참여 물질
| 역할 | 이름 | HCID | 투입량 |
|---|
| 반응물 | Cholesterol | HCID 5997 | — |
| 반응물 | (2R,3S,4R,5R)-2,3,4,5,6-pentahydroxyhexanal | HCID 107526 | — |
| 반응물 | Colfosceril Palmitate | HCID 452110 | — |
| 반응물 | Sildenafil Citrate | HCID 135413523 | — |
| 반응물 | Sildenafil ammonium sulphate | HCID 136330136 | — |
| 용매 | Ethanol | HCID 702 | — |
| 생성물 | Sildenafil | HCID 135398744 | — |
반응 단계
The lipids (DPPC:cholesterol=55:45 mol %) were dissolved in ethanol and the solution was injected into a sildenafil/ammonium sulphate solution (pH 3.5-4.5), whereupon, immediately after spontaneous vesicle formation, a 5% glucose solution (pH 7), which comprised further sildenafil citrate, was added for dilution and alkalinization of the reaction mixture, i.e. of the resulting liposome suspension. As a result of the production of this H+ gradient immediately after the vesicle formation, sildenafil is not only included in the liposomes in one step but is also retained there in a stable manner. The amount of sildenafil included liposomally in this manner was likewise in a range of about 160 to 230 nmol of sildenafil per μmol of total lipids (DPPC+cholesterol)—depending on the pH or H+ gradient.
출처 및 근거
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|
| 특허 번호 | US08524274B2 |
|---|
| 출처 데이터셋 | uspto-grants-2013_09 |
|---|
| ORD ID | ord-c327fe2a3cd64e28b5e7e204d8e172a1 |
|---|
| 출처 메모 | uspto-grants-2013_09 |
|---|
