WO2013044736A1

WO2013044736A1 - Traditional chinese medicine composition for external use in treating xerophthalmia and the preparation method thereof

Info

Publication number: WO2013044736A1
Application number: PCT/CN2012/081389
Authority: WO
Inventors: 金明
Original assignee: Jin Ming
Priority date: 2011-09-27
Filing date: 2012-09-14
Publication date: 2013-04-04
Also published as: CN102357196A; CN102357196B

Abstract

Traditional Chinese medicine composition for external use in treating xerophthalmia and preparation method thereof, wherein the raw material of the traditional Chinese medicine composition consists of Radix Scutellariae, Herba Menthae, Radix Trichosanthis, Flos Chrysanthemi, Rhizoma Polygonati and Broneolum Syntheticum.

Description

Traditional Chinese medicine composition for external treatment of dry eye syndrome and preparation method thereof

Technical field

The invention relates to a pharmaceutical composition and a preparation method thereof, in particular to a traditional Chinese medicine composition for external treatment of dry eye and a preparation method thereof.

Background technique

With the acceleration of social development and the pace of life, occupational diseases represented by dry eye have become common diseases, frequently-occurring diseases, and refractory diseases in ophthalmology. The survey shows that the United States accounted for 13.3% between 43 and 84 years old, 17.0% in Japan, 28.7% in Canada and 10.3% in Australia. The causes of dry eye syndrome are numerous and the pathological process is complicated. It is a common eye disease in ophthalmology. The tear secretion is obviously reduced or the tear component is abnormal. The tear film rupture time is shortened, the corneal epithelium is detached, and fluorescein staining is positive. Since the tear film can no longer afford its barrier, immune regulation and mechanical removal of debris and antimicrobial effects, the sensory nerve-rich cornea is directly exposed to the outside world, plus viscous debris deposited in the conjunctival ridge and the filamentous cornea Exfoliation of the epithelium leads to a series of clinical symptoms. The most common symptoms are eye fatigue, foreign body sensation, dryness, burning sensation, long-sightedness, eyesight, photophobia, and redness.

The causes of dry eye syndrome are extremely complicated, people's living and working environment are improved, and the popularity of air conditioners and computers is increasing. The incidence of dry eye syndrome is significantly higher than before. There is information that the incidence of dry eye is increased by 10% per year due to the emergence of computers. There are more and more patients in the clinic due to "eye discomfort", and a large part of them may be dry eye syndrome. However, as a general inflammatory treatment during treatment, the patient's symptoms have not completely disappeared or improved, and even worsened, which will lead to serious ocular surface diseases, including complications such as corneal surface abrasion stellate keratitis and corneal ulcer, and eventually lead to corneal opacity and The serious consequences of vision loss.

At present, the measures for prevention and treatment of dry eye are relatively limited. In the light, the artificial tears are relieved for a long time, but the preservative has a detrimental effect on the tear film; the moderate person can wear a silicone eye mask, a wet room mirror, a goggle, and therapeutic. Contact lens or implanted small puncture embolus to maintain the retention of tears in the eye; severe cases of eyelid suture to prevent the occurrence of complication such as corneal degeneration. In short, although there are many treatment methods, but there are many drawbacks. The efficacy is not certain, and the problem of the patient's own tear quality and quantity cannot be fundamentally improved.

Summary of the invention

It is an object of the present invention to disclose a traditional Chinese medicine composition for external use for treating dry eye.

Another object of the present invention is to disclose a method for preparing a traditional Chinese medicine composition for external use for treating dry eye.

The object of the present invention is achieved by the following technical solutions:

The composition of the drug substance of the pharmaceutical composition of the present invention is:

Astragalus 5-50 parts by weight Mint 3-45 parts by weight Trichosanthin 5-50 parts by weight Chrysanthemum 1-40 parts by weight Yellow essence 3-45 parts by weight Boring piece 0.1-5 parts by weight. The drug substance composition of the pharmaceutical composition of the present invention is preferably:

Astragalus 10-40 parts by weight Mint 5-35 parts by weight Trichosanthin 10-40 parts by weight Chrysanthemum 5-30 parts by weight Yellow essence 5-35 parts by weight Boring piece 0.5-3 parts by weight. The drug substance composition of the pharmaceutical composition of the present invention is preferably:

Astragalus 15-30 parts by weight Mint 10-25 parts by weight Trichosanthin 15-30 parts by weight Chrysanthemum 7-20 parts by weight Yellow essence 10-25 parts by weight Boring piece 0.7-1.5 parts by weight The drug substance composition of the pharmaceutical composition of the present invention is preferably:

Astragalus 20 parts by weight Mint 15 parts by weight Trichosanthin 20 parts by weight

Chrysanthemum 10 parts by weight Huang Jing 15 parts by weight Boron 1 part by weight

The preparation method of the above pharmaceutical composition of the present invention is as follows: taking astragalus, mint, trichosanthin, huangjing, chrysanthemum, adding 2-8 times (weight times) water for 1 to 4 times, each time for 30 to 150 minutes, combining the extracts, After filtration, the filtrate is concentrated to a clear paste having a relative density of 1.05 to 1.35, and the borneol and the clear paste are mixed, and a conventional excipient is added to prepare a clinically accepted dosage form.

