Oral soft capsule compound preparations for curing cold

Abstract

The invention provides a medicine composition. The medicine composition is a soft capsule that can effectively treat cold and comprises active drug components, a solvent and a co-solvent. The soft capsule can not only solve the problems of leakage and crystallization existing in existing preparation and remarkably improve the beneficial effects of the medicine composition. Compared with products sold in the market, the medicine composition provided by the invention has more remarkable stability and better treat result.

Description

technical field [0001] The invention relates to a pharmaceutical composition which can effectively treat colds, and the composition can significantly enhance the preparation stability and clinical effect of the composition. Background technique [0002] As a national basic medical insurance drug, national essential drug and OTC Class A product, Fenmamei Soft Capsule is currently widely used clinically. Due to its definite clinical curative effect, its research and continuous development and discussion are increasingly attracting people skilled in the art. of great interest. [0003] Acetaminophen is the most used in the prescription, and the other two chemical raw materials, dextromethorphan hydrobromide and pseudoephedrine hydrochloride, are used in small amounts and have good solubility, so the preparation is much simpler and easier than acetaminophen and paracetamol is white to off-white crystalline powder state, through the solubility experiment research to raw material...

AI Technical Summary

Problems solved by technology

[0004] WO9805314A teaches the use of propylene glycol, polyethylene glycol 400, water and sodium acetate to dissolve acetaminophen. The ratio of the three is 30%: 40%: 30%, and sodium acetate is also added, which can only dissolve paracetamol at most. 200mg / ml of acetaminophen; if the soft capsule is prepared according to the above concentration, on the one hand, such a large amount of water cannot be used (during the drying process of the soft capsule, the water will migrate into the skin of the soft capsule and be removed); The use of sodium acetate can easily lead to leakage of soft capsules

Illustrate by WO9805314A, low-molecular-weight alcohols are limited to promoting the dissolution of paracetamol in polyethylene glycol solution, even if can further increase the solubility of paracetamol in polyethylene glycol by means of sodium acetate, also still Cannot exceed the limit of 200mg / ml

[0005] Using basic excipients to increase the solubility of liquid preparations containing acetaminophen is easy for those skilled in the art, because acetaminophen water injection uses sodium hydroxide as a solubilizer Yes, but as we all know, the acetaminophen raw material itself can only remain stable under the condition of neutral pH, overacid or overalkaline will cause it to decompose and change color, and the composition is red or even black, although it is easy to However, how to solve the stability problem of acetaminophen while ensuring the solubility remains to be further studied by those skilled in the art

[0006] The carbohydrates or polyhydric alcohols used in CN1348359A just utilize the sweet taste and refreshing feeling brought by it, and the effect is only to cover up the unpleasant taste brought by the active ingredients (including acetaminophen), and the effect is exerted. The reason is that during the chewing process, the soluble components dissolve due to contact with saliva, thereby creating a special way for the active ingredient to be released. The entire document, including the claims and examples, refers to substances that will have an unpleasant taste. Simple physical mixing of the active ingredient with a sweet soluble ingredient followed by micronization, there is no description of how the active ingredient is dissolved throughout the document

[0007] CN1311672A has utilized the method for promoting the dissolving action of acetaminophen in polyethylene glycol solution described in WO9805314A, avoided the propylene glycol with high viscosity and selected ethanol, but the large amount of use of ethanol is obviously not suitable for soft capsule preparations, the reason is as follows : first ethanol is easy to volatilize, on the one hand the preparation of soft capsule and pressing process all need heating and insulation, and the adding of ethanol makes whole process can't realize heating, is not suitable for the preparation requirement of the present invention; On the other hand the characteristic of soft capsule dosage form is just There is always a dynamic between the content and the capsule skin. The moisture in the soft capsule skin enters the content, and the active ingredients and solvents in the content enter the soft capsule skin. If the solvent in the content is in a volatile state, it will After that, it will volatilize, so that the active ingredient crystallizes out due to the large amount of volatilization of ethanol during the drying and storage of the soft capsule, causing the product to be unqualified

[0010] So far, there is no one or literature report on how to solve the solubility and stability problems of acetaminophen at the same time, especially teach us how to realize the stability of the clarified liquid containing acetaminophen with a concentration greater than 200mg / ml. the solution