Osmotically controlled‐delivery of metoprolol in man: in vivo performance of Oros systems with different durations of drug release.

Godbillon, J.; Gérardin, A.; Richard, J.; Leroy, D; J, Moppert

doi:10.1111/j.1365-2125.1985.tb02765.x

Cited by 9 publications

(2 citation statements)

References 9 publications

(10 reference statements)

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“…As in previous studies (Godbillon et 1985) there was a delay in the onset c release from the Oros system probably the time required to achieve sufficien pressure within the core to initiate drug Corresponding lag phases were obser in vivo drug absorption profiles. How presence of similar but shorter dela: infusion profiles suggests some phy!…”

Section: Discussionsupporting

confidence: 55%

Influence of site of drug delivery on the systemic availability of metoprolol: comparison of intragastric infusion and 14/190 Oros administration.

Warrington¹,

Barclay²,

John³

et al. 1985

Brit J Clinical Pharma

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The influence of the site of drug delivery on the systemic availability of metoprolol has been evaluated by measuring plasma drug concentrations in six healthy volunteers after administration of a continuous 13.5 h intragastric infusion and a 14/190 Oros controlled‐ release dosage form, on two separate occasions. The same total amount of drug was administered at the same rate on both occasions but the Oros system moved through the gut whereas the site of the infusion was constant. The differences between treatments were confined largely to the period 6‐15 h after dosing when lower plasma concentrations were obtained after administration of the Oros system. The levels after 20 h were higher for Oros, however, reflecting its longer duration of drug release. The amount of drug reaching the circulation was 19.8% less for the Oros preparation compared with intragastric infusion but this was not due to incomplete release since the residual amounts of drug in three systems recovered from faeces corresponded to less than 12% of the administered dose. Analysis of the plasma profiles by the Wagner‐ Nelson method indicated a reasonable agreement between in vitro release and in vivo absorption. The appearance of drug in plasma was delayed for both treatments, and for Oros the apparent absorption rate slowed 6 h after dosing. Plasma profiles after 14/190 metoprolol Oros were consistent with prolonged in vivo delivery and absorption from the gut. The absorption process, however, was associated with some reduction both in the rate, after 6 h, and in the total amount reaching the circulation.

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Section: Discussionsupporting

confidence: 55%

Influence of site of drug delivery on the systemic availability of metoprolol: comparison of intragastric infusion and 14/190 Oros administration.

Warrington¹,

Barclay²,

John³

et al. 1985

Brit J Clinical Pharma

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“…The amount of drug reaching the circulation after Oros was thus little altered by food, in contrast with the marked increase noted by for the conventional tablet. This discrepancy is probably Svensson et al, 1983), and its relationship to total absorption times for the conventional and Oros preparations (2.5 h and 14 h for 90% absorption, respectively; Godbillon et al, 1985).…”

Section: Analytical Proceduresmentioning

confidence: 99%

Influence of food on the absorption of metoprolol administered as an Oros drug delivery system to man.

Lecaillon¹,

Massias²,

Schoeller³

et al. 1985

Brit J Clinical Pharma

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1 The influence of food on the release, absorption and metabolism of metoprolol has been studied after single administration of a 19/190 Oros system to eight healthy volunteers on four occasions, once after an overnight fast, and just before each of three daily meals (breakfast, lunch and dinner). 2 The plasma concentration-time profiles under the four test conditions were virtually identical, and no statistically significant differences in mean areas under the curves between 0 and 32 h, peak concentrations, or times to peak, were detected. 3 The absorption of metoprolol was unaffected by food intake, with 80-90% of the amount absorbed reaching the systemic circulation within 10 h. 4 The ratios of areas under the curve for ax-hydroxymetoprolol to its parent drug were in the same range for the four treatments, and similar to those reported after conventional tablets. 5 The in vivo release and absorption of drug from the Oros system, and its systemic availability, were not influenced by concomitant ingestion of food.

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Metoprolol oros: Reducing medication stress in hypertension

Murphy¹,

Wheatley²

1989

Stress Med.

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Antihypertensive drug therapy constitutes a “life sentence” of drug‐taking for the patient and reduction of medication stress, by a simplified dose regime helps to ensure patient compliance. Metoprolol Oros (Metoros) contains 190 mg of metoprolol fumarate which allows continuous release of the drug by osmotic pressure to provide adequate therapeutic dose levels for 24 hours. Metoprolol Oros was compared to conventional metoprolol 100 mg bd in 60 newly diagnosed hypertensive patients for 12 weeks, following a one‐week control period. Significant reductions in pulse rate and systolic and diastolic blood pressures occurred in both groups but were significantly greater with metoprolol Oros (p<0.05). Thus, with metoprolol Oros the mean blood pressure fell from 177/103 to 150/84 and with metoprolol fumarate bd from 175/104 to 159/92 mm Hg. by the end of the trial. There were no significant differences between changes in supine and upright blood pressures in either group. The commonest side‐effect with metoprolol Oros was lassitude occuring in six cases (9 per cent) (metoprolol bd three cases, 10 per cent); whilst in the metoprolol fumarate bd group it was nocturia (six cases, 21 per cent) (Oros three cases, 10 per cent). There were no statistically significant between‐group differences in respect of any side‐effects. It was concluded that the trial had demonstrated metoprolol Oros to be an effective method of reducing blood pressure with superior results to the conventional form of the drug.

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Osmotically controlled‐delivery of metoprolol in man: in vivo performance of Oros systems with different durations of drug release.

Cited by 9 publications

References 9 publications

Influence of site of drug delivery on the systemic availability of metoprolol: comparison of intragastric infusion and 14/190 Oros administration.

Influence of site of drug delivery on the systemic availability of metoprolol: comparison of intragastric infusion and 14/190 Oros administration.

Influence of food on the absorption of metoprolol administered as an Oros drug delivery system to man.

Metoprolol oros: Reducing medication stress in hypertension

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