Hot-melt extrusion process for preparing indometacin quick release preparation from multi-element auxiliary materials

Abstract

The invention discloses a hot-melt extrusion process for preparing an indometacin quick release preparation from multi-element auxiliary materials and belongs to the field of pharmacy. The method comprises the following steps of: crushing indometacin and medicinal auxiliary materials, and after screening the powder with a 60 to 120-mesh sieve, uniformly mixing the powder into a physical mixture; according to the melting points or the glass transition temperatures of the medicament and the auxiliary materials, setting the extrusion temperature of a double-screw hot melt extruder to be between 50 and 150 DEG C, after the extrusion temperature reaches the preset temperature, starting a screw, adding the prepared physical mixture into the extruder, and extruding the physical mixture into strips through the screw; and after crushing the strips, screening the powder with a 20 to 80-mesh sieve to obtain medicinal solid dispersoid particles or powder. The auxiliary materials comprise the following components in percentage by weight: 10 to 90 percent of polymer, 5 to 50 percent of plasticizer, 0 to 10 percent of lubricant, 0 to 5 percent of surfactant and 0 to 20 percent of disintegrant. A sugar alcohol with a relatively low softening point or melting point, and the like, serving as the plasticizer, is added into the polymer with a relatively high softening point or melting point so as to reduce the extrusion temperature and make the extrusion process easy. The prepared indometacin solid dispersoid has the characteristic of quickly dissolving out.

Description

technical field [0001] The invention belongs to the technical field of pharmacy, especially designs a multi-component excipient system suitable for preparing quick-release drug solid dispersion by hot-melt extrusion method, and provides a process for preparing quick-release drug solid dispersion by hot-melt extrusion method. Background technique [0002] Indomethacin belongs to Class II in the Biopharmaceutics Classification System (BCS), that is, it has high permeability to biofilms, but poor water solubility, and the dissolution and dissolution of drugs become the main bottleneck for the absorption of such drugs. Utilization is primarily determined by dissolution rate. Methods to improve the solubility and dissolution of poorly soluble drugs include microcrystalline micronization of drugs, nanonization, solubilizers, solubilizers, polymer micelles, microencapsulation, cyclodextrin inclusion and solid dispersion technology Wait. At present, solid dispersion technology has...

AI Technical Summary

Problems solved by technology

However, there are not many excipients that can be used to prepare immediate-release solid dispersions by hot-melt extrusion. The commonly used ones are polyethylene glycol, poloxamer, etc., but they have a low melting point and are easy to liquefy during hot-melt extrusion. , is not easy to mix with drugs, and is not easy to form; other polymers reported in the literature such as: copolyvinylpyrrolidone vinyl acetate (PVP-VA64), povidone (PVP-including PVPK30 / 25, etc.), cross-linked polydimensional Ketone (PVPP), polyvinyl alcohol polyethylene glycol copolymer (IR), hydroxypropyl methylcellulose (HPMC), etc. have high melting points, and require a higher temperature to soften when used alone, or even not soften at all. On the one hand, it is not conducive to the high dispersion of the drug, on the other hand, it is not conducive to the smooth progress of the hot melt extrusion process

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