Shandong Binzhou Zhiyuan Biotechnology Co.,Ltd

    Shandong Binzhou Zhiyuan Biotechnology Co.,Ltd

    Tel: +86-543-2616568

    Fax: +86-543-2605568


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

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Hydroxypropyl Beta Cyclodextrin In Ophthalmic Preparations In The Progress Of Application

1. Increase the solubility of drugs  In the CD conical body cavity, because the hydroxyl group on the molecule is mainly distributed on the periphery of the cavity, the oxygen atom is located in the middle part of the cavity, so the cavity is hydrophobic, and the outside of the cavity is hydrophilic. In aqueous solution, CD lipophilic cavity water molecules form hydrogen bonds with the tendency not to meet and water molecules than the solution with more high enthalpy and high enthalpy of water molecules is the driving force of the energy of the system is reduced, so the lipophilic drug molecules or lipophilic structure can through the replacement of the water molecules inside the CD cavity and the formation of inclusion complexes, re - use the CD cavity and hydrophilic, and the solubility increases. HP-B-CD through to 3-CD hydroxypropylation and destruction of the intramolecular hydrogen bond, make their water solubility increased significantly, and more significant to improve the dissolution of drug solubility.
2.Improve the stability of drugs
Eye drops are the most common form of eye use, but the presence of hydrolysis, photolysis, oxidation, in vitro heterogeneous, and enzymatic hydrolysis and so on, so that drug degradation, stability and reduce. If HPCD is used in combination with the drug molecules into its internal cavity, can form a so-called "molecular capsule", and to prevent the degradation of drugs. The stability of HP-B-CD was determined by the inclusion of the drug, and the stability of the drug was determined by the inclusion degree and the degradation rate of the inclusion compound. The increase of inclusion degree and the decrease of the degradation rate of the drug in the inclusion compound will increase the stability of the drug.
3.Enhanced drug corneal permeability
The eye to the administration of the drug molecules must has a certain degree of hydrophilicity to table through the eye by tears and hydrophilic mucin consisting of aqueous liquid layer. At the same time, also has certain fat soluble through partial fat soluble biofilm (cornea, conjunctiva, etc.) into the eye tissue. At present, the HP-B-CD increasing corneal drug penetration mechanism mainly have two different views: (1) that HP-B-CD through the destruction of the corneal cell membrane, or through penetrate into the cell membrane or through from cell membrane extraction of fat soluble substances such as cholesterol and phospholipids to increase penetration. II think due to HP-B-CD molecule is relatively large and water soluble shell, making it difficult through corneal partial fat soluble, so presumably HP-B-CD actually just as fat soluble carrier of drug molecules, increase the solubility of drugs in water, and through the water liquid layer is transported to the corneal surface and by diffusion through the cornea into ocular tissue and water soluble drug molecules with HP-B-CD showed poor compatibility, and does not have the effect. After a mechanism that drugs through the mucin layer is controlled by diffusion and drug through the cornea is controlled by membrane, when low concentration of HP-B-CD and drug of corneal permeability coefficient with the increase of the concentration of HP-B-CD increases, when the supply pool of drug in the saturated state, drug thermodynamic activity the highest (drug through the trend of corneal max); and when the HP-B-CD excessive, due to the thermodynamic activity of the drug supply pool decreased, corneal drug penetration coefficient decreases with the increase of the concentration of HP-B-CD.
4.Reduce the eye irritation of drugs
Usually drops in drugs are required to give a higher concentration, coupled with some drugs itself has certain stimulation. Therefore, the eye tissues easily produced stimulation is eye to common fault for drugs. HP-B-CD can reduce the eye irritation of ophthalmic preparations, the following ways: first, through the inclusion of stimulating drugs, and to cover up their irritation. Second, to replace the eye tissue irritation accessories. Through increasing the corneal permeation rate of the drug, the bioavailability of the drug is increased, the concentration of the drug is reduced, and the stimulation of the high concentration drug is reduced.

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