Impact of physical properties of formulations on bioavailability of active substance: current and novel drugs with cyclosporine

Andrýsek, Tomáš

doi:10.1016/s0161-5890(03)00077-4

Cited by 37 publications

(18 citation statements)

References 8 publications

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“…It has been recognized that SNEDDS enhanced the bioavailability of several preparations in humans and animals with an increase in its in vitro drug release characteristics [15,16] . However, in some reports, the bioavailability has not increased even though the in vitro dissolution rate or emulsification rate has increased [17,18] .…”

Section: Discussionmentioning

confidence: 99%

Bioavailability Assessment of Vitamin A Self-Nanoemulsified Drug Delivery Systems in Rats: A Comparative Study

Taha

Ghorab²,

Zaghloul³

2007

Med Princ Pract

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Objectives: To assess and compare the bioavailability of three different oral dosage forms of vitamin A in rats. The formulations included vitamin A self-nanoemulsified drug delivery (SNEDD) optimized formulation-filled capsule (F1), vitamin A SNEDD optimized formulation compressed tablet (F2) and vitamin A oily solution-filled capsules without any additives (control, F3). Materials and Methods: Bioavailability was assessed after a single oral dose of the three formulations using three groups of rats, each group comprising 6 rats. Blood samples were collected at baseline and over the next 8 h. Plasma was separated and extracted to obtain the drug, which was measured by HPLC. Statistical data analysis was performed using the Student t test and ANOVA with p < 0.05 as the minimal level of significance. Results: From the pharmacokinetic parameters, both F1 and F2 showed improved bioavailability compared to F3. The values of AUC ± SD were 3,080.7 ± 190.2, 2,137.1 ± 130.5 and 1,485.2 ± 80.1 ng·h/ml for F1, F2 and F3, respectively. The T_max was 1 h in case of F1 and F2 as compared to 1.5 h for F3. The C_max ± SD was 799.5 ± 48.5, 656.2 ± 64.4 and 425.8 ± 33.1 for F1, F2 and F3, respectively. The increase in AUC, C_max and T_max was significant (p < 0.05). The bioavailability calculated from the AUC for F1 and F2 relative to F3 was 207.4 and 143.8%, respectively. The bioavailability increased almost twofold and 1.4 times for F1 and F2, respectively. Conclusions: The study showed that the newly developed vitamin A SNEDD formulations increased the rate and extent of drug absorption compared to the oily drug solution. The present investigation demonstrated that vitamin A SNEDD optimized formulations, either as filled capsules or as compressed tablets, were superior to its oily solution with regard to their biopharmaceutical characteristics.

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Section: Discussionmentioning

confidence: 99%

Bioavailability Assessment of Vitamin A Self-Nanoemulsified Drug Delivery Systems in Rats: A Comparative Study

Taha

Ghorab²,

Zaghloul³

2007

Med Princ Pract

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“…24) In this previous report, the AUC increased as the particle size decreased, and only the formulation whose particle size was under 100 nm exhibited a desirable bioavailability. However, the type of surfactant used for the formulation with large particles (>150 nm) was different from the formulation with small particles (<60 nm); thus, as reported in another study, 25) bioavailability can be affected not only by particle size but also by the characteristics of surfactants on the particle surface. The improved bioavailability provided by self-emulsifying formulations is believed to be due to a larger particle surface area, improved aqueous solubility of drugs, and the enhancement of intestinal membrane permeability produced by local disturbance of the cell membrane.…”

Section: Discussionmentioning

confidence: 83%

Comparison of Particle Size and Dispersion State among Commercial Cyclosporine Formulations and Their Effects on Pharmacokinetics in Rats

Shibata¹,

Saito²,

Kawanishi³

et al. 2012

CHEMICAL & PHARMACEUTICAL BULLETIN

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Generic versions of Neoral, a microemulsion capsule formulation of cyclosporine, have been approved worldwide. However, there are concerns about the quality and efficacy of the generics due to the formulation specificity and differences in inactive ingredients among products. In this study, we measured the physicochemical properties of both the innovator and the generic formulations, and compared their bioavailability in rats. When the capsule contents were dispersed in water, the absorbance (600 nm wavelength) of generic products was higher than that of the innovator. Whereas the dispersion solution of the innovator in Fed State Simulated Intestinal Fluid was nearly clear, that of all the generics became white and turbid. The mean diameter of the microemulsion (or emulsion) formed in water by the generics was 39.7, 57.7, 64.5, and 74.8 nm, all of which were larger than that of the innovator (26.4 nm). Although the T max of the generics tended to be long relative to that of the innovator, there were no significant differences between the innovator and generics with regard to maximum blood concentration (C max ) or area under the curve (AUC). These results suggest that the physicochemical differences between the innovator and the generics will not have a significant effect on C max or AUC, which is necessary to ensure bioequivalence.

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“…It is a potent immunosuppressive agent that has been approved for over 30 years by the US FDA for prophylaxis of organ rejection in kidney, liver, and heart transplants (1, 2). Initially oral Sandimmune ® was introduced into European market in 1981 as a self-emulsifying drug delivery system (SEDDS) formulation containing Labrafil ® M1944CS, olive oil and ethanol (3)(4)(5). When dispersed in water, this formulation forms an oil-inwater coarse macroemulsion with high polydispersity values (3).…”

Section: Introductionmentioning

confidence: 99%

“…Initially oral Sandimmune ® was introduced into European market in 1981 as a self-emulsifying drug delivery system (SEDDS) formulation containing Labrafil ® M1944CS, olive oil and ethanol (3)(4)(5). When dispersed in water, this formulation forms an oil-inwater coarse macroemulsion with high polydispersity values (3). In 1994 again CyA was introduced as a self-microemulsifying drug delivery system (SMEDDS) formulation containing Cremophor RH40, corn oil glycerides, propylene glycol and ethanol under the brand name of Sandimmune Neoral ® (Currently known as Neoral ® ) (2,5).…”

Section: Introductionmentioning

confidence: 99%

Pharmacokinetics of Orally Administered Poly(Ethylene Oxide)-block-Poly(ε-Caprolactone) Micelles of Cyclosporine A in Rats: Comparison with Neoral®

et al. 2018

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Impact of physical properties of formulations on bioavailability of active substance: current and novel drugs with cyclosporine

Cited by 37 publications

References 8 publications

Bioavailability Assessment of Vitamin A Self-Nanoemulsified Drug Delivery Systems in Rats: A Comparative Study

Bioavailability Assessment of Vitamin A Self-Nanoemulsified Drug Delivery Systems in Rats: A Comparative Study

Comparison of Particle Size and Dispersion State among Commercial Cyclosporine Formulations and Their Effects on Pharmacokinetics in Rats

Pharmacokinetics of Orally Administered Poly(Ethylene Oxide)-block-Poly(ε-Caprolactone) Micelles of Cyclosporine A in Rats: Comparison with Neoral®

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