Medicament comprising a highly potent long-lasting beta2-agonist in combination with other active ingredients
A technology of active ingredients and compositions, applied in the field of pharmaceutical compositions containing high-efficiency and long-acting β2-agonists and other active ingredients, can solve problems such as undetermined effective and safe doses
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Embodiment 1
[0069] Example 1 - In vitro test of the anti-inflammatory efficacy of the composition of the invention on a human U-937 derived macrophage cell line
[0070] U-937 cells were incubated with 10 ng / ml phorbol myristate acetate and subjected to macrophage differentiation for 48 hours.
[0071] Cells were then treated with 1 μg / ml lipopolysaccharide (LPS) or LPS and a concentration range of β 2 -Agonists, corticosteroids or combinations together. TNF[alpha] and IL-10 were assayed after different times of incubation. Media was collected and cells were lysed for cyclic adenosine 3',5'-monophosphate (cAMP) assay.
[0072] TNFα and IL-10 were measured in the medium by a commercially available ELISA assay, and simultaneously by a commercially available 3 The H-cAMP assay system measures cAMP.
[0073] in the absence and presence of 10 -10 and 10 -8 The concentrations of M provided by TA 2005 were used to determine the corticosteroid dose-response curve. Inhibition of TNFa and IL-...
Embodiment 2
[0075] Example 2 - In vivo test of the anti-inflammatory efficacy of the composition of the invention in a Sephadex-induced pulmonary edema model
[0076] Rat pulmonary edema induced by Sephadex is a model leading to inflammatory cell infiltration and persistent interstitial edema. Evaluation with another long-acting beta 2 Anti-inflammatory activity of TA 2005 alone and in combination with budesonide compared with the adrenoceptor agonist, formoterol.
[0077] Sephadex beads (5 mg / ml) were administered intratracheally to anesthetized rats (200-250 g) at a dose volume of 1 ml / kg. The control group received 1 ml / kg saline.
[0078] The test substances are suspended in saline and suitably diluted in Sephadex suspension for intratracheal administration.
[0079] Twenty-four hours after administration, the animals were sacrificed, and the lungs were removed and weighed. The percent inhibition of Sephadex-induced edema was then determined.
[0080] Intratracheal instillation...
Embodiment 3
[0082] Example 3 -Effect of TA 2005 and budesonide combination on acetaldehyde-induced bronchoconstriction in guinea pigs
[0083] Control of bronchoconstriction induced by acetaldehyde (AcCHO) by TA 2005 has been studied in anesthetized artificially ventilated guinea pigs according to the experimental animal model described by Berti et al., Arzneim-Forsch / Drug Res 1994;44:323-326 and neuroinflammatory capacity.
[0084] Intravenous injection of AcCHO resulted in dose-dependent bronchoconstriction accompanied by increased blood histamine and Evans blue extravasation in tracheal tissue, indicating altered vascular permeability.
[0085] The protective activity of TA 2005 (0.1-10 pmol), formoterol (0.3-30 pmol) or budesonide (31.25-500 nmol) was determined after intratracheal perfusion alone or in combination.
[0086] All effects of AcCHO were effectively antagonized by TA 2005 and formoterol. However, TA 2005 was almost twice as effective as formoterol in preventing bronch...
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