WO2004067017A1

WO2004067017A1 - Feng-you-jing spray

Info

Publication number: WO2004067017A1
Application number: PCT/CN2003/001089
Authority: WO
Inventors: Chengfei Zhang; Huihong Zhang
Original assignee: Beijing Orientking Pharmaceutical Science & Technology Co., Ltd.
Priority date: 2002-12-31
Filing date: 2003-12-19
Publication date: 2004-08-12
Also published as: AU2003292859A1; CN1424105A

Abstract

The invention relates to a FENG-YOU-JING in form of spray, it consists of liquid medicine and device for spray, the said liquid medicine is formulated by main component FENG-YOU-JING, additive, and medicinal solvent, in which the liquid medicine composes of methol, methyl salicylate, camphor, eucalyptus oil, eugenol, additive, and medicinal solvent, and the device for spray consists of manual pump and bottle, in which the bottle is glass bottle.

Description

Wind olein spray

The invention relates to a medicinal preparation, in particular to a prescription, a preparation process and a spray device of wind olein spray.

Background technique

Fengyoujing is an over-the-counter medicine for traditional Chinese medicine. It is an indispensable medicine for people traveling at home. Especially in summer, Fengyoujing is popular for its good mosquito repellent and anti-inflammatory, analgesic, cool, antipruritic and wind-repellent effects. . At present, liquid wind olein only has one formulation of tincture, and a single formulation brings many inconveniences to people. For example: When people use wind olein as a mosquito repellent in summer, they usually apply wind olein on the body. It is impossible to apply the whole body evenly. Only some parts can be selected. The part is irritating, and the part that is not applied is still vulnerable to mosquito attack. For articles (such as bedding) and space to repel mosquitoes, people usually apply on the articles, or force the wind oil essence to fall on the articles. This has the disadvantages of inconvenience, unevenness, and poor mosquito repellency. Dead corners (such as under the bed) that are inaccessible and easy to hide are even unusable. Fengyoujing is also used to treat abdominal pain orally. Because the bottle mouth of Fengyoujing is very small, it can only be thrown out vigorously when used orally. The use is very inconvenient and the dosage is not accurate. In summary, the inconvenience of using Fengyoujing tincture limits the wider use of Fengyoujing and affects the effectiveness of Fengyoujing in driving mosquitoes.

Summary of the Invention

The invention uses wind oil essence to make a spray, which has the following advantages: 1) When used to repel mosquitoes on human bodies and objects, it can be distributed evenly by spraying a few times easily, and achieves a good mosquito repellent effect. 2) The insect repellent can be sprayed directly into the air, and the insect repellent can be sprayed out of the hand. 3) As oral spray can be used with a fixed-dose manual pump, as long as it is sprayed into the cup according to the dosage, it can be taken by adding water, the dosage is accurate. 4) The solvent used has a wide range of sources and is cheap, and the preparation process used is simple and suitable for industrial production. The above advantages are resolved In view of the shortcomings of Fengyoujing tincture, it also produces unexpected effects such as the treatment of toothache, which is difficult to apply in the mouth, and the spray is easy. For the itching and pain relief on the skin, the spray is more convenient than the application.

The invention is composed of a medicinal solution prepared from the main medicine and auxiliary materials of wind olein and a spray device. According to the present invention, the term "wind olein" refers to the wind olein contained in the ministerial standard. The weight ratio of the main drug is 10-40% menthol, 5-35% methyl salicylate, and camphor 0. 5-5%, eucalyptus oil 0.5-5%, eugenol 0.5-5%, and excipients 5-80%. 01-1% ， pharmaceutically acceptable solvent weight, wherein the excipients include an additive and a pharmaceutically acceptable solvent, and the additive includes a flavoring agent such as a flavor, a weight ratio of 1-20%, and a coloring agent such as chlorophyll, a weight ratio of 0.01-1%, a pharmaceutically acceptable solvent weight The ratio is 3-70%.

The preferred prescription composition of the main medicine is 320 g of menthol, 260 g of methyl salicylate, 30 g of camphor, 30 g of eucalyptus oil, 30 g of eugenol, 100 g of essence, lg of chlorophyll, and the solvent is added to 1000 g.

According to the present invention, the term "> aerosol" refers to a formulation containing no propellant and releasing the contents in the form of a mist or the like by the pressure of a hand pump.

