Abstract
In this paper, nicotinic acid, benzoic acid and p-nitrobenzoic applied in clinical were used as the model drugs. Small molecular drugs with carboxyl were PEGylated via degradable ester bonds by two-step process. The yield of products were 80%-85%. The small molecular drugs will be released by the degradation of ester bonds. The macromolecular prodrugs were characterized by IR, 1H-NMR and DSC. The results suggeste that small molecular drugs are conjugated to PEG. Products are dissolvable in most organic solvents such as CH2Cl2, THF, CH3CH2OH., CHCl3, CH3COCH3, DMF., DMSO. The solubility of the products has been improved in aqueous solutions. The example of PEG-(nicotinic acid)2 had been discussed detailedly.
| Original language | English |
|---|---|
| Pages (from-to) | 143-146 |
| Number of pages | 4 |
| Journal | Gaofenzi Cailiao Kexue Yu Gongcheng/Polymeric Materials Science and Engineering |
| Volume | 24 |
| Issue number | 1 |
| State | Published - Jan 2008 |
Keywords
- Modification
- Nicotinic acid
- Polyethylene glycol
- Small molecule drugs
- Two-step process