Neutron activation-based gamma scintigraphy in pharmacoscintigraphic evaluation of an Egalet® constant-release drug delivery system

Marvola, Janne; Kanerva, Hanna; Slot, Lillian; Lipponen, Maija; Kekki, Tommi; Hietanen, Heikki; Mykkänen, Sirpa; Ariniemi, Kari; Lindevall, Kai; Marvola, Martti

doi:10.1016/j.ijpharm.2004.05.022

Cited by 19 publications

(7 citation statements)

References 15 publications

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“…This nonlinear time scaling denotes that the processes explored in vivo and in vitro were not consistently similar, that is, the in vivo process was slower when time increased compared to in vitro. As described in (29), the presence of the formulation was monitored through the small intestine, ascendant and transverse colon, and descendent colon by scintigraphy. The rate of absorption was estimated to decrease gradually in each part of the intestine.…”

Section: Time Scaling and Lag Time Correctionmentioning

confidence: 99%

“…This modeling of absorption could directly be linked to the observed plasma curves and the GI transit. The nonlinear time scaling could also be explained by where the tablet was in the GI tract and the resulting absorption rates (see (18,29) for more explanation). In this latter case, the time scaling is linked with observed physiology and is thus validated by observation.…”

Section: Time Scaling and Lag Time Correctionmentioning

confidence: 99%

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In vitro–In Vivo Correlations: Tricks and Traps

Cardot

Davit

2012

AAPS J

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Abstract. In vitro-in vivo correlation (IVIVC) is a biopharmaceutical tool recommended to be used in development of formulation. When validated, it can speed up development of formulation, be used to fix dissolution limits and also as surrogate of in vivo study. However, as do all tools, it presents limitations and traps. The aim of the present paper is to investigate five common traps which could limit either the setting or use of IVIVC (1) using mean or individual values; (2) correction of absolute bioavailability; (3) correction of lag time and time scaling; (4) flip-flop model; and (5) predictability corrections.

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Section: Time Scaling and Lag Time Correctionmentioning

confidence: 99%

Section: Time Scaling and Lag Time Correctionmentioning

confidence: 99%

In vitro–In Vivo Correlations: Tricks and Traps

Cardot

Davit

2012

AAPS J

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“…The safety requirement was that any net g peak area not originating from 153 Sm should not exceed 0.3% of the 153 Sm main peak at 103 keV and that the total net peak areas not originating from 153 Sm should not exceed 1% of the 153 Sm main peak. The capsules were kept in a radioactive storage room until the study day to allow for decay of the unwanted short-lived activated by-products, primarily sodium-24 ( 24 Na) [15,16,19].…”

Section: Neutron Activationmentioning

confidence: 99%

“…Neutron-activated 153 Sm has successfully been used in various drug delivery and pharmacology studies [13][14][15][16]. We have extensive experience with the production and use of 153 Sm as a tracer for studying the transit and release of oral dose forms such as enteric-coated matrix tablets [17,18].…”

Section: Introductionmentioning

confidence: 99%

Neutron-activated 153Sm-ion-exchange resin as a tracer for gastrointestinal scintigraphy

Yeong

Abdullah

et al. 2011

Nuclear Medicine Communications

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Nuclear medicine techniques are well established for the investigation of gastrointestinal (GI) motility and transit. Ion-exchange resins radiolabelled with ⁹⁹mTc and ¹¹¹In are widely used as nonabsorbable radiopharmaceutical markers, with ¹¹¹In being preferred for whole-gut transit studies. This radionuclide, however, is not produced in many countries and may be expensive when obtained through international shipment. This study describes the use of neutron-activated ¹⁵³Sm-resin as an alternative tracer for use in GI scintigraphic investigation. A measure of 50 mg of stable samarium-152 chloride (¹⁵²SmCl₃) was incorporated into 100 mg of cation-exchange resin and irradiated in a neutron flux of 1 × 10¹³ cm⁻² s⁻¹ for 100 s to achieve an activity of 5 MBq after 66 h. Aliquots of ¹¹¹In-radiolabelled resin (5 MBq) were prepared for comparison of labelling and stability. Radiolabelling efficiencies were obtained by washing resin with distilled water, and the activity lost was measured. The radiolabelled resins were immersed in simulated gastric and intestinal fluid environments, and the retention of ¹⁵³Sm³⁺ and ¹¹¹In³⁺ was measured over a 24 h period. At 66 h after production, 91.15 ± 12.42% of ¹⁵³Sm was bound to the resin after washing in distilled water, whereas radiolabelling with ¹¹¹In achieved 99.96 ± 0.02% efficiency. Both radiolabelled resins demonstrated almost 100% stability in simulated intestinal fluid and >90% stability in artificial gastric juice over 24 h. The performance of neutron-activated ¹⁵³Sm-resin is similar to that of ¹¹¹In-resin and can be used as an alternative tracer for GI transit studies when In is not available.

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“…In this case, a radionuclide imaging technique was developed. Gammascintigraphy is one of the techniques widely used to study local and time-specific formulation, because it can trace the drug delivery process non-invasively in real time (Newman et al, 2003;Marvola et al, 2004Marvola et al, , 2008. In present studies, we combined the above two in-vivo research techniques to obtain more accurate data.…”

Section: Introductionmentioning

confidence: 99%

Effects of alga polysaccharide capsule shells on in-vivo bioavailability and disintegration

Guo

et al. 2012

Chin. J. Ocean. Limnol.

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Gelatin has been used in hard capsule shells for more than a century, and some shortcomings have appeared, such as high moisture content and risk of transmitting diseases of animal origin to people. Based on available studies regarding gelatin and vegetable shells, we developed a new type of algal polysaccharide capsule (APPC) shells. To test whether our products can replace commercial gelatin shells, we measured in-vivo plasma concentration of 12 selected volunteers with a model drug, ibuprofen, using high performance liquid chromatography (HPLC), by calculating the relative bioavailability of APPC and Qualicaps® referenced to gelatin capsules and assessing bioequivalence of the three types of shells, and calculated pharmacokinetic parameters with the software DAS 2.0 (China). The results show that APPC shells possess bioequivalence with Qualicaps® and gelatin shells. Moreover, the disintegration behavior of four types of shells (APPC, Vegcaps®, Qualicaps® and gelatin shells) with the content of lactose and radioactive element ( 99m Tc) was observed via gamma-scintigraphic images. The bioavailability and gamma-scintigraphic studies showed that APPC was not statistically different from other vegetable and gelatin capsule shells with respect to in-vivo behavior. Hence, it can be concluded that APPCs are exchangeable with other vegetable and gelatin shells.

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Neutron activation-based gamma scintigraphy in pharmacoscintigraphic evaluation of an Egalet® constant-release drug delivery system

Cited by 19 publications

References 15 publications

In vitro–In Vivo Correlations: Tricks and Traps

In vitro–In Vivo Correlations: Tricks and Traps

Neutron-activated 153Sm-ion-exchange resin as a tracer for gastrointestinal scintigraphy

Effects of alga polysaccharide capsule shells on in-vivo bioavailability and disintegration

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