LID-PEG-PLGA controlled-release nano microsphere and preparation method thereof

Abstract

The invention discloses an LID-PEG-PLGA controlled-release nano microsphere and a preparation method thereof. The microsphere is the controlled-release microsphere which contains medicinal lidocaine and a degradable carrier. The degradable carrier contains polylactic-glycolic acid and PEG-2000. The mass percentage of the lidocaine in the controlled-release microsphere is 30 to 35 percent. The preparation method comprises the following steps of: preparing the carrier into matrix solution; dispersing the lidocaine into the matrix solution and preparing the lidocaine into an oil phase; mixing the oil phase and the aqueous solution of polyvinyl alcohol, and performing ultrasonic emulsification on the mixture under a water bath condition to obtain W / O-type protogala; mixing the W / O-type protogala and the aqueous solution of polyvinyl alcohol again, and further emulsifying the mixture into W / O / W-type complex emulsion; volatilizing the emulsion by reducing pressure at the normal temperature to obtain cured lidocaine-carried nano microsphere; and scattering, blending, packaging, freezing, sterilizing and the like. The medicament loading rate of the controlled-release nano microsphere can be up to 15 to 22 percent; the entrapment rate can be up to 68 to 78 percent; and the half-life period can be prolonged to 3 to 4 days. Therefore, the microsphere has relatively good effect of burst in the first day after the microsphere is taken and good effect of slow release in later days.

Description

technical field [0001] The invention relates to a lidocaine-loaded slow-release microsphere and a preparation method thereof. Background technique [0002] Lidocaine (Lidocaine, LID), also known as xylocaine, chemical name: N-(2,6-xylyl)-2-(diethylamino)acetamide. Lidocaine has an obvious inhibitory effect on the central nervous system and is a commonly used local anesthetic in clinical practice. After 2006, people discovered its potential new clinical use, which can be used as an early treatment drug for severe trauma. However, because lidocaine can dilate peripheral blood vessels, drug absorption through blood vessels will be accelerated, which will shorten the period of action; at the same time, because lidocaine has a short biological half-life (only 1.5 to 2 hours), it is clinically Just need small dose frequent administration to maintain its drug effect when using, and this just brings bigger misery and inconvenience to the patient. Therefore, it is of great signific...

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Problems solved by technology

However, since its drug loading is only (12.48 ± 0.26)%, and its encapsulation efficiency is only (54.30 ± 0.89)%, so when prolonging the action time of LID one-time administration, reducing the number of administrations and increasing biological In terms of utilization, there are still some deficiencies

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