Absorption and tissue tolerance of ricobendazole in the presence of hydroxypropyl-β-cyclodextrin following subcutaneous injection in sheep

Wu, Zimei; Tucker, Ian G.; Razzak, Majid; Yang, Lin; McSporran, Keith; Medlicott, Natalie J.

doi:10.1016/j.ijpharm.2010.07.002

Cited by 16 publications

(16 citation statements)

References 42 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Complexation with cyclodextrins has been intensively investigated as a solubilization approach for parenteral formulations. In agreement with our recent results, cyclodextrin formulations of poorly water-soluble drugs have shown little or no tendency for drug precipitation after intramuscular injection [25]. It is worth noting that most of the progress achieved to improve bioavailability of BZDs has been in formulation design [18], [28]–[29].…”

Section: Discussionsupporting

confidence: 90%

“…Irritation and post-injection precipitation are concerns in parenteral drug delivery for poorly water-soluble drugs [25]. The greater water solubility of the main active albendazole metabolite, albendazole sulphoxide (also named ricobendazole), was the starting point in the development of an injectable formulation for use in cattle currently available in some Latin American countries [26].…”

Section: Discussionmentioning

confidence: 99%

“…1–2), which produces irritation at the site of sc administration. Recently, a CD-based formulation of ricobendazole for parenteral use has demonstrated adequate tissue tolerability and bioavailability [25], but is not available in the veterinary market. Complexation with cyclodextrins has been intensively investigated as a solubilization approach for parenteral formulations.…”

Section: Discussionmentioning

confidence: 99%

See 2 more Smart Citations

Exploring the Potential of Flubendazole in Filariasis Control: Evaluation of the Systemic Exposure for Different Pharmaceutical Preparations

et al. 2014

View full text Add to dashboard Cite

The goal of elimination of the human filariases would benefit greatly from the use of a macrofilaricidal agent. In vivo trials in humans and many experimental animal models suggest that flubendazole (FLBZ) is a highly efficacious macrofilaricide. However, since serious injection site reactions were reported in humans after parenteral FLBZ administration, the search for alternative pharmaceutical strategies to improve the systemic availability of FLBZ and its metabolites has acquired urgency in both human and veterinary medicine. The goal of the current work was to compare the systemic exposure of FLBZ formulated as either an aqueous hydroxypropyl-β-cyclodextrin (CD) or aqueous carboxymethyl cellulose (CMC) suspension or a Tween 80-based formulation (TWEEN) in rats and jirds (Meriones unguiculatus). Healthy animals of both species were allocated into four experimental groups of 44 animals each: FLBZ-CDoral and FLBZ-CDsc, treated with the FLBZ-CD formulation by the oral or subcutaneous routes, respectively; FLBZ-TWEENsc, dosed subcutaneously with the FLBZ-TWEEN formulation; and FLBZ-CMCoral, treated orally with the FLBZ suspension. The FLBZ dose was 5 mg/kg. FLBZ and its hydrolyzed (H-FLBZ) and reduced (R-FLBZ) metabolites were recovered in plasma samples collected from rats and jirds treated with the different FLBZ formulations. In both species, FLBZ parent drug was the main analyte recovered in the bloodstream. In rats, FLBZ systemic exposure (AUC0-LOQ) was significantly (P<0.05) higher after the FLBZ-CD treatments, both oral (4.8±0.9 µg.h/mL) and subcutaneous (7.3±0.6 µg.h/mL), compared to that observed after oral administration of FLBZ-CMC suspension (0.93±0.2 µg.h/mL). The same differences were observed in jirds. In both species, parenteral administration of FLBZ-TWEEN did not improve the systemic availability of FLBZ compared to FLBZ-CDoral treatment. In conclusion, formulation approaches that enhance the availability of flubendazole in the rat and jird may have therapeutic implications for a drug with poor or erratic bioavailability.

