Absorption characteristics of sustained release theophylline capsules administered in applesauce

Green, Elaine R.; Green, Andrew W.; Lanc, Robert; Slaughter, Richard L.; Middleton, Elliott

doi:10.1016/s0022-3476(81)80862-1

Cited by 15 publications

(1 citation statement)

References 4 publications

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“…The relatively rapid absorption results in complete bioavailability. Green et al (1981) studied the absorption characteristics of'Slo-Phyllin Gyrocaps' 250mg when the capsule was swallowed whole with 240ml of water and also in a crossover design when taken with water but with the capsule contents emptied and mixed with two teaspoonfuls of apple sauce. An oral solution was used as reference and 12 nonsmoking adults aged 20 to 31 years participated in the study.…”

Section: 'Theograd' (Abbott Laboratories Uk)mentioning

confidence: 99%

Food Interactions with Sustained-Release Theophylline Preparations1

Jonkman

1989

Clinical Pharmacokinetics

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Currently, theophylline is being used predominantly as sustained-release capsules or tablets. In the mid-seventies the first preparations for use with a dosage interval of 12 hours (twice-daily preparations) were introduced. Since 1983, theophylline preparations that can be given with an interval of 24 hours (once-daily preparations) have become available. The release of theophylline from some of these products can be influenced (either increased or decreased) by concomitant intake of food. With some preparations the composition of the meal (especially the fat content) has an influence on the degree of effect. The consequence may be an effect on the rate of absorption or on the amount absorbed, or both simultaneously. This could result in an unexpected shift of the plasma theophylline concentration. Such a shift is therapeutically undesirable, because theophylline has a fairly narrow therapeutic range. A review is given of those food interactions with the sustained-release theophylline preparations, both twice-daily and once-daily products, that are currently on the world market. Special attention is paid to the specific (bio)pharmaceutical characteristics of the different products, and to the influence of the composition and timing of the meals. For each preparation the effect of food on the following pharmacokinetic parameters is discussed: area under the plasma concentration-time curve, peak plasma drug concentration and time to reach this peak. Where possible, the results for both adults and children are discussed. There are indications that children are more susceptible to food-effects than adults. The regulatory aspects are mentioned briefly. Clinically important effects of food have been observed with the following twice-daily products: 'Theo-Dur Sprinkle', 'Theolair SR' (= 'Nuelin SR') and 'Theograd'. Pronounced effects could have an even greater impact with once-daily preparations, as the total daily dose will be given at a single time. A particularly sudden release of a major part of the dose ('dose-dumping') may result in toxic plasma concentrations. Among these products, clinically important effects in children have been reported with 'Theo-24' and 'Uniphyl'.

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Section: 'Theograd' (Abbott Laboratories Uk)mentioning

confidence: 99%

Food Interactions with Sustained-Release Theophylline Preparations1

Jonkman

1989

Clinical Pharmacokinetics

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Clinical Evaluation – In Vivo Bioequivalence Assessment of MR Formulations

Soulele

Macheras

2022

Oral Drug Delivery for Modified Release Formulations

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Theophylline A “State of the Art” Review

1983

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Theophylline is a bronchodilator and respiratory stimulant that is effective in the treatment of acute and chronic asthma, Cheyne-Stokes respirations, and apnea/bradycardia episodes in newborns. It is also used as an adjunct in the treatment of congestive heart failure and acute pulmonary edema, but it has no established efficacy in patients with chronic irreversible airways obstruction. Benefits and risks from theophylline relate directly to serum concentration, which is a function of both dose and elimination characteristics of the drug in an individual patient. When used to treat acute symptoms, an initial loading dose based on a mean volume of distribution is required to rapidly obtain maximum bronchodilator effect. Because of large interpatient differences in elimination, constant intravenous infusion rates for continued therapy must be guided by monitoring serum theophylline concentration at intervals until a steady-state serum concentration is reached within the 10-20 micrograms/ml therapeutic range. Intravenous, oral or rectal solutions and plain uncoated tablets are appropriate for acute therapy, while reliably absorbed slow-release formulations offer therapeutic advantages for the management of chronic asthma, particularly in patients with rapid elimination. Dosage for long-term therapy is determined by starting with low doses that allow virtually complete acceptance of the medication followed by gradual increases, if tolerated, at three day intervals until mean age-specific doses are reached. Subsequent adjustment in dosage regimens are then based upon serum concentration measurements. Most clinical laboratories now measure theophylline, and newer systems have been developed to provide emergency results within minutes at a reasonable cost. In cases of theophylline poisoning, the drug must be rapidly removed to prevent life-threatening toxicity. When serum concentrations are in excess of 60 micrograms/ml charcoal hemoperfusion dialysis may be indicated, even in the absence of obvious signs of toxicity.

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Absorption characteristics of sustained release theophylline capsules administered in applesauce

Cited by 15 publications

References 4 publications

Food Interactions with Sustained-Release Theophylline Preparations1

Food Interactions with Sustained-Release Theophylline Preparations1

Clinical Evaluation – In Vivo Bioequivalence Assessment of MR Formulations

Theophylline A “State of the Art” Review

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