Characteristics and uses of hydroxypropyl-β-cyclodextrin

Hydroxypropyl-β-cyclodextrin, also known as (2-hydroxypropyl)-β-cyclodextrin, is the 2-, 3-, and The hydrogen atom in the hydroxyl group at the 6-position is replaced by a hydroxypropyl group to become a hydroxypropoxy group. Like β-CD, HP-β-CD not only has excellent encapsulation effect on many compounds and improves the solubility and stability of the encapsulated substances, but also has high water solubility and improves the encapsulation drug in vivo. Advantages of release rate and bioavailability. In addition, HP-β-CD is a drug excipient with the most extensive safety data collected without adverse side effects. HP-β-CD can also be used as protein protective agent and stabilizer.

Features and Safety

1. HP-beta-CD has high water solubility at room temperature, generally more than 50%, so it cannot be crystallized in alcohol aqueous solution.

2. The selectivity of HP-beta-CD and β-CD to the enveloped substances is different, and the molecular ratio of the envelope of some substances may be changed.

3. HP-beta-CD is basically not catabolized or accumulated in the human body. Most of the oral HP-beta-CD is excreted in the stool, and the parenteral administration is basically excreted in the urine.

4. HP-beta-CD can promote the rapid release of enveloped substances in vivo.

5. Compared with β-CD or other derivatives (such as methylated-beta-CD), HP-beta-CD has lower surface activity, lower hemolytic activity, and is safer to use.

In terms of the safety of HP-beta-CD. Based on systematic subacute and chronic toxicity studies, HP-beta-CD does not cause disease or death in mice. After intravenous injection into rabbits, HP-beta-CD was rapidly eliminated from the blood and excreted with urine, and there were no adverse symptoms after continuous injection. Intravenous administration of 200 mg/kg HP-beta-CD in mice and monkeys showed no clinical effect. Simple oral or intravenous injection of HP-beta-CD doses up to 15g/kg or 10g/kg, respectively, is not lethal to monkeys. Human clinical studies have shown that HP-beta-CD is administered orally, intravenously, intravenously, nasally, sublingually and ocularly, without adverse reactions and irritation to skin, eyes and muscles. This shows that HP-beta-CD is very safe for biology.

Use of hydroxypropyl-β-cyclodextrin

In the pharmaceutical industry, it is an ideal injection solubilizer and pharmaceutical excipient due to its relatively low relative surface activity and hemolytic activity and no irritation to muscles. It can improve the water solubility of poorly soluble drugs, increase the stability of the drugs, improve the bioavailability of the drugs, increase the efficacy of the drugs or reduce the dosage, adjust or control the release speed of the drugs, and reduce the toxic and side effects of the drugs. It can be used for oral drugs, injections, mucosal drug delivery systems, transdermal drug delivery systems, carriers of lipophilic targeted drugs, and can also be used as protein protective agents and stabilizers.

Used as stabilizer, emulsifier, deodorant, etc. in cosmetic raw materials, it can reduce the irritation of organic molecules in cosmetics to skin and mucous membrane tissue, enhance the stability of active ingredients, prevent the volatilization and oxidation of nutrients; increase insoluble flavors, Water solubility of fragrance; maintain slow release and long-lasting fragrance.

In food, it can improve the stability and long-term effect of nutritional molecules, mask or correct the bad smell and taste of food nutritional molecules, improve the production process and product quality, and increase the shelf life of products.