Fed and fasted state gastro-intestinal in vitro lipolysis: In vitro in vivo relations of a conventional tablet, a SNEDDS and a solidified SNEDDS

Christophersen, Philip C.; Christiansen, M. Skytte; Holm, René; Kristensen, Jakob; Jacobsen, Jette Bredahl; Abrahamsson, Bertil; Müllertz, Anette

doi:10.1016/j.ejps.2013.09.007

Cited by 74 publications

(45 citation statements)

References 50 publications

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“…As shown in Figure 6, a milky emulsion is formed for MAS in the centrifuge tube while we could see clear desorption of oil from GFS and MSG. Similarly, various authors have reported poor drug and/or oil release from a carrier like MAS [30]. The obtained observations are comparable with Kang et al who reported slow and incomplete ibuprofen release from SMEDD formulation loaded with MAS [32].…”

Section: Oil Desorption Studysupporting

confidence: 94%

Comparative evaluation of porous silica based carriers for lipids and liquid drug formulations

Choudhari¹,

Reddy²,

Monsuur³

et al. 2014

Open Material Sciences

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Conversion of liquid and semisolid lipids into free flowing powders is an advantageous technique, as the carriers display high surface area, strong adsorption capacity, ease of processing, and ability to generate lipid loaded free flowing powders which can be converted to solid dosage forms like tablets and capsules. A combination of density, adsorption capacity and desorption is found to be of importance in the selection of the right adsorbent. Adsorbents like magnesium aluminium silicates (MAS), granulated fumed silica (GFS) and mesoporous silica gel (MSG) were characterized by flow property measurements, particle size, scanning electron microscopy (SEM) and pore structure by mercury (Hg) intrusion study. SEM results reveal adsorbent morphology, whereas an intrusion-extrusion study reveal pore size distributions. Tablets and capsules of oil loaded adsorbents were prepared by conventional methods. Oil loaded adsorbents were evaluated for the ability to convert oil into powder, easy of processing into tablets and capsules, and release of the loaded oil (Vitamin E) or active (Glyburide). All adsorbents possess good flow property while MSG has higher density than GFS and MAS. This helps to deliver maximum active per unit volume. A wider pore size distribution of MAS was observed in comparison to MSG and GFS. MAS exhibited poor oil release from powder and its formulations, whereas GFS demonstrated closely similar release to MSG. Maximum 70% oil loaded MSG can be delivered in tablet dosage form and MSG can deliver the highest amount in limited volume capsules due to its high density. Hence, lower density and poor oil release from MAS limit its applications in solid oral drug delivery, while both MSG and GFS proved to be suitable.

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Section: Oil Desorption Studysupporting

confidence: 94%

Comparative evaluation of porous silica based carriers for lipids and liquid drug formulations

Choudhari¹,

Reddy²,

Monsuur³

et al. 2014

Open Material Sciences

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“…pH 6.80). Some authors [7,39,49,[55][56][57][58] have partially resolved this, by performing back-titrations and defining a correction factor to determine the real extent of lipolysis. In the light of this, back-titration experiments were undertaken at pH 11.50, immediately after direct titrations had been performed.…”

Section: In Vitro Lipolysis Of Equimolar Amounts Of Different Triglycmentioning

confidence: 98%

Chain length affects pancreatic lipase activity and the extent and pH–time profile of triglyceride lipolysis

Benito-Gallo

Franceschetto

Wong

et al. 2015

European Journal of Pharmaceutics and Biopharmaceutics

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Triglycerides (TG) are one of the most common excipients used in oral lipid-based formulations. The chain length of the TG plays an important role in the oral bioavailability of the co-administered drug. Fatty acid (FA) chain-length specificity of porcine pancreatic lipase was studied by means of an in vitro lipolysis model under bio-relevant conditions at pH 6.80. In order to determine the total extent of lipolysis, back-titration experiments at pH 11.50 were performed. Results suggest that there is a specific chain length range (C2-C8) for which pancreatic lipase shows higher activity. This specificity could result from a combination of physicochemical properties of TGs, 2-monoglycerides (2-MGs) and FAs, namely the droplet size of the TGs, the solubility of 2-MGs within mixed micelles, and the relative stability of the FAs as leaving groups in the hydrolysis reaction. During experimentation, it was evident that an optimisation of lipolysis conditions was needed for tighter control over pH levels so as to better mimic in vivo conditions. 1M NaOH, 3.5 mL/min maximum dosing rate, and 3 μL/min minimum dosing rate were the optimised set of conditions that allowed better pH control, as well as the differentiation of the lipolysis of different lipid loads.

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“…Furthermore, it appears that in the case of the non-ionisable com-603 pound such as fenofibrate, the risk of reduced in vivo absorption due to digestion-induced drug precipitation is low [14,23,31]. 605 However, in the case of weak bases, in particular, there is potential 606 for formulation digestion by intestinal lipases to result in a loss of 607 solubilisation and cause precipitation [32,33]. These effects appear 608 to be drug and formulation specific and currently need to be 609 assessed on a case by case basis [34].…”

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confidence: 97%

“…Food effect 31 In vitro in vivo correlations (IVIVC) 32 Poorly water soluble drugs (PWSD) 33 3 4 a b s t r a c t 35 Novel formulations that overcome the solubility limitations of poorly water soluble drugs (PWSD) are 36 becoming ever more critical to a drug development process inundated with these compounds. There is 37 a clear need for developing bio-enabling formulation approaches to improve oral bioavailability for 38 PWSD, but also to establish a range of predictive in vitro and in silico biopharmaceutics based tools for 39 guiding formulation design and forecasting in vivo effects.…”

mentioning

confidence: 99%

Lipidic dispersion to reduce food dependent oral bioavailability of fenofibrate: In vitro, in vivo and in silico assessments

O’Shea

Faisal

Ruane‐O’Hora

et al. 2015

European Journal of Pharmaceutics and Biopharmaceutics

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Fed and fasted state gastro-intestinal in vitro lipolysis: In vitro in vivo relations of a conventional tablet, a SNEDDS and a solidified SNEDDS

Cited by 74 publications

References 50 publications

Comparative evaluation of porous silica based carriers for lipids and liquid drug formulations

Comparative evaluation of porous silica based carriers for lipids and liquid drug formulations

Chain length affects pancreatic lipase activity and the extent and pH–time profile of triglyceride lipolysis

Lipidic dispersion to reduce food dependent oral bioavailability of fenofibrate: In vitro, in vivo and in silico assessments

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