Ganciclovir absolute bioavailability and steady-state pharmacokinetics after oral administration of two 3000-mg/d dosing regimens in human immunodeficiency virus— and cytomegalovirus-seropositive patients

Anderson, Roger; Griffy, Kay; Jung, Donald; Door, Albert; Hulse, James D.; Smith, Randall B.

doi:10.1016/0149-2918(95)80107-3

Cited by 80 publications

(44 citation statements)

References 6 publications

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“…6c (29,45-47). The bioavailability of GCV after oral administration was studied by Anderson and coworkers (48). Their results confirmed that the degradation of GCV occurred under gastric pH conditions.…”

Section: Analysis Of the Physicomechanical Behavior Of The Lyomatrixsupporting

confidence: 53%

Intestinal Targeting of Ganciclovir Release Employing a Novel HEC-PAA Blended Lyomatrix

et al. 2015

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Abstract. A hydroxyethylcellulose-poly(acrylic acid) (HEC-PAA) lyomatrix was developed for ganciclovir (GCV) intestine targeting to overcome its undesirable degradation in the stomach. GCV was encapsulated within the HEC-PAA lyomatrix prepared by lyophilization. Conventional tablets were also prepared with identical GCV concentrations in order to compare the GCV release behavior from the lyomatrix and tablets. GCV incorporation (75.12%) was confirmed using FTIR, DSC, and TGA. The effect of GCV loading on the microstructure properties of the lyomatrix was evaluated by SEM, AFM, and BET surface area measurements. The in vitro drug release study showed steady and rapid release profiles from the GCV-loaded lyomatrix compared with the tablet formulation at identical pH values. Minimum GCV release was observed at acidic pH (≤40%) and maximum release occurred at intestinal pH values (≥90%) proving the intestinal targeting ability of the lyomatrix. Kinetic modeling revealed that the GCV-loaded lyomatrix exhibited zero-order release kinetics (n=1), while the tablets were best described via the Peppas model. Textural analysis highlighted enhanced matrix resilience and rigidity gradient (12.5%, 20 Pa) for the GCV-loaded lyomatrix compared to the pure (7%, 9.5 Pa) HEC-PAA lyomatrix. Bench-top MRI imaging was used to confirm the mechanism of GCV release behavior by monitoring the swelling and erosion rates. The swelling and erosion rate of the tablets was not sufficient to achieve rapid zero-order GCV release as with the lyomatrix. These combined results suggest that the HEC-PAA lyomatrix may be suitable for GCV intestinal targeting after oral administration.

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Section: Analysis Of the Physicomechanical Behavior Of The Lyomatrixsupporting

confidence: 53%

Intestinal Targeting of Ganciclovir Release Employing a Novel HEC-PAA Blended Lyomatrix

et al. 2015

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“…GCV is a synthetic purine nucleoside analogue of guanine and is effective for treatment and chronic suppression of cytomegalovirus (CMV) retinitis in immune compromised patients and for prevention of CMV disease in transplant patients [18] . GCV is a weak base having poor oral bioavailability (6-7%) due to its highly polar nature [19] . Due to poor oral bioavailability, currently GCV is given orally at dose of 1000 mg thrice a day.…”

mentioning

confidence: 99%

Preparation and Characterization of Ganciclovir Loaded Glutathione Modified Gold Nanoparticles

Kiroula¹,

Negi²

2016

pharmaceutical-sciences

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Kiroula, et al.: Glutathione-modified Gold Nanoparticles of GanciclovirThis article reports that ganciclovir-loaded gold nanoparticles were developed via glutathione surface modification. Citrate-reduced gold nanoparticles were prepared first from chloroauric acid. Further the surface of gold nanoparticles was modified with glutathione. Then ganciclovir was loaded onto the glutathione-modified gold nanoparticles through the reaction between carboxyl group of glutathione and amino group of ganciclovir. Gold nanoparticles were characterized by photon correlation spectroscopy, transmission electron microscopy and infrared spectroscopy. Drug loading of 87.27±2.52% was observed for ganciclovir-loaded gold nanoparticles. The particle size distribution of gold nanoparticles ranged from 26.3 to 31 nm. Thus ganciclovir-loaded gold nanoparticles were successfully prepared, which might further improve the oral bioavailability of ganciclovir.

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“…Oral absorption of ganciclovir is delayed, with a time to peak concentration T max ranging between 2 and 14 h, depending on the type of transplanted organ and the conditions under which the medication is administered [13][14][15][16] . Absorption of ganciclovir is also erratic and incomplete, with a mean bioavailability of 4.5 % ( ± 1 %) under fasting conditions [17] .…”

Section: Absorption and Distributionmentioning

confidence: 99%

The Role of Ganciclovir in Transplantation

Bowman

Brennan

2010

Immunotherapy in Transplantation

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Ganciclovir absolute bioavailability and steady-state pharmacokinetics after oral administration of two 3000-mg/d dosing regimens in human immunodeficiency virus— and cytomegalovirus-seropositive patients

Cited by 80 publications

References 6 publications

Intestinal Targeting of Ganciclovir Release Employing a Novel HEC-PAA Blended Lyomatrix

Intestinal Targeting of Ganciclovir Release Employing a Novel HEC-PAA Blended Lyomatrix

Preparation and Characterization of Ganciclovir Loaded Glutathione Modified Gold Nanoparticles

The Role of Ganciclovir in Transplantation

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