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Pharmaceutical composition, patch, and preparation methods and application of pharmaceutical composition and patch

A composition and drug technology, applied in the direction of drug combination, pharmaceutical formula, heterocyclic compound active ingredients, etc., can solve the problem of not being able to achieve long-term continuous analgesic effect, and achieve good safety effect

Pending Publication Date: 2019-07-23
张洁
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The technical problem to be solved by the present invention is to overcome the common limitation of local anesthetic preparations in the prior art that they cannot achieve long-term continuous analgesic effect, and provide a pharmaceutical composition, patch and preparation method thereof, application

Method used

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  • Pharmaceutical composition, patch, and preparation methods and application of pharmaceutical composition and patch
  • Pharmaceutical composition, patch, and preparation methods and application of pharmaceutical composition and patch
  • Pharmaceutical composition, patch, and preparation methods and application of pharmaceutical composition and patch

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0076] A kind of raw material composition of pharmaceutical composition, its composition is as shown in the following table:

[0077] Element mass percentage / % Lidocaine 4 Pemulen TR-2 0.24 sodium hydroxide 0.13 water Top up to 100

[0078] The preparation method of the pharmaceutical composition is as follows:

[0079] Sodium hydroxide and suspending agent Carbomer Pemulen TR-2 are added to water and stirred until a homogeneous viscous liquid is obtained. Then, add lidocaine crystals, heat to 80° C., stir rapidly, and cool to room temperature to obtain the product.

[0080] Effect data: the obtained pharmaceutical composition is recorded as formula A, and the obtained pharmaceutical composition is a viscous solution containing dissolved lidocaine and undissolved lidocaine, wherein the undissolved lidocaine exists in the form of suspended crystals In a viscous solution; the pH of the resulting pharmaceutical composition is greater tha...

Embodiment 2

[0082] A kind of raw material composition of pharmaceutical composition, its composition is as shown in the following table:

[0083] Element mass percentage / % Lidocaine 5 Pemulen TR-2 0.24 sodium hydroxide 0.13 starch 0.3 water Top up to 100

[0084] The preparation method of the pharmaceutical composition is as follows:

[0085] Sodium hydroxide and suspending agent Carbomer Pemulen TR-2 are added to water and stirred until a homogeneous viscous liquid is obtained. Then, add lidocaine crystals and starch, heat to 80° C., stir rapidly, and cool to room temperature to obtain the product.

[0086]Effect data: the obtained pharmaceutical composition is recorded as formula B, and the obtained pharmaceutical composition is a viscous solution containing dissolved lidocaine and undissolved lidocaine, wherein the undissolved lidocaine exists in the form of suspended crystals In a viscous solution; the pH of the resulting pharmaceutical...

Embodiment 3

[0088] A kind of raw material composition of pharmaceutical composition, its composition is as shown in the following table:

[0089] Element mass percentage / % Lidocaine 5 Pemulen TR-2 0.25 sodium hydroxide 0.14 starch 0.3 glycerin 15 water Top up to 100

[0090] The preparation method of the pharmaceutical composition is as follows:

[0091] Sodium hydroxide and suspending agent Carbomer Pemulen TR-2 are added to water and stirred until a homogeneous viscous liquid is obtained. Then, add lidocaine crystals, starch and glycerin, heat to 80° C., stir rapidly, and cool to room temperature to obtain the product.

[0092] Effect data: the obtained pharmaceutical composition is recorded as formula C, and the obtained pharmaceutical composition is a viscous solution containing dissolved lidocaine and undissolved lidocaine, wherein the undissolved lidocaine exists in the form of suspended crystals viscous solution; the resulting ...

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Abstract

The invention discloses a pharmaceutical composition, a patch, and preparation methods and application of the pharmaceutical composition and the patch. The pharmaceutical composition comprises a simplex anesthetic active ingredient, wherein the anesthetic active ingredient is composed of anesthetic active components dissolved in water and anesthetic active components in undissolved state; mass percentage of the anesthetic active ingredient in the pharmaceutical composition is higher than 2%; mass percentage of the anesthetic active components dissolved in water in the pharmaceutical composition is lower than 1%; and the anesthetic active ingredient is selected from lidocaine, tetracaine, bupivacaine, atecaine, cincocaine, dibucaine, eticaine, levobupivacaine, mepivacaine, propivacaine, ropivacaine, trimethylcaine, benzocaine or procaine. The pharmaceutical composition and the patch are capable of achieving continuous analgesic effects for 12-30 hours; moreover, the patch is capable ofresisting certain external pressing force so as to protect the covered formula layers from being squeezed out, thereby maintaining thickness of the formula layers.

Description

technical field [0001] The invention relates to a pharmaceutical composition, a patch and a preparation method and application thereof. Background technique [0002] Local anesthetic preparations are used to prevent or treat pain on the skin or mucous membranes, for example: 2% lidocaine hydrochloride gel is used to relieve pain associated with sunburn; An emulsion of low-point co-incorporating oil droplets with prilocaine, which is used for anesthesia of intact skin before surgery with pain; Lidoderm, a curing gel patch containing 5% lidocaine, which is used to relieve band Postherpetic neuralgia (the skin itself is intact); Pliaglis is an emulsion containing 7% lidocaine and 7% tetracaine in the form of low-point co-integrating oil drops for painful preoperative intact skin of anesthesia. However, each of the above local anesthetics has serious limitations. For example: lidocaine hydrochloride gel does not anesthetize intact skin; prilocaine in EMLA can cause methemoglo...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K45/00A61K9/70A61K47/36A61K47/32A61K47/38A61K47/10A61P31/22A61P29/00A61P25/00A61P35/00A61P3/10A61P25/02A61P19/02A61P19/08A61P19/06A61P17/04A61P17/02
CPCA61K45/00A61K9/7023A61K47/36A61K47/32A61K47/38A61K47/10A61K9/70A61P17/02A61P19/02A61P3/10A61P35/00A61P17/04A61P19/08A61P19/06A61P29/00A61P31/22A61P25/02A61P25/00A61K31/167A61K31/245A61K31/445A61P23/02A61K9/703A61K47/02A61K31/381A61K31/47A61K31/4418A61K47/14A61K47/34
Inventor 张洁
Owner 张洁
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