β-シクロデキストリン 化学特性,用途語,生産方法
外観
白色～ほとんど白色, 結晶性粉末～粉末
定義
本品は、6~8のグルコピラノースからなる環状多糖類であり、次の化学式で表される。
環状構造：6~8
溶解性
水に易溶, エタノール及びアセトンにほとんど不溶。水に溶けやすく、エタノール及びアセトンにほとんど溶けない。
無機性値/有機性値
3230/840
用途
光学分割剤。
化粧品の成分用途
キレート剤、吸着剤
効能
封鎖剤
化学的特性
white powder
天然物の起源
A derivative of naturally occurring starch.
使用
β-Cyclodextrin is a cyclic oligosaccharide produced from starch via enzymatic conversion. β-Cyclodextrin is commonly used to produce HPLC columns allowing chiral enantiomers separation.
調製方法
Cyclodextrins are manufactured by the enzymatic degradation of
starch using specialized bacteria. For example, β-cyclodextrin is
produced by the action of the enzyme cyclodextrin glucosyltransferase
upon starch or a starch hydrolysate. An organic solvent is
used to direct the reaction that produces β-cyclodextrin, and to
prevent the growth of microorganisms during the enzymatic
reaction. The insoluble complex of β-cyclodextrin and organic
solvent is separated from the noncyclic starch, and the organic
solvent is removed in vacuo so that less than 1 ppm of solvent
remains in the β-cyclodextrin. The β-cyclodextrin is then carbon
treated and crystallized from water, dried, and collected.
製造方法
Usually produced commercially from Bacillus macerans or B. circulans fermentation of starch or starch hydrolysate.
精油の成分
In addition to carvone, the oil contains d-limonene, carveol, diacetyl furfural, methyl alcohol, acetic
aldehyde and other substances. Caraway oil consists of 3.5 to 7% volatile and fatty oils; resin, sugar, tannin, mucilage.
一般的な説明
Beta-Cyclodextrin is the most abundant and cheap cyclic oligosaccharide that forms inclusion complexes with several drug molecules. Its main application is in tablet and capsule formulations.
Pharmaceutical secondary standards for application in quality control, provide pharma laboratories and manufacturers with a convenient and cost-effective alternative to the preparation of in-house working standards.
安全性
Cyclodextrins are starch derivatives and are mainly used in oral and
parenteral pharmaceutical formulations. They are also used in
topical and ophthalmic formulations.
Cyclodextrins are also used in cosmetics and food products, and
are generally regarded as essentially nontoxic and nonirritant
materials. However, when administered parenterally, β-cyclodextrin
is not metabolized but accumulates in the kidneys as insoluble
cholesterol complexes, resulting in severe nephrotoxicity.
Cyclodextrin administered orally is metabolized by microflora in
the colon, forming the metabolites maltodextrin, maltose, and
glucose; these are themselves further metabolized before being
finally excreted as carbon dioxide and water. Although a study
published in 1957 suggested that orally administered cyclodextrins
were highly toxic, more recent animal toxicity studies in rats and
dogs have shown this not to be the case, and cyclodextrins are now
approved for use in food products and orally administered
pharmaceuticals in a number of countries.
Cyclodextrins are not irritant to the skin and eyes, or upon
inhalation. There is also no evidence to suggest that cyclodextrins
are mutagenic or teratogenic.
β-Cyclodextrin
LD50 (mouse, IP): 0.33 g/kg(16)
LD50 (mouse, SC): 0.41 g/kg
LD50 (rat, IP): 0.36 g/kg
LD50 (rat, IV): 1.0 g/kg
LD50 (rat, oral): 18.8 g/kg
LD50 (rat, SC): 3.7 g/kg
貯蔵
Cyclodextrins should be stored in a tightly sealed container, in a
cool, dry place.Cyclodextrins are stable in the solid state if
protected from high humidity.
純化方法
Recrystallise β-cyclodextrin from water and dry it for 12hours in a vacuum at 110o, or 24hours in a vacuum at 70o. The purity is assessed by TLC on cellulose containing a fluorescent indicator. [Taguchi, J Am Chem Soc 108 2705 1986, Tabushi et al. J Am Chem Soc 108 4514 1986, Orstam & Ross J Phys Chem 91 2739 1987.] [Beilstein 19 IV 6287, 19/12 V 801.]
規制状況(Regulatory Status)
Included in the FDA Inactive Ingredients Database: α-cyclodextrin
(injection preparations); β-cyclodextrin (oral tablets, topical gels);
γ-cyclodextrin (IV injections).
Included in the Canadian List of Acceptable Non-medicinal
Ingredients (stabilizing agent; solubilizing agent ); and in oral and
rectal pharmaceutical formulations licensed in Europe, Japan, and
the USA.
β-シクロデキストリン 上流と下流の製品情報
原材料
準備製品