Hydroxypropyl - beta-cyclodextrin

Hydroxypropyl - beta-cyclodextrin.

Properties: white, sweet, odorless

Content: 98% or higher

Solubility: more than 80g/100ml

Substitution degree: 3-9

Moisture: 6.0% or less

Chloride: less than or equal to 0.05%

Ash: 0.5% or less

Heavy metal: less than 0.001%

Total of bacteria: less than 1000 CFU/g

Mold and yeast: less than 100 CFU/g

Pathogenic bacteria: no Negative.

Product introduction.

Hydroxypropyl - beta-cyclodextrin (hydroxypropyl - beta-cyclodextrin CD) is a hydroxyalkyl derivative of b-cyclodextrin. It like beta cyclodextrin, not only for many compounds have good envelope effect, can improve the stability of the enveloping substance, and high solubility in water, can improve the envelope drug release rate and bioavailability. In this paper, the properties, applications and preparation methods of hydroxypropyl - beta-cyclodextrin are reviewed, and its application in medical research is provided.

1. Hydroxypropyl. The characteristics of beta-cyclodextrin.

In the Chinese rmacopoeia, the insoluble and insoluble drugs accounted for about a third of the drugs in the list of essential medicines, increasing the solubility of these drugs in water to improve the efficacy and significance. The use of b-cyclodextrin or its derivatives to increase the water solubility of the drug is a widely studied method for many years. But the low solubility of a cyclodextrin itself limits its application; Hydroxypropyl one eight. Cyclodextrin has good water solubility, high thermal stability, low hemolysis, low e and effective drug solubilization, and is considered to be extremely promising for injection. It has the following features.

1.1 hydroxypropyl -B- cyclodextrin, at normal temperature, has a high water solubility, usually more than 50% (at room temperature, the solubility is 750 mg/ml, while the beta -CD is 18 mg/ml).

1.2 hydroxypropyl - a cyclodextrin and B 1 cyclodextrin have different selectivity to the envelope, which may be different for certain substances.

1.3 hydroxypropyl - beta-cyclodextrin and B. Cyclodextrin is not metabolized or accumulated in the human body. Oral hydroxypropyl - beta-cyclodextrin is mostly excreted in complete form with the stool; Non-intestinal drug delivery, basically in complete form with urine excreted in vitro; However, B- cyclodextrin is low in water solubility, and the non-intestinal drug has renal cannot be used as an injection.

1.4 hydroxypropyl - a cyclodextrin is less active than B cyclodextrin or other derivatives (such as methylation - a cyclodextrin), with low hemolytic activity and safer use.

The application of hydroxypropyl - cyclodextrin has been widely concerned because of the above characteristics of hydroxypropyl - beta-cyclodextrin. It is mainly applied in the following aspects:

2. Increase the water solubility of insoluble drugs.

Because hydroxypropyl is a good solubility of cyclodextrin, insoluble drugs can significantly increase water solubility after it is coated. So it is an ideal solubilizer for insoluble drugs. Shao wei et al. used hydroxypropyl 1. The results showed that baicalin was dissolved in water from 0. 112 mg/ml increased to 2. 743mg/ml, the solubility increased by 24. 5 times.

2.2 increase the drug stability of hydroxypropyl. Beta-cyclodextrin can better increase the stability of the envelope drugs. For example: estradiol with hydroxypropyl. The biodegradable half-life is 1. Two years to four years.

2.3 reduction of drug side effects hydroxypropyl -B cyclodextrin can effectively reduce the e effects of drugs. For example, the angiectasis drug nimodipine is difficult to dissolve in water, and oral administration is easy to be affected by the liver. 0. 5 mol/L hydroxypropyl -B- cyclodextrin can increase its solubility by 6O times and reduce the irritation of muscle by J. Hydroxypropyl. B. Cyclodextrin can also relieve the injection pain caused by etomidate.

2.4 to improve the drug utilization, the inclusion of hydroxypropyl B- cyclodextrin and refractory drugs can not only increase drug solubility and dissolution rate, but also improve oral bioavailability. Bear to oxygen, for example, bile acid by hydroxypropyl after a B a cyclodextrin envelope, disintegration time and listed products are the same, but completely and rapid dissolution, healthy subjects oral bioavailability and peak concentration is more than twice as many commercially available products.

3. Preparation method of hydroxypropyl - beta-cyclodextrin inclusion.

3.1 dissolution method (1) if the substance being enveloped is a water-soluble substance, the enveloped substance and hydroxypropyl can be transferred. Beta. The cyclodextrin is partially dissolved in water. (2) if the substance is insoluble in water, the enveloping substance can be dissolved in ethanol, methanol and other solvents; The hydroxypropyl -p cyclodextrin is dissolved in water or alcohol, and the two solutions are mutually soluble or miscible.

3.2 the method of promoting envelope reaction will be carried out at room temperature or low temperature:

High speed stirring; Ultrasonic treatment; (1) the colloid mill grinds; It can promote envelop reaction by homogenizing (high pressure or low pressure).

3.3 the samples after the drying envelope of the enveloping complex can be decompressed and dried and crushed, or spray drying or freeze-drying method can be used.

4. Detection of envelope complex.

Fluorescence spectrometry can be used to determine the formation constant or fluorescence anisotropy of the envelope. In addition, nuclear magnetic resonance method, high performance liquid chromatogra or thin layer chromatogra were used to analyze the envelope of hydroxypropyl - cyclodextrin on some substance.

The above mentioned envelope method is for reference only. Different treatment methods can be chosen for different substances. Even if it is the same treatment method, it will get different envelop effect due to different processing temperature, concentration of solution, length of treatment and different processing strength.

Hydroxypropyl times he dose cyclodextrins have security, good intermiscibility with blood, don't change effect, increase the water-soluble, stability, etc., are considered to be more promising drug carrier material. With the development of science and technology, the application of hydroxypropyl - cyclodextrin in traditional Chinese medicine will be more and more extensive. It will definitely go to the rmaceutical industry and play its unique role in mass production.