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Method of rapidly achieving therapeutic concentrations of zolmitriptan for treatment of migraines and cluster headaches

A delivery system and coating technology, applied in the field of zolmitriptan and triptan delivery

Pending Publication Date: 2020-04-21
伊默吉克斯美国公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Several attempts have been made to use transdermal microneedle patches for effective drug delivery; however, rapid release of drug from and use of microneedle systems for rapid therapy, optimization and development of effective microneedle shapes and sizes, while also accommodating sufficient Dosage of Drugs Proves Difficult to Reach

Method used

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  • Method of rapidly achieving therapeutic concentrations of zolmitriptan for treatment of migraines and cluster headaches
  • Method of rapidly achieving therapeutic concentrations of zolmitriptan for treatment of migraines and cluster headaches
  • Method of rapidly achieving therapeutic concentrations of zolmitriptan for treatment of migraines and cluster headaches

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0221] Example 1 - Zolmitriptan Coating Formulation, Characterization and Physical Properties

[0222] Zolmitriptan is a weak base with a pKa of 9.6. Solubility measurements were performed by adding excess zolmitriptan base to 0.5 ml of 0.1 M acid and rotating the suspension overnight at 2 to 8 °C. The suspension is then centrifuged. The supernatant was then collected and the concentration of dissolved zolmitriptan was subsequently determined. Table 2 presents the solubility results of zolmitriptan in various acids.

[0223] Table 2: Solubility of zolmitriptan in various acids at 2 to 8 °C

[0224] water solvent Solubility (mg / mL) citric acid 88.6 tartaric acid 63.3 maleic acid 50.5 Succinic acid 59.1 HCl 33.3 Deionized water 1.3

[0225] Zolmitriptan exhibits good solubility in various acids. It was noted that the rheological behavior of the zolmitriptan solution was affected by the counterion in the formulation used fo...

Embodiment 2

[0256] Example 2——Ex vivo human skin

[0257]The ex vivo Franz human skin finite dose model is a tool for studying transdermal absorption of topically applied drugs. The model uses isolated human torso skin mounted in a specially designed diffusion cell that maintains the skin at a temperature and humidity matching typical in vivo conditions. A limited dose (eg, 2 mg / cm 2 to 10mg / cm 2 A formulation of a semisolid, or transdermal delivery system) is applied to the outer surface of the skin, and drug absorption is measured by monitoring its rate of emergence in a receptor solution submerged on the inner surface of the skin. Data defining total absorption, absorption rate, and skin content can be determined in this model.

[0258] medication. The zolmitriptan patch was applied to ex vivo skin using an applicator. Immediately after dosing, the patch and skin were mounted on the Franz diffusion cell.

[0259] Dermal receptor medium. Standard phosphate buffered saline (pH 7...

Embodiment 3

[0283] Embodiment 3——M207 patch stability

[0284] The M207 patch assembly was irradiated by e-beam and gamma radiation at doses up to 25 kGy. The subsequently irradiated patch assembly was placed stably under storage conditions of 25°C / 60%RH and 40°C / 75%RH. Results for the e-beam and gamma irradiated M207 patches are shown in Tables 11-17.

[0285] Table 11: Purity of non-irradiated and e-beam irradiated zolmitriptan patches stored at 25°C / 60%RH and 40°C / 75%RH (L / N 203149)

[0286]

[0287]

[0288] Table 12: ZP-Zolmitriptan content of non-irradiated and e-beam irradiated zolmitriptan patches stored at 25°C / 60%RH and 40°C / 75%RH (L / N 203149)

[0289]

[0290]

[0291] Table 13: Purity of gamma irradiated zolmitriptan patches stored at 25°C / 60%RH and 40°C / 75%RH (L / N203154)

[0292]

[0293] Table 14: ZP-Zolmitriptan content of non-irradiated and gamma-irradiated zolmitriptan patches stored at 25°C / 60%RH and 40°C / 75%RH (L / N 203154)

[0294]

[0295]

[0...

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Abstract

Compositions, devices and methods employing therapeutic concentrations of a triptan for treatment of migraine are described. Also described are methods and apparatuses for delivery of zolmitriptan forachieving a Tmax as quick as 2 minutes and not later than 30 minutes in the majority of subjects.

Description

technical field [0001] The present invention relates to the field of transdermal or intradermal delivery of pharmaceutical formulations, and more particularly to the delivery of triptans, including zolmitriptan. Background technique [0002] According to the Migraine Research Foundation, migraine affects 30 million men, women and children in the United States. Most migraines last from 4 hours to 24 hours, but some last as long as 3 days. According to published research, 63% of migraine sufferers experience between 1 and 4 migraines per month. The incidence in women (approximately 18%) is at the same level as asthma and diabetes combined. About one-third of people affected by migraines have 3 or more migraines per month, and more than half report severe impairment or require bed rest. Migraines are most prevalent in the third decade of life, affecting both productivity and quality of life. In surveys of contributing factors to hope for migraine therapy, rapid relief consi...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61M37/00A61K31/422
CPCA61K9/0021A61M37/0015A61K31/422A61M2037/0023A61P25/06
Inventor 马哈茂德·艾美瑞唐纳德·凯勒曼敖义
Owner 伊默吉克斯美国公司