show abstract

Section: Discussionsupporting

confidence: 90%

Section: Discussionmentioning

confidence: 99%

Section: Discussionmentioning

confidence: 99%

See 1 more Smart Citation

Exploring the Potential of Flubendazole in Filariasis Control: Evaluation of the Systemic Exposure for Different Pharmaceutical Preparations

et al. 2014

View full text Add to dashboard Cite

show abstract

“…Similarly, the longer mean residence time observed for the reference formulation (p < 0.05) is likely to be the result of slow re-dissolution of precipitated PCZ (Wu et al, 2010). Similarly, the longer mean residence time observed for the reference formulation (p < 0.05) is likely to be the result of slow re-dissolution of precipitated PCZ (Wu et al, 2010).…”

Section: Pharmacokineticsmentioning

confidence: 93%

In vitro and in vivo evaluation of a posaconazole‐sulfobutyl ether‐β‐cyclodextrin inclusion complex

Wang

Jiang

Cai

et al. 2018

Biomedical Chromatography

View full text Add to dashboard Cite

Posaconazole (PCZ) is a triazole antifungal agent with an extended spectrum of antifungal activity. It is approved for the prophylaxis of invasive fungal infections in patients with neutropenia or in hematopoietic stem cell transplant recipients undergoing high-dose immunosuppressive therapy for graft-vs-host disease, and for the treatment of fungal infections. However, its pharmacological effects are severely limited owing to its poor solubility and low bioavailability. In order to solve these problems, a sulfobutyl ether-β-cyclodextrin compound was used to prepare an intramuscular injection to improve the bioavailability of posaconazole. The extracorporeal dissolution rate of posaconazole was markedly improved by this inclusion complex with >90% being released within 5 min, and the in vivo pharmacokinetics were studied using a HPLC/MS/MS method for quantifying posaconazole and the posaconazole-sulfobutyl ether-β-cyclodextrin inclusion complex in rat blood. Posaconazole and an internal standard, itraconazole, were extracted by protein precipitation using acetonitrile. The concentration range of posaconazole was 0.05-4.0 μg/mL with good linearity (r = 0.9980), the peak concentrations of pure posaconazole and the inclusion complex were 0.565 ± 0.102 μg/mL and 1.12 ± 0.091 μg/mL, the values for AUC were 12.2 ± 2.5 and 19.9 ± 2.5 μg h/mL, and the values for AUC were 16.4 ± 3.2 and 25.0 ± 3.5 μg h/mL, respectively. The main pharmacokinetics parameters showed significant differences (P < 0.01). Compared with pure posaconazole, the posaconazole-sulfobutyl ether-β-cyclodextrin inclusion complex markedly improved the bioavailability of posaconazole.

show abstract

“…However, one of the concerns associated with these solubilization approaches is that these formulations often lead to products that cause injection site reactions. Moreover, even if the drugs are soluble in the formulation, post‐injection drug precipitation (PDP) may occur to both intravenous and extravascular injections . The occurrence of PDP is a major concern due to the potential local injection site reactions, haemolysis and thrombophlebitis associated with intravenous formulations, and has been reported to be responsible for poor and erratic drug absorption and tissue damage following intramuscular/subcutaneous injections …”

Section: Introductionmentioning

confidence: 99%

In-vitro prediction of bioavailability following extravascular injection of poorly soluble drugs: an insight into clinical failure and the role of delivery systems

Hassan

Shaw

2013

Journal of Pharmacy and Pharmacology

Self Cite

View full text Add to dashboard Cite

show abstract

Absorption and tissue tolerance of ricobendazole in the presence of hydroxypropyl-β-cyclodextrin following subcutaneous injection in sheep

Cited by 16 publications

References 42 publications

Exploring the Potential of Flubendazole in Filariasis Control: Evaluation of the Systemic Exposure for Different Pharmaceutical Preparations

Exploring the Potential of Flubendazole in Filariasis Control: Evaluation of the Systemic Exposure for Different Pharmaceutical Preparations

In vitro and in vivo evaluation of a posaconazole‐sulfobutyl ether‐β‐cyclodextrin inclusion complex

In-vitro prediction of bioavailability following extravascular injection of poorly soluble drugs: an insight into clinical failure and the role of delivery systems

Contact Info

Product

Resources

About