| 摘要 |
Optimal ratios of pharmaceutical compositions of beta-1 and beta-2 agonists with their respective antagonists. Safer, more cost-effective drugs for heart and lung therapies are made by combining specific antagonists with their agonists to prevent desensitization of cellular receptors, reducing some of the unwanted side-effects of the agonist drugs alone. Determining the optimal concentration of an antagonist or inhibitor, which is necessary to prevent desensitization, without causing unnecessary and unwanted inhibition, creates a new class of pharmaceuticals. To derive an optimum ratio for a specific composition, a formulative method is provided to detail how competitive antagonists of the receptor should be combined with agonists, in specific proportions, to maximize and maintain receptor response throughout drug administration. The "optimal ratio" methodology used to determine a specific agonist/antagonist composition, to prevent beta-1 or beta-2 receptor desensitization, is experimentally verified and validated for specific compositions. Alteration of a specific ratio is practiced to account for the pharmacokinetic/dynamic differences between animals and humans and within human populations.
|