The above dosage forms may be in the form of tablets, pills, granules, effervescent agents and the like.

The composition preparation of the present invention is preferably administered by atomization by an ultrasonic atomizing device in clinical use.

When the preparation of the composition of the invention is used clinically, the medicine is dissolved in hot water of 80-100 degrees Celsius, Dissolve the vapors that are emitted to fumigate the eye.

The preparation of the composition of the invention can be atomized and administered by connecting an ultrasonic atomizing device, and the preparation of the composition of the invention is placed in a container of the ultrasonic atomizer, and the medicine is atomized by the action of ultrasonic waves to form atomized molecules. Introduced into the ocular surface via a soft rubber tube.

The invention also provides a wet compress comprising the above composition, the preparation method of the wet compress is as follows: taking astragalus, mint, trichosanthin, huangjing, chrysanthemum, adding 2-8 times (weight times) water to extract 1 ~ 4 times Each time 30 ~ 150 minutes, the extracts were combined, filtered, and the filtrate was concentrated to a clear density of 1.05 ~ 1.35. The borneol and the clear paste were mixed, mixed thoroughly, and then added with 40%-80% ethanol for 24 hours to precipitate. The ethanol is then recovered to an alcohol-free taste, and after refrigerated, it is placed in a non-woven carrier.

The traditional Chinese medicine composition has significant improvement effects in prolonging tear film breakage time, increasing tear flow, improving corneal staining, and improving conjunctival hyperemia. Treatment of dry eye syndrome: The statistical cure rate is 8.33%, the effective rate is 50.69%, the effective rate is 38.89%, the inefficiency is 2.09%, and the total effective rate is 97.91%. The traditional Chinese medicine composition has good effect for treating dry eye syndrome. effect.

Experimental example 1 clinical experimental data

1, data and methods

1.1 General Information 144 cases were outpatients, 70 males and 84 females; aged 23-81 years, mean age (45.6 ± 8.2) years.

1.2 Diagnostic criteria This time, the standard developed by Professor Zhang Hancheng of China in 1987 [2], the traditional three examination methods include Schirmer I test, BUT measurement and corneal fluorescence staining.

1.3 diagnosis method:

1. 3. 1 Tear secretion test (Schirmer): Measure the amount of tear base production. In the absence of surface anesthesia, place the Schirmer test paper (), one end folded in the middle and outer 1/3 of the lower jaw, drooping along the rim, and remove the filter paper after 5 minutes to measure the length of the tear soaked test paper. For example, < 5mm/5min is strongly positive ( ++ ), < 10mm/5min is positive ( + ).

1. 3. 2 tear film break time (BUT): Respond to the stability of the tear film. Using a glass rod, fluorescein sodium was applied to the lower eyelid of the patient, and the patient was closed. The time between the opening of the eye and the appearance of the first dark spot on the surface of the cornea was observed under a slit lamp, which is the BUT. < 10s is positive ( + ). 1. 3. 3 corneal fluorescein staining: reaction corneal epithelial defect. No staining is 0 points, each quadrant is divided into light, medium and heavy grades, so a total of 0 ~ 12 points, it is generally considered that <1 is normal.

1.4 Symptom score: The diagnosis of dry eye depends on subjective symptoms in the absence of signs:

According to the 2004 National Symposium on Diagnosis and Treatment of Dry Eyes, the criteria are as follows: asymptomatic score is 0, symptomatic frequency is <3 times/week, and after relaxation, it can be relieved to 1 point, between 1 and 5 points. For 2 ~ 4 points, symptoms often appear, affecting quality of life and work, medication can be relieved to 5 points, symptoms appear between 5 ~ 9 points for 6 ~ 8 points, continue to appear, seriously affecting quality of life, medication can not alleviate It is 9 points.

Efficacy was determined according to the scoring method: efficacy index (η) = [ ' total score before treatment - total score after treatment) 总 total score before treatment] X 100%. η>70% is markedly effective; 70%>η>30% is effective; η<30% is invalid; η<0 is force weight.

