ヒドロキシプロピル-β-シクロデキストリン 化学特性,用途語,生産方法
外観
白～淡黄色、結晶性粉末～粉末
定義
本品は、シクロデキストリン(*)のヒドロキシプロピルエーテルであり、次の化学式で表される。
参照表示名称：シクロデキストリン
用途
製剤包接、安定剤等の研究用。
化粧品の成分用途
キレート剤、乳化安定剤
化学的特性
White to slightly yellow powder
使用
2-Hydroxypropyl-β-cyclodextrin (HBC) is a widely used modified cyclodextrin, the lipophilic cavity formed by 7 glucose units. Drug solubility in water is greatly enhanced by complexing with 2-Hydroxypropyl-β-cyclodextrin.
調製方法
Hydroxypropyl betadex is prepared by the treatment of an alkaline
solution of b-cyclodextrin with propylene oxide. The substitution
pattern can be influenced by varying the pH. Formation of O-6 and
O-2 substituted products is favored by high and low alkali
concentration, respectively. The mixture of products produced
may be refined by preparative chromatography.
一般的な説明
(2-Hydroxypropyl)-β-cyclodextrin, a hydroxyalkyl derivative, finds application as a formulation vehicle that is used to enhance the solubility of the drugs in aqueous solutions for the successful delivery of medical agents to biological systems. It is generally employed as a substitute for α-, β- and γ-cyclodextrins.
応用例（製薬）
Hydroxypropyl betadex has been widely investigated in pharmaceutics
and has principally been used as a solubilizer for
hydrophobic molecules in oral liquids,oral solids, parenterals,
pressurized metered dose inhalers, dry powder inhalers,
and topical formulations. It has also been shown to act as a
stabilizer during processing and storage of formulations.
Hydroxypropyl betadex inclusion complexes have been reported
to show mechanical properties distinct from the pure materials.
The reported advantage of hydroxypropyl betadex over unsubstituted
b-cyclodextrin is its greater water solubility.
副作用
2-Hydroxypropyl-β-cyclodextrin (HP-beta-CD) has been shown to be well tolerated in humans, with the main adverse event being diarrhoea and there have been no adverse events on kidney function, documented to date[1].
安全性
The pharmaceutical toxicology of hydroxypropyl betadex has been
reviewed, and in general, the material was found to be of low
toxicity. It has been suggested that hydroxypropyl betadex may
have a synergistic toxic effect with, for example, carcinogens, by
increasing their solubility and thus bioavailability.
貯蔵
Store in well-closed containers.
規制状況(Regulatory Status)
Included in oral and parenteral medicinal products. Included in an
injectable preparation licensed in the UK for intramuscular or
intravenous administration.
ヒドロキシプロピル-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