The spray device used in the present invention is composed of a manual pump (also called a valve system) and a bottle body. The valve system may adopt a quantitative valve system or a non-quantitative valve system, preferably a quantitative Gangmen system, such as the quantitative of the German Pfeiffer company (Pfeiffer). Spray pump. The basic composition of the valve system is the basic pump, screw cap, immersion tube, gasket, push button, spray head, integrated atomizer and protective cover. Among them, the immersion tube may not be used, but the spray bottle needs to be inverted when using. 05- 0. 20ml。 Each spray dose of the spray bottle is 0. 02- 0. 3ml, preferably 0. 05-0. 20ml. The bottle used in the present invention is a glass bottle. Plastic spray bottles are usually used for medicinal use. However, during the implementation of the present invention, it was unexpectedly discovered that wind oil essence liquid will be lost after long-term storage in plastic bottles. There is no loss (see the experimental research section), which may be due to the certain volatility of wind oil and the certain permeability of plastic bottles.

The medicinal solution of the present invention is composed of the main drug of wind olein, an additive and a solvent. Viscosity is an important factor affecting spray performance (see Table 1, provided by Taiwan System Spray Co., Ltd.). Increasing viscosity increases the shape of the spray and the size of the droplets becomes larger. Generally, the viscosity of the solution When the degree exceeds a certain range, it cannot be atomized. The patent CN1346298 proves that the fragrance with a viscosity of more than 6.4 centipoise cannot be atomized in its device through an example. The present invention proves that when a manual pump is used, the viscosity is above 55 centipoise. It cannot be atomized. Through in-depth research on the interaction between the main drug of wind olein and solvents with different viscosities, the present invention surprisingly found that: the main drug of wind olein can increase the viscosity of low-viscosity solvents, while for high-viscosity solvents, wind olein The main drug can greatly reduce its viscosity (see the experimental research section), a result that cannot be taught by the prior art. For high-viscosity solvents (such as polyethylene glycol 400, propylene glycol, liquid paraffin, fatty oils, etc.), the solvent itself is laborious to spray (spraying labor makes it difficult for people to use) or cannot be sprayed. Can form a good spray. For low-viscosity solvents (such as ethanol, ethyl acetate, etc.) Although the main ingredient of wind olein increases its viscosity, the increase is small, and the resulting drug solution can still form a very good spray.

Table 1 Factors affecting spray performance

* Increased solid cone and hollow cone; reduced fan spray

** Depends on the fluid being sprayed and the nozzle used

The solvent used in the present invention is selected from one or a mixture of liquid paraffin, ethanol, propylene glycol, ethyl acetate, glycerin, isopropyl myristate, polyethylene glycol, and fatty oils, and preferably liquid Body paraffin, absolute ethanol, polyethylene glycol, isopropyl myristate, and most preferably liquid paraffin. The viscosity of the drug solution prepared by using the solvent in the present invention is 55 centipoise or less, preferably 27 centipoise or less.

The preparation process of the present invention is: take menthol and camphor, add an appropriate amount of solvent, and then add eucalyptus oil, methyl salicylate, eugenol, flavor, and appropriate amount of chlorophyll, add solvent, mix well, leave it for 24 hours, and take a clear solution , Dispensed in a glass spray bottle, tighten the hand pump, that's it.

The following experimental research studies the viscosity of the wind olein solution and the material of the spray bottle.

Experimental research

1.Effect of wind olein solution with different viscosity on spray performance

Viscosity is the property of a liquid and is the resistance of a liquid to changes in the shape or arrangement of its constituents during flow. Liquid viscosity is the main factor that affects the formation of spray shapes, and it is also an important factor that determines the size of droplets. As the viscosity of liquid increases, the particle size of droplets increases. High viscosity liquids require higher lower pressures to form a spray shape and produce a narrow spray angle. For this type of wind oil essence spray sprayed by hand pump, the spray pressure is constant, and the solution with a viscosity exceeding a certain limit may not be able to form a spray, and the solution forming the spray may not have a suitable spray shape and droplets. Size, it is necessary to conduct a viscosity study on the drug solution to find a drug solution with a suitable viscosity for spraying.

