Shanghai Zaiqi Bio-Tech Co,. Ltd

Be your reliable partner in China.

Home > News > Content
Application Of SBE-β-CD In Poorly Soluble Pharmaceutical Preparations
- Jan 06, 2019 -

Cyclodextrin (CD) is a cyclic oligomer obtained by α-1,4-glucosidic linkage obtained by fermentation of glucosyltransferase under anhydrous conditions, usually α- , β- and γ-CD, containing 6, 7, and 8 glucopyranose molecules, respectively. The β-CD hole size is considered to be the most suitable for inclusion of various drug molecules, but its disadvantages such as small water solubility, high nephrotoxicity, and strong hemolysis limit its application in injections. For this purpose, a hydrophilic derivative of sulfonate has been developed. Sulfobutyl ether Beta cyclodextrin Sodium (SBE-β-CD). SBE-β-CD is a polyanionic β-cyclodextrin derivative. The molecule is in the shape of a truncated cone. The inside of the round table is hydrophobic, and the hydrophilic sulfobutyl ether substituent is externally connected. The alkyl ether part of the inner and side chains of the round table can be compared. Well-suited for hydrophobic drug molecules, has the advantages of increased drug solubility, improved drug stability and other functions and safety, can improve the bioavailability of drugs, reduce adverse reactions, especially suitable for the development of poorly soluble drug injections, and Other areas of pharmaceutical preparations have also found wide application. Application in Injection For the injection of a poorly water-soluble drug into an injection, various methods for improving the solubility of the drug have been available, but all have certain drawbacks. If the latent solvent causes an inflammatory reaction, the aqueous medium is diluted or injected into the body, and the drug crystal may be precipitated instantaneously; the micelle formed by the surfactant may cause damage to the biofilm and has limited solubilizing ability; the polymer auxiliary material (such as polyvinylpyrrolidone) It usually has only a small binding constant with the drug, and thus often causes precipitation of the drug. Β-cyclodextrin, which is widely used for solubilizing drugs, is safe for oral administration, but when used for parenteral administration, especially injections, it can cause strong hemolytic and injurious nephrotoxicity. The cause of nephrotoxicity is that β-cyclodextrin is not metabolized by the human body after injection, and forms complex precipitates and needle crystals with cholesterol in the renal tubules [29]. There are currently 9 injections that have been solubilized with SBE-β-CD (see Table 2). Among them, in 40% of SBE-β-CD solution, the solubility of ziprasidone mesylate increased from 0.9 mg/ml to 44 mg/ml [38]. The antiarrhythmic drug amiodarone is almost insoluble in water. SBE-β-CD solubilization technology can simplify the prescription and avoid the use of unsafe adjuvant polysorbate 80 and benzyl alcohol in the prescription of Cordazone hydrochloride injection. Adverse reactions such as blood pressure changes and central nervous system depression caused by these excipients. In addition, when SBE-β-CD is combined with cefixime or melphalan, it can inhibit its hydrolysis [39-40] and improve chemical stability; SBE-β-CD contains sevoflurane, which can improve the drug. Bioavailability and blood-brain barrier permeability, reducing dose and reducing the production of degradation products [41]. Some of the injectable products in the development using SBE-β-CD are shown in Table 3. In other pharmaceutical applications, SBE-β-CD also plays a role in improving the solubility of poorly soluble drugs, reducing the interaction between drugs, improving stability, converting liquid drugs into microcrystalline powders, and reducing the gastrointestinal tract. The irritating and masking effects of the road and the eye [6]. Conclusion In addition to the classical entrapment mechanism, the solubilization mechanism of SBE-β-CD forms a hydrophobic region composed of alkyl ether moiety of sulfobutyl group to enhance the inclusion effect; charged sulfonic acid group There is a charge interaction with the drug molecule; aggregation and supersaturation stabilization play an important role. SBE-β-CD is not easy to aggregate due to its good water solubility and negative charge repulsion. However, when it is combined with a drug, nanoscale aggregates are generally formed under the influence of the drug. The supersaturation stabilization indicates that the SBE-β-CD solution has good physical stability and is safer to use when diluted. The crystal form of the drug substance, the pH of the solution, and other excipients all affect the inclusion effect of SBE-β-CD on the drug. The optimization process such as reaction temperature and inclusion method can also improve the inclusion effect. SBE-β-CD will continue to help more formulation of difficult-to-dose and unstable drugs due to its excellent safety, strong solubilization and stabilization.

Online customer service
Online customer service system