Bioavailability and in Vivo Release Behavior of Controlled-Release Multiple-Unit Theophylline Dosage Forms in Beagle Dogs, Cynomolgus Monkeys, and Göttingen Minipigs

Ikegami, Kengo; Tagawa, Kozo; Ôsawa, Takashi

doi:10.1002/jps.20537

Cited by 22 publications

(11 citation statements)

References 16 publications

Supporting

Mentioning

Contrasting

Unclassified

Order By: Relevance

“…Either species appeared to be an adequate model for the evaluation of the modified-release form. Ikegami et al (2006) studied controlled-release theophylline absorption in dogs, monkeys, and pigs (Göttingen; 10-12 kg). Even after 20 hours of fasting, delay in absorption in pigs was seen.…”

Section: Evaluation Of Formulationsmentioning

confidence: 99%

Porcine Prediction of Pharmacokinetic Parameters in People: A Pig in a Poke?

Tang

Mayersohn

2018

Drug Metab Dispos

View full text Add to dashboard Cite

The minipig has become an animal of considerable interest in preclinical drug development. It has been used in toxicology research and in examining/establishing regulatory guidelines as a nonrodent animal model. We have reviewed some basic issues that one would want to consider in the development and testing of any animal model for humans. The pig is a reasonable alternative to the dog, but there are some clear limitations and unexplained disparities in the literature, which require further study; primary among these is the need for standardization in choice of breed and sex and routine protocols. The minipig offers numerous advantages over other established animal models, and it has similarities to the human with regard to anatomy, physiology, and biochemistry. The gastrointestinal tract is structurally and functionally similar to humans. This appears to be true for enzymes and transporters in the gut as well, but more study is needed. One major concern is assessment of oral drug absorption, especially with regard to potential food effects due to gastric emptying differences, yet this does not appear to be a consistent observation. Hepatic metabolism seems to reflect enzymatic patterns in humans, with some differences. Kidney function seems similar to humans but requires further study. We have analyzed literature data that suggest the pig would offer a reasonable model for human oral bioavailability and for allometric predictions of clearance. The minipig appears to be the model for dermal absorption in humans, and we discuss this in terms of literature data and our own in-house experience.

show abstract

Section: Evaluation Of Formulationsmentioning

confidence: 99%

Porcine Prediction of Pharmacokinetic Parameters in People: A Pig in a Poke?

Tang

Mayersohn

2018

Drug Metab Dispos

View full text Add to dashboard Cite

show abstract

“…As a result, the drug was driven out through the orifice by the expanding bottom layer. A theory can be used to describe the drug releasing process [7][8][9]. Generally, the drug release rate (dm=dt) of a single drug core and the volume imbibition rate of water (dv=dt) of oral osmotic tablet can be described like this:…”

Section: Design and Theory Of Bilayer Drug Release Oral Osmotic Tabletmentioning

confidence: 99%

Bilayer tablets of Paliperidone for Extended release osmotic drug delivery

Chowdary

Napoleon

2017

IOP Conf. Ser.: Mater. Sci. Eng.

View full text Add to dashboard Cite

Abstract. The purpose of this study is to develop and optimize the formulation of paliperidone bilayer tablet core and coating which should meet in vitro performance of trilayered Innovator sample Invega. Optimization of core formulations prepared by different ratio of polyox grades and optimization of coating of (i) sub-coating build-up with hydroxy ethyl cellulose (HEC) and (ii).enteric coating build-up with cellulose acetate (CA). Some important influence factors such as different core tablet compositions and different coating solution ingredients involved in the formulation procedure were investigated. The optimization of formulation and process was conducted by comparing different in vitro release behaviours of Paliperidone. In vitro dissolution studies of Innovator sample (Invega) with formulations of different release rate which ever close release pattern during the whole 24 h test is finalized.

show abstract

“…The centrifugal granulator is proved to be a very successful and efficient piece of equipment due to its ease of handling, variable controlling parameters, and operational feasibility to obtain spherical multi-layered pellets with desired release characteristics. In previous studies, centrifugal granulators have been used in developing sustained release pellets and enteric coated pellets (Hu et al, 2006;Ikegami et al, 2006) with desired mechanical and dissolution properties.…”

Section: Introductionmentioning

confidence: 99%

In vitro and in vivo evaluations of ketoprofen extended release pellets prepared using powder layering technique in a rotary centrifugal granulator

et al. 2011

View full text Add to dashboard Cite

In the present study, an extended release pellet dosage form of ketoprofen was prepared using powder layering technique. A combination of ethyl cellulose (45 cps) and shellac polymers was used as a binder (12% w/w polymer) during drug layering and an extended release coating (1:3 ratio at 2%, 4% and 7% w/w polymer) within the same apparatus. The coated pellets were characterized for sphericity, Hardness-Friability Index, and drug content, and also underwent scanning electron microscopy. In vitro dissolution was performed in 900 mL of phosphate buffer (pH 6.8) using paddle apparatus at 100 rpm. Ethyl cellulose and shellac when used as binders during drug loading did not extend ketoprofen release beyond 3 h. However, coating of the drug loaded pellets using ethyl cellulose and shellac resulted in an extended release profile of about 10 h. Using Higuchi's model and the Korsmeyer equation, the drug release mechanism from the pellets was found to be an anomalous type involving diffusion and erosion. Scanning electron microscopy was used to visualize the pellet morphology and drug release mechanism during dissolution testing. In vivo evaluations of the extended release pellets in rats indicated a significant increase in the time to reach maximum concentration (t(max)) and extent of absorption (AUC(0-∞)) compared to the ketoprofen immediate release tablet blend dispersed and dosed. In conclusion, extended release pellets of ketoprofen could perform therapeutically better than conventional dosage forms, leading to improved efficacy for a prolonged period.

show abstract

Bioavailability and in Vivo Release Behavior of Controlled-Release Multiple-Unit Theophylline Dosage Forms in Beagle Dogs, Cynomolgus Monkeys, and Göttingen Minipigs

Cited by 22 publications

References 16 publications

Porcine Prediction of Pharmacokinetic Parameters in People: A Pig in a Poke?

Porcine Prediction of Pharmacokinetic Parameters in People: A Pig in a Poke?

Bilayer tablets of Paliperidone for Extended release osmotic drug delivery

In vitro and in vivo evaluations of ketoprofen extended release pellets prepared using powder layering technique in a rotary centrifugal granulator

Contact Info

Product

Resources

About