Application of Hydroxypropyl-β-cyclodextrin in Pharmaceutical Industry

Hydroxypropyl-β-cyclodextrin (referred to as HP-β-CD) is a hydroxyalkylated derivative of β-cyclodextrin. Hydrogen atoms of C-2, C-3 and C-6 3 hydroxyl groups in each glucose residue of β-cyclodextrin (β-CD) can be replaced with hydroxypropyl (-CH 2 CHOHCH 3 ). After substitution, 2-HP-β-CD, 3-HP-β-CD, 2,3-DHP-β-CD, 2,6-DHP-β-CD, 2,3,6-THP-β-CD Equivalents.

HP-β-CD is amorphous, easily soluble in water, low in hemolytic activity, less irritating, low toxic and side effects, and high in safety. As long as the dose is properly controlled, it can be used in different routes of administration. Therefore, it is a better drug co-solvent and stabilizer.

Application in pharmacy

1. For oral drugs

Many water insoluble drugs, volatile drugs, or unstable drugs can be encapsulated with β-CD to increase the water solubility and stability of the drug. At higher concentrations, β-CD tends to crystallize, affecting the effect of use. However, HP-β-CD has good water solubility, high solubilization ability to the drug, and does not precipitate even at high concentrations. After the inclusion, the drug releases rapidly in the body, which can greatly increase the bioavailability of the drug. The aforementioned carbamazepine, glibenclamide and itraconazole are all good examples.

2. For injection

For poorly water-soluble drugs, propylene glycol or prolocarbene is usually used as a cosolvent or emulsion. These types of preparations have certain toxic and side effects. Injection excipients require high water solubility, good safety, and ideal for HP-β-CD. Its water solubility is more than 50%, it has good fluidity, low hemolytic activity, no stimulation to muscles, and can increase the stability of the drug. Many drugs have been prepared with H P-β-CD injections. 5.3 HP-β-CD for Mucosal Drug Delivery System

3. For corneal administration

Eye drops made with HP-β-CD have low viscosity, no irritation, and can increase the bioavailability of the cornea to drugs. For example, the carbonic anhydrase inhibitor acetazolamide reduces intraocular pressure and is used to treat glaucoma. However, its water solubility is extremely poor and its bioavailability is low. Inclusion of HP-β-CD promotes drug penetration through the cornea and increases bioavailability. Another example is the use of HP-β-CD can reduce the hemolytic activity of diclofenac, improve the corneal permeability of drugs.

4. for other mucosal administration

Medications that are encapsulated with HP-β-CD are also suitable for sublingual or tracheal instillation. Tracheal instillation of CD inclusion complexes of drugs in rats was faster than oral, rectal, and nasal administration. The order of bioavailability was: drug-β-CD (65.9±12.8%) <drug-DM-β-CD (73.9±13.2)<drug-HP-β-CD (79.8+12%).

Hydroxypropyl-β-cyclodextrin has many applications in many industries. It plays a lot of roles in pharmaceutical and chemical industry. As long as the dosage is properly controlled, it can be used in different routes of drug delivery. It should be selected by big brands and manufacturers at the time of purchase. Hydroxypropyl-beta-cyclodextrin.