US 12,403,107 B2
Lipid pharmaceutical preparation and application thereof
Jie Zhang, Zhejiang (CN); and Peike Tang, Zhejiang (CN)
Assigned to HUZHOU INNOVATION PHARMACEUTICAL CO., LTD., Zhejiang (CN)
Appl. No. 17/603,015
Filed by HUZHOU INNOVATION PHARMACEUTICAL CO., LTD., Zhejiang (CN)
PCT Filed Apr. 15, 2020, PCT No. PCT/CN2020/084832
§ 371(c)(1), (2) Date Oct. 12, 2021,
PCT Pub. No. WO2020/211762, PCT Pub. Date Oct. 22, 2020.
Claims priority of application No. 201910299949.9 (CN), filed on Apr. 15, 2019.
Prior Publication US 2022/0193014 A1, Jun. 23, 2022
Int. Cl. A61K 31/167 (2006.01); A61K 9/00 (2006.01); A61K 9/06 (2006.01); A61K 31/155 (2006.01); A61K 31/245 (2006.01); A61K 31/381 (2006.01); A61K 31/445 (2006.01); A61K 31/47 (2006.01); A61K 45/00 (2006.01); A61K 45/06 (2006.01); A61K 47/24 (2006.01); A61K 47/28 (2006.01); A61K 47/36 (2006.01); A61K 47/44 (2017.01); A61P 23/02 (2006.01); A61P 29/00 (2006.01); A61P 31/02 (2006.01); A61P 31/04 (2006.01)
CPC A61K 31/167 (2013.01) [A61K 9/0014 (2013.01); A61K 9/06 (2013.01); A61K 31/155 (2013.01); A61K 31/245 (2013.01); A61K 31/381 (2013.01); A61K 31/445 (2013.01); A61K 31/47 (2013.01); A61K 45/00 (2013.01); A61K 45/06 (2013.01); A61K 47/24 (2013.01); A61K 47/28 (2013.01); A61K 47/36 (2013.01); A61K 47/44 (2013.01); A61P 23/02 (2018.01); A61P 29/00 (2018.01); A61P 31/02 (2018.01); A61P 31/04 (2018.01)] 19 Claims
 
1. A lipid pharmaceutical preparation, wherein, the lipid pharmaceutical preparation comprises a local anesthetic, a lipid substance and sodium hyaluronate; and the local anesthetic is lidocaine;
the lipid substance is lecithin;
wherein the lipid pharmaceutical preparation comprises by mass percentage: 5%-30% of lidocaine, 55%-85% of lecithin and 8%-15% of sodium hyaluronate.
 
13. A lipid pharmaceutical preparation, wherein, the lipid pharmaceutical preparation comprises the following components: lidocaine, lecithin and soybean oil,
wherein, the mass percentage of the lidocaine in the lipid pharmaceutical preparation is 15%-21%, 17%-21%, or 17%-20%, the mass percentage of the lecithin in the lipid pharmaceutical preparation is 62%-77% or 70%-75%, and the mass percentage of the soybean oil in the lipid pharmaceutical preparation is 6%-12% or 8%-10%; and wherein
after the lipid pharmaceutical preparation is embedded into human tissue of a subject, under the erosion of body fluids, the lidocaine in the lipid pharmaceutical preparation is released in a slow-release manner from the lipid pharmaceutical preparation to the surface of the human tissue contacted by the lipid pharmaceutical preparation, and makes the subject's average blood drug concentration peak at the maximum dose not higher than 5000 ng/mL, the effective analgesic time is not shorter than 24 hours; and wherein, the maximum dose is 0.5 g of the lipid pharmaceutical preparation/kg body weight.