Paeonol self-microemulsion preparation and preparation method thereof

Abstract

The invention discloses a paeonol self-microemulsion preparation and a preparation method thereof. The paeonol self-microemulsion preparation is prepared from raw materials in percentage by weight asfollows: 0.1%-35% of paeonol, 5%-70% of oil phase, 5%-80% of an emulsifier and 5%-60% of a co-emulsifier, the liquid self-microemulsion preparation is prepared or a solid self-microemulsion preparation is further prepared from the liquid self-microemulsion preparation and an adsorbent. The paeonol self-microemulsion preparation and the preparation method thereof have the advantages as follows: theproblem of low paeonol solubility is solved, solubility of a drug is greatly increased, and in-vivo bioavailability of the drug is improved; by means of the solid self-microemulsion, softening and oil spilling of a traditional soft capsule can be improved, and stability of the preparation is improved; the required raw materials are easily available, the method is simple and feasible, special equipment is not needed, large-scale industrial production is facilitated, and the economic benefits are remarkable.

Description

technical field [0001] The invention relates to a paeonol self-microemulsion preparation and a preparation method thereof, belonging to the technical field of medicine. Background technique [0002] Paeonol, also known as paeonol, is mainly an active ingredient extracted from the root bark of peony and peony of Ranunculaceae Paeoniae genus and the dry root or whole plant of Rumoaceae Xu Changqing. The chemical name is 2- Hydroxy-4-methoxyacetophenone. It has good pharmacological activities in antibacterial and anti-inflammatory, antipyretic and analgesic, immune regulation, anti-tumor, anti-oxidation and anti-allergic aspects, and has broad development prospects. There are paeonol ointment, paeonol (sodium sulfonate ) injections and paeonol tablets and other preparations are mostly used for cardiovascular and cerebrovascular diseases, tumors, inflammation, allergies and immune system diseases. However, the drug has disadvantages such as volatile, poor water solubility, sho...

AI Technical Summary

Problems solved by technology

However, the drug has shortcomings such as volatile, poor water solubility, short half-life in vivo, and low bioavailability. In recent years, research on its new dosage form has become increasingly active.

[0003] The apparent oil-water partition coefficient of paeonol is 2.4 ~ 2.6, which belongs to the second class drug in the biopharmaceutics classification system (BCS), and its solubility can be improved by appropriate solubilization technology. The key point is that although the purpose of improving solubility can be achieved theoretically, there are many ways to increase solubility in the existing technology, but there is a lack of a practical technical means that is simple, easy to implement, high in yield, low in cost and significant in effect, which has become an obstacle Barriers to new formulation development

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