Betadex Sulfobutyl Ether Sodium 化学特性,用途語,生産方法
化学的特性
β-Cyclodextrin, sulfobutyl ethers, sodium salts is a cyclic oligosaccharide containing seven D-(t)- glucopyranose units attached by α(1→4) glucoside bonds. Sulfobutylether b-cyclodextrin is an anionic bcyclodextrin derivative with a sodium sulfonate salt separated from the hydrophobic cavity by a butyl spacer group. The substituent is introduced at positions 2, 3, and 6 in at least one of the glucopyranose units in the cyclodextrin structure. Introducing the sulfobutylether (SBE) into b-cyclodextrin can produce materials with different degrees of substitution, theoretically from 1 to 21; the hepta-substituted preparation (SBE7-b-CD) is the cyclodextrin with the most desirable drug carrier properties. Sulfobutylether b-cyclodextrin occurs as a white amorphous powder.
調製方法
Sulfobutylether β-cyclodextrin is prepared by alkylation of bcyclodextrin
using 1,4-butane sultone under basic conditions. The degree of substitution in b-cyclodextrin is controlled by the
stoichiometric ratio of β-cyclodextrin to sultone used in the process.
Toxicity evaluation
Sulfobutylether b-cyclodextrin sodium (SBECD) has been associated with toxic effects in the kidney. Doses up to 1500 mg/kg produced no histopathological evidence of toxicity in dog kidneys.
安全性
Sulfobutylether b-cyclodextrin is derived from b-cyclodextrin,
which is nephrotoxic when administered parenterally.
However, studies have shown that sulfobutylether bcyclodextrin
is well tolerated at high doses, when administered via
intravenous bolus injections, orally, and by inhalation. Up to
9 g/day may be administered by IV infusion in a licensed
voriconazole formulation. The safety following high doses of
sulfobutylether β-cyclodextrin intravenous administration in
humans is continually being investigated.
Sulfobutylether β-cyclodextrin has been subjected to an extensive
battery of in vitro and in vivo genotoxicity and pharmacological
evaluations. No genotoxic or mutagenic changes were
observed with sulfobutylether β-cyclodextrin administration. Sulfobutylether
β-cyclodextrin is biocompatible and exhibits no
pharmacological activity. It is rapidly eliminated unmetabolized
when administered intravenously.
貯蔵
Sulfobutylether b-cyclodextrin(182410-00-0) is stable in the solid state and should be protected from high humidity. It should be stored in a tightly sealed container in a cool, dry place.
It will reversibly take up moisture without any effect on the appearance of the material at humidities up to 60% RH. Equilibration at RH values above 60% will result in deliquescence. Once in this state, the material can be dried, but will give a glasslike product. This water absorption behavior is typical of amorphous hygroscopic materials.
Sulfobutylether b-cyclodextrin is stable in aqueous solutions at values above about pH 1. It can degrade in highly acidic (pH < 1) solutions, particularly at elevated temperatures, producing the ring-opened form, followed by hydrolysis of the a(1-4) glucoside bonds.
Sulfobutylether b-cyclodextrin solutions may be autoclaved.
不和合性
The preservative activity of benzalkonium chloride is reduced in the
presence of sulfobutylether b-cyclodextrin.
規制状況(Regulatory Status)
Sulfobutylether β-cyclodextrin is included in IV and IM injectable
products currently approved and marketed in the USA, Europe, and
Japan. It is included in the FDA Inactive Ingredients Database for
IM and IV use. Its use by other routes, including SC, oral,
inhalation, nasal and ophthalmic, is being evaluated in clinical
studies.
Betadex Sulfobutyl Ether Sodium 上流と下流の製品情報
原材料
準備製品