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Sustained-release anesthetic compositions and methods of preparation thereof

A technology of anesthetics and components, applied in the field of drug delivery systems, which can solve the problems of cumbersome manufacturing procedures and high costs

Pending Publication Date: 2020-05-19
TLC BIOPHARMACEUTICALS INC +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] Some of the above-mentioned embodiments of the disclosed technology failed to highly entrap the drug, that is, failed to achieve a high drug to lipid ratio (high drug to lipid ratio), although some of the embodiments of the disclosed technology showed that their formulations had sufficient The ratio of drug to lipid, however, its manufacturing process is cumbersome and costly. Therefore, there is still an urgent need to improve and simplify the preparation process of sustained-release local anesthetics

Method used

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  • Sustained-release anesthetic compositions and methods of preparation thereof
  • Sustained-release anesthetic compositions and methods of preparation thereof
  • Sustained-release anesthetic compositions and methods of preparation thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0045] Preparation of ropivacaine composition

[0046] Hydrogenated soybean phosphatidylcholine (HSPC), 1,2-dimyristoyl-sn-glycero-3-phosphocholine (DMPC) and 1,2-dipalmitoyl-sn-glycero-3-phosphate-(1 '-rac-glycerol) (sodium salt) (DPPG) was purchased from NOF Corporation. Cholesterol was purchased from Sigma-Aldrich and ropivacaine was purchased from Apollo Scientific or Dishman. All other chemicals were purchased from Sigma-Aldrich.

[0047] In order to prepare several highly entrapped lipid structures, different molar ratios of lipid mixtures and ropivacaine were used, and the constituent samples were listed as follows: HSPC:cholesterol:ropivacaine=1.5:1:2.2, HSPC:cholesterol :ropivacaine=2:1:2.9, DMPC:cholesterol:ropivacaine=2:1:2.9, and DMPC:DPPG:cholesterol:ropivacaine=1.85:0.15:1:2.9. The above-prepared lipid and ropivacaine are mixed and dissolved in tert-butanol or tert-butanol-water co-solvent system (1:1 volume ratio) to form a liquid phase structure. Each liqui...

Embodiment 2

[0051] Qualitative results of ropivacaine composition

[0052] The above-mentioned prepared samples were tested for association efficiency by the method described below. 200 microliters of each ropivacaine composition was transferred to a centrifuge and centrifuged at 3000 xg for 5 minutes at 4°C. After removing the supernatant, ropivacaine-embedded multilamellar vesicles were obtained and resuspended to a final volume of 200 μL. A reference standard of absorbance is established using a solution of the test drug (eg, ropivacaine) of known concentration. The amount of ropivacaine in the original ropivacaine composition and embedded ropivacaine multilamellar vesicles was measured by a UV / visible spectrophotometer. Association efficiency represents the ratio of entrapped ropivacaine multilamellar vesicles relative to the amount of drug in the ropivacaine composition. The D:PL of ropivacaine-embedded multilamellar vesicles was calculated by multiplying the D:PL of highly entrap...

Embodiment 3

[0057] Pharmacokinetic study of ropivacaine composition

[0058] Pharmacokinetic studies were performed using female Sprague-Dawley rats cannulated in the jugular vein. Rats were housed in a living room with a 12-hour light / 12-hour dark cycle, and water and food were provided for the rats to obtain freely. The ropivacaine composition was prepared according to the method in Example 1, wherein the high embedding lipid structure of DMPC: cholesterol: ropivacaine = 2: 1: 2.9 and the pH value of 5.5, 6.0 and 6.5 respectively A 50 mM histidine buffer solution was hydrated; a ropivacaine solution was obtained by dissolving ropivacaine hydrochloride monohydrate in 0.9% NaCl at a concentration of 24.0 mg / mL. Various ropivacaine compositions and ropivacaine solutions were administered subcutaneously to each group of rats (3 or 4 rats in each group) with a dose of ropivacaine of 20.0 mg / kg rat body weight, to The in vivo pharmacokinetic curves of rats in each group were compared. Bloo...

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Abstract

Provided is an anesthetic composition for locally administrating an amide-type anesthetic into a subject in need thereof. The anesthetic composition has multilamellar vesicles with en trapped amide-type anesthetic prepared by hydrating a highly entrapped lipid structure comprising an amide-type anesthetic and a lipid mixture with an aqueous buffer solution at a pH higher than 5.5. Also provided isa method to prepare an anesthetic composition using a simpler and more feasible process for large-scale manufacture and for providing a high molar ratio of amide-type anesthetic to phospholipid content as compared to the prior art. This anesthetic composition has a prolonged duration of efficacy adapted to drug delivery.

Description

[0001] Cross reference to related applications [0002] This application claims priority to U.S. Provisional Application 62 / 550,983, filed August 28, 2017, and U.S. Provisional Application 62 / 621,730, filed January 25, 2018, the entire contents of which are incorporated by reference way incorporated into this article. [0003] background technical field [0004] This invention relates to drug delivery systems for producing sustained release anesthetic compositions. The present invention is concerned with methods of preparing such drug delivery systems. The present invention also relates to sustained-release pharmaceutical compositions suitable for use in drug delivery systems, which have a prolonged duration of drug effect. Background technique [0005] Several approaches to the development of sustained-release local anesthetic formulations have been reported, including 1) the use of a dehydration-rehydration method (US Patent No. 6,926,905) to prepare multilamellar lipo...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K9/107A61K9/127A61K31/167
CPCA61K9/0019A61K9/1075A61K9/127A61K9/1272A61K31/445A61K47/22A61K47/28A61P23/02A61P23/00A61K9/06A61K47/24
Inventor 洪基隆高颢文林宜谕郭松声
Owner TLC BIOPHARMACEUTICALS INC
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