IVIVC for Fenofibrate Immediate Release Tablets Using Solubility and Permeability as In Vitro Predictors for Pharmacokinetics

Buch, Philipp; Holm, Per; Thomassen, Jesper Qvist; Scherer, Dieter; Branscheid, Robert; Kolb, Ute; Langguth, Peter

doi:10.1002/jps.22148

Cited by 31 publications

(23 citation statements)

References 14 publications

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“…The technology advantages were clearly shown in Phase I and Phase II trials, which confirmed that LCP-Tacro enables broader absorption in the GI tract and sustains consistent tacrolimus concentrations [34], even in patients that may be poor absorbers or rapid metabolizers [ via a tablet matrix that helps establish a 'flatter' PK profile as compared to Prograf [35]. Currently, there is another product on the market utilizing MeltDose technology -the first MeltDosebased product, Fenofibrate Immediate Release Tablets (Fenoglide TM ), is approved by the FDA and marketed in the USA [36,37].…”

Section: Overview Of the Marketmentioning

confidence: 99%

Once-daily LCP-Tacro MeltDose tacrolimus for the prophylaxis of organ rejection in kidney and liver transplantations

Grinyó

Petruzzelli

2014

Expert Review of Clinical Immunology

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Tacrolimus is a cornerstone of the immunosuppression regimen for prevention of allograft rejection in kidney and liver transplantations, with efficacy proven in many clinical trials. The currently available and extensively used tacrolimus formulations are flawed by large inter-and intra-individual variability, low bioavailability, wide peak-to-trough fluctuations and a narrow therapeutic index. Drug delivery technology can significantly impact the pharmacologic action of a drug, influencing its pharmacokinetic and subsequent therapeutic profile. LCP-Tacro is a novel, prolonged-release, MeltDose Ò formulation of tacrolimus designed for once-daily administration. A hallmark differentiation between this formulation and other once-and twice-daily tacrolimus products is the proprietary MeltDose drug delivery technology which is designed to improve the bioavailability of drugs with low water solubility. Considering the studies conducted to date, once-daily LCP-Tacro has shown improved pharmacokinetic properties, rapid achievement of therapeutic trough levels, consistent exposure, non-inferior efficacy and similar safety, with lower tacrolimus dose than other tacrolimus formulations. World-wide there were an estimated 77,800 kidney transplants performed in 2012 (69% of all transplants) and 23,986 liver transplants (21% of all transplants) [1]. Data from the US show that, in 2013 more than half of the 28,953 transplants performed were kidney transplants (58.3%, n = 16,894) [2]; liver transplants were the next most frequent, comprising 22.2% (n = 6455) of all US transplants [2]. The number of individuals in need of organ transplantation outweighs the availability of organs -as of June 2014; data from the Organ Procurement and Transplantation Network showed that 100,967 individuals were on the waitlist for a kidney transplant and 15,758 individuals were on the waitlist for a liver transplant [3]. For individuals who receive a transplant, lifelong administration of immunosuppressive medications are required to prevent organ rejection. The arsenal of immunosuppressive drugs has evolved greatly since the beginnings of successful organ transplantation. A combination of azathioprine and corticosteroids was the original mainstay regimen in the early period of organ transplantation. A major advance in immunosuppression for prevention of allograft rejection came in the late 1970's with the advent of the calcineurin inhibitor (CNI) cyclosporine A [4][5][6]. The 'cyclosporine era' of the 1980's saw greatly improved short-and mid-term graft survival following transplantation. Immunosuppressive drugs have continued to evolve and the availability of improved drugs and regimens has contributed largely to the current high short-and long-term survival rates (survival following living donor transplant, 1-year kidney: 98%; 5-year kidney: 90%; 1-year liver: 90%; 5-year liver: 77%) [2]. In 1994, the EMA approved another CNI, tacrolimus, , Astellas Pharma US, Inc.), for the prophylaxis of organ rejection in kidney, liver and heart transplant ...

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Section: Overview Of the Marketmentioning

confidence: 99%

Once-daily LCP-Tacro MeltDose tacrolimus for the prophylaxis of organ rejection in kidney and liver transplantations

Grinyó

Petruzzelli

2014

Expert Review of Clinical Immunology

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“…(Ingels et al, 2004;Ingels et al, 2002) demonstrated that FaSSIF could be used in Caco-2 cell studies, whereas FeSSIF could not. Studies investigating the possibility of combining both dissolution and permeability using BMM have also been published, describing excellent in vitro in vivo correlations (IVIVC) (Buch et al, 2010), however, generally it is difficult to get these models to function as the cell layer is very sensitive to the BMM. Therefore, there clearly is a need for a different cell system or another artificial barrier capable of withstanding the harsh BMMs.…”

Section: And the Phospholipid Vesicle Basedmentioning

confidence: 99%

Permeapad™ for investigation of passive drug permeability: The effect of surfactants, co-solvents and simulated intestinal fluids (FaSSIF and FeSSIF)

Bibi

Cagno

Holm

et al. 2015

International Journal of Pharmaceutics

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“…Due to the expense, time, labor, and need for human subjects/animals when performing in vitro measurements of drug release kinetics, in vitro release is gaining greater attention as a surrogate test for product performance. Indeed, in vitro release testing is commonly used as a predictor of in vivo behavior, historically with traditional dosage forms like capsules and tablets (i.e., dissolution), and more recently with novel dosage forms like injectable biodegradable microspheres and implants [15][16][17]. Generally, in vitro release studies are performed at 37 ∘ C (physiological temperature), though in some instances testing at elevated temperatures has been explored to characterize drug release from a variety of dosage forms [18,19].…”

Section: Introductionmentioning

confidence: 99%

A Review of In Vitro Drug Release Test Methods for Nano-Sized Dosage Forms

D’Souza

2014

Advances in Pharmaceutics

218

169

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This review summarizes the methods used to study real-time (37 ∘ C) drug release from nanoparticulate drug delivery systems and establish an IVIVC. Since no compendial standards exist, drug release is currently assessed using a variety of methods including sample and separate (SS), continuous flow (CF), dialysis membrane (DM) methods, and a combination thereof, as well as novel techniques like voltametry and turbidimetry. This review describes the principle of each method along with their advantages and disadvantages, including challenges with set-up and sampling. The SS method allows direct measurement of drug release with simple set-up requirements, but sampling is cumbersome. With the CF method, sampling is straightforward but the set-up is time consuming. Set-up as well as sampling is easier with the DM, but it may not be suitable for drugs that bind to the membrane. Novel methods offer the possibility of real-time drug release measurement but may be restricted to certain types of drugs. Of these methods, Level A IVIVCs have been obtained with dialysis, alone or in combination with the sample and separate technique. Future efforts should focus on developing mathematical models that describe drug release mechanisms as well as facilitate formulation development of nano-sized dosage forms.

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IVIVC for Fenofibrate Immediate Release Tablets Using Solubility and Permeability as In Vitro Predictors for Pharmacokinetics

Cited by 31 publications

References 14 publications

Once-daily LCP-Tacro MeltDose tacrolimus for the prophylaxis of organ rejection in kidney and liver transplantations

Once-daily LCP-Tacro MeltDose tacrolimus for the prophylaxis of organ rejection in kidney and liver transplantations

Permeapad™ for investigation of passive drug permeability: The effect of surfactants, co-solvents and simulated intestinal fluids (FaSSIF and FeSSIF)

A Review of In Vitro Drug Release Test Methods for Nano-Sized Dosage Forms

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