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A 5% solution of metaproterenol, 10 whiffs (1.5 mg) q.i.d., was administered from a hand bulb nebulizer to 28 asthmatics for 60 days. Spirometry in double-blind, crossover tests against an 0.5% isoproterenol solution on days 0-1 and 59-60 and global evaluations of response showed that metaproterenol was more effective and longer acting. No tolerance to metaproterenol developed. Side-effects were negligible.
Penetration and permeation of griseofulvin into and across the rat skin after application of three ointment formulations containing either dimethylacetamide (DMAC) or diethylene glycol monoethylether (DGME) or the ointment base alone (control--without DMAC or DGME) were studied, in vitro. Penetration and permeation of griseofulvin into and across the human skin after application of DGME ointment was also studied. Permeation of griseofulvin across the rat skin was highest for the DMAC ointment, followed by the DGME ointment and lowest for the control. Concentration of griseofulvin in the upper layers of the skin (i.e., surface to 100 micron depth) was also highest for DMAC and lowest for the control. However, the skin levels from the DGME ointment could not be distinguished (statistically) from the other two formulations. In comparison to rat skin, human skin is much less permeable. Amount of griseofulvin (from DGME ointment) that permeated through the rat skin was 14 times the amount that permeated through the human skin. Concentration of griseofulvin in the upper layers of the rat skin were 4 times the concentration of the drug in the upper layers of the human skin. The concentration of griseofulvin in the various layers of the human skin after one topical application were far greater than those reported after prolonged peroral administration.
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The bioavailability of papaverine, administered as sustained release capsules, an elixir, and soft gelatin capsules, was studied with volunteers. Blood samples were assayed for papaverine, using a gas chromatographic method, following the administration of single 150 mg doses of papaverine HC1. The elixir and the soft gelatin capsule resulted in nearly identical papaverine blood levels, while peak levels, area under the blood level-time curve, and plasma levels 0.5, 1.0, 1.5, and 2.0 hours after dosing with the sustained release capsule were significantly (p less than 0.01) lower.
This article encompasses a brief discussion of the principles of pharmacodynamics of different types of drugs and the mechanisms of absorption at different sites in the gastrointestinal tract. The importance of factors such as the pH, the unstirred layer or microclimate, gastric emptying, intestinal contact time, metabolism in the gut wall, and bacterial degradation in the colon is discussed. Methods that can be used to alter the absorption of drugs such as formulation in a viscous form, a form that floats in the stomach, position release forms, combination with other drugs that may influence absorption, etc. are examined in detail.
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The pharmacokinetics and relative bioavailability of pentoxifylline, from a new sustained-release formulation (Oxopurin) and from a standard sustained-release formulation (Trental-400), were compared in 8 healthy adult male volunteers. After a single oral dose of 400 mg Oxopurin, a mean maximal plasma concentration (Cmax) of 164 +/- 62 micrograms/l was obtained after 2.2 h (tmax). After an identical dose of Trental-400, a peak plasma concentration of 123 +/- 33 micrograms/l was obtained after 2.4 h. Plasma levels of pentoxifylline were determined by a new HPLC assay which was developed as part of this study and makes possible monitoring plasma levels of pentoxifylline for 14 h after a single dose. The mean relative bioavailability of pentoxifylline from Oxopurin was 1.30 +/- 0.19 relative to that of Trental-400. As the rate and the extent of absorption of pentoxifylline was not significantly different after the administration of the two investigated formulations, it can be concluded that Oxopurin is bioequivalent to Trental-400.
The pharmacokinetics and relative bioavailability of diclofenac sodium from a new sustained-release formulation (Effekton-100) and from a standard sustained-release formulation (Voltaren-Retard) were compared in 11 healthy adult male volunteers. After a single oral dose of 100 mg Effekton-100, a mean maximal plasma concentration (Cmax) of 497 +/- 120 ng/ml was obtained after 7.4 h (tmax). After an identical dose of Voltaren-Retard, a peak plasma concentration of 654 +/- 329 ng/ml was obtained after 6.4 h. Plasma levels of diclofenac were determined by a new HPLC assay which was developed as part of this study and makes possible monitoring plasma levels of diclofenac for 24 h after a single dose. The mean bioavailability of diclofenac from Effekton-100 was 0.97 +/- 0.28 relative to that of Voltaren-Retard. As the rate and the extent of absorption of diclofenac sodium was not significantly different after the administration of the two investigated formulations, it can be concluded that Effekton-100 is bioequivalent to Voltaren-Retard.
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A simple and rapid liquid chromatographic method is described for the determination of propranolol hydrochloride in pharmaceutical preparations. The separation was achieved on a reverse-phase octylsilane (C8) column by using a mobile phase composed of a mixture of 0.5 g dodecyl sodium sulfate in 18 mL (0.15 M) H3PO4 plus 90 mL methanol, 90 mL acetonitrile, and 52 mL water. Detector response was linear for 0.03-3.1 mg/mL of propranolol. Recoveries from synthetic mixtures ranged from 99.6 to 101.7%. The results obtained by the proposed method were similar to those obtained by the USP XXI method.
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The potential of powdered soybean protein (SBP) as a vehicle for controlled drug release was investigated, using theophylline as the model drug, an in vitro dissolution test and in vivo absorption studies in beagle dogs. The results of the dissolution test demonstrated that the addition of SBP to the tablet brought about retarded dissolution of theophylline. In the in vivo absorption study, Tmax values for theophylline-SBP tablets were larger than those for tablets containing only theophylline; there was no difference in AUC between the two tablets. In addition, there was no detectable difference in the results with theophylline-SBP and Theodur tablets. The practical usefulness of SBP as a vehicle for controlled release tablets was confirmed not only from our in vitro experiment, but also from our in vivo absorption test using beagle dogs.
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