Drop pills of oleanolic acid, and preparation method

Abstract

A dripping pill of oleanolic acid for treating chronic metastatic hepatitis 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 a medicine for treating chronic persistent hepatitis prepared from traditional Chinese medicines. Background technique [0002] Oleanolic acid (oleanolic acid) is a pentacyclic triterpenoid compound, which mostly exists in plants in the form of free or glycosides, and its distribution is wide. There are 126 kinds of plants containing oleanolic acid. Oleanolic acid can significantly reduce the serum alanine aminotransferase of animals with experimental liver damage, reduce the degeneration and necrosis of liver cells, the inflammatory response and fibrosis of liver tissue, promote the regeneration of liver cells, and accelerate the repair of necrotic tissue . For the treatment of viral persistent chronic hepatitis, it can significantly improve symptoms, signs and liver function. In addition, it has the effect of correcting protein metabolism disorders. It...

AI Technical Summary

Problems solved by technology

[0003] Oleanolic acid tablets and capsules are currently sold in the market. Because oleanolic acid is insoluble in water and has strong hydrophobicity, the dissolution rate and dissolution rate of oleanolic acid tablets or capsules are low, poor absorption, and low bioavailability. The proportion of excipients is large, it is inconvenient for patients to take it, and the compliance is poor, which affects the therapeutic effect of oleanolic acid

Application number: 03157672.9, application date: 2003.9.6, applicant: Nanchang Hongyi Technology Co., Ltd., invention name: oleanolic acid dripping pills and its preparation method; application number: 03112181.0, application date: 2003.04.21, application ( Patent right) Person: Shandong Provincial Academy of Traditional Chinese Medicine, name of invention: a drug for treating acute and chronic hepatitis and its preparation process. The above two patent documents provide a kind of chronic persistent hepatitis, chronic active hepatitis, primary liver The drop pill medicine of diseases such as cirrhosis, liver poisoning also provides preparation method, and this drop pill medicine uses polyethylene glycol and other auxiliary materials to make drop pill with oleanolic acid fine powder; Although this drop pill overcomes the defect of present tablet, The dissolution rate is accelerated, but the drop pill has the defect that the natural degree of the excipients used is not high

[0004] Current drop pill preparations generally face the following problems: 1. The pure natural degree of drop pill auxiliary materials is not high: at present, most of the drop pill base auxiliary materials are chemical synthetic products, and the natural degree is relatively low. The search for new alternative base auxiliary materials, especially the natural degree The search for high-alternative matrix excipients and the determination of its preparation process are very difficult things, because the preparation conditions required for common and possible natural matrix excipient substitutes are very harsh, and the temperature of the excipients and the drop-pill dripping conditions are all The key to affecting the preparation and molding of dropping 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.