Hydroxypropyl beta cyclodextrin powder

What is Hydroxypropyl beta cyclodextrin powder

Hydroxypropyl beta cyclodextrin powder is a white powder with good solubility in water and can also be dissolved in 50% ethanol and methanol. It has a certain relative hygroscopicity. However, the relative surface activity and hemolytic activity are relatively low. It is not irritating to muscles and is an ideal injection solubilizer and drug excipient.

It is a widely used modified cyclodextrin, which is formed by 7 glucose units to form a lipophilic cavity. The hydrogen atoms in the 2-, 3-, and 6-hydroxyl groups of each glucose residue can be replaced by hydroxypropyl groups. 2-Hydroxypropyl-β-cyclodextrin is mainly the product of the substitution of the hydrogen atom of the 2-hydroxyl group. After the drug is complexed with hydroxypropyl-β-cyclodextrin, the water solubility will be greatly enhanced. The number of 2-hydroxypropyl groups is between 5 and 14. . The introduction of hydroxypropyl breaks the intramolecular cyclic hydrogen bond of β-cyclodextrin, while maintaining the cyclodextrin cavity, it overcomes the main disadvantage of poor water solubility of β-cyclodextrin. It is one of the most intensively studied and widely used cyclodextrin derivatives. It is mainly used in the food, medicine, and cosmetics industries.
1. In the field of food and spices, it can improve the stability and long-term effect of nutritional molecules, cover or correct the bad smell and taste of food nutritional molecules, and improve production processes and product quality. The product has good solubility in water. It can be miscible with water in any proportion with a substitution degree of 4 or above, and can also be dissolved in 50% ethanol and methanol.
2. It can be used as a stabilizer, emulsifier, deodorant, etc. in cosmetic raw materials to reduce the irritation of organic molecules in cosmetics to skin and mucous membrane tissues, enhance the stability of active ingredients, and prevent the volatilization and oxidation of nutrients. It has a certain relative hygroscopicity. Increase the water solubility of insoluble flavors and spices; maintain the sustained release and persistence of fragrance.
3. In the pharmaceutical industry, it is an ideal injection solubilizer and drug excipient because of its relatively low relative surface activity and hemolytic activity and no irritation to muscles. It can improve the water solubility of insoluble drugs, increase drug stability, improve drug bioavailability, increase the efficacy of drugs or reduce the dosage, adjust or control the release rate of drugs, and reduce drug toxicity and side effects. It can be used for oral drugs, injections, mucosal drug delivery systems (including nasal mucosa, rectum, cornea, etc.), transdermal absorption drug delivery systems, carriers of lipophilic targeted drugs, and can also be used as a protective agent and stabilizer for proteins.
Hydroxypropyl beta cyclodextrin is one of the derivatives of β-cyclodextrin. Natural cyclodextrin and its derivatives are cyclic oligosaccharides obtained by enzymatic cyclization of starch. It is the substitution product of hydroxypropyl ether of β-cyclodextrin under alkaline conditions. The hydroxyl groups in cyclodextrin are replaced by hydroxypropyl groups, which makes it highly water-soluble (≥ 600mg/mL). Its unique ring structure gives the molecule a hydrophilic outer surface and a hydrophobic inner cavity. The degree of substitution of the entire molecule is 7 molar substitutions (the average number of hydroxyl groups substituted per monomer is called the molar substitution). The 7 monomers may have different numbers of hydroxyl groups substituted, so that each molecule has a combination of multiple different degrees of substitution.
Depending on the degree of substitution, the physical and chemical properties may be slightly different. Its osmotic pressure and viscosity are also suitable for injectable drug formulations, and it remains hypotonic over a wide range of concentrations. The concentration can reach 200mM, which supports the recommended limit for subcutaneous injection (osmotic pressure 600 mOsm/kg, viscosity 20mPas).

Application:

1. Increase drug solubility and improve bioavailability
Solubility is the inherent physical and chemical property of drugs. Increasing solubility can accelerate the dissolution and release of drugs in gastrointestinal fluid, increase drug absorption and enhance efficacy. In the inclusion complex, the drug changes the molecular stereo arrangement in the unit cell of its original crystal structure, and enters the inner cavity of Hydroxypropyl beta cyclodextrin in a molecular state. Due to its high hydrophilicity, it is more conducive to the rapid dissolution of drugs in the gastrointestinal tract, improves its solubility in water, further improves the bioavailability of drugs, enhances drug efficacy and reduces the dosage. Therefore, after inclusion with the drug, the proportion, type, inclusion conditions, preparation method of the inclusion complex and the existence form of the drug can affect the solubility of the drug in the inclusion complex.
2. Increase the stability of drugs
Some drugs will degrade due to exposure to light, heat and oxygen, thereby losing some or all of their efficacy, and cannot achieve the requirement of maintaining stable properties within the 3-5 year validity period of the drug under normal circumstances. If this product is used to encapsulate it, the drug is enclosed in the inner cavity, which can effectively reduce photolysis, oxidation and thermal damage, and is conducive to maintaining the stability of the drug.
3. Relieve and improve local irritation
Drugs entering the inner cavity of this product can avoid direct contact with biological surfaces, reduce the probability of drugs entering non-target tissues and cells, and reduce their toxic side effects. At the same time, because its inclusion complex can penetrate into the tissue well, its therapeutic effect will not be greatly reduced. The protective effect on muscle tissue is mainly due to the weak affinity of the hydrophilic inclusion complex of the drug for the myofiber cell membrane, which reduces the damage of drug injection to muscle tissue.
4. Regulate the release rate of drugs
For general oral drugs, it can play 4 controlled release effects through its inclusion complex on drugs, namely immediate release, delayed release (time-controlled release), extended release and controlled release. Selecting the right (different degrees of substitution) and rationally designing oral drug formulations can improve or regulate the release rate.
5. Enhance the corneal permeability of drugs
For example, the corneal permeability of nitrocarpine can be increased by nearly 4 times.
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