Sodium sulfobutyl beta-cyclodextrin (trade name Captisol) is an anionic, highly water-soluble β-CD derivative successfully developed by Cydex Corporation in the United States in the 1990s. It can well incorporate drug molecules to form non-covalent complexes, thereby improving the stability, water solubility, and safety of drugs, reducing nephrotoxicity, alleviating drug hemolysis, controlling drug release rate, and masking bad odors. Compared with β-CD, it has better water solubility, less hemolysis, and low nephrotoxicity. It is a new type of pharmaceutical excipient with very broad application prospects.
Sulfonbutyl-β-cyclodextrin Sulfonbutyl-β-cyclodextrin sodium is the product of β-cyclodextrin and 1,4-butane sultone substitution. The substitution reaction can occur at the 2, 3, and 6 carbon hydroxyl positions of the β-CD glucose unit. Since β-CD is composed of 7 pyranose glucoses connected by α-(1, 4) glycosidic bonds, there are 21 sites where substitution reactions may occur. Theoretically, a β-cyclodextrin derivative with a degree of substitution of 21 (7 primary hydroxyl groups, 6-OH, 14 secondary hydroxyl groups 2, 3-OH) can be obtained. However, due to the limitations of steric hindrance and reaction conditions, the degree of substitution generally does not exceed 10%. Therefore, the product obtained by this reaction is a very complex mixture.
Product Application
1. Application in injections
1-1. Function: Solubilizer, stabilizer, improve the solubility and stability of poorly soluble drugs, and develop poorly soluble drugs into injections.
1-2. Example: Use sulfobutyl beta-cyclodextrin sodium to improve the solubility of 112859-71-9 Fluasterone, docetaxel, voriconazole, ibuprofen, and indomethacin; use sulfobutyl beta-cyclodextrin sodium to improve the stability of carmustine;
2. Application in oral preparations
2-1. Function: Solubilizer, stabilizer, improve the bioavailability of poorly soluble drugs.
2-2. Example: Use sulfobutyl beta-cyclodextrin sodium to improve the bioavailability of flunarizine, danazol, prednisolone, and prasugrel.
3. Application in ophthalmic preparations
3-1. Function: Solubilizer, stabilizer, reduce drug irritation.
3-2. Example: Using sulfobutyl beta-cyclodextrin sodium to improve the irritation and stability of pilocarpine, dipivoxil, balofloxacin, and ganciclovir
4. Application in nasal preparations
4-1. Function: Increase the permeability of the nasal mucosa, improve the solubility and stability of drugs, and improve the metabolic rate of drugs at the target site of administration.
4-2. Example: Using sulfobutyl beta-cyclodextrin sodium to improve the solubility and stability of midazoline.
5. Ointment
5-1. Function: Improve the solubility and stability of drugs.
5-2. Example: Using sulfobutyl beta-cyclodextrin sodium to improve the solubility and stability of nimesulide.
