one of the main active ingredients and the main source of bitterness of the medicinal material.

[0042] The traditional Chinese medicine compound Xiexin Decoction, recorded in the volume of "Synopsis of the Golden Chamber", is a famous and important prescription. It is composed of rhubarb, Coptis chinensis and Scutellaria baicalensis. Its commercially available products are capsules and granules. Capsules are difficult to swallow for special groups (about 1 / 4 of patients) who have difficulty swallowing solid preparations, such as children or elderly patients. The heavier ones, although sweeteners are added to cover up the taste, can easily cause a bitter and sweet smell, which seriously affects children's compliance with medica...

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PUM

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Abstract

The invention discloses a method for modifying bitter taste of berberine, berberine hydrochloride and related compound preparations. The method includes: adding cation exchange resin into berberine (hydrochloride) water solution or compound water solution containing berberine (hydrochloride), and stirring to separate for 0.5-3.0 hours at 15-45 DEG C, wherein pH of the water solution is 4-7 and the amount of the cation exchange resin is 0.6-10 times as much as that of berberine. The method is low in accessory amount, fine in reproducibility, high in adaptability, and has no side effects and no interference to release of principal components of drugs, and can effectively improve taste of berberine (hydrochloride) and compounds containing berberine (hydrochloride).

Description

technical field [0001] The invention belongs to the technical field of traditional Chinese medicine preparations, and in particular relates to a method for improving the bitterness of berberine, berberine hydrochloride and related compound preparations by using a cation exchange resin. Background technique [0002] Berberine is an alkaloid with a typical bitter taste, mostly in the form of hydrochloride, called berberine hydrochloride. (hydrochloric acid) berberine has significant antibacterial activity. It exists in many traditional Chinese medicines, such as Coptis chinensis, Cortex Phellodendron, Sangezhen, Gongluomu, and Huangteng, and is the main active ingredient of this medicinal material. Due to the strong bitterness of berberine (hydrochloride), the taste of its monomer preparation or the compound preparation of traditional Chinese medicine containing berberine (hydrochloride) is very poor, which seriously affects the compliance of drug application. According to th...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/32A61K31/4375A61K36/29A61K36/59A61K36/718A61K36/756
Inventor 王优杰徐德生梁爽冯怡阮克锋
Owner SHANGHAI ZHANGJIANG ENG RES CENT OF MODERN PREPARATION TECH OF TRADITIONAL CHINESE MEDICINE
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