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Pulmonary delivery alters the disposition of raloxifene in rats
- Source :
- The Journal of pharmacy and pharmacologyReferences. 72(2)
- Publication Year :
- 2019
-
Abstract
- Objective Pulmonary delivery is an effective way to improve the bioavailability of drugs with extensive metabolism. This research was designed to study the different pharmacokinetic behaviours of small molecule drug after pulmonary delivery and intragastric (i.g) administration. Methods Raloxifene, a selective estrogen receptor modulator with low oral bioavailability (~2%), was chosen as the model drug. Studies were conducted systematically in rats, including plasma pharmacokinetics, excretion, tissue distribution and metabolism. Key findings Results showed that raloxifene solution dosed by intratracheal (i.t) administration exhibited relatively quick plasma elimination (t1/2 = 1.78 ± 0.14 h) and undetected absorption process, which was similar with intravenous injection. Compared with i.g administration, the bioavailability increased by 58 times, but the major route of excretion remained faecal excretion. Drug concentration on the bone and the target efficiency were improved by 49.6 times and five times, respectively. Benefited from quick elimination in the lung, chronic toxicity might be ignored. Conclusions Pulmonary administration improved the bioavailability of raloxifene and further increased the distribution on the target organ (bone), with no obvious impact on its excretory pattern.
- Subjects :
- Selective Estrogen Receptor Modulators
Pharmaceutical Science
Biological Availability
Absorption (skin)
Pharmacology
030226 pharmacology & pharmacy
Excretion
Rats, Sprague-Dawley
03 medical and health sciences
0302 clinical medicine
Drug Delivery Systems
Pharmacokinetics
medicine
Distribution (pharmacology)
Animals
Raloxifene
Tissue Distribution
Chronic toxicity
business.industry
Bioavailability
Rats
Selective estrogen receptor modulator
030220 oncology & carcinogenesis
Raloxifene Hydrochloride
Female
business
medicine.drug
Half-Life
Subjects
Details
- ISSN :
- 20427158
- Volume :
- 72
- Issue :
- 2
- Database :
- OpenAIRE
- Journal :
- The Journal of pharmacy and pharmacologyReferences
- Accession number :
- edsair.doi.dedup.....ef34be7d7eb3281beb284cad8fd43028