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    Add: Boxing Economic Development Zone, Binzhou, Shandong, China

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Applications Of Hydroxypropyl-β-cyclodextrin On The Injection

Hydroxypropyl-β-cyclodextrin is β-cyclodextrin by hydroxyalkylated derivatives, their good water solubility of water-insoluble drugs have a more significant effect solubilization, which has been used abroad solubilizing agent for injection. The materials received are set out in the European Pharmacopoeia (Fourth Edition) Supplement. Although hydroxypropyl-β-cyclodextrin itself preclinical safety testing already has a certain basis, intravenous formulation in clinical trials are underway, but so far it does not know its security Collecting Medical Education Network depth, should continue its in-depth studies to further expose its possible side effects and should not be used as a routine accessories of the widely used injections.

Cyclodextrins can be used with the appropriate size and polarity of the material to form inclusion complexes, to increase the solubility of insoluble substances medical education network collected and dissolution rate of certain substances to improve stability and bioavailability, to achieve liquid substances powder of other purposes. In such products, β-cyclodextrin is most widely used. β cyclodextrins are available, for oral administration because of its low water solubility, parenteral administration may cause kidney damage, causing hemolysis and necrosis at the injection site toxicity, and can not meet the needs of intravenous administration. Hydroxypropyl-β-cyclodextrin is β-cyclodextrin hydroxy substituted derivatives thereof, having a large water solubility, low renal toxicity, haemolysis, high safety characteristics, and relatively wide safety data collection, toxic fewer side effects, is the first injectable formulations can be used cyclodextrin derivative, and a growing concern.

As a relatively new pharmaceutical excipients, hydroxypropyl-β-cyclodextrin as having good water solubility and insoluble drug solubilization good effect in China has been considerable attention. In addition to a large number of studies have reported, the State Food and Drug Administration has approved oral digoxin and hydroxypropyl-β-cyclodextrin (accessories) for clinical trials. In addition, information about its solubilization of artemisinin-based intravenous injection were reported.

Although hydroxypropyl-β-cyclodextrin has good water solubility and solubilization effect, but the U.S. Food and Drug Administration (FDA) approved so far only itraconazole and levonorgestrel acting subcutaneous injection implants using the excipients. There are two domestic manufacturers of the materials together with a medical education network collected corresponding preparations ongoing clinical studies, has not yet approved for production. Data shows that the materials have some renal toxicity and hemolysis, there are also carcinogenic, but there may be unknown to more serious side effects.

Hydroxypropyl-β-cyclodextrin of different degrees can be changed as the main drug inherent pharmacokinetic properties, tissue distribution characteristics, may cause safety and efficacy issues, it is not as a general injection materials used, select the As a powder increase / co-solvent should be careful. Using the specific varieties solubilizer To apply for clinical trials, the need to provide adequate security basis; Even injection grade hydroxypropyl-β-cyclodextrin approved for marketing, the use of the solubilizing Free Classified five varieties may also be because the reason and need for clinical trials. According to practical experience, and the State Food and Drug Administration analysis of existing data, the use of hydroxypropyl-β-cyclodextrin must pay attention to the following questions:

The first is the preparation of hydroxypropyl-β-cyclodextrin in an amount and concentration. Excessive use may cause side effects such as nephrotoxicity, solubilizing excipients to the pharmaceutical is not suitable to make large volume injection, water injection can be considered made. Followed by the auxiliary source of the problem. Although the country has injection grade hydroxypropyl-β-cyclodextrin into clinical studies, but has not yet approved for production, so far, there were only oral and topical level of approval. The third is a prescription diluted drugs medical education network collected behavior - whether there will be diluted with water to precipitate the problem is uncertain. Although literature that hydroxypropyl-β-cyclodextrin itself is soluble in water, and the formation of soluble complexes for the AL type, that is proportional to the drug concentration and the concentration of cyclodextrin increases, but related to the specific species , the results may vary. The fourth is the inclusion method. Cyclodextrin many ways, you must choose a method can achieve large-scale production. In the volatile oil cyclodextrin, a laboratory magnetic stirrer sometimes used for inclusion or inclusion by ultrasound technique, these methods can not be achieved in large-scale production, according to the actual situation instead colloid mill or stirred slurry method inclusion, etc., to explore the optimal inclusion laboratory conditions in the pilot also needs to preferably, but not directly applied to laboratory conditions.

Currently, hydroxypropyl-β-cyclodextrin preparations for intravenous administration related research is very active, but few products listed, indicating that there are still many problems to be solved. Such as hydroxypropyl-β-cyclodextrin and its inclusion in the body is not yet in-depth understanding of security, can not accurately predict the in vivo distribution patterns. We should clearly understand the current research status at registration according to the specific species, prescription, indications, usage, dosage, treatment period and other comprehensive medical education network collected to consider in order to ensure the safety and clinical effectiveness and make full use of its special characteristics inclusion, actively develop and take advantage of this multi-functional new materials, the development of better efficacy of the intravenous formulation.

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