What is Hydroxypropyl Beta cyclodextrin ?
Hydroxypropyl Beta cyclodextrin ( HP-β-CD, HPBCD ) is a hydrophilic derivative that is a condensation of beta-cd and 1, 2-epoxypropane.The hydroxyl groups in R 1, R2, and R3 of the beta-cd were randomly replaced by hydroxypropyl, generating 2-hp-a-cd, 2, 3-hp-a-cd, 2, 6-hp-a-cd, and 2,3, 6-hp-beta-cd and other homologues.By the hydroxypropylation of beta-cd, the hydrogen bond in the molecule was destroyed, and the water solubility was increased significantly.Beta - CD water-soluble about 1.85% (w/v, 25 ℃), while the HPBCD soluble in water, solubility > 50% (w/v) at room temperature, even more than can be as high as 75% (w/v).When the concentration is <40%, the liquidity is good, not sticky.
According to incomplete statistics, the United States, France, Germany, Italy, Japan, Belgium, Iceland, New Zealand, Switzerland, Argentina and other countries already had dozens of CDS and their derivatives containing drugs, dosage form has tablet, including sublingual tablet, capsule, sugar pill, injection, suppositories, oral liquid, oral lotion (including wash liquid), ointment, etc;The drugs involved with piroxicam, prostaglandin E1 and E2, benzyl acid ester, iodine, dexamethasone, nitroglycerin, cephalosporins for Ann, hydrocortisone, itraconazole, librium, garlic oil, etc.
The HPBCD is the first of its kind to be approved by the FDA for intravenous injection of beta-cd derivatives.American Johnson & Johnson 40%HPBCD solubilized itraconazole oral liquid and intravenous injection have been listed.SDA in China also approved 2%HPBCD solubilized digoxin oral solution for clinical trials, and the HPBCD solubilized artemisinin intravenous injection will be approved for clinical study.
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