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Water-free pharmaceutical compositions suitable for local anaesthetics

A technology for local anesthetics and compositions, applied in the field of anhydrous pharmaceutical compositions, can solve problems such as not mentioned, and achieve the effect of simplifying the sterilization process

Inactive Publication Date: 2013-01-23
PHARMANEST AB
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] Although it may be useful to use the composition in question as a drug delivery system for a local anesthetic in alkaline form effective for topical application, the above-mentioned document does not mention how to obtain such a formulation, either Appropriate adhesion to safely exert appropriate anesthesia while also being conveniently administered by traditional invasive means suitable for administering the formulation to internal body sites

Method used

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  • Water-free pharmaceutical compositions suitable for local anaesthetics
  • Water-free pharmaceutical compositions suitable for local anaesthetics
  • Water-free pharmaceutical compositions suitable for local anaesthetics

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Example 1. Methods of Manufacturing and Evaluating Lipid-Based Local Anesthetic-Containing Formulations

[0035] The following procedure was used to prepare lipid formulations containing ropivacaine and lidocaine for in vitro testing in batch sizes of 20-200 g.

[0036] Weigh out the desired amount of local anesthetic in a 250ml (1000ml) round bottom flask. Absolute ethanol is added in an amount of approximately 20-25 ml for each gram of local anesthetic. The mixture was treated with an ultrasonic water bath set at 50-65° C., depending on the solid fat content of the lipid used, until a clear liquid was obtained. This usually completes within a few minutes. The lipid components (see below) are then added and the resulting mixture is subjected to an ultrasonic water bath until a clear homogeneous liquid is obtained.

[0037] The alcohol was evaporated on a rotary evaporator at a pressure of about 25 mbar and a temperature of about 40-60° C. until the weight of the f...

Embodiment 2

[0071] Example 2. In Vitro Release of Local Anesthetics from Pharmaceutical Compositions

[0072] The release of lidocaine from the pharmaceutical composition containing 5% lidocaine prepared according to Example 1 was measured twice.

[0073] result in figure 1 shown in . A stable release of lidocaine from different drug formulations can be observed.

Embodiment 3

[0074] Example 3. Evaluation of Appearance at 37°C

[0075] A pharmaceutical composition containing 5% lidocaine or 5% ropivacaine was prepared according to Example 1. Examples of stabilizing compositions are shown in Table 4. After the preparation was completed, the formulation was equilibrated in a constant temperature water bath at 37°C.

[0076] Table 4. Appearance at 37°C and ejectability at room temperature (approximately 25°C) of stable lipid-based formulations containing lidocaine and ropivacaine

[0077]

[0078]

[0079]

[0080]

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Abstract

The present invention relates to a water-free pharmaceutical composition comprising one or more local anaesthetics in base form and which is suitable for topical administration. The composition further comprises a lipid vehicle comprising long-chain triglycerides (LCT) and at least 10 % by weight of medium-chain monoglycerides (MCM) selected so the composition has an at least semi-solid appearance at the body temperature at the site of administration. The invention further relates to methods of producing and sterilizing the compositions.

Description

technical field [0001] The present invention relates to anhydrous pharmaceutical compositions comprising a local anesthetic and a lipid carrier for topical administration. The pharmaceutical composition can be used to reduce pain associated with many clinical conditions and clinical procedures. Background technique [0002] Local anesthetics are commonly used to suppress nociceptive pain and are usually administered by local injection. Pharmaceutical compositions for local injection generally include a local anesthetic at a concentration of 1%-2%. [0003] In preparing pharmaceutical compositions for topical administration, it is preferred to have the local anesthetic present in relatively high concentrations, for example at a concentration of 5% or higher. [0004] Amide local anesthetic, ATC code N01BB, is pK a A weak base of about 8. Thus, in aqueous solutions at neutral pH, these local anesthetics exist primarily in their acidic forms. However, the acidic form is ch...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/06A61K47/14A61K31/445A61K31/167
CPCA61K47/14A61K31/167A61K31/445A61K9/0014
Inventor M·松德贝里A·布罗丁A·卡尔松
Owner PHARMANEST AB
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