Bioadhesive compositions of local anaesthetics

A technology for local anesthetics and bioadhesion, which is used in anesthetics, drug combinations, active ingredients of heterocyclic compounds, etc.

Inactive Publication Date: 2013-01-09
PHARMANEST AB
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, none of these applications gives any indications for local anesthetic compositions of long-acting anesthetics that are also particularly effective at in vivo locations (with many special requirements regarding administration, sterility, stability, safety and efficacy). specific guidance

Method used

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  • Bioadhesive compositions of local anaesthetics
  • Bioadhesive compositions of local anaesthetics
  • Bioadhesive compositions of local anaesthetics

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0095] Example 1. Formulations using a lyotropic phase

[0096] Preliminary tests were performed on the lyotropic phase system in Table 2 to determine the feasibility of this approach. Research has found that by mixing glyceryl monoolein (GMO), oleic acid and water, a gel (very similar to a cubic phase) is formed. In the prepared formulation, ropivacaine was mixed with GMO, oleic acid and water to form a white gel.

[0097] Table 2. Initial testing of lyotropic phase systems.

[0098] Addition of water refers to the addition of NaOH (aqueous solution) to adjust the pH of the composition containing the local anesthetic to 8.5.

[0099]

Embodiment 2

[0100] Example 2. Formulations containing GMOs and oleic acid

[0101] The different excipients in the composition are related to the amount of ropivacaine in the formulation. In Table 3, formulations containing different concentrations of ropivacaine are listed. The table is categorized by the concentration of increased ropivacaine in the formulation. The different combinations of these components result in a gel-like formulation in which ropivacaine is dissolved. The phase properties of the formulations were investigated using crossed-polarizers to distinguish between lamellar and cubic phases in colloidal formulations.

[0102] Table 3A. Ropivacaine, Lipids – GMO, Organic Acids – Oleic Acid

[0103] Studying formulations that gel in situ

[0104]

[0105]

[0106] It should be noted that pH has a significant effect on the viscosity of the formulation, with higher pH closer to pH 9 increasing the viscosity. Both the pH of the formulation and the amount of wate...

Embodiment 3

[0110] Example 3. Formulations in which GMOs were replaced with other lipids

[0111] The GMOs in the prepared formulations were replaced by technical grade GMOs and other lipids as listed below. The different excipients in the composition are related to the amount of ropivacaine in the formulation. The contents of the prepared formulations are listed in Tables 4-6. All investigated lipids could form gel formulations with lamellar and cubic phase structures. Since all lipids used in this study can form gels, this allows flexibility in the choice of components used in the formulation.

[0112] Table 4. Ropivacaine, lipids – technical grade GMO, organic acid – oleic acid

[0113] Studying formulations that gel in situ

[0114]

[0115] GDOs are co-used with different brands of GMOs in Tables 5 and 6:

[0116] GMO-Monoolein (Rylo MG19, min 96% monoglycerides, max 4% diglycerides)

[0117] GDO-Glyceryl Dioleate (Rylo MG19Pharma, min 94% diglycerides, max 1% monoglycerid...

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Abstract

The present invention relates to a gelling bioadhesive pharmaceutical composition comprising one or more local anaesthetics in base form and which is suitable for topical administration. The compositions have anisotropic organic phase behaviour that admits swelling at administration site with excess water.

Description

technical field [0001] The present invention relates to novel long-acting pharmaceutical compositions for topical administration containing local anesthetics. The pharmaceutical composition can be used to reduce pain associated with clinical symptoms 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 contain a local anesthetic at a concentration of 1%-2%. [0003] In preparing pharmaceutical compositions for topical administration, it is preferred that the local anesthetic is present in relatively high concentrations. [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 charged and therefore less suitable for crossing biological membranes....

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/06A61K9/00A61K31/445
CPCA61L2/0023A61K47/44A61K9/0024A61K31/167A61K47/26A61K31/445A61K31/245A61K9/06A61K47/14A61P23/02A61K47/30
Inventor M·松德贝里A·布罗丁J·古斯塔夫松
Owner PHARMANEST AB
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