[experimental method]

Take menthol and camphor, add an appropriate amount of solvent, and then add eucalyptus oil, methyl salicylate, eugenol, flavor, and chlorophyll, add solvent (see Table 2 for the composition of the drug and the solvent), mix well, and let stand for 24 hours. Take the clarified solution and measure the viscosity with a Vickers viscometer (Yangzhou Hongqi Glass Instrument Factory, Jiangsu) (method is the first method of VIG viscosity measurement method in Appendix of Chinese Pharmacopoeia 2000 Edition 2000), and fill it into a spray bottle (standard spray pump 0 . 10ml thread 18/415 Germany Pfeiffer Company China), screw the hand pump, spray, record the spray index, the results are shown in Table 3.

Table 3 Viscosity and fogging indicators of various solvents and wind oil essences

It can be seen from the above experimental results that solvents or wind olein drug solutions with a viscosity below 27 centipoise can be sprayed better with this spray pump. Within this range, the smaller the viscosity, the smaller the spraying force required, and Above 55 centipoise, it is difficult to spray with a manual pump. 2. Selection of packaging bottles

Each prescription of wind oil essence was packaged in a plastic spray bottle and a glass spray bottle, respectively, and stored at 25 ° C for 6 months. After being placed and placed, they were accurately weighed (Adventure electronic balance, Ohaus), and the chemical liquid was calculated. Amount of loss. The results are shown in Tables 4 and 5.

Table 4 Loss of wind oil essence plastic bottle packaging after 6 months

Table 5 Loss of air olein glass bottle after 6 months of storage Solvent or prescription Weight before storage Weight loss after storage (%)

(g) (g)

Formula 1 10.12 10.01 1.08 Formula 2 10.16 10.23-0.69 Formula 3 10.28 10.09 1.85 Formula 4 9.95 9.97 -0.20 Formula 5 10.54 10.31 2.18 Formula 6 10.23 10.28 -0.49 Formula 7 9.97 9.82 1.50 Formula 8 10.05 9.73 3.18 Formula 9 10.22 10.07 1.47 It can be seen from the above results that the wind oil essence liquid will be lost after long-term storage in plastic bottles, but the weight change of glass oil wind oil essence liquid is small, which may be due to the certain volatility of wind oil essence. The bottle has some air permeability.

The following examples are provided to further illustrate the present invention, but not to limit the scope of the present invention.

Menthol 320 g

Methyl salicylate 260 g

Camphor 30 g

Eucalyptus oil 30 g

Eugenol 30 g

Flavor lOOg

Chlorophyll 1 g

Ethanol to 1000 g

Preparation process: Take menthol and camphor, add an appropriate amount of ethanol, and then add eucalyptus oil, methyl salicylate, eugenol, flavor, and appropriate amount of chlorophyll, add ethanol to 1000g, mix well, leave it for 24 hours, take the clear solution, Dispensed in a glass spray bottle and screwed on the hand pump.

Take this wind oil essence spray for spraying. The spray has a solid cone shape. In the area covered, the droplets are uniformly distributed, round, and the droplets are small.

Example 2

Menthol 320 g

Methyl salicylate 260 g

Camphor 30 g

Eucalyptus oil 30 g

Eugenol 30 g

Flavor lOOg Chlorophyll 1 g

Liquid ballast to 1000 g

Preparation process: Take menthol and camphor, add an appropriate amount of liquid paraffin, and then add eucalyptus oil, methyl salicylate, eugenol, flavor, and appropriate amount of chlorophyll, add liquid stone field to make 1000g, mix well, let stand for 24 hours, and clarify The liquid is dispensed into a glass spray bottle, and the hand pump is tightened, and the liquid is obtained.

Take this wind oil essence spray for spraying. The spray has a solid cone shape. In the area covered, the droplets are distributed uniformly, in a garden shape, and the droplets are small.

Example 3

Menthol 320 g

Methyl salicylate 100 g

Camphor 30 g

Eucalyptus oil 30 g

Eugenol 30 g ''

Flavor lOOg

Chlorophyll 1 g

Ethyl acetate to 1000 g

Preparation process: Take menthol and camphor, add an appropriate amount of ethyl acetate, and then add eucalyptus oil, methyl salicylate, eugenol, flavor, and appropriate amount of chlorophyll, add ethyl acetate to make 1000g, mix well, and let stand for 24 hours. Take the clear solution, dispense it into a glass spray bottle, and tighten the hand pump to get it.

Take this wind oil essence spray for spraying. The spray has a solid shape. In the area covered, the droplets are uniformly distributed, round, and the droplets are small.

