Shandong Binzhou Zhiyuan Biotechnology Co., LTD
The introduction of hydroxypropyl breaks the molecular inner ring hydrogen bond of beta-cyclodextrin, it overcomes the major shortcoming of poor water solubility of beta-cyclodextrin. (2-hydroxypropyl)-beta-cyclodextrin is one of cyclodextrin derivatives with most in-depth and widest application, it is mainly used in food, pharmaceutical and cosmetics industries.
Appearance : white powder
Hydroxypropy-beta-cyclodextrin has very high water solubility in normal temperature, generally more than 50%. In room temperature, its solubility is 750mg/ml, but the solubility of beta-cyclodextrin is 18mg/ml.
The selectivity of hydroxypropy-beta-cyclodextrin for inclusion compound is different with beta-cyclodextrin. The molecular proportion for some materials inclusion can be different.
Hydroxypropy-beta-cyclodextrin and beta-cyclodextrin are basically not being decomposed and metabolized in human body, and also not accumulated. Oral hydroxypropy-beta-cyclodextrin can basically be totally excreted in the stools in complete form. For parenteral routes, it can basically be totally excreted in the urine in complete form. But beta-cyclodextrin has low water solubility, parenteral routes has renal toxicity and can`t be used for injection.
Comparing with beta-cyclodextrin or other derivatives, for example,methylation-beta- cyclodextrin, hydroxypropy-beta-cyclodextrin has low hemolytic activity, using more safety.
Hydroxypropy-beta-cyclodextrin can be applied in the following aspects:
1. To increase water solubility of poorly soluble drugs.
Hydroxypropy-beta-cyclodextrin has big solubility, the water solubility of poorly soluble drugs can be significantly increased with inclusion of hydroxypropy-beta-cyclodextrin, so it Is an ideal solubilizer for the insoluble drugs. Baicalin with inclusion of hydroxypropy-beta-cyclodextrin, its solubility in water is increased to 2.743mg/ml from 0.112 mg/ml, the solubility is increased by 24.5 times.
2. To enhance the stability of drugs.
Hydroxypropy-beta-cyclodextrin can better to increase the stability of the inclusion compound. For example, estradiol is enveloped by hydroxypropy-beta-cyclodextrin, placed at room temperature, the half-life of its degradation is prolonged from 1.2 years to 4 years.
3. To reduce the side effects of drugs
Hydroxypropy-beta-cyclodextrin can efficiently reduce toxic and side effects. For example, the blood vessel dilation drug nimodipine is difficult to soluble in water, it can have first-pass effect with taking orally. 0.05 mol/L hydroxypropy-beta-cyclodextrin can Increase its solubility 60 times, decreased the irritation to muscle. Hydroxypropy-beta-cyclodextrin can alleviate the injection pain caused by of etomidate.
4. To improve the utilization of drugs
Hydroxypropy-beta-cyclodextrin is prepared into inclusion compound with poorly soluble drugs, it not only can increase solubility and dissolution rate of drugs, but can improve the oral bioavailability. For example, ursodeoxycholic acid is enveloped by hydroxypropy-beta-cyclodextrin, disintegration time is the same as the listed products, but dissolve quickly and completely, for health volunteers oral bioavailability and peak concentrations are more than two times that of commercially available products.
Application of hydroxypropy-beta-cyclodextrin
1. Hydroxypropy-beta-cyclodextrin application in pharmaceutical industry.
In pharmaceutical industry, its relative surface activity and hemolytic activity is low, and no irritation to muscle, so it is an ideal injection solubilizing agent and drug excipients. Hydroxypropy-beta-cyclodextrin can enhance the solubility of poorly soluble drugs, increase drug stability, improve biologic utilization of drugs, increase efficacy of drugs or decrease dosage, can adjust or control the drug release rate, reduce the side effects of drugs. Hydroxypropy-beta-cyclodextrin can be used for oral medicine, injections, mucosal drug delivery systems, carrier of lipophilic targeted drugs. Hydroxypropy-beta-cyclodextrin can also be used for protective agent and stabilizer for protein.
2. Hydroxypropy-beta-cyclodextrin application in cosmetics industry.
Hydroxypropy-beta-cyclodextrin can be used as stabilizer, emulsifier, deodorant, and etc. in cosmetics raw materials, it can reduce the stimulation of organic molecules in cosmetics to skin and mucous membrane tissue, enhance stability of active ingredients, prevent volatilization and oxidation of nutrients. It can increase water solubility of insoluble flavors and fragrances, keep sustained release and lasting of aroma.
3. Hydroxypropy-beta-cyclodextrin application in food industry.
In food industry hydroxypropy-beta-cyclodextrin can enhance stability and long residual action of nutrient molecules, it can cover or rectify bad smell and taste of food nutrient elements, can improve production process and product quality, and increase shelf life of product.
Hydroxypropy-beta-cyclodextrin applications in medical field
1. Hydroxypropy-beta-cyclodextrin can increase water solubility of poorly soluble drugs.
Hydroxypropy-beta-cyclodextrin is easy to dissolve in water, the solubility at room temperature is generally greater than 50 g/100mL, even up to 80 g/100mL or more. When the concentration is less than 40%, the fluidity is good, the viscosity is not big. For the pharmaceutical industry it can improve the solubility of drugs, without using organic solvents, surfactants and lipids. The insoluble drug can significantly increase water solubility with inclusion of hydroxypropy-beta-cyclodextrin. After drugs form complex with hydroxypropy-beta-cyclodextrin, the increase of its concentration is linear with the increase of hydroxypropy-beta-cyclodextrin concentration.
2. Hydroxypropy-beta-cyclodextrin can increase the stability of drugs and improve the bioavailability of drugs.
In the storage process drugs will be affected by light, heat, humidity, and many other factors, which can directly affect drugs quality. So stability is an important investigation index. Once hydroxypropy-beta-cyclodextrin includes drugs, drugs enter into hole, it can play a role in preventing drug volatilization, sublimation, oxidation and light decomposition. The drugs inclusion with hydroxypropy-beta-cyclodextrin has fast dissolving speed, quick release, can increase the absorption of organism for drugs, it is beneficial to improve the bioavailability of drugs.
3. Hydroxypropy-beta-cyclodextrin can reduce the toxic and side effects of drugs.
Hydroxypropy-beta-cyclodextrin can make complexation for indissolvable drugs and converse route of medication, which can significantly reduce toxicity and irritation of drugs on human body.
Hydroxypropy-beta-cyclodextrin can be used for oral drugs, injections, mucosal drug delivery system Including nasal mucosa, rectum, cornea, etc, transdermal drug delivery system, carrier of lipophilic targeted drugs. Hydroxypropy-beta-cyclodextrin can also be used for protective agent and stabilizer for protein.