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Pharmaceutical composition containing an anionic drug, and a production method therefor

一种阴离子药物、组合物的技术，应用在药物组合、含有效成分的医用配制品、非有效成分的医用配制品等方向，能够解决无法容易地穿过细胞膜等问题

Active Publication Date: 2015-04-29
SAMYANG HLDG CORP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

siRNA is also known to not easily cross cell membranes due to its strong negative charge

Method used

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  • Pharmaceutical composition containing an anionic drug, and a production method therefor
  • Pharmaceutical composition containing an anionic drug, and a production method therefor
  • Pharmaceutical composition containing an anionic drug, and a production method therefor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0093] Example 1. Synthesis of AC-cholesterol (3β[N-(aminoethane)carbamoyl]cholesterol)

[0094] AC-cholesterol was synthesized by reacting cholesterol chloroformate (Sigma-Aldrich) with ethylenediamine (Sigma-Aldrich) as follows.

[0095] 1 g (2.23 mmol) of cholesterol chloroformate was dissolved in 20 ml of chloroform, 20 equivalents of ethylenediamine were diluted with 30 ml of chloroform in a separate reaction vessel and the temperature was maintained at 4°C. The cholesterol chloroformate solution was slowly introduced into the reaction vessel containing ethylenediamine, and then the mixture was allowed to react at room temperature for 3 hours. After the reaction, the solvent was removed using a rotary evaporator (Buchi, R-2055), and the residue was redissolved in a small amount of chloroform, followed by a saturated solution of NaCl and NaCO 3 Extract to recover the chloroform layer.

[0096] Then, the solvent was removed with a rotary evaporator, and the residue was di...

Embodiment 2

[0098] Example 2. Synthesis of MC-cholesterol (3β[N-(N'-methylaminoethane) carbamoyl]cholesterol)

[0099] MC-cholesterol was synthesized and purified by the same method as in Example 1, except that N-methylethylenediamine (Sigma-Aldrich) was used instead of ethylenediamine in 10 equivalents of cholesterol chloroformate. The yield is 62%. Synthesis and purity of MC-cholesterol by 1 Confirmed by H-NMR, the results are shown in image 3 middle. 99% or better in purity.

Embodiment 3

[0100] Example 3. Polymerization of mPEG-PLA (monomethoxyethylene glycol polylactide) block copolymer (A-B) (molecular weight 2,000-1,750 Daltons)

[0101] 5 g of monomethoxypolyethylene glycol (molecular weight 2,000 Dalton or less, NOF corporation) was added to a 100 ml double-neck round bottom flask, and heated to 100° C. under reduced pressure (1 mmHg) for 3 hours to dehydrate . Dry nitrogen is filled in the reaction flask, injects reaction catalyst stannous octoate (Sn(Oct) with the amount (5mg) of 0.1wt% lactide 2 , Sigma-Aldrich). The reaction mixture was stirred for 30 minutes and the pressure was reduced to 1 mmHg at 110° C. for 1 hour to remove toluene, which is a solvent for dissolving the catalyst. Purified lactide (5 g, Purac) was added and the mixture was heated to 130° C. for 12 hours. The formed polymer was dissolved in ethanol, and diethyl ether was added to precipitate the polymer. The precipitated polymer was dried in a vacuum oven for 48 hours.

[0102...

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Abstract

Disclosed are an anionic drug-containing pharmaceutical composition comprising: an anionic drug as an active ingredient; a cationic lipid; and an amphiphilic block copolymer, wherein the anionic drug forms a complex with the cationic lipid, and the complex is entrapped in the micelle structure of the amphiphilic block copolymer, and a method for preparing the same. The pharmaceutical composition may increase stability of the anionic drug in blood or in a body fluid, and it may enable intracellular delivery to improve efficacy of anionic drugs.

Description

technical field [0001] The present disclosure relates to a pharmaceutical composition containing an anionic drug and a preparation method thereof, the pharmaceutical composition comprising: an anionic drug as an active ingredient, a cationic lipid and an amphiphilic block copolymer, wherein the anionic drug is combined with the cationic lipid The substance forms a complex, and the complex is embedded in the micellar structure of the amphiphilic block copolymer. Background technique [0002] In therapy with anionic drugs, especially nucleic acid materials, safe and effective drug delivery techniques have been studied for a long time, and various delivery systems and delivery techniques have been developed. In particular, a delivery technology using a viral delivery system using an adenovirus or a retrovirus or the like and a non-viral delivery technology using a cationic lipid, a cationic polymer, etc. have been developed. [0003] However, the technology using a virus deliv...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/127A61K31/7105A61K31/711A61K31/70A61K31/56A61K31/353A61K39/235A61K39/21
CPCA61K9/0019A61K9/1075A61K31/353A61K31/56A61K31/70A61K31/7105A61K31/711A61P43/00A61K47/50A61K9/127
Inventor 金世浩孙智娟罗文豪崔成源徐敏孝
Owner SAMYANG HLDG CORP
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