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Improvement of intestinal absorption of human calcitonin by chemical modification with fatty acids: Synergistic effects of acylation and absorption enhancers
- Source :
- International Journal of Pharmaceutics. 134:47-57
- Publication Year :
- 1996
- Publisher :
- Elsevier BV, 1996.
-
Abstract
- To improve the intestinal absorption of human calcitonin (hCT), novel lipophilic derivatives of hCT were synthesized by chemical modification with short-chain length fatty acids such as acetic acid and caproic acid, and the intestinal absorption and stability of these derivatives were examined in rats. The intestinal absorption properties of hCT and its acyl derivatives, acetylated hCT (Ac-hCT) and caproylated hCT (Cap-hCT), were estimated by measuring its hypocalcemic effects. Their intestinal absorption and stability in the intestinal mucosal homogenates were improved by increasing the carbon number of the fatty acid. Furthermore, we investigated the effects of co-administered absorption enhancers, sodium glycocholate (Na-GC), N-lauryl-β-D-maltoside (LM), sodium deoxycholate (Na-DC) and sodium salicylate (Na-Sal), on the intestinal absorption of hCT and its acyl derivatives. Their intestinal absorption was slightly enhanced by the addition of various absorption enhancers except for Na-Sal. However, the extent of the promoting effect was a little higher for a native hCT rather than for acyl-hCT derivatives. These results suggested that it may be possible to achieve the further absorption enhancement of hCT by using a combination of acylation and absorption enhancers.
- Subjects :
- chemistry.chemical_classification
Sodium
Pharmaceutical Science
Fatty acid
chemistry.chemical_element
Absorption (skin)
Caproic Acid
Intestinal absorption
Acylation
chemistry.chemical_compound
Acetic acid
surgical procedures, operative
chemistry
Biochemistry
immune system diseases
hemic and lymphatic diseases
Sodium salicylate
Subjects
Details
- ISSN :
- 03785173
- Volume :
- 134
- Database :
- OpenAIRE
- Journal :
- International Journal of Pharmaceutics
- Accession number :
- edsair.doi...........9138ab5119a809171317889411675163