Effect of Polymorphism on the Dissolution Behavior and Gastrointestinal Absorption of Chlortetracycline Hydrochloride

The existence of the two crystalline forms of chlortetracycline hydrochloride (CTC-HCI) was confirmed by infrared spectroscopy and X-ray diffraction. From the dissolution studies with crystalline powder and compressed disk, an appreciable difference in the dissolution behavior in water was detected...

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Bibliographic Details
Published inChemical & pharmaceutical bulletin Vol. 22; no. 3; pp. 638 - 642
Main Authors ITO, KEIJI, MIYAZAKI, SHOZO, ARITA, TAKAICHI, HORI, RYOHEI
Format Journal Article
LanguageEnglish
Published Japan The Pharmaceutical Society of Japan 1974
Japan Science and Technology Agency
Subjects
Animals
Chlortetracycline - blood
Chlortetracycline - metabolism
Chlortetracycline - urine
Digestive System - metabolism
Humans
Intestinal Absorption
Male
Polymorphism, Genetic
Rabbits
Solubility
Spectrophotometry, Infrared
X-Ray Diffraction
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ISSN0009-2363
1347-5223
DOI10.1248/cpb.22.638

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Summary:The existence of the two crystalline forms of chlortetracycline hydrochloride (CTC-HCI) was confirmed by infrared spectroscopy and X-ray diffraction. From the dissolution studies with crystalline powder and compressed disk, an appreciable difference in the dissolution behavior in water was detected between the two forms. In order to determine the effect of polymorphism on the gastrointestinal absorption of CTC-HCl, blood plasma levels obtained in rabbits after intraduodenal administration and cumulative amounts excreted in human subjects after oral administration of the two forms were compared. The results indicated that polymorphic state of CTC-HCl significantly influences bioavailability of the CTC-HCl.
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ISSN:0009-2363
1347-5223
DOI:10.1248/cpb.22.638