December 31, 2020
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Methyl beta cyclodextrin (me - β - CD) is an alkylated derivative of β - cyclodextrin (β - CD). Because me - β - CD is not only water-soluble, but also soluble in organic solvents, and has strong drug inclusion ability, it is an important product, and pharmaceutical industry pays great attention to it. However, because of its strong hemolysis, its application has been shadowed. In recent years, however, solubilization of oral drugs, suppository, transdermal absorbent, nasal spray and other small dose of insoluble drugs has become a hot topic.
Me - β - CD is the most effective cosolvent for insoluble substances and the best stabilizer for many chemical substances. Me - β - CD is widely used in medicine, food, pesticide, cosmetics, daily chemicals, chemical industry, dyeing and finishing of textiles, chromatographic analysis and functional materials due to its excellent solubility and inclusion, and its solubility in water and organic solvents.
Me - β - CD has good inclusion ability and solubility. However, its outstanding disadvantage is that it has strong hemolysis. Me - β - CD is not suitable for injection because of its hemolysis and irritation to mucosa. However, in the latest review of me - β - CD, it is also mentioned that only at a higher concentration, me - β - CD will damage the cell membrane, and at a lower concentration, it will not produce any hemolysis, and it will play a protective role in the stability of the cell membrane. Therefore, for drugs with poor solubility and high activity, me - β - CD can be used in some preparations when the dosage is very low. For example, radioactive markers can be solubilized with DM - β - CD, which does not accumulate in the body and is quickly excreted through the kidney. At present, the marketed drugs containing DM- beta -CD formula have been released by chlorphenicol /Me- beta -CD eye drops of Portugal Oftalder company, the trade name is Clorocil, and 17- EDI /Me- nasal aerosol spray of French Servier company, the trade name is Aerodiol.
Methyl beta cyclodextrin (MBCD) has been widely used abroad. As a potential functional pharmaceutical excipient in China, the research of MBCD can promote its application in China.
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