1.5 treatment methods

1.5.1 Chinese medicine preparation

Recipe: Astragalus 20g, Mint 15g, Trichosanthin 20g, Chrysanthemum 10g, Polygonatum 15g, Borneol lg; The above formula is added with water (conventional water) for 2 times, combined with decoction, added with borneol, and the drug is concentrated to 100 ml.

1.5.2 How to use

Each time, 1.15 Chinese herbal decoction 20ml is placed in the ultrasonic low-temperature atomizer container, and connected with an atomizing tube. The ultrasonic wave is used to form the atomized molecules directly to the eye, and the low-temperature cold fog cold smoke temperature is low. The air temperature around the eyelid is about 3 ° C ~ 5 ° C, controlled at 8 ° C ~ 17 ° C. The range and magnitude of this control are measured by thermometer test observations. The patient opened the eye for treatment, the spray mouth was about 2 ~ 3cm away from the eyes, and the atomization amount was maintained at 2ml/min or more, 20min each time, once a day, 7 times for one course of treatment, and the therapeutic effect was measured after one course of treatment.

1.6 statistical methods

Statistical analysis was performed using SPSS 17.0 statistical software. The difference was significant at P < 0.05.

2. Results

2.1 overall efficacy results It can be seen from Table 1 that the cure rate of dry eye patients is 8.33%, the effective rate is 50.69%, the effective rate is 38.89%, the inefficiency is 2.09%, and the total effective rate is 97.91%.

Table 1 Results of symptoms and signs before and after treatment

Case number Recovery (%) Effective (%) Effective (%) Invalid (%) Total efficiency (%)

144 12 (8.33) 73 ( 50.69 ) 56 (38.89) 3 (2.09) 97.91%

2.2 Comparison of symptoms and signs before and after treatment

As can be seen from Table 2, the subjective symptoms and physical signs scores were significantly different before and after treatment (P < 0.05).

Table 2 Comparison of symptoms and signs before and after treatment

Points

Pre-treatment P value after treatment

Total scores of symptoms and signs 13.12±2.81 3.78±1.70 <0.05

2.3 Comparison of various indicators before and after treatment

It can be seen from Table 3 that the traditional Chinese medicine composition has statistical differences in prolonging tear film breakage time, increasing tear flow rate, and improving corneal staining.

Table 3 Comparison of indicators before and after treatment (x±S)

Tear film rupture time tear river height tear secretion test - 角 corneal staining

(S) (mm) (mm/5min) (minutes) before treatment 3.88±1.72 0.13±0.094 5.23±2.65 6.6±2.09 After treatment 4.42±1.61 0.14±0.095 7.10±3.05 3.62±1.90

P value <0.05 <0.05 <0.05 <0.05

2.4 The comparison of subjective symptoms before and after treatment is as follows:

Table 4 Symptom comparison before and after treatment

Before treatment

Significantly

Heavy mouth

Cognac 68 (97.1%) 36 ( 52.9% ) 13 ( 19.1% ) 18 (26.5%)

1 ( 1.5%)

Visual fatigue 61 (87.1%) 12 ( 19.8%) 11 ( 18.0%) 38 ( 62.2% ) 0

(0)

Foreign body sensation 55 (78.6%) 17 (30.9%) 13 (23.6%) 25 (45.5%) 0

(0) Visual blur 43 (61.4%) 12 (27.9%) 12 (27.9%) 19 (44.2%) 0

(0)

Photophobia 43 (61.4%) 10 (23.3%) 12 (27.8%) 21 (48.8%) 0

(0)

Eye red 35 ( 50.0% ) 9 (25.7%) 7 ( 20.0% ) 19 (54.3%) 0

(0)

Pain 33 (47.1%) 9 (27.3%) 8 (24.2%) 15 (45.5%) 1

(3.0%)

Tears 24 ( 34.3% ) 6 (25.0%) 7 ( 29.2% ) 11 (45.8%) 0

(0)

Burning sensation 8 ( 22.9% ) 4 ( 50.0% ) 3 ( 37.5% ) 1 ( 12.5% ) 0

(0)

2.5 The improvement of conjunctival hyperemia before and after treatment is as follows:

Table 5: Improvement of conjunctival hyperemia before and after treatment Before treatment After treatment Before treatment After treatment Before treatment After treatment

Degree of congestion ( + + + ) 〉〉 ( + + ) ( + + ) »( + ) ( + ) »

( - )

Number of cases 40 81 23 Percent 27.78 % 56.25 % 15.97%

3. Conclusion

The traditional Chinese medicine composition has significant improvement effects in prolonging tear film breakage time, increasing tear flow, improving corneal staining, and improving conjunctival hyperemia. Treatment of dry eye syndrome: The statistical cure rate is 8.33%, the effective rate is 50.69%, the effective rate is 38.89%, the inefficiency is 2.09%, and the total effective rate is 97.91%; indicating that the traditional Chinese medicine composition has good treatment for dry eye syndrome. The role.

