Devices and methods for delivery of pharmaceutical compositions
Inventors
Assignees
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Publication Number
US-11191934-B2
Publication Date
2021-12-07
Expiration Date
Abstract
Described herein are devices for delivering pharmaceutical compositions to individuals in need thereof. Also described herein are methods of using the devices described herein to deliver pharmaceutical compositions to individuals in need thereof.
Core Innovation
The invention relates to delivering a naloxone-containing formulation to nasal mucosa of an individual having an opioid overdose. The method uses a delivery device that includes a nasal applicator having a shaft with an application tip coupled to the shaft, and an absorbent material coupled to the applicator tip. The absorbent material retains a naloxone-containing formulation and delivers naloxone HCl to a portion of the nasal mucosa between 1.5 cm and 3.0 cm from an opening of the nasal passage.
The method is characterized by inserting the applicator tip into the nasal passage a single time and contacting the nasal mucosa without the applicator penetrating the surface of the nasal mucosa. The formulation includes a naloxone concentration of at least 45 mg/mL, and the delivered amount is from 0.1 mg to 20 mg of naloxone HCl. Following delivery, plasma naloxone HCl pharmacokinetics are characterized by a measured T_max at least 20% less than T_max administered using the same dose via a nasal spray.
In another aspect, treating an opioid overdose includes inserting a nasal applicator with a tip comprising an absorbent material, wherein the absorbent material comprises a pre-metered dose of an aqueous naloxone-containing formulation. The naloxone-containing formulation comprises a naloxone HCl concentration from 45 mg/mL to 90 mg/mL, water, naloxone HCl, citric acid, ethylenediamine tetraacetic acid, benzalkonium chloride, and sodium chloride, with a viscosity from 0.1 centipoise to 10 centipoise at 20°C and a pH from 3.5 to 5.5.
Claims Coverage
The document contains two independent claims. Across these claims, the inventive features are centered on non-penetrating intranasal delivery using an absorbent-material nasal applicator tip loaded with a specified naloxone HCl concentration formulation, with delivery characterized by a reduced measured T_max versus nasal spray.
Non-penetrating single-time intranasal absorbent applicator delivery
Receiving, by the user, a delivery device comprising a nasal applicator with a shaft and an application tip, an absorbent material coupled to the applicator tip retaining a naloxone-containing formulation (naloxone concentration at least 45 mg/mL), inserting the applicator tip into the nasal passage a single time, and contacting the absorbent material with a portion of the nasal mucosa between 1.5 cm and 3.0 cm from an opening without the applicator penetrating the surface of the nasal mucosa; delivering 0.1 mg to 20 mg of naloxone HCl to the nasal mucosa and obtaining a measured T_max at least 20% less than T_max administered using the same dose via a nasal spray to thereby treat the opioid overdose.
Pre-metered aqueous absorbent-tip naloxone formulation with defined composition and T_max reduction
Treating an opioid overdose by inserting a nasal applicator into a nasal passage, the nasal applicator comprising a tip with an absorbent material comprising a pre-metered dose of an aqueous naloxone-containing formulation; the naloxone-containing formulation comprising naloxone HCl concentration from 45 mg/mL to 90 mg/mL, water, naloxone HCl, citric acid, ethylenediamine tetraacetic acid, benzalkonium chloride, and sodium chloride, viscosity from 0.1 centipoise to 10 centipoise at 20°C, and pH from 3.5 to 5.5; contacting nasal mucosa between 1.5 cm to 3.0 cm from an opening to deliver a therapeutically effective amount of naloxone HCl to systemic circulation; wherein measured T_max is at least 20% less than T_max administered using the same dose via a nasal spray.
The independent claims cover methods for treating opioid overdose by intranasal delivery of naloxone HCl using a nasal applicator tip with an absorbent material that retains or provides a pre-metered formulation, with delivery to a defined nasal mucosa location and a pharmacokinetic requirement of reduced measured T_max compared to nasal spray.
Stated Advantages
Improved pharmacokinetics, characterized by a measured T_max at least 20% less than T_max administered using the same dose via a nasal spray.
Delivers a therapeutically effective amount of naloxone HCl to systemic circulation for treating the opioid overdose.
Delivers naloxone HCl to the nasal mucosa without the applicator penetrating the surface of the nasal mucosa.
Lower required dose of naloxone HCl (0.1 mg to 20 mg delivered to the nasal mucosa) while treating the opioid overdose.
Documented Applications
Treating an opioid overdose in an individual in need of such treatment by delivering naloxone HCl to nasal mucosa and systemic circulation.
Treating an opioid overdose in an individual in need of such treatment by intranasal delivery of naloxone HCl to nasal mucosa using the stated nasal applicator and formulation.
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