New type slightly soluble oral medicine self-emulsification preparation and preparation method thereof

Abstract

The invention provides a new type slightly soluble oral medicine self-emulsification preparation. The preparation comprises a self-emulsification medicine-releasing part and a water-soluble solid carrier, wherein the self-emulsification medicine-releasing part contains slightly soluble medicine, oil phase, surface active agent, cosurfactant and oversaturation matter. The invention also provides a preparation method for the self-emulsification preparation, which comprises a spray drying method or a solvent melting method. After the self-emulsification preparation is taken orally, the self-emulsification preparation can form the emulsion with a grain size smaller than 1mum emulsion with a grain size smaller than 100nm in body, so as to promote the solubility and digestion degree of the slightly soluble medicine, improve the absorption and bioavailability of the medicine and reduce the influence of the food on the medicine absorption as well as reduce the dose of the surface active agent and the cosurfactant in the self-emulsification preparation, enhance the stability and safety of the self-emulsification preparation and be suitable for industrializing production.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to a novel oral drug delivery system for poorly soluble drugs, in particular to a novel oral solid self-emulsifying preparation for poorly soluble drugs and a preparation method thereof. Background technique [0002] For most drugs, oral administration is the preferred route of administration for clinical administration, especially long-term administration, because of its economy, safety, and strong patient compliance. When administered orally, the physicochemical properties of the drug, especially the solubility, will have an important impact on its absorption and bioavailability in the gastrointestinal tract. That is to say, the drug should be dissolved in the digestive juice first, then pass through the mucous membrane of the digestive tract in a water-soluble molecular state through passive diffusion or active transport and other absorption mechanisms, and then enter the blood ci...

AI Technical Summary

Problems solved by technology

But in actual production and use, there are some defects in liquid self (micro) emulsification preparation: the cost of soft capsule or liquid-filled hard capsule form is high, and in some capsules with self (micro) emulsification system as content , alcohols and other volatile co-solvents or co-emulsifiers tend to migrate into the capsule shell, thereby reducing the solubility of poorly soluble drugs and causing drug precipitation

There are its injections on the market, 3 times a day, poor compliance, oral tablets because Vinpocetine is almost insoluble in water, oral bioavailability is only 7%, and absorption is affected by food

Patent application number: 200510137888.4 discloses a vinpocetine solid lipid nanoparticle for oral or injection administration and its preparation process, which includes a therapeutically effective amount of vinpocetine and pharmaceutically acceptable phospholipids, emulsifiers, lipids quality materials and additives, there are still organic solvent residues and industrialization problems; the patent applicant has also applied for a patent (application) number: 200610019616.9 discloses a common vinpocetine oral self-microemulsification drug delivery system and Its preparation method is soft capsule and oral liquid, non-solid preparation form, and does not mention adding supersaturation-promoting substances, and there are also problems of improvement in stability and safety.

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