The Absorption of<sup>99m</sup>Tc-alendronate Given by Rectal Route in Rabbits

Aşıkoğlu, Makbule; Özgüney, Işık; Özcan, İpek; Orumlu, O.; Güneri, Tamer; Köseoğlu, Kamil; Özkılıç, Hayal

doi:10.1080/10837450801949509

Cited by 12 publications

(4 citation statements)

References 24 publications

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“…The most important disadvantage of AL, however, is its low oral bioavailability (under 1%) caused by several factors such as low permeability due to its negatively charged molecules; short plasma half-time (T ½ = 0.5–2 h), its chelatation by Ca 2+ ions resulting in non-absorbable complexes [8]. For these reasons, recent research on AL has been focused on increasing its bioavailability by formulation in modified release pharmaceutical dosage forms intended for oral administration or for other routes of administration (e.g., transdermal, pulmonary, nasal or rectal mucosa) [9,10,11]. The development of new systems of administration and transport is a priority direction of research in increasing the efficiency of osteoporosis medication both in terms of drug bioavailability and of patient compliance [12,13,14].…”

Section: Introductionmentioning

confidence: 99%

Alendronate-Loaded Modified Drug Delivery Lipid Particles Intended for Improved Oral and Topical Administration

Ochiuz

Grigoraş²,

Popa

et al. 2016

Molecules

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Abstract:The present paper focuses on solid lipid particles (SLPs), described in the literature as the most effective lipid drug delivery systems that have been introduced in the last decades, as they actually combine the advantages of polymeric particles, hydrophilic/lipophilic emulsions and liposomes. In the current study, we present our most recent advances in the preparation of alendronate (AL)-loaded SLPs prepared by hot homogenization and ultrasonication using various ratios of a self-emulsifying lipidic mixture of Compritol 888, Gelucire 44/14, and Cremophor A 25. The prepared AL-loaded SLPs were investigated for their physicochemical, morphological and structural characteristics by dynamic light scattering, differential scanning calorimetry, thermogravimetric and powder X-ray diffraction analysis, infrared spectroscopy, optical and scanning electron microscopy. Entrapment efficacy and actual drug content were assessed by a validated HPLC method. In vitro dissolution tests performed in simulated gastro-intestinal fluids and phosphate buffer solution pH 7.4 revealed a prolonged release of AL of 70 h. Additionally, release kinetics analysis showed that both in simulated gastrointestinal fluids and in phosphate buffer solution, AL is released from SLPs based on equal ratios of lipid excipients following zero-order kinetics, which characterizes prolonged-release drug systems.

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Section: Introductionmentioning

confidence: 99%

Alendronate-Loaded Modified Drug Delivery Lipid Particles Intended for Improved Oral and Topical Administration

Ochiuz

Grigoraş²,

Popa

et al. 2016

Molecules

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“…It has some GI adverse effects such as gastritis, gastric ulcer, and esophagitis. Asikoglo et al (67) developed in their study a rectal formulation of ALD as an alternative to oral route and investigate d t h e a b s o r p t i o n o f i t b y u s i n g g a m m a scintigraphy. For this reason, ALD was labelled with Technetium-99m ( 99m Tc) by direct method.…”

Section: Suppository Formulationsmentioning

confidence: 99%

Conventional and Novel Pharmaceutical Dosage Forms on Prevention of Gastric Ulcers

Özgüney¹

2011

Peptic Ulcer Disease

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“…The physicochemical diffusion study was carried out to compare the permeability of ALD from different suppository bases (14). For this purpose, 0.5 g agar was dissolved in 24 mL water at 100ºC water bath.…”

Section: Physicochemical Diffusion Test Of Suppositoriesmentioning

confidence: 99%

“…ALD was directly labeled by 99m Tc with small modification on previously described (14). ALD (5 mg) was dissolved in saline (0.5 mL).…”

Section: Radiolabeling Studiesmentioning

confidence: 99%

Comparative bone uptake study of alendronate sodium from vaginal suppositories prepared with polyethylene glycol and massa estarinum bases

Özdemir¹,

Köseoğlu²,

Aşıkoğlu³

2013

mpj

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The unique properties like rich blood supply and the large surface area makes vagina an important area for systemic drug delivery (15). The advan-ABSTRACT: The aim of this study was to compare the bone uptake of alendronate sodium (ALD) from vaginal suppositories prepared with massa estarinum AB (ME) and polyethylene glycol 1500 (PEG) bases. For this purpose, ALD was radiolabeled with 99m Tecnetium Pertechnetate ( 99m Tc) by direct method. Radiochemical purity and stability of 99m Tc-ALD was performed with chromatographic studies. 99m Tc-ALD containing suppositories were prepared with ME and PEG bases. Physical properties of suppositories were evaluated. The physicochemical diffusion study was carried out to compare the release of ALD from different suppository bases. The bone uptake of 99m Tc-ALD was observed by gamma scintigraphy studies. 99m Tc-ALD containing suppositories were administrated to rabbits via vaginal route. The scintigraphic images were obtained with a gamma camera at different time intervals up to 240 minutes. According to our studies, radiochemical purity of 99m Tc-ALD was observed more than 95% up to 6 hours. At 240 minutes of physicochemical diffusion studies, released ALD has 0.620 ± 0.091 mm and 10.465 ± 0.651 mm diameter zone from ME and PEG base suppositories respectively. According to the gamma scintigraphy studies, although no bone uptake observed after ME suppositories application, rabbit's bones were clearly visible after PEG suppositories applied. The results of physicochemical diffusion and gamma scintigraphy studies were found compatible in each other.

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The Absorption of^99mTc-alendronate Given by Rectal Route in Rabbits

Cited by 12 publications

References 24 publications

Alendronate-Loaded Modified Drug Delivery Lipid Particles Intended for Improved Oral and Topical Administration

Alendronate-Loaded Modified Drug Delivery Lipid Particles Intended for Improved Oral and Topical Administration

Conventional and Novel Pharmaceutical Dosage Forms on Prevention of Gastric Ulcers

Comparative bone uptake study of alendronate sodium from vaginal suppositories prepared with polyethylene glycol and massa estarinum bases

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The Absorption of99mTc-alendronate Given by Rectal Route in Rabbits

Cited by 12 publications

References 24 publications

Alendronate-Loaded Modified Drug Delivery Lipid Particles Intended for Improved Oral and Topical Administration

Alendronate-Loaded Modified Drug Delivery Lipid Particles Intended for Improved Oral and Topical Administration

Conventional and Novel Pharmaceutical Dosage Forms on Prevention of Gastric Ulcers

Comparative bone uptake study of alendronate sodium from vaginal suppositories prepared with polyethylene glycol and massa estarinum bases

Contact Info

Product

Resources

About

The Absorption of^99mTc-alendronate Given by Rectal Route in Rabbits