The effects of the above experimental examples can be achieved by the following examples.

DETAILED DESCRIPTION OF THE INVENTION Example 1:

Take Astragalus 20g, Mint 15g, Trichosanthin 20g, Chrysanthemum 10g, Polygonatum 15g, add 5 times the amount of water for 3 times, each time for 90 minutes, combine the extracts, filter, combine the filtrate, reserve, take borneol lg, borneol and filtrate mixing. Example 2:

Take Astragalus 40g, 10g of mint, 10g of trichosanthin, 30g of Polygonatum, 20g of chrysanthemum, respectively, remove, wash, dry, add 6 times (weight) water extraction 3 times, each time 120 minutes, combine the extract, filter, take The filtrate was concentrated to a clear density of 1.15. The borneol 3g and the clearing paste were mixed, and the tablet was added to a conventional excipient to prepare a tablet. When used, the tablet was fumigated with hot water to dissolve the steam.

Example 3:

Take Astragalus 38g, Peppermint 8g, Trichosanthes 15g, Polygonatum 35g, Chrysanthemum 18g for impurity removal, washing, drying, add 6 times (weight) water extraction 4 times, each time 60 minutes, combine the extract, filter, take The filtrate was concentrated to a clear paste having a relative density of 1.30, 4 g of borneol and a clear paste were mixed, and a conventional excipient of the pellet was added to prepare a pellet, and the pellet was administered by steam fumigation with hot water.

Example 4:

Take Astragalus 25g, Mint 8g, Trichosanthin 15g, Polygonatum 30g, Chrysanthemum 18g for impurity removal, washing, drying, add 5 times (weight) water extraction 3 times, each time 120 minutes, combine the extract, filter, take The filtrate was concentrated to a clear density of 1.3, the borneol 2g and the clear paste were mixed, thoroughly mixed and added to 45% ethanol for 24 hours. After the precipitation, the ethanol was recovered to an alcohol-free taste, and after 24 hours of refrigeration, it was placed in a non-woven carrier. , made into a wet compress.

Example 5

Take Astragalus 20g, Peppermint 7g, Trichosanthin 20g, Polygonatum 30g, Chrysanthemum 35g for impurity removal, washing, drying, add 7 times (weight) water extraction 4 times, each time 90 minutes, combine the extract, filter, take The filtrate was concentrated to a clear paste having a relative density of 1.32. The borneol 3g and the clear paste were mixed, and the granule conventional excipient was added to prepare a granule. When used, the granules were fumigated with hot water dissolved steam.

Claims

Claim

A traditional Chinese medicine composition for external use for treating dry eye, characterized in that the raw material composition of the traditional Chinese medicine composition is:

Astragalus 5-50 parts by weight Mint 3-45 parts by weight Trichosanthin 5-50 parts by weight Chrysanthemum 1-40 parts by weight Yellow essence 3-45 parts by weight Boring piece 0.1-5 parts by weight.

2. The traditional Chinese medicine composition according to claim 1, wherein the raw material composition of the traditional Chinese medicine composition is:

Astragalus 10-40 parts by weight Mint 5-35 parts by weight Trichosanthin 10-40 parts by weight Chrysanthemum 5-30 parts by weight Yellow essence 5-35 parts by weight Boring piece 0.5-3 parts by weight.

3. The traditional Chinese medicine composition according to claim 1, wherein the raw material composition of the traditional Chinese medicine composition is:

Astragalus 15-30 parts by weight Mint 10-25 parts by weight Trichosanthin 15-30 parts by weight Chrysanthemum 7-20 parts by weight Yellow essence 10-25 parts by weight Boring piece 0.7-1.5 parts by weight.

4. The traditional Chinese medicine composition according to claim 1, wherein the raw material composition of the traditional Chinese medicine composition is:

Chrysanthemum 10 parts by weight Huang Jing 15 parts by weight Boron 1 part by weight.

The method for preparing a traditional Chinese medicine composition according to any one of claims 1 to 4, wherein the method comprises: taking astragalus, mint, trichosanthin, huangjing, chrysanthemum, and adding 2 to 8 times by weight of water to extract 1 to 4 Then, each time 30 ~ 150 minutes, the extracts were combined, filtered, and the filtrate was concentrated to a clear density of 1.05 ~ 1.35. The borneol and the clear paste were mixed, and the conventional excipients were added to make a clinically accepted dosage form.

6. Use of a traditional Chinese medicine composition according to any one of claims 1 to 4 for the preparation of a medicament for the treatment of dry eye by external administration.

7. The use of a traditional Chinese medicine composition according to claim 6 for the preparation of a medicament for treating dry eye by atomization.