Development of a self-emulsifying formulation that reduces the food effect for torcetrapib

Perlman, Michael E.; Murdande, Sharad B.; Gumkowski, Michael J.; Shah, T.S.; Rodricks, C.M.; Thornton‐Manning, Janice R.; Freel, D.; Erhart, L.C.

doi:10.1016/j.ijpharm.2007.09.015

Cited by 67 publications

(43 citation statements)

References 18 publications

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“…103,104 The solvent capacity of triglyceride vehicles for some compounds may be improved by blending them with other mixed glycerides, that is, diglycerides (DG) and monoglycerides (MG), and free fatty acids (FA). The simplest lipid formulation is one in which a compound is dissolved in a digestible oil, usually a long chain triglyceride (LCT, e.g., vegetable oil) or a medium chain triglyceride (MCT, e.g., fractionated coconut oil).…”

Section: Classification Of Lipid Based Fill Formulationsmentioning

confidence: 99%

“…104,117,130 The method is modified when developing a solution fill formulation for softgel encapsulation to take the water migration processes occur in a softgel into account. 104,117,130 The method is modified when developing a solution fill formulation for softgel encapsulation to take the water migration processes occur in a softgel into account.…”

Section: Fill Formulation Developmentmentioning

confidence: 99%

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Soft Gelatin Capsules (Softgels)

Gullapalli

2010

Journal of Pharmaceutical Sciences

107

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Section: Classification Of Lipid Based Fill Formulationsmentioning

confidence: 99%

Section: Fill Formulation Developmentmentioning

confidence: 99%

Soft Gelatin Capsules (Softgels)

Gullapalli

2010

Journal of Pharmaceutical Sciences

107

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“…C max of F2 was highest among all the three formulations evaluated. The role of particle size in the performance of the formulation in vivo is generally less important than formulators have assumed (Perlman et al, 2008). The main reason for this is that as soon as the dispersed formulation leaves the stomach it encounters the formidable digestive power of the small intestine .…”

Section: Bioavailability Studymentioning

confidence: 99%

Role of lipid-based excipients and their composition on the bioavailability of antiretroviral self-emulsifying formulations

Chudasama

Patel

Nivsarkar³

et al. 2014

Drug Delivery

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The objective of this study was to develop self-emulsifying drug delivery system (SEDDS) to improve solubility and enhance the oral absorption of the poorly water-soluble drug, nevirapine. This lipid-based formulation may help to target the drug to lymphoid organs where HIV-1 virus resides mainly. The influence of the oil, surfactant and co-surfactant types on the drug solubility and their ratios on forming efficient and stable SEDDS were investigated in detail. Two SEDDS (F1 and F2) were prepared and characterized by morphological observation, droplet size and zeta potential determination, cloud point measurement and in vitro diffusion study. The influence of droplet size on the absorption from formulations with varying concentration of oil and surfactant was also evaluated from two self-emulsifying formulations. Oral bioavailability of nevirapine SEDDS was checked by using rat model. Results of diffusion rate and oral bioavailability of nevirapine SEDDS were compared with marketed suspension. The absorption of nevirapine from F1 and F2 showed 1.92 and 1.98-fold increase (p50.05) in relative bioavailability, respectively, compared with that of the suspension. There was no statistical significant difference (p50.05) between F1 and F2 in their AUC and C max . This indicated that there was apparent poor correlation between the droplet size and in vivo absorption. However, nevirapine in SEDDS showed higher ex vivo stomach and intestinal permeability and in vivo absorption than the marketed suspension, suggesting that the SEDDS may be a useful delivery system for targeting nevirapine to lymphoid organs.

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“…The latter concentrate of an evolving microemulsion, in particular, has been subject to intensive research. Some recent applications showed increased oral bioavailability of oridonin 7 , vinpocetine 8 , and fenofibrate 9 , whereas other authors observed the reduction of a food effect 10,11 .…”

Section: Introductionmentioning

confidence: 99%