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Capsaicin beta-cyclodectrin inclusion-compound and liposome and gel of inclusion-compound

A technology of cyclodextrin inclusion compound and capsaicin, which is applied in the direction of liposome delivery, non-active ingredients of polymer compounds, drug combination, etc., can solve problems such as flushing, low solubility in water, strong irritation of cream, etc., and achieve The quality is stable and easy to control, the production process is simple, and the effect of improving the skin penetration rate

Inactive Publication Date: 2009-08-19
LOGISTICS UNIV OF CAPF
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] However, the oil-water partition coefficient of capsaicin is too high, resulting in very small solubility in water, which is very unfavorable for human body absorption, so the bioavailability is also very low
And because capsaicin has very strong skin irritation, common capsaicin cream is more irritating, and skin burning sensation, tingling sensation and flushing may occur at the medication site, and continuous medication for more than 3 to 4 days is required to make the patient tolerance
Although liposomes of capsaicin can reduce the irritation of capsaicin, the solubility of capsaicin has little improvement
Therefore, the above-mentioned side effects limit the clinical application of capsaicin to a large extent.

Method used

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  • Capsaicin beta-cyclodectrin inclusion-compound and liposome and gel of inclusion-compound
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  • Capsaicin beta-cyclodectrin inclusion-compound and liposome and gel of inclusion-compound

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1～12

[0030] Preparation and Apparent Solubility Determination of Capsaicin β-Cyclodextrin Inclusion Compound

[0031] Weigh an appropriate amount of β-cyclodextrin according to Table 1, pour it into 100ml of distilled water, stir to dissolve; take another 0.075g of capsaicin, and pour it into the above-mentioned β-cyclodextrin solution; Stir for 4 hours to obtain a solution capsaicin β-cyclodextrin inclusion compound; freeze-dry to obtain a solid capsaicin β-cyclodextrin inclusion compound. Place the prepared capsaicin β-cyclodextrin inclusion compound under the temperature conditions of 25°C, 37°C, and 45°C respectively, add appropriate amount of water, take a sample after equilibrating for 72 hours, filter it with a 0.45 μm microporous membrane, and directly Inject into high-performance liquid chromatograph and analyze, calculate the apparent solubility of capsaicin, the result is as follows figure 1 shown.

[0032] Table 1 The amount of β-cyclodextrin used in Examples 1-12 (%)...

Embodiment 13～15

[0035] Preparation and in vitro release evaluation of capsaicin β-cyclodextrin inclusion complex

[0036] Weigh an appropriate amount of capsaicin and β-cyclodextrin (β-CD) into water, shake in a water bath shaker at a constant temperature (100 cycles / min) at 37°C for 24 hours to obtain capsaicin β-cyclodextrin inclusion compound. Take the dialysis membrane and install it on the Franz diffusion cell, add 7.0mL ethanol-7.4PBS solution into the receiving cell as the receiving solution, keep the temperature at (37±1)°C, add 2mL of capsaicin inclusion compound sample into the supply cell. Samples were taken at 0.5, 1, 1.5, 2, 2.5, 3, 3.5, and 4 hours, and the capsaicin content of the samples was determined by HPLC to calculate the cumulative drug penetration. At the same time, 0.075% capsaicin cream and hydrogel were used as controls. The results showed that the 4-hour cumulative release percentage of the inclusion compound was greater than that of capsaicin cream (30%) and hydro...

Embodiment 16～ Embodiment 27

[0040]Preparation of capsaicin β-cyclodextrin inclusion complex and its gel and evaluation of percutaneous permeability in vitro

[0041] Add capsaicin, β-cyclodextrin and other auxiliary materials weighed according to the amount into water, and shake in a water bath shaker at a constant temperature (100 cycles / min) at 37°C for 24 hours to obtain capsaicin β-cyclodextrin inclusion compound. Another prescribed amount of carbomer is added to the clathrate solution, stirred evenly, then triethanolamine is added, stirred, and left to stand until the carbomer swells completely to obtain capsaicin β-cyclodextrin inclusion compound gel. The isolated mouse skin was installed on the Franz diffusion cell, the receiving solution and the temperature were maintained as above, and 2 mL of capsaicin inclusion compound and capsaicin inclusion compound gel were respectively added to the supply cell. Samples were taken at 2, 4, 6, 7, 8, 9, 10 and 11 hours respectively, and the capsaicin content...

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Abstract

The invention discloses a capsaicin beta-cyclodextrin inclusion compound, as well as liposome and gel thereof. The capsaicin beta-cyclodextrin inclusion compound is prepared by the following method: (1) beta-cyclodextrin is dissolved in an aqueous phase and prepared into a solution, and the solution is added with capsaicin or a capsaicin solution so as to obtain a mixed solution of capsaicin and beta-cyclodextrin; and (2) the solution-type capsaicin beta-cyclodextrin inclusion compound is obtained from the mixed solution prepared in a step (1) through at least one treatment mode of standing, heating, stirring, ultrasound or grinding. The apparent solubility of the capsaicin of the inclusion compound increases by 2 to 20 times. In vitro transdermal study shows that the capsaicin inclusion compound can obviously raise the transdermal rate of medicine by 5 to 20 times as compared with cream and hydrogel, and obviously reduce the irritation of capsaicin at skin. Besides transdermal drug administration, the prepared inclusion compound and the inclusion compound liposome can also be orally taken, injected or administrated in bladders. In addition, the invention is simple in production process, and the quality is stable and easy to control.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to a capsaicin beta-cyclodextrin inclusion compound and liposome and gel of the inclusion compound. Background technique [0002] Capsaicin, also known as capsaicin, is an alkaloid widely present in ripe fruits of peppers. Capsaicin mainly acts on substance P on C-type sensory neurons, and some unmyelinated slow conduction fibers in C-type nerve fibers can conduct skin pain and pathological itching. In response to noxious stimuli, C-type nerve fibers release substance P to cause hypersensitivity. When the local substance P is reduced by the application of drugs, it can prevent the conduction of certain types of pain, itching and other sensations. 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 axonal transport is ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/48A61K47/32A61K47/34A61K47/38A61K47/42A61K9/00A61K9/127A61K31/165A61P29/00A61K47/10A61K47/69
Inventor 张莉李宏树王晓辉申去非袁园王雪超陈莉
Owner LOGISTICS UNIV OF CAPF
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