Capsicine microemulsion and microemulsion gel rubber

A technology of microemulsion gel and capsaicin, applied in the direction of emulsion delivery, organic active ingredients, antipyretics, etc., can solve the problems that limit the clinical application of capsaicin, reduce skin irritation, increase skin penetration rate, The effect of simple production process

Inactive Publication Date: 2008-01-23
LOGISTICS UNIV OF CAPF
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This limits the clinical application of capsaicin to a certain extent

Method used

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  • Capsicine microemulsion and microemulsion gel rubber
  • Capsicine microemulsion and microemulsion gel rubber
  • Capsicine microemulsion and microemulsion gel rubber

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1- Embodiment 6

[0024] Preparation method: Weigh the drug and auxiliary materials according to the amount, mix them, and stir them evenly to obtain the microemulsion. In vitro transdermal evaluation: Male Sprague Dawley rats (body weight 150-300g) were killed by neck dislocation, the abdominal skin was peeled off, the rat hair was cut off with an electric shaver, and the adhesions in the subcutaneous tissue were cut off mechanically, and then wiped with isopropanol. The subcutaneous fat tissue was removed, rinsed with isopropanol with water, soaked in normal saline, and kept frozen until use. Put the mouse skin on the Franz diffusion cell, with the outer side of the mouse skin facing the supply pool, add 7.0 mL of ethanol-7.4PBS solution in the receiving pool as the receiving solution, keep the temperature at (37±1) °C, add pepper containing Alkaline microemulsion sample 2mL (or g). Samples were taken at 2, 3, 4, 6, 8, 10 and 12 hours respectively, and all receiving media were replaced. Afte...

Embodiment 7- Embodiment 12

[0028] Table 2

[0029]

[0030] Preparation method: the method of embodiment 7~embodiment 10 is the same as embodiment 1. The preparation method of Examples 11 to 12 is as follows: first weigh the prescribed amount of hydroxypropylmethylcellulose or carbomer, add propylene glycol, stir evenly, slowly add water to the full amount under stirring, soak until the hydroxypropylmethylcellulose Or the carbomer swells completely and evenly, then add other drugs and excipients in the prescription, and stir evenly. This preparation method can accelerate the swelling of the polymer material, and compared with the preparation of the microemulsion first and then the preparation of the gel, there is no difference in the final product. The in vitro transdermal evaluation method is the same as in Example 1-Example 6.

Embodiment 13- Embodiment 27

[0031] Embodiment 13-Example 27 see Table 3

[0032] Table 3 (unit: g)

[0033]

[0034] (Continued from previous page)

[0035] propanol

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Abstract

The invention discloses a capsicine microemulsion and microemulsion gelatin. The capsicine microemulsion is prepared with the following methods: (1) according to quality percentage, measure: 0.001 per cent to 5 per cent of capsicine, 1 per cent to 90 per cent of oil phase, 0 to 80 per cent of surfactant, 1 per cent to 90 per cent of cosurfactant, 1 per cent to 90 per cent of water pahse and 0 to 40 per cent of energizer; (2) mix the components evenly, or mix them with a mixer, or emulsify them with an emulsifying machine, or grind them with a colloid mill. Compared with capsicine cream and hydrogel, the microemulsion in the invention can outstanding improve the drug skin penetration rate by 2 to 6 times, effectively reduce the capsicine's pungency to skin and can be administrated via skin penetration, oral taking, injection or intravesical medication with simple production process, stable and controllable quality.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to a microemulsion and a microemulsion gel preparation. Background technique [0002] Capsaicin, also known as capsaicin, is an alkaloid widely present in the ripe fruits of peppers. Capsaicin may mainly act on substance P on C sensory neurons, and some unmyelinated slow conduction fibers in C-type nerve fibers can conduct skin pain and pathological itching. Hyperesthesia due to the release of substance P in response to noxious stimuli can prevent some types of pain sensation when drugs are used to reduce local substance P. The non-central analgesic effect of topical capsaicin is due to the action of capsaicin on peripheral nerve axons, resulting in the elimination of small sensory neurons and their terminal substance P, initially blocked by axonal transport, and subsequently decreased substance P synthesis, Similar to the effect of resection or ligation of nerves, but doe...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K31/136A61P29/00
Inventor 张莉张鹏威齐刚陈莉李丽高翔石峰魏平平
Owner LOGISTICS UNIV OF CAPF
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