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Therapeutic compositions for intranasal administration of ketorolac

A composition, a nasal technique, applied in the field of pain treatment, can solve the problems such as the time of the maximum concentration of 5HT1D that no one has mentioned

Inactive Publication Date: 2007-12-05
ROXRO PHARMA INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

No data were provided to support this hypothesis, and no one mentioned the time to reach the maximum concentration of 5HT1D

Method used

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  • Therapeutic compositions for intranasal administration of ketorolac
  • Therapeutic compositions for intranasal administration of ketorolac
  • Therapeutic compositions for intranasal administration of ketorolac

Examples

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example 1

[0089] This example describes the preparation of compositions of the invention for nasal administration. Prepare solutions according to the proportions shown in Table 1. Lidocaine hydrochloride was added to the solution to obtain the compositions of the present invention shown in Table 2.

[0090] Table 1

[0091] Ketorolac Tromethamine, USP 15%

[0092] Sodium EDTA, NF 0.02%

[0093] Potassium Phosphate, NF (qs up to pH 7.2)

[0094] Water for Injection USP (appropriate amount) 100g

[0095] Table 2

[0096] Component I II III

[0097] Ketorolac Tromethamine, USP 15% 15% 15%

[0098] Sodium EDTA, NF 0.02% 0.02% 0.02%

[0099] Potassium phosphate, NF (as appropriate until pH 7.2)

[0100] Lidocaine hydrochloride 4% 5% 6%

[0101] Water for injection USP (appropriate amount) 100g 100g 100g

example 2

[0103] This example describes a phase I clinical study conducted to determine intrinsic activity (i.a.) when the presence of lidocaine hydrochloride in nasally administered ketorolac formulations had a negative impact on the PK profile of ketorolac (dual Blind, randomized 4-way crossover study). The results show that the PK profile is enhanced by the presence of the anesthetic lidocaine hydrochloride (5-6% w / v) in the preferred formulation and otherwise not negatively affected. In addition, the safety and tolerability data of the formulations were also evaluated.

[0104] The clinical study included 16 healthy volunteers recruited for the study, each volunteer receiving 4 nasal spray formulations, 3 of which were compositions representing aspects of the present invention. There is a rest period of 3-7 days between each administration. The 4 aqueous spray compositions were prepared as follows:

[0105] KT(1) L(2) NaEDTA(3) K 3 PO 4 (4) water (5)

[0106] A: 15% 0 0...

example 3

[0120] This example describes a study in postoperative patients to compare the safety, tolerability and pharmacokinetics (PK) of 3 intranasal (IN) ketorolac tromethamine formulations.

[0121] The study was a double-blind, parallel study in postoperative patients. Individuals received 1 of 3 IN ketorolac tromethamine formulations (30 mg) or placebo. Two of these formulations are preferred formulations of the invention. A total of 60 individuals were included in the study, with 15 individuals enrolled in each group. Each formulation was administered IN to each subject (one spray into each nostril).

[0122] Eligible postoperative patients for this study included those aged 18 to 60 years who were within 20% of ideal body weight (MetLife Male and Female Height and Weight Table (1999 edition)).

[0123] Each individual is randomly assigned to receive one of the following treatments:

[0124] □ Treatment A (composition known in the art) - single IN dose of 30 mg ketorolac trom...

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PUM

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Abstract

Therapeutic compositions, particularly sprayable aqueous compositions, comprise ketorolac or a pharmaceutically acceptable salt, in combination with a local anesthetic, such as lidocaine hydrochloride. The compositions are nasally administered to a subject in need thereof to treat pain or inflammation and have the benefit of reduced stinging and improved efficacy, compared to known nasally administered compositions.

Description

technical field [0001] The present invention relates to a therapeutic composition having anesthetic and anti-inflammatory activity and suitable for intranasal administration comprising as active ingredients ketorolac or a pharmaceutically acceptable salt thereof and a local anesthetic to reduce stinging sensation and enhance efficacy. The present invention also relates to providing a medical method for nasally administering the composition to a subject for the treatment of pain, wherein the subject has reduced stinging sensation and improved efficacy compared to known compositions. Background technique [0002] Ketorolac or 5-benzoyl-2,3-dihydro-1H-pyrrolazine-1-carboxylic acid having the following formula (I): [0003] [0004] It has been known for many years (US Patent No. 4,089,969) and is used in human therapy as a tromethamine salt with analgesic and anti-inflammatory effects. US Patent No. 4,089,969 is incorporated herein by reference. [0005] The racemic form a...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/407A61P25/06A61K31/167A61P29/00A61K9/08
CPCA61K9/0043A61K31/167A61K31/407A61P25/00A61P25/04A61P25/06A61P29/00A61K2300/00
Inventor 罗杰·怀廷拉马钱德兰·提鲁科特
Owner ROXRO PHARMA INC
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