The Absorption of99mTc-alendronate Given by Rectal Route in Rabbits

Autor:	Kamil Köseoğlu, İpek Özcan, Işık Özgüney, Makbule Asikoglu, Hayal Ozkilic, Oya Orumlu, Tamer Güneri
Rok vydání:	2008
Předmět:	Male endocrine system congenital hereditary and neonatal diseases and abnormalities medicine.medical_specialty Chemical Phenomena endocrine system diseases Chemistry Pharmaceutical Administration Oral Biological Availability Pharmaceutical Science Polyethylene glycol Absorption (skin) Suppository Gastroenterology Diffusion Food-Drug Interactions chemistry.chemical_compound Pharmacokinetics Administration Rectal Internal medicine medicine Animals Alendronate Bone Density Conservation Agents Chemistry Physical Alendronic acid Technetium nutritional and metabolic diseases General Medicine Surgery Bioavailability Intestinal Absorption Solubility chemistry Rectal Absorption Isotope Labeling Rectal administration Rabbits medicine.drug
Zdroj:	Pharmaceutical Development and Technology. 13:213-220
ISSN:	1097-9867 1083-7450
DOI:	10.1080/10837450801949509
Popis:	Alendronate sodium (ALD) is a bisphosphonate medication used in the treatment and prevention of osteoporosis. Absorption of ALD as oral formulation is very poor (0.5%-1%). Its bioavailability can decrease with food effect. It has some gastrointestinal adverse effects such as gastritis, gastric ulcer, and esophagitis. The aim of this study was to develop a rectal formulation of ALD as an alternative to oral route and to investigate the absorption of it by using gamma scintigraphy. For this reason, ALD was labeled with Technetium-99m ((99m)Tc) by direct method. The radiochemical characterization of the (99m)Tc-ALD was carried out by paper chromatography, thin layer chromatography, and electrophoresis methods. The labeling efficiency of (99m)Tc-ALD was found 99% without significant changes until 6 h postlabeling at room temperature. The rectal suppositories containing (99m)Tc-ALD were prepared by fusion method using polyethylene glycol (PEG) 1500. The (99m)Tc-labeled ALD suppositories were administrated to rabbits by rectal route. Serial scintigrams over all bodies of the rabbits were obtained at different time intervals using a gamma camera. We found that the rectal absorption of (99m)Tc-ALD from suppository formulation was possible. According to our results, this formulation of ALD can be suggested for the therapy of osteoporosis as an alternative route.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c74b7ef577936ae45ba590170f264303 https://doi.org/10.1080/10837450801949509 Zobrazit plný text záznamu Plný text ve formátu PDF Plný text ve formátu HTML
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