Menthol 400 g

Methyl salicylate 50 g

Camphor 30 g 30 g

lOOg

Vegetarian 1 g

Isopropyl myristate to 1000 g

Preparation process: Take menthol and camphor, add an appropriate amount of isopropyl myristate, and then add eucalyptus oil, methyl salicylate, eucalyptus butanol, flavor, and chlorophyll, and add myristic acid iso-green oil.

The propyl ester was made into 1000g, mixed with the hook, and left to stand for 24 hours. The clear solution was taken and dispensed into a glass spray bottle, and the hand pump was tightened to obtain it.

Example 5

Menthol 400 g

Camphor 30 g

Eucalyptus oil 30 g

Eugenol 30 g

Flavor lOOg

(Chlorophyll 1 g

Propylene glycol to 1000 g

Preparation process: Take menthol and camphor, add an appropriate amount of propylene glycol, and then add eucalyptus oil, methyl salicylate, eugenol, flavor, and appropriate amount of chlorophyll, add propylene glycol to 1000g, mix well, leave it for 24 hours, and take a clear solution. Dispensed in a glass spray bottle and screwed on the hand pump.

Take this wind oil essence spray for spraying. The spray has a solid cone shape. In the area covered, the droplets are uniformly distributed, round, and the droplets are small. Example 6 Menthol 320 g

Methyl salicylate 260 g

Camphor 30 g

Eucalyptus oil 30 g

Eugenol 30 g

Flavor 100g

Chlorophyll 1 g

Polyethylene glycol 400 to 1000g

Preparation process: Take menthol and camphor, add an appropriate amount of polyethylene glycol 400, and then add eucalyptus oil, methyl salicylate, eugenol, flavor, and appropriate amount of chlorophyll, add polyethylene glycol 400 to 1000 g, mix well, and mix Set for 24 hours, take the clear solution, dispense it into a glass spray bottle, and tighten the hand pump to get it.

Take this wind oil essence spray for spraying. The spray has a solid cone and a slightly larger spray angle. In the area covered, the droplets are uniformly distributed, round, and the droplets are small.

Example 7

Menthol 320 g

Methyl salicylate 260 g

Camphor 30 g

Eucalyptus oil 30 g

Eugenol 30 g

Flavor lOOg

Chlorophyll 1 g

Add solvent to 1000g

Preparation process: Take menthol and camphor, add an appropriate amount of mixed solvent, then add eucalyptus oil, methyl salicylate, eugenol, flavor, and appropriate amount of chlorophyll, add mixed solvent to make 1000g, mix well, let stand for 24 hours, and clarify The liquid is dispensed into a glass spray bottle, and the hand pump is tightened to obtain it. Note: The mixed solvent is liquid paraffin: isopropyl myristate = 50: 50 Take this wind oil essence spray spray, the spray is a solid cone, the spray angle is slightly larger, in the area of the cover, the droplets are uniformly distributed, showing Round, small droplets.

Claims

Rights request

A medicinal solution prepared by spraying wind oil essence, comprising menthol, methyl salicylate, camphor, eucalyptus oil, eugenol, an additive and a pharmaceutically acceptable solvent.

2. The pharmaceutical composition according to claim 1, wherein the viscosity of the medicinal solution is 55 centipoise or less.

3. The pharmaceutical composition according to claim 1, wherein the weight ratio of the main drug is 10-40% of menthol, 5-35% of methyl salicylate, 0.5-5% of camphor, and 0.5_5% of eucalyptus oil. , Eugenol 0.5-5%, additives and solvents 5-80%.

4. The pharmaceutical composition according to claim 1, wherein the pharmaceutically acceptable solvent is selected from the group consisting of liquid paraffin, anhydrous ethanol, propylene glycol, glycerol, ethyl acetate, isopropyl myristate, polyethylene glycol, and fatty oils. Species or mixtures.

5. The pharmaceutical composition according to claim 1, wherein the pharmaceutically acceptable solvent is liquid paraffin, anhydrous ethanol, polyethylene glycol, isopropyl myristate.

6. The pharmaceutical composition according to claim 1, wherein the pharmaceutically acceptable solvent is liquid paraffin.

7. 'A medicinal spray system comprising a pharmaceutical composition and a spray device as defined in one of claims 1 to 6.

8. The spray system according to claim 7, wherein the spray device is composed of a manual pump and a bottle.

02-0. 3ml。 9. The manual pump according to claim 8, wherein each dose of the drug solution sprayed from the spray device is 0.02-0. 3ml.

10. The bottle body according to claim 8, wherein the bottle is made of glass.