Cyclodextrin Technology by J. Szejtli

By J. Szejtli

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In animals which survived the treatment, the symptoms disappeared rapidly, generally within 24- hours [ 92 1. After 168h, the LDso was 24-8 mg/kg for male rats and 505 mg/kg for the females [ 314 1. Quite different results were also observed, for example upon subcutaneous administration of 1000 mg/kg ~-cyclodextrin to 10 male and 10 female rats, all animals survived the treatment. c. LDso was about 3700 mg/kg [ 312 1. Daily injections of 200mg of a-cyclodextrin (equivalent to 84-0 mg/kg) over seven days resulted in a strong swelling of the kidneys, and their light yellowish-brown discolouration.

With y-cyclodextrin a stronger change results in the spectrum of bromocresol green than with the other cyclodextrins. This enables a rapid, semiquantitative determination of the y-cyclodextrin [ 154- J. The calmagite, 1- (1hydroxy-4--methyl-2-phenylazo)-2-naphthol-4-sulphonic acid, is apparently specific for y-cyclodextrin. Other cyclodextrins do not form complexes with this metal indicator, and its bright red colour at 550nm depends only on the y-cyclodextrin concentration [ 126 1. A fluorophotometric method is based on a strong increase of the fluorescence of dansyl chloride (5-dimethylamino-l-naphthalenesulphonyl chloride), dansyl leucine and l-anilinonaphthalene-8-sulphonate, caused by the B-cyclodextrin [ 160 1.

The literature on the CGT enzyme has been summarised up to 1962 [ 83 1 and to 1978 [ 345 1 in former monographs. The chemical synthesis of cyclodextrin has been published recently [ 278 l, this is however only a scientific achievement. Cyclodextrins can be industrially produced only by enzymic conversion of starch, utilising the CGT enzyme. This enzyme is of fundamental importance in the production of cyclodextrins. Extensive work has been dedicated to CGT enzyme kinetics [ 20,21,25,26, 30,162 l.

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