PURPOSE: To study the use of long chain triglycerides (LCT) as a lymphotropic carrier of (3)H-seocalcitol by comparing the lymphatic transport and the portal absorption of (3)H-seocalcitol when dissolved in a (1) LCT solution or a (2) reference solution without lipid containing propylene glycol (PG). MATERIALS AND METHODS: A lymph cannulated conscious rat model was dosed orally with (3)H-seocalcitol dissolved in either LCT or PG. Lymph was collected continuously, and blood was sampled over 9 h. (3)H-seocalcitol in blood and lymph and triglycerides in lymph were analysed. RESULTS: A statistically significantly (p < 0.05) higher recovery of the dosed (3)H-seocalcitol was found in the intestinal lymph upon administration of the LCT solution (1.3 +/- 0.6%) compared to the PG solution (0.5 +/- 0.4%). The portal absorption of (3)H-seocalcitol was significantly (p < 0.05) higher from the LCT solution (16.2 +/- 2.2%) than from the PG solution (10.8 +/- 0.8%). CONCLUSIONS: The LCT solution resulted in a statistical significantly higher level of lymphatic and portal transport of (3)H-seocalcitol compared with the PG solution. However, even though LCT facilitates the formation of chylomicrons, (3)H-seocalcitol favours absorption directly to the portal blood probably due to the moderate lipophilicity of the molecule.
PURPOSE: To study the use of long chain triglycerides (LCT) as a lymphotropic carrier of (3)H-seocalcitol by comparing the lymphatic transport and the portal absorption of (3)H-seocalcitol when dissolved in a (1) LCT solution or a (2) reference solution without lipid containing propylene glycol (PG). MATERIALS AND METHODS: A lymph cannulated conscious rat model was dosed orally with (3)H-seocalcitol dissolved in either LCT or PG. Lymph was collected continuously, and blood was sampled over 9 h. (3)H-seocalcitol in blood and lymph and triglycerides in lymph were analysed. RESULTS: A statistically significantly (p < 0.05) higher recovery of the dosed (3)H-seocalcitol was found in the intestinal lymph upon administration of the LCT solution (1.3 +/- 0.6%) compared to the PG solution (0.5 +/- 0.4%). The portal absorption of (3)H-seocalcitol was significantly (p < 0.05) higher from the LCT solution (16.2 +/- 2.2%) than from the PG solution (10.8 +/- 0.8%). CONCLUSIONS: The LCT solution resulted in a statistical significantly higher level of lymphatic and portal transport of (3)H-seocalcitol compared with the PG solution. However, even though LCT facilitates the formation of chylomicrons, (3)H-seocalcitol favours absorption directly to the portal blood probably due to the moderate lipophilicity of the molecule.
Authors: Natalie L Trevaskis; Claire L McEvoy; Michelle P McIntosh; Glenn A Edwards; Ravi M Shanker; William N Charman; Christopher J H Porter Journal: Pharm Res Date: 2010-03-11 Impact factor: 4.200