CN108785383B

CN108785383B - Antibacterial gynecological external medicine composition and preparation method and application thereof

Info

Publication number: CN108785383B
Application number: CN201810973297.8A
Authority: CN
Inventors: 李晓; 胡亮亮
Original assignee: Hubei Xiangruifeng Yew Technology Co ltd
Current assignee: HUBEI XIANGRUIFENG YEW TECHNOLOGY Co.,Ltd.
Priority date: 2018-08-24
Filing date: 2018-08-24
Publication date: 2021-04-20
Anticipated expiration: 2038-08-24
Also published as: CN108785383A

Abstract

The invention discloses an antibacterial gynecological external medicine composition, a preparation method and an application thereof, wherein the medicine composition comprises the following substances in parts by weight: 1-10 parts of taxus chinensis extract, 1-10 parts of scutellaria baicalensis extract, 0.5-5 parts of radix sophorae flavescentis extract and 0.5-5 parts of fructus cnidii extract. The application of the invention comprises different dosage forms, the dosage forms comprise the traditional Chinese medicine composition and pharmaceutically acceptable carriers, and the dosage forms are lotion, gel and vaginal effervescent tablets. The antibacterial gynecological external medicine composition disclosed by the invention has the advantages that the taxus chinensis is used as a monarch drug, the scutellaria baicalensis is used as a ministerial drug, and the fructus cnidii and the radix sophorae flavescentis are used as adjuvants, so that the antibacterial and anti-inflammatory effects of the compound traditional Chinese medicine composition are ensured, and meanwhile, the compound traditional Chinese medicine composition can also be used for clearing heat, removing dampness, killing parasites, relieving itching, eliminating stagnation and reducing swelling, the medicine effect is improved, the recovery. The invention has simple preparation process and uniform and stable medicine quality.

Description

Antibacterial gynecological external medicine composition and preparation method and application thereof

Technical Field

The invention relates to the technical field of gynecological medicines, in particular to an antibacterial gynecological external medicine composition and a preparation method and application thereof.

Background

Gynecological inflammation is the most common disease of women, mainly refers to inflammation of female genitals, and various female organs can have acute and chronic inflammation, and specifically comprises female vulvitis, vaginitis, cervicitis and pelvic inflammation; according to pathogens, the traditional Chinese medicine can be divided into mycotic vaginitis, bacterial vaginitis and trichomonas vaginitis, and has the characteristics of high morbidity, difficult radical treatment, easy relapse and the like.

With the change of life style, the work rhythm is accelerated, the immunity is reduced and other factors, so the incidence rate of gynecological inflammation continuously rises and the trend of the gynecological inflammation is younger. The gynecological inflammation not only affects the daily life of women along with pruritus and burning sensation, but also harms the health and even reaches family members.

The existing administration modes for treating gynecological inflammation are divided into injection, oral administration and external application, and patients are more prone to take external medicines due to large toxic and side effects and slow effect of the injection and the oral administration. The external medicine is also divided into Chinese patent medicine, chemical medicine and Chinese and western medicine mixture. The chemical drugs are mainly antibiotics, and the drugs have very obvious antibacterial and anti-inflammatory effects and quick response, but the drug resistance caused by over-dependence on the antibiotics can increase the treatment difficulty and have no effect on the complications of gynecological inflammation; the Chinese patent medicine is prepared by extracting pure Chinese medicines, has complex components and difficult control of bacteriostatic effect; the Chinese and western medicine mixture is a Chinese patent medicine, and is added with a proper amount of chemical medicines, so that the antibacterial effect is ensured, but the problem of drug resistance is still faced.

The patent application number is 'CN 201310233570.0', the name is 'a pharmaceutical composition for treating gynecological inflammation', and relates to a pharmaceutical composition for treating gynecological inflammation, which is prepared by taking yew active extract, camphor and peppermint oil as raw materials and a pharmaceutically acceptable carrier as a matrix. The pharmaceutical composition provided by the invention can improve the comprehensive utilization value of the taxus chinensis, and the prepared pharmaceutical composition has better anti-inflammatory effect. However, the composition has the defect that the inhibition effect of the taxus chinensis on gram-positive bacteria is not ideal, the gynecological inflammation complications can not be treated basically, and the drug effect needs to be improved.

