Absorption of a pharmacological dose of vitamin D₃ from two different lipid vehicles in man: Comparison of peanut oil and a medium chain triglyceride

Abstract

The absorption of a pharmacological dose of vitamin D, from two different lipid vehicles, peanut oil, containing long chain fatty acids, and a medium chain triglyceride was compared. Serial measurements of the serum concentration of vitamin D, after dosage were made. The serum levels of 25-hydroxyvitamin D,, the major circulating vitamin D3 metabolite, were also determined. The analytical methods used were based on HPLC. In the fasting state, the serum levels of vitamin D, were significantly higher after administration in peanut oil than after administration in the medium chain triglyceride. When the vitamin D3 dose was ingested together with food no difference between the two formulations was observed. Only small inter-formulation differences in serum 25-hydroxyvitamin D, levels were detected. The results indicate that the presence of long chain fatty acids facilitates the absorption of vitamin D, KEY WORDS Vitamin D3 Lipid vehicle Absorption

Use of in vitro lipid digestion data to explain the in vivo performance of triglyceride-based oral lipid formulations of poorly water-soluble drugs: Studies with halofantrine

“…On first examination, the data appear contradictory and some reveal better performance for MCT 21,22 whilst others suggest a preference for LCT 13,[23][24][25] (see Ref. 14 for a review). However, closer examination reveals that the two studies performed using either fasted healthy humans or dogs 13,24,25 showed, in agreement with our results, higher drug exposure after administration of poorly water-soluble compounds in LCT solution formulations. All the other studies (including all those where MCT was shown to be most preferable) were conducted in rats.…”

Improvement of Oral Bioavailability of N-251, a Novel Antimalarial Drug, by Increasing Lymphatic Transport with Long-Chain Fatty Acid-Based Self-Nanoemulsifying Drug Delivery System

“…Long-chain fatty acids and their glycerides are well known to be transported to the lymphatic system after absorbed from the small intestine (29). It was also reported that lipids with long-chain fatty acids promote the transport of drugs into the lymphatic system more effectively than those with short-and/or medium-chain fatty acids (15)(16)(17). Furthermore, SNEDDS/SMEDDS formulations composed of lipids with long-chain fatty acids were reported to result in the lymphatic transport of larger amount of drugs than those with medium-chain fatty acids (30,31).…”

“…Since the ratio of lymphatic transport of drugs was reported to be de pendent on the nature of oils used (15)(16)(17)30,31,37), the ratios were also independently defined as a F and a B for LC-SNEDDS F and MC-SNEDDS B, respectively. In the case of N-251, Fa can be assumed to be unity because N-251 was considered to be almost completely absorbed as described above.…”

“…Although medium-chain fatty acid-based SNEDDS (MC-SNEDDS) was prepared first, the improvement of bioavailability by MC-SNEDDS was not enough due to the high hepatic firstpass elimination of N-251. Therefore, long-chain fatty acidbased SNEDDS (LC-SNEDDS) were prepared second for aiming to enhance the bioavailability by circumventing the hepatic first-pass elimination since lipids with long-chain fatty acids promote the transport of drugs into the lymphatic system more effectively than those with short-and/or medium-chain fatty acids (15)(16)(17). In vivo oral absorption of N-251 and the lymphatic transport after absorption were evaluated for several SNEDDS formulations.…”

Biodisponibilidade de vitaminas lipossolúveis

“…Ácidos graxos de cadeia longa provenientes do óleo de amendoim facilitaram a absorção de vitamina D presente, quando comparada a doses farmacológicas dessa vitamina 29 .…”