Analgesics for nasal administration

analgesics and compositions, applied in the field of analgesic compositions, can solve the problems of prolonged analgesia, and increase the residence time of analgesic in the nasal cavity, and achieve the effects of rapid uptake, increased residence time of analgesic in the nasal cavity, and fast onset of analgesia

Inactive Publication Date: 2005-06-30
IONIX PHARMA +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0023] Improved analgesic formulations for nasal administration have now been devised. Rapid uptake of the analgesic across the nasal mucosa into the plasma can be achieved, which results in fast onset of analgesia. Further, the residence time of the analgesic in the nasal cavity can be increased, which results in prolonged analgesia. An improved profile of absorption of the analgesic into the systemic circulation can thus be achieved.

Problems solved by technology

Rapid uptake of the analgesic across the nasal mucosa into the plasma can be achieved, which results in fast onset of analgesia.
Further, the residence time of the analgesic in the nasal cavity can be increased, which results in prolonged analgesia.

Method used

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  • Analgesics for nasal administration
  • Analgesics for nasal administration
  • Analgesics for nasal administration

Examples

Experimental program
Comparison scheme
Effect test

example 1

Nasal Solution Containing Buprenorphine (4 mg / ml) and Pectin

[0168] 5 g of pectin (SLENDID (trade mark) 100, CP Kelco, Denmark) was dissolved by stirring into approximately 180 ml of water for injection (WFI) (Baxter, UK). 1075 mg of buprenorphine hydrochloride (MacFarlan Smith, UK) and 12.5 g of dextrose (Roquette) were dissolved into the pectin solution. 1.25 ml of phenylethyl alcohol (R. C. Treat, UK) and 50 mg of propyl hydroxybenzoate (Nipa, UK) were dissolved into the pectin / buprenorphine solution. The solution was adjusted to 250 ml using WFI. 1M hydrochloric acid (BDH, UK) was added to adjust the pH to 3.6.

[0169] The final product was a slightly turbid solution 4.3 mg / ml buprenorphine hydrochloride (corresponding to 4 mg / ml buprenorphine), 20 mg / ml pectin, 50 mg / ml dextrose, 5 μl / ml phenylethyl alcohol and 0.2 mg / ml propyl hydroxybenzoate. The pH of the solution was 3.6, as mentioned above. The osmolality of the solution was 0.46 osmol / kg.

[0170] Single dose nasal spray dev...

example 2

Nasal Solution Containing, Buprenorphine (2 mg / ml) and Pectin

[0171] 5 g of pectin is dissolved by stirring into approximately 180 ml of WFI. 538 mg of buprenorphine hydrochloride and 12.5 g of dextrose are dissolved into the pectin solution. 1.25 ml of phenylethyl alcohol and 50 mg of propyl hydroxybenzoate are dissolved into the pectin / buprenorphine solution. The solution is adjusted to 250 ml using WFI.

[0172] The final product is a slightly turbid solution containing 2.16 mg / ml buprenorphine hydrochloride (corresonding to 2 mg / ml buprenorphine), 20 mg / ml pectin, 50 mg / ml dextrose, 5 μl / ml phenylethyl alcohol and 0.2 mg / mil propyl hydroxybenzoate.

[0173] 123 μl of the above solution is filled into a Valois Monospray single dose nasal spray device (Pfeiffer, Germany). Actuation of the device will deliver a dose of 100 μl of liquid containing 200 μg of buprenorphine and 2 mg of pectin.

example 3

Nasal Solution Containing Buprenorphine (4 mg / ml), Chitosan and HPMC

[0174] 0.75 g of HPMC (Methocel (trade mark) E4M, Colorcon, UK) was dispersed into approximately 125 ml of pre-heated (70-80° C.) water for injection (WFI) (Baxter, UK). The HPMC dispersion was stirred in an ice bath until a clear solution had formed. 1.25 g of chitosan glutamate (Protosan (trade mark) UPG213, Pronova, Norway) was dissolved in the HPMC solution. 75 mg of 50% w / w benzalkonium chloride solution (Albright and Wilson, UK) was dispersed in. 10 ml of WFI and transferred with an additional 40 ml of WFI to a 250 ml volumetric flask. 1075 mg of buprenorphine hydrochloride (MacFarlan Smith, UK) and 12.5 g of dextrose (Roquette, UK) were transferred into the volumetric flask. The chitosan / HPMC solution and an additional 40 ml of WFI were added to the flask. The solution was adjusted to pH 3.4 using 1M hydrochloric acid solution (BDH, UK) and the flask contents adjusted to 250 ml using WFI.

[0175] The final pr...

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Abstract

An analgesic and a delivery agent are combined in a pharmaceutical composition such that, on introduction into the nasal cavity of a patient to be treated, the analgesic may be delivered to the bloodstream to produce within 30 minutes a therapeutic plasma concentration, Cther, of 0.2 ng / ml or greater which is maintained for a duration Tmaint of at least 2 hours. The analgesic may be an opioid analgesic or a non-steroidal anti-inflammatory drug.

Description

FIELD OF THE INVENTION [0001] The invention relates to analgesic compositions and their use. BACKGROUND OF THE INVENTION [0002] A wide variety of compounds can act as analgesics. Two important classes of analgesics are opioid analgesics and non-steroidal anti-inflammatory drugs (NSAIDs). [0003] Opioid analgesics exhibit morphine-like properties. Opioids can be sub-classified on the basis of their receptor specificity. Mu-agonist opioids provide intense analgesia. These opioids can be long-acting (e.g. methadone) or short-acting (e.g. remifentanil). Mixed agonist / antagonist opioids (e.g. butorphanol and buprenorphine) are partial agonists (the former at mu and kappa receptors and the latter at the mu receptor) and can produce good quality analgesia. They produce less respiratory depression and constipation than high efficacy mu agonists. [0004] As a class, opioids are associated with a number of undesirable side-effects, including respiratory depression, nausea, vomitting, dizziness,...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K9/08A61K9/00A61K9/12A61K31/195A61K31/196A61K31/405A61K31/407A61K31/485A61K31/54A61K31/5415A61K45/00A61K47/02A61K47/10A61K47/14A61K47/18A61K47/26A61K47/34A61K47/36A61K47/38A61M11/00A61M15/08A61P5/24A61P15/00A61P25/02A61P25/04A61P27/16A61P29/00A61P43/00
CPCA61K9/0043A61K31/195A61K31/196A61K31/405A61K31/407A61K47/38A61K31/54A61K31/5415A61K47/34A61K47/36A61K31/485A61P15/00A61P25/02A61P25/04A61P27/16A61P29/00A61P43/00A61P5/24A61K9/08
Inventor BIRCH, PHILLIP JOHNHAYES, ANN GAILWATTS, PETER JAMESCASTILE, JONATHAN DAVID
Owner IONIX PHARMA
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