Disclosure of Invention

The invention aims to overcome the defects of the prior art and provides an antibacterial gynecological external medicine composition, which takes taxus as a monarch drug and is assisted by traditional Chinese medicines such as scutellaria baicalensis, fructus cnidii, radix sophorae flavescentis and the like, so that the antibacterial and anti-inflammatory effects of the compound traditional Chinese medicine composition are ensured, and meanwhile, the compound traditional Chinese medicine composition can also clear heat, remove dampness, kill parasites, relieve itching, dissipate stagnation and reduce swelling, improve the medicine effect, shorten the recovery time and improve the life quality; radix Sophorae Flavescentis and fructus Cnidii are used as adjuvant drugs for adjuvant treatment of gynecological inflammation complications, and have effects of improving drug effect and accelerating healing.

The invention is realized by the following steps:

the invention aims to provide an antibacterial gynecological external medicine composition, which comprises the following substances in parts by weight: 1-10 parts of taxus chinensis extract, 1-10 parts of scutellaria baicalensis extract, 0.5-5 parts of radix sophorae flavescentis extract and 0.5-5 parts of fructus cnidii extract.

The invention also aims to provide a preparation method of the antibacterial gynecological external medicine composition, which comprises the following steps:

step 1, drying and crushing the taxus chinensis, the scutellaria baicalensis, the radix sophorae flavescentis and the fructus cnidii respectively;

step 2, leaching the Chinese medicine powder obtained in the step 1 with hot water to obtain leaching liquor of different Chinese medicines;

and 3, combining the corresponding traditional Chinese medicine leaching liquor obtained in the step 2, concentrating in vacuum, and spray-drying the concentrated liquor to obtain the antibacterial gynecological external medicine composition.

The invention also aims to provide a preparation prepared from the pharmaceutical composition, which comprises the pharmaceutical composition and a pharmaceutically acceptable carrier, wherein the preparation is lotion, gel, vaginal effervescent tablets, emulsion, cream, tincture, lotion, liniment, plastics or spray.

Preferably, the lotion comprises the following substances in parts by weight: 8-15 parts of the pharmaceutical composition, 0.1-0.5 part of menthol, 0.1-0.5 part of borneol and 1-3 parts of ethanol.

Preferably, the gel comprises the following substances in parts by weight: 0.5-1.4 parts of the pharmaceutical composition, 0.05-0.2 part of menthol, 0.05-0.2 part of borneol, 0.5-1 part of gel matrix and 1-5 parts of ethanol.

Preferably, the vaginal effervescent tablet comprises the following substances in parts by weight: 5-10 parts of the pharmaceutical composition, 25-35 parts of effervescent disintegrant, 20-30 parts of filler, 1-5 parts of glidant, 0.2-0.6 part of lubricant and 24-32 parts of adhesive.

The efficacy and activity of each main raw material medicine are as follows:

1. chinese yew: also known as yew. Branches and leaves of taxus chinensis are used as a medicine, have slightly sweet, bitter and flat taste, have the effects of reducing swelling, resolving masses, inducing menstruation, inducing diuresis and the like, and are mainly used for treating diseases such as abdominal mass accumulation, edema, dysuria, rheumatic arthralgia and the like. The compendium of materia medica records that it has the efficacy of treating cholera, typhoid, expelling toxin and the like. The modern traditional Chinese medicine finds that the taxus chinensis is rich in taxane compounds, polysaccharide, flavone, sequoyitol and the like, so that the taxus chinensis has the effects of resisting tumors, regulating immunity, resisting inflammation, sterilizing, resisting viruses, resisting rheumatism, reducing blood sugar and the like.

