Dropping pills containing Isocarboxazid and method for preparing the same

Abstract

The invention provides an isocarboxazid dripping pill and a process for preparation. The invention overcomes the shortcomings of the prior dripping pills that pure natural degrees of findings which are used by the prior dripping pills are not high, and chemosynthesis findings which are commonly used are not in food additives catalogs of some countries, and tastes of the dripping pills are worse. The invention is a pharmaceutical preparation whose natural degree is higher, safety is stronger, and side effect is lower. The medicament is mainly used to depressive patients who are resistant to tricyclic antidepressants. The invention is effective on depression with anxiety and hysteria.

Description

technical field [0001] The invention relates to a pharmaceutical preparation and a preparation method thereof, in particular to an isocarboxazid dripping pill and a preparation method thereof. Background technique [0002] Isocarboxazid is a monoamine oxidase inhibitor antidepressant, which irreversibly combines with monoamine oxidase A and B in the brain and affects the metabolism of monoamine neurotransmitters. Norepinephrine and 5-hydroxytryptamine) content increased, play an antidepressant effect. Isocarboxazid is well absorbed from the gastrointestinal tract and oxidatively metabolized in the liver. The plasma concentration reaches the peak value 3-5 hours after oral administration, and the action time lasts for 10 days, and the metabolites are excreted by the kidneys. Animal experiments have shown that isocarboxazid can be excreted in milk. Currently, only tablets are available on the market, and it is clinically used in patients with depression who are ineffective ...

AI Technical Summary

Problems solved by technology

[0003] Isocarboxazid has a weak odor and is slightly soluble in water. Its tablet disintegration time is long, the dissolution rate and dissolution rate are low, the absorption is poor, the bioavailability is low, and the proportion of excipients is large. Children, the elderly, and bedridden patients It is inconvenient to take and poor compliance for patients with dysphagia, which affects the therapeutic effect of isocarboxazid

Application number 200310100913.2, date of application: 2003.10.8, applicant: Nanchang Hongyi Technology Co., Ltd., name of invention: Isocarboxazid dripping pills and its preparation method The patent literature provides a drop pill preparation and its preparation method. The drop pill overcomes the defect of the present tablet and accelerates the dissolution rate, but the drop pill has the defect that the natural degree of the adjuvant used 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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