Bioavailability of a New Sustained-Release Anhydrous Theophylline Product

1996 ◽  
Vol 24 (4) ◽  
pp. 331-339 ◽  
Author(s):  
G Tatsis ◽  
G Tsoukalas ◽  
A Haviaras ◽  
A Peristerakis ◽  
V Filaditaki ◽  
...  

The bioavailability of a new sustained-release anhydrous theophylline product (Theophylline Lavipharm®) was evaluated and compared with the bioavailability of a well-established product, Theodur®. Two groups of 12 healthy non-smokers were given single doses of 200 or 300 mg of each product and two groups of 12 patients with asthma or chronic obstructive lung disease were given doses of 200 or 300 mg of each product every 12 h for 5-day periods. The values of the area under the plasma theophylline concentration against time curve (AUC), the maximum plasma theophylline concentration ( Cmax) and the time taken to reach Cmax (Tmax) for the two products did not differ significantly in the healthy groups or in the patients. The minimum and the average plasma theophylline concentrations and the fluctuation index were also calculated for the patients and there were no significant differences between the values for the two products. The new anhydrous theophylline product, Theophylline Lavipharm®, appears to show very similar bioavailability to Theodur®. No adverse reactions to the new product were reported.

1987 ◽  
Vol 15 (6) ◽  
pp. 352-360
Author(s):  
S. Giosue' ◽  
D Bernocchi ◽  
D. Parola ◽  
R. Munno ◽  
P. Mancini

A sustained-release theophylline preparation in capsule form was compared with standard slow-release theophylline tablets for variation in plasma theophylline concentration, effectiveness and tolerability in 30 adults with chronic broncho-obstructive pathology. They were administered every 12 h and blood samples were collected after 8 days of treatment during the steady-state period. In this double-dummy crossover study, the sequence of the two regimens (sustained-release capsules versus tablets) was selected at random. The results of this study demonstrate that plasma theophylline levels remain within the therapeutic range for both preparations. Effectiveness and tolerability of the two drugs were satisfactory.


1990 ◽  
Vol 9 (3) ◽  
pp. 179-182 ◽  
Author(s):  
A.H. Al-Shareef ◽  
D.C. Buss ◽  
E.M. Allen ◽  
P.A. Routledge

1 The effects of charcoal and sorbitol, alone and in combination, were investigated in eight healthy female volunteers who received 600 mg slow-release theophylline (two 300 mg capsules) . 2 The area under the plasma concentration time curve to 24 h (AUC0-24) after theophylline alone was significantly greater than after both the charcoal and charcoal plus sorbitol phase. 3 Charcoal and charcoal with sorbitol also significantly reduced the maximum plasma theophylline concentration ( Tmax) and time to maximum concentration ( Cmax). 4 Sorbitol significantly increased Cmax and shortened Tmax. 5 Although sorbitol did not reduce the adsorptive efficacy of charcoal, its use alone may be deleterious in poisoning with sustained-release theophylline products.


1988 ◽  
Vol 16 (6) ◽  
pp. 452-458 ◽  
Author(s):  
G. Tatsis ◽  
J. Danos ◽  
M. Gaga ◽  
D. Pantelakis ◽  
M. Veslemes ◽  
...  

In a single-blind crossover study, two slow release theophylline preparations were evaluated in 18 patients with chronic bronchitis or asthma without cardiac, renal or liver disease. After randomization into two groups, patients were treated, in a crossover study design, with 600 mg choline theophyllinate or 300 mg anhydrous theophylline administered orally every 12 h for 7 days. A 2-day washout period separated the two periods of treatment evaluation. Blood samples in which plasma theophylline concentration was to be measured were taken at 7.30 a.m., 2.00 p.m. and 7.30 p.m. during the last 5 days of therapy with each drug. The mean fluctuation in plasma theophylline concentration was ≤40% in all 18 patients taking choline theophyllinate yet in only 15 (83%) patients administered anhydrous theophylline. Salbutamol inhaler was more frequently required for the relief of bronchospasm when taking anhydrous theophylline than when taking choline theophyllinate (total of 41 vs 25 puffs, respectively, over 7 days). Drug-related adverse reactions occurred in four patients while taking anhydrous theophylline and in one patient while taking choline theophyllinate.


1977 ◽  
Vol 11 (1) ◽  
pp. 12-18 ◽  
Author(s):  
Leslie Hendeles ◽  
Lyle Bighley ◽  
Robert H. Richardson ◽  
Charles D. Hepler ◽  
Jan Carmichael

Use of recommended IV aminophylline dosage regimens in 48 older, acutely ill, hospitalized patients with chronic obstructive pulmonary disease (COPD) resulted in excessive plasma theophylline concentrations in 29 percent of these patients. A mean dose of 0.89 mg/kg/hr produced a plasma concentration which ranged from 7 to 52 mcg/ml with a mean of 21.9 mcg/ml. Plasma theophylline concentration was determined spectrophotometrically from plasma samples drawn at least 12 hours after a loading dose and initiation of a constant infusion. Severity of toxicity strongly correlated with the plasma theophylline concentration in 18 patients. Nausea and/or vomiting preceded life-threatening drug-induced arrhythmias and seizures less than half the time. Tachycardia was found to be the most consistent symptom associated with toxicity. These patients had lower plasma clearances than otherwise healthy younger adult asthmatics and healthy volunteers. Toxicity and identifiable risk factors for excessive plasma levels strongly correlated with reduced plasma clearance. Dosage modifications based upon plasma clearances from COPD patients without concurrent functional abnormalities and those with liver dysfunction and cardiac decompensation ranged from 0.7 to 0.12 mg/kg/hr. This study clearly demonstrates the poor correlation between dose and plasma concentration and the strong relationship between toxicity and plasma concentration. These results as well as those previously reported mandate that the relatively simple, rapid and inexpensive theophylline plasma measurement be used in all patients receiving IV aminophylline for longer than 24 hours in order to prevent toxicity.


Author(s):  
Anna Viktorovna Katicheva ◽  
Nikolai Andreyevich Brazhenko ◽  
Olga Nikolaevna Brazhenko ◽  
Anna Georgievna Chuikova

In modern conditions, chronic tobacco intoxication and chronic obstructive pulmonary disease are widespread and affect the health and life expectancy of patients. Among patients with tuberculosis, chronic tobacco intoxication and COPD are also widespread. Against the background of smoking and chronic obstructive pulmonary disease in patients with tuberculosis of the respiratory system, bronchial obstruction, hypoxemia, impaired capillary pulmonary blood flow, and a decrease in the diffusion capacity of the lungs are determined. A comorbid state is accompanied by the development of oxidative stress, systemic inflammation, endothelial dysfunction. Such changes in combination with dyslipidemia contribute to the development of multifocal atherogenesis, systemic arterial hypertension and the rapid development of cardiovascular pathology


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