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Dropping pills containing ubenimex and method for preparing the same

A technology of ubimethoxine and dripping pills, applied in the field of medicine, can solve the problems of low degree of pure naturalness, low dissolution rate and dissolution rate, and low degree of pureness of the excipients of dripping pills, so as to reduce the irritating smell of drugs, improve the The effect of high oral pH and pure natural degree

Inactive Publication Date: 2008-06-11
TIANJIN TASLY PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Ubenimex is odorless, bitter in taste, and slightly soluble in water. Its capsule disintegrates for a long time, has low dissolution rate and dissolution rate, poor absorption, low bioavailability, and a large proportion of excipients. Children, the elderly, and bedridden patients It is inconvenient to take and poor compliance for patients with dysphagia, which affects the therapeutic effect of Ubenimex
Application number: 200310100917.0, application date: 2003.10.8, applicant: Nanchang Hongyi Technology Co., Ltd., invention name: Ubenimex dripping pills and its preparation method The patent literature provides a drop pill preparation and its preparation method, The drop pill medicine uses polyethylene glycol and other auxiliary materials to make Ubenimex into drop pills; although the drop pill overcomes the defects of the current preparation and accelerates the dissolution rate, the drop pill has the natural degree of the auxiliary materials used. defect
[0005] 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 dropping pill preparation is a new type of Chinese medicine preparation with high efficiency and quick effect. The shortcomings and deficiencies of traditional Chinese medicine preparations in the past, but the current drop pill preparations generally face the following problems: 1. The drop pill auxiliary materials are not purely natural: at present, most of the drop pill base auxiliary materials are chemically synthesized, and the natural degree is low. New alternatives The search for matrix excipients, especially the search for alternative matrix excipients with a high degree of naturalness and the determination of their preparation process, is also very difficult, because the preparation conditions required for common and possible substitutes for natural matrix excipients are very harsh. And its dripping pill dripping conditions are the key to affect the preparation of dripping 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.
[0006] In order to change the long-term situation that the base excipients of drop pills are mainly chemically synthesized excipients, and solve the problem that the base of drop pills is currently facing a low level of naturalness, it is increasingly unable to meet people's requirements for returning to nature, taking pure natural medicines 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; the present invention has invented a toxic and side effect through a large number of experiments and research on preparation technology. Pure Chinese medicine dripping pill preparation with low cost, significant curative effect, moderate price, and suitable for industrialized large-scale production

Method used

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  • Dropping pills containing ubenimex and method for preparing the same
  • Dropping pills containing ubenimex and method for preparing the same
  • Dropping pills containing ubenimex and method for preparing the same

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0058] (a) Take ubenimex fine powder 6.0g, xylitol 18.3g, starch 6.7g for later use;

[0059] (b) Mix xylitol and starch evenly, add the above-mentioned ubenimex fine powder and mix thoroughly, heat and melt the mixture at 64°C, and stir evenly for 10 to 30 minutes, keep warm, drip at 64°C, The caliber of the dropper is 1.2-2.5 mm, drop into the methyl silicone oil at 30°C to make 1000 drop pills, drain the drop pills and wipe off the cooling liquid, and the product is ready.

Embodiment 2

[0061] (a) Take 20g of ubenimex fine powder, 76.9g of lactitol, and 23.1g of starch for later use;

[0062] (b) Mix lactitol and starch evenly, add the above-mentioned ubenimex fine powder and mix thoroughly, heat and melt the mixture at 64°C, stir evenly, and stir for 10 to 30 minutes, keep warm, drip and drip at 64°C The caliber of the tube is 1.2-2.5 mm, drop into the methyl silicone oil at 45°C to make 3000 drop pills, drain the drop pills and wipe off the cooling liquid, and the product is ready.

Embodiment 3

[0064] (a) Take ubenimex fine powder 40g, xylitol 71.4g, and gum arabic 28.6g for later use;

[0065] (b) Mix xylitol and gum arabic evenly, add the above-mentioned ubenimex fine powder and mix well, heat and melt the mixture at 64°C, stir evenly, keep stirring for 10-30 minutes, keep warm, and drop at 64°C 1. The caliber of the dropper is 1.2-2.5 mm, drop into the methyl silicone oil at 35°C to make 4000 drop pills, drain the drop pills and wipe off the cooling liquid to get final product.

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Abstract

The invention provides a medicament which can enhance immune function. 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.

Description

technical field [0001] The invention relates to the field of medicine, in particular to a dropping pill containing ubenimex and a preparation method thereof. Background technique [0002] Ubenimex is a compound isolated from the culture fluid of Streplomyces of ivorecticuli, which can competitively inhibit aminopeptidase B (aminopeptidase B) and leucineaminopeptidase (Leucineaminope Ptidase). Enhance the function of T cells, enhance the killing activity of NK cells, and increase the synthesis of colony-stimulating factors to stimulate the regeneration and differentiation of bone marrow cells, interfere with the metabolism of tumor cells, inhibit tumor cell proliferation, and induce tumor cell apoptosis. Activate the immune function of human cells, stimulate the production and secretion of cytokines, and promote the production and proliferation of anti-tumor effector cells. [0003] Ubenimex is well and rapidly absorbed after oral administration, and the plasma concentration...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/198A61K9/20A61K47/40A61K47/38A61K47/36A61K47/26A61P35/02A61P35/00A61P37/04A61J3/06
Inventor 李永强郑永锋
Owner TIANJIN TASLY PHARMA CO LTD
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