Pharmaceutical composition containing anionic drug and preparation method thereof
A technology of anionic drugs and compositions, applied in the direction of drug combinations, medical preparations containing active ingredients, medical preparations with non-active ingredients, etc., can solve the problems of not being able to easily pass through the cell membrane
- Summary
- Abstract
- Description
- Claims
- Application Information
AI Technical Summary
Problems solved by technology
Method used
Image
Examples
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...
PUM
| Property | Measurement | Unit |
|---|---|---|
| molecular weight | aaaaa | aaaaa |
| particle diameter | aaaaa | aaaaa |
| number average molecular weight | aaaaa | aaaaa |
Abstract
Description
Claims
Application Information
Login to View More