Dipyridamole self-nanoemulsion preparation and preparation method thereof

Abstract

The invention discloses a dipyridamole self-nanoemulsion preparation and a preparation method thereof, and belongs to the technical field of pharmaceutical preparations. The self-nanoemulsion preparation is prepared from dipyridamole and blank self-nanoemulsion, the blank self-nanoemulsion is prepared from an oil phase, an emulsifier and a co-emulsifier, the dosage of the oil phase is 40-50% of the weight of the blank self-nanoemulsion, and the weight ratio of the emulsifier to the co-emulsifier is 2: 1-4: 1. The preparation method comprises the following steps: preparing the oil phase, the emulsifier and the co-emulsifier into a blank self-nanoemulsion under a stirring condition, adding the dipyridamole, and performing stirring to obtain the drug-loaded self-nanoemulsion. The self-nanoemulsion preparation disclosed by the invention can be spontaneously emulsified in water to form a nanoemulsion solution which is less than 100nm in particle size, clear and uniform in appearance and good in stability, and the precipitation rate of dipyridamole in the stomach and intestine can be reduced after the nanoemulsion is orally taken, so that the oral absorption and bioavailability of the medicine are improved.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to a dipyridamole self-nanometer emulsion preparation and a preparation method thereof. Background technique [0002] Dipyridamole (DIP), also known as dipyridamole, is a yellow crystalline powder that is unstable to light, so it needs to be kept away from light and sealed. Dipyridamole was developed by West Germany Bellinger in 1961 as a coronary vasodilator for the treatment of angina pectoris; in the 1960s, it was discovered that it has anti-platelet and inhibits platelet adhesion and aggregation, and it is clinically used for prevention and treatment Thromboembolic diseases; dipyridamole was subsequently found to have broad-spectrum antiviral and immunomodulatory effects. Recent studies have also found that dipyridamole can reverse the multidrug resistance of tumor cells, and it can be used in combination with antineoplastic drugs have a synergis...

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Problems solved by technology

Patent CN106692067A discloses a solid dispersion containing dipyridamole and an orally disintegrating tablet. The preparation is prepared from dipyridamole, a carrier and an organic solvent by spray drying, wherein the carrier is hydroxypropyl methylcellulose , at least one of polyethylene caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer and hydroxypropyl methylcellulose succinate; the solid dispersion prepared by this method can improve the drug in gastrointestinal fluid However, the degree of crystallization of the inhibitory drug in intestinal juice is limited. In addition, due to the introduction of organic solvents in the preparation process, special spray drying equipment is required, and the production investment cost is relatively high.

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