Supersaturated solid self-emulsifying preparation and preparation method thereof

Abstract

The invention discloses a supersaturated solid self-emulsifying preparation and a preparation method thereof. The supersaturated solid self-emulsifying preparation is prepared from a devitrification inhibitor and a difficult-to-dissolve medicine solid self-emulsifying system, wherein the difficult-to-dissolve medicine solid self-emulsifying system is prepared from mesoporous silicon dioxide SBA-15 and a difficult-to-dissolve medicine liquid self-emulsifying transmitting system; the liquid self-emulsifying transmitting system is composed of a difficult-to-dissolve medicine, an oil phase, an emulsifying agent and an auxiliary emulsifying agent; the devitrification inhibitor is an amphiphilic high molecular polymer Soluplus. The devitrification inhibitor Soluplus has a crystallization inhibiting effect through inhibiting nucleation of the supersaturated difficult-to-dissolve medicine and the growth speed of crystals; a supersaturated state of a medicine solution is kept and the absorption of the difficult-to-dissolve medicine is guaranteed; the bioavailability is high and the supersaturated solid self-emulsifying preparation has good development and application prospects.

Description

Technical field [0001] The invention belongs to the technical field of pharmaceutical preparations. More specifically, the invention relates to a supersaturated solid self-emulsifying preparation and a preparation method thereof. Background technique [0002] Oral administration is the most common, simplest and most acceptable route of administration for patients. After the drug enters the gastrointestinal tract orally, it first needs to go through a dissolution process before it can be absorbed by the body, and then exert the drug effect. BCS II drugs in the Biopharmaceutical Classification System (BCS) have low solubility and high permeability, and their dissolution in the digestive tract often becomes the rate-limiting link in the absorption of such drugs. Statistics show that the proportion of BCS II drugs in the marketed drugs is 40%, and the proportion of drugs in research and development is as high as 70%. The low bioavailability caused by the poor solubility of BCS II d...

AI Technical Summary

Problems solved by technology

[0004] However, in the insoluble drug SSEDDS, the drug exists in the solid phase carrier in an amorphous state. Because there is no constraint of lattice energy, the drug molecule dissolves rapidly, and the self-emulsifying component desorbs from the solid phase carrier after meeting water and spontaneously emulsifies to form O / In W emulsion, the drug molecules are further solubilized in the emulsion droplets, resulting in the apparent solubility of the drug in the gastrointestinal tract far exceeding its equilibrium solubility, forming a supersaturated solution

The solution is a thermodynamically unstable system, and the drug will spontaneously precipitate crystals, which will make the apparent solubility of the drug tend to be extremely low, resulting in a decrease in drug concentration and absorption, which will eventually affect the bioavailability and efficacy of the drug in vivo.

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