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Sustained-release anesthetic compositions and methods of preparation thereof

A composition and anesthetic technology, applied in the field of sustained-release pharmaceutical composition, can solve problems such as lengthy steps and high production costs, and achieve the effect of avoiding inconvenience

Pending Publication Date: 2020-10-30
TLC BIOPHARMACEUTICALS INC +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] In order to achieve the purpose of improving drug efficacy, using lipid-based delivery vehicles with high drug loading (for example: high drug-lipid ratio (high drug to lipid ratio)], conventional methods for the preparation of lipid-based dosage forms with high drug loading , generally involving lengthy steps and high production costs

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

[0061] Method for preparing ropivacaine composition from multiple phospholipids

[0062] Phospholipids, including DLPC, DMPC, DPPC, DOPG, DOPC, DOPS, DOPA, Egg PC, Egg PE, POPE, cardiolipin, and DMPA were purchased from NOF Corporation (Tokyo, Japan), or Lipoid GmbH (Ludwigshafen, Germany) ); Cholesterol was purchased from Sigma-Aldrich (Darmstadt, Germany) or Dishman Pharmaceuticalsand Chemicals (Gujarat, India), and ropivacaine was purchased from Apollo Scientific (Cheshire, UK) or Dishman Pharmaceuticals and Chemicals; all others The chemicals were purchased from Sigma-Aldrich.

[0063] In order to prepare lipid cakes, ropivacaine was mixed with different lipid mixtures in Table 1 at a drug relative phospholipid ratio (D:PL) of 1.458 micromole / micromole, ie, phospholipid:cholesterol:ropivaca Because=2:1:2.9. Mix lipid and ropivacaine, and dissolve in tert-butanol or tert-butanol-water co-solvent (volume ratio 1:1) to form a liquid phase structure. After freezing each liquid-p...

Embodiment 2

[0067] Characterization of ropivacaine composition

[0068] The sample prepared in Example 1 will be tested for its association efficiency by the method described below. 200 microliters of ropivacaine composition was centrifuged at 3000xg for 5 minutes at 4°C. After removing the supernatant, obtain the separated lipid substrate mixture and resuspend it to 200 microliters; use a test drug solution of known concentration (such as ropivacaine) to establish a reference standard for its absorbance. An ultraviolet / visible light spectrophotometer was used to measure the amount of ropivacaine drug in the original ropivacaine composition and the separated lipid substrate mixture. The association efficiency represents the ratio of the separated lipid substrate mixture to the amount of drug in the ropivacaine composition. The D:PL lipid cake of the separated lipid matrix complex is calculated by multiplying the D:PL of the lipid cake by the association efficiency, which is called "final D...

Embodiment 3

[0077] Preparation of ropivacaine composition containing different phospholipids

[0078] The sources of phospholipids, cholesterol, ropivacaine, and all other chemicals are detailed in Example 1.

[0079] In order to prepare a lipid cake, ropivacaine and different lipid mixtures are mixed at a molar ratio of phospholipid:cholesterol:ropivacaine=2:1:2.9, where the phospholipid is DMPC and one of the other phospholipids in Table 2. The molar ratio of DMPC: a kind of other phospholipid in the phospholipid is 1.8:0.2. After the lipid is mixed with ropivacaine, it is dissolved in tert-butanol to form a liquid phase structure. After each liquid phase structure sample is frozen for 30 to 60 minutes, freeze-drying is continued until the next day to obtain a lipid cake.

[0080] The lipid cake was hydrated with 50 mM histidine buffer (pH 6.5) at room temperature to form a ropivacaine composition, and then the association efficiency and particle size distribution were measured.

[0081] In t...

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Abstract

Provided is an anesthetic composition for locally administering a local anesthetic agent to a subject in need thereof. The anesthetic composition has a lipid based complex prepared by hydrating a lipid cake containing a local anesthetic agent and a lipid mixture with an aqueous buffer solution at a pH higher than 5.5. Also provided is a method to prepare an anesthetic composition using a simpler and more robust for large-scale manufacture and for providing a high molar ratio of local anesthetic agent to phospholipid content as compared to the prior art. This anesthetic composition has a prolonged duration of efficacy adapted to drug delivery.

Description

[0001] Related applications [0002] This application claims the rights and interests of U.S. Application No. 62 / 650,912 filed on March 30, 2018, and the entire disclosure of the case is incorporated herein by reference. [0003] background Technical field [0004] The present invention relates to a drug delivery system for producing sustained-release anesthetic compositions. The present invention relates to a method of preparing this drug delivery system. The present invention also relates to a sustained-release pharmaceutical composition suitable for a drug delivery system, which has an extended duration of drug effect. Background technique [0005] Several methods for the development of sustained-release local anesthesia have been reported. Examples are as follows: adding dibucaine free base, dibucaine HCl, and bupivacaine HC1 Into the polymer matrix, mix 1:4 with 1,3-bis(p-carboxyphenoxy)propane-sebacic acid anhydride (1,3-bis(p-carboxyphenoxy)propane-sebacic acid anhydride) to...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K47/24A61K47/28A61K31/00
CPCA61K9/1277A61K47/24A61K47/28A61K31/445A61P23/02A61K45/00A61K9/0014A61P25/00A61K9/127
Inventor 洪基隆曾雲龙赖俊延俞宛妮高颢文林宜谕
Owner TLC BIOPHARMACEUTICALS INC
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