Drop pills of vanillin fine powder and preparation method

Abstract

A dripping pill of vanillin powder for treating convulsion features high natural level and safety and low toxic by-effect. Its preparing process is also disclosed.

Description

technical field [0001] The invention relates to the field of medicine, in particular to an anticonvulsant drug made from vanillin fine powder. Background technique [0002] Animal experiments have confirmed that vanillin can significantly reduce the spontaneous activity of mice, prolong the hypnotic time of cyclohexobarbital sodium, and can resist convulsions caused by pentylenetetrazol in mice, but it has no effect on convulsions caused by electric shock in mice; It can resist the epileptic brain waves induced by pentylenetetrazol in rabbits. Vanillin is mainly absorbed through the intestinal tract, with an absorption rate of over 98%, and a serum protein binding rate of 71%±1%. It easily passes through the blood-brain barrier and is mainly excreted through the kidneys. It is clinically used for petit mal seizures and as an adjuvant drug for various types of epilepsy. [0003] Only vanillin tablets are currently sold. Vanillin has a fragrance, is unstable to light, and i...

AI Technical Summary

Problems solved by technology

Vanillin has a fragrance, is unstable to light, and is slightly soluble in water. The disintegration time of vanillin tablets is long, the dissolution rate and dissolution rate are low, the absorption is poor, the bioavailability is low, the amount of excipients is large, and it is inconvenient for patients to take it. Poor compliance, affecting the therapeutic effect of vanillin

Application number: 03159200.7 Application date: 2003.9.10, applicant: Nanchang Hongyi Technology Co., Ltd., name of invention: vanillin dripping pills and its preparation method The patent literature provides the use of polyethylene glycol and other auxiliary materials to make vanillin fine powder The method that becomes drop pill; Although this drop pill overcomes the defect of present tablet, has accelerated dissolution speed, but the defect that the natural degree of the adjuvant that this drop pill exists is not high

[0004] With the global expansion of the market and the requirement of human beings to return to nature, the use of drugs with low toxicity and side effects, especially pure natural drugs, has become the first choice of people. The preparation is a kind of high-efficiency, quick-acting new Chinese medicine preparation, which overcomes the shortcomings and deficiencies of the previous Chinese medicine preparations, but the current drop pill preparations generally face the following problems: 1. The natural degree of drop pill auxiliary materials is not high: at present, the drop pill matrix Most of the excipients are chemical synthetic products with a low degree of naturalness. It is very difficult to find new alternative matrix excipients, especially the search for alternative matrix excipients with a high degree of naturalness and the determination of their preparation process, because currently common and possible The preparation conditions required for the substitutes of natural matrix excipients are very harsh, and the temperature of excipients and the droplet dripping conditions are the key factors affecting the preparation of droplet pills

If the melting temperature of the excipient is too high, the viscosity will be low and the plasticity will be poor. If the melting temperature of the excipient is too low, although the plasticity is strong, the dropping pills have disadvantages such as easy sticking and deformation. The accessories are very hard work

2. Problems encountered in the export of dripping pills: With the development of the economy, the market is becoming more and more internationalized, and China is also trying to adapt to this trend. Currently, Chinese medicine dripping pills, which are used as health food, have been successfully exported to many countries, but There are also many problems at present, because different countries have different approvals for the excipients selected for the preparation of Chinese medicine dripping pills, especially in Europe with developed industries, which have stricter regulations on food excipients and pharmaceutical excipients, and the drops exported as health food The chemically synthesized auxiliary materials (such as polyethylene glycol) selected for pill preparations are not listed in the food additive catalogs of some countries, which is very unfavorable for Chinese medicine dripping pill preparations to enter the international market, and has become a stumbling block for Chinese medicine to enter the international market. Therefore, looking for One or more new matrix excipients that can be accepted by the international market are particularly important and urgent

3. Disadvantages of mouthfeel and speed of onset of action: Poor taste of traditional Chinese medicine and its preparations is one of its major characteristics. When people take certain medicines, they are far more afraid of the bad taste of the medicine than they are of the disease. What's more, some patients give up the treatment of traditional Chinese medicine because they can't overcome the bad taste or smell of traditional Chinese medicine or its preparations. For example, making the medicine into capsules or sugar-coated tablets can improve the taste and reduce stimulation, but the disintegration speed is prolonged. , which is not conducive to the rapid onset of the drug, and is not suitable for some diseases, especially those that require the rapid onset of the drug

4. Difficult preparation process for industrial production of dripping pills: In the replacement process of dripping pill preparation auxiliary materials, it is very difficult to determine the preparation process for industrial production, such as the melting temperature of matrix auxiliary materials, dripping temperature, auxiliary materials and The ratio of the drug, the ratio of the caliber of the dropper, and the condensing agent are all factors that affect the drop pills. Therefore, it is time-consuming and expensive to replace the matrix and be suitable for industrial production.

[0005] In order to change the long-term situation that the base auxiliary materials of dropping pills are mainly chemically synthesized auxiliary materials, solve the problem that the base of dropping pills is currently facing a low degree of naturalness, which is increasingly unable to satisfy people. It is required to return to nature, take the problem of pure natural medicine with low toxicity and no side effects; it can also solve some problems encountered in the export process of Chinese medicine preparations, especially dripping pill preparations, and enhance the competitiveness of the international market; A large number of experiments and research on preparation technology have invented a pure Chinese medicine dripping pill preparation with low toxic and side effects, significant curative effect, moderate price and suitable for industrialized large-scale production.

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