(1) Diminishing inflammation and inhibiting bacteria: the taxus chinensis contains a large amount of tannin, and the tannin has the effects of inhibiting bacteria and inflammation, inhibiting various harmful bacteria in the air, and having very obvious treatment effects on nephritis, hepatitis, gastritis, enteritis, sphagitis, gynecological inflammation, prostatitis, hemorrhoid, rheumatoid and the like;

(2) improving immunity: the yew contains more than 90 effective components required by human body, and can improve immunity and antiviral ability of human body. The health-care product has the effects of reducing blood sugar for hyperglycemia patients, has very obvious effects on hypertension, hyperlipidemia, high blood viscosity, nephropathy, hepatopathy, dysmenorrheal and the like, particularly can reduce urine protein loss, recover the natural function of a human body, enhance the immunity and eliminate various diseases in sprouts;

(3) antioxidant: the taxus chinensis fruit is rich in taxol protein, various mineral substances such as calcium, phosphorus, iron and the like and various vitamin substances, and is the best plant with natural antioxidant (anti-aging) substances;

(4) cancer prevention and treatment: taxol contained in Taxus chinensis var mairei has a unique anticancer mechanism and higher anticancer activity, can prevent the propagation of cancer cells and inhibit the migration of tumor cells, has no obvious adverse reaction, is known as the most important anticancer active substance in the field of natural medicines at present, and has remarkable curative effect on ovary and breast cancer proved by the clinical research in the United states. In addition, the medicine also has certain effect on hypertension, diabetes and coronary heart disease;

2. scutellaria baicalensis: the root is used as a medicine, has bitter taste and cold property, and has the efficacies of clearing heat and drying dampness, purging fire and removing toxicity, stopping bleeding, preventing miscarriage and the like. It can be used for treating epidemic febrile disease, upper respiratory infection, cough due to lung heat, yellow gallbladder due to damp-heat, pneumonia, dysentery, hemoptysis, conjunctival congestion, threatened abortion, hypertension, carbuncle, furuncle, and sore. The scutellaria decoction has an inhibiting effect on escherichia coli, staphylococcus, candida albicans, dysentery bacillus, candida albicans and the like, and researchers also find that the water decoction of the scutellaria decoction has an inhibiting effect on specific inflammations.

3. Flavescent sophora root: the root is bitter in taste and cold in nature. Has effects of clearing heat, eliminating dampness, killing parasites, relieving itching, and promoting urination. Can be used for treating dysentery, hematochezia, jaundice, anuria, leucorrhea with red and white discharge, pudendal swelling, pudendal pruritus, eczema, skin pruritus, scabies, tinea, leprosy, trichomonas vaginitis, etc. The sophora flavescens decoction has obvious inhibition effect on dysentery bacillus, staphylococcus aureus, escherichia coli, tubercle bacillus and the like. It can be used for treating trichomonas vaginitis.

4. Fructus cnidii: the fruit is pungent and bitter in flavor and warm in nature. Has effects of eliminating dampness, dispelling pathogenic wind, killing parasites, relieving itching, warming kidney, and tonifying yang. Can be used for treating pudendal pruritus, scabies, tinea, eczema, pruritus, sexual impotence, cold womb, leukorrhagia due to cold-dampness, and lumbago due to damp arthralgia; it can be used for treating eczema of vulva, pruritus vulvae, and trichomonal vaginitis.

Compared with the prior art, the invention has the following advantages and effects:

1. according to the antibacterial gynecological external medicine composition provided by the invention, the taxus chinensis is used as a monarch medicine, and the scutellaria baicalensis is used as a ministerial medicine, so that the defect that the inhibition effect of the taxus chinensis on gram-positive bacteria is not ideal is overcome, and the antibacterial performance of the medicine is ensured; the specific compounds of yew polysaccharide and yew flavone have effects of resisting oxidation, improving immunity, and promoting vaginal flora balance; radix Sophorae Flavescentis and fructus Cnidii are used as adjