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Liquid naloxone spray

A naloxone and liquid technology, applied in the direction of organic active ingredients, drug delivery, medical preparations of non-active ingredients, etc., can solve problems such as low bioavailability, discomfort between doses of patients, and the need for repeated administration

Inactive Publication Date: 2019-06-21
HIKMA PHARMA USA INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Rapid metabolizer may require repeated dosing or cause patient discomfort between doses
Enteral administration has low bioavailability due to hepatic first-pass metabolism

Method used

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  • Liquid naloxone spray
  • Liquid naloxone spray
  • Liquid naloxone spray

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0182] Embodiment 1: the preparation of the naloxone preparation containing ethanol

[0183] First, ethanol and USP purified water were degassed separately to prepare liquid spray formulations. Next, ethanol and purified water were purged with nitrogen, respectively. Soluble excipients were then dissolved in ethanol or purified water based on solubility. Next, the solutions are combined. Add naloxone to the final solution and mix until dissolved.

[0184] Strawberry flavoring is used as a raw material for flavoring.

[0185] Table 1 Stable Liquid Naloxone Spray Formulations

[0186]

[0187] value = %w / w

Embodiment 2

[0188] Embodiment 2: the stability test of naloxone preparation

[0189] The formulations listed in Table 1 were tested for stability at 40°C and 55°C ± 2°C, 75% ± 5% relative humidity for 8 weeks. Stability data were collected at zero, one, two, three, four and eight weeks at 55°C and at zero, four weeks and eight weeks at 40°C. Assays and impurity detection were performed using high performance liquid chromatography with UV detector. The assay is performed at 288 nm and expressed as % of initial concentration. All impurities were analyzed at 240 nm and expressed as % area. The amounts of specific impurities are listed in Tables 2A to 2F and 3A to 3H as area percentages of the total impurity amounts for each formulation. "BQL" means "below quantifiable limit" and "ND" means "not detected".

[0190] Table 2A to 2F. Stability of liquid naloxone spray formulations stored at 40°C ± 2°C, 75% ± 5% relative humidity qualitative data

[0191] 2A Stability of Control Formul...

Embodiment 3

[0222] Example 3: Droplet Test

[0223] To determine the spray profile of Formulation #5A, it was subjected to a standardized drop test. A challenge in preparing a sublingual and / or intranasal spray formulation of naloxone is that it must be able to produce spray droplets greater than 10 microns in diameter. Aerosol droplets 10 microns or smaller can be inhaled into the lungs. Optimum particle sizes for sublingual and intranasal spray droplets are 20 to about 200 microns in diameter. It is desirable for formulations to have a droplet size close to 20 as this increases surface area and increased surface area exposure is a factor contributing to high bioavailability. Sublingual and intranasal formulations should be able to maintain a consistent droplet size throughout their shelf life.

[0224] Droplet analysis is performed using standard laser analysis procedures known to those skilled in the art. Droplet size distribution (Dv10, Dv50, Dv90 and Span tested at two distance...

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PUM

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Abstract

The invention provides stable liquid formulations containing naloxone, a pharmaceutically acceptable salt, or a derivative thereof. The invention further provides methods for treating opioid dependence, opioid overdose, and congenital insensitivity to pain with anhidrosis by administering the liquid formulations of the present invention intranasally to a patient in need thereof. Further, the invention provides a method of treating opioid dependence-, opioid overdose, and congenital insensitivity to pain with anhidrosis by administering intranasally the naloxone formulations of the present invention.

Description

technical field [0001] The present invention relates to a liquid spray preparation containing naloxone, its pharmaceutically acceptable salt or its derivative. The present invention also relates to the treatment of opioid dependence, opioid overdose and congenital insensitivity to pain by administering to a patient in need thereof a liquid spray formulation comprising naloxone, a pharmaceutically acceptable salt thereof, or a derivative thereof. The method of hyperhidrosis. Background technique [0002] Naloxone has the following structure and is synthesized from thebaine: [0003] [0004] Naloxone is most commonly used to treat patients suffering from opioid dependence or overdose because it is a competitive mu-opioid antagonist that blocks the effects of opioids. Naloxone is currently available at (Suboxone is a registered trademark of Reckitt Benckiser Healthcare (UK) Ltd.) Available in tablet or sublingual film strip formulations. Contains buprenorphine and nal...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/485A61K47/18A61K9/00
CPCA61K9/00A61K47/18A61K31/485A61K9/0043A61K47/10A61K47/183A61K9/08
Inventor 基兰·阿曼查席瓦妮·希兰帕里斯瑞穆尔蒂·波塔闫宁兴文卡特·R·格斯空达艾什瓦汉·纳拉亚南
Owner HIKMA PHARMA USA INC
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