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Single dose and steady-state pharmacokinetics of 4 mg and 8 mg oral salbutamol controlled-release in patients with bronchial asthma

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Summary

Fifteen patients with asthma were given salbutamol controlled-release (SCR) 4 mg or 8 mg twice daily for seven days, in a randomised double-blind cross-over design. Plasma salbutamol levels were measured after the first and fifteenth doses for a 12 h period following drug ingestion.

At steady-state the geometric mean values for Cmax were 8.2 ng/ml for 4 mg, and 16.1 ng/ml for 8 mg. Median tmax values were 300 and 240 min respectively. The geometric mean AUC (0–12) were 4507 ng·min·ml−1 and 8980 ng·min/ml. Peak to trough fluctuation ratios were 0.577 and 0.572.

There were no significant differences between 4 mg or 8 mg formulations, for any of the parameters measured, after appropriate corrections for dose. The concentration-time profiles at steady-state showed little fluctuation in plasma salbutamol levels over the twelve hour dosing interval. These results show that 4 mg and 8 mg formulations of SCR provide smooth plasma profiles at steady-state with a twice daily dosing regime.

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References

  • Britton M (1988) A multicentre comparison of 8 mg salbutamol controlled release (SCR) tablets b. d. versus theophylline slow release tablets (300 mg) b. d. in control of reversible airways obstruction. Eur Respir J [Suppl 2] 1: 197s

  • Callaghan B, Ryan W, Hagstad H, Tegner K, Kotaniemi J (1986) A multicentre study of a new controlled-release formulation of salbutamol (salbutamol CR) compared with a titrated dose of slow-release theophylline (Theodur) in the treatment of chronic obstructive airways disease. Bull Eur Physiopathol Respir [Suppl 8] 22: 1115

    Google Scholar 

  • Cochran WG, Cox GM (1957) Note on the statistical analysis of the results: In: Experimental designs. Wiley, New York, pp 45–94

    Google Scholar 

  • Crompton GK (1982) Problems patients have using pressurised aerosol inhalers. Eur J Respir Dis [Suppl 119] 63: 101–104

    Google Scholar 

  • Dahl R (1988) A multicentre trial of salbutamol controlled release tablets (volmax) and standard salbutamol tablets (ventolin) in the management of asthma and chronic bronchitis. Eur Respir J [Suppl 2] 1: 306s

  • Davies RJ, Ferguson H, Herdman MJ, Ollier S (1988) Oral controlled release albuterol: its effect on asthmatic symptoms and bronchial hyperresponsiveness. Am Rev Respir Dis [Suppl] 137: 32

    Google Scholar 

  • Hutchings MJ, Paull JD, Morgan DJ (1983) Determination of salbutamol in plasma by high performance liquid chromatography with fluorescence detection. J Chromatogr 277: 423–426

    Google Scholar 

  • Jenne JG, Chick TW, Strickland RD, Wall FJ (1977) Subsensitivity of beta-responses during therapy with a long acting beta-2 preparation. J Allergy Clin Immunol 59: 383–390

    Google Scholar 

  • Jenne JW, Valcarenghi G, Druz WS, Starkey PW, Yu C, Shaughnessy TK (1986) Comparison of tremor responses to orally administered albuterol and terbutaline. Am Rev Respir Dis 134: 708–713

    Google Scholar 

  • Koch GG (1972) The use of nonparametric methods in the Statistical analysis of the two-period change-over design. Biometrics 28: 577–588

    Google Scholar 

  • Legge JS, Gaddie J, Palmer KNV (1971) Comparison of two oral selective beta-2 adrenergic stimulant drugs in bronchial asthma. Br Med J I: 637–639

    Google Scholar 

  • Maesen FP, Measen V, Smeets JJ (1986) Comparison of a controlled release tablet of salbutamol given twice daily with a standard tablet given four times daily in the management of chronic obstructive lung disease. Eur J Clin Pharmacol 31: 431–436

    Google Scholar 

  • Milroy R, Carter R, Carlyle DL, Boyd G (1987) Pharmacology of salbutamol with a new controlled release salbutamol preparation. Am Rev Respir Dis [Suppl] 135: A228

  • Morgan DJ, Paull JD, Richmond BH, Wilson-Evered E, Ziccone SP (1986) Pharmacokinetics of intravenous and oral salbutamol and its sulphate congugate. Br J Clin Pharmacol 22: 587–593

    Google Scholar 

  • Neilson NH, Weeke B, Ostlener L, Wilkinson P, Kay A, Williams I, Ng SH, Wouters FM, Beamer HM (1988) Salbutamol controlled release (Volmax) — A comparison with standard salbutamol tablet (ST) in the treatment of chronic obstructive airway disease (COAD). Eur Respir J [Suppl 2] 1: 306s

  • Nelson HS, Raine D Jr, Doner C, Posey WC (1977) Subsensetivity to the bronchodilator action of albuterol produced by chronic administration. Am Rev Respir Dis 116: 871–878

    Google Scholar 

  • Sykes RS, Reese ME, Meyer MC (1987) Pharmacokinetic properties of a new sustained-release albuterol preparation, volmax. J Allergy Clin Immunol 79: 152

    Google Scholar 

  • Theeuwes F (1975) Elementary osmotic pump. J Pharm Sci 64: 1987–1991

    Google Scholar 

  • Tsanakas JN, Bannister OH, Baxter P (1988) Tachyphylaxis does not occur after long-term administration of salbutamol controlled release (Volmax: SCR). Eur Respir J [Suppl 2] 1: 202s

  • Walker SR, Evans ME, Richards AJ, Paterson JW (1972) The clinical pharmacology of oral and inhaled salbutamol. Clin Pharmacol Ther 13: 861–867

    Google Scholar 

  • Watson JM, Richens A (1974) The effects of salbutamol and terbutaline on physiological tremor, bronchial tone and heart rate. Br J Clin Pharmacol 1: 223–227

    Google Scholar 

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Part of this paper has been presented in abstract form to the British Thoracic Society, Newcastle, July 1988

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Lipworth, B.J., Clark, R.A., Dhillon, D.P. et al. Single dose and steady-state pharmacokinetics of 4 mg and 8 mg oral salbutamol controlled-release in patients with bronchial asthma. Eur J Clin Pharmacol 37, 49–52 (1989). https://doi.org/10.1007/BF00609424

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  • DOI: https://doi.org/10.1007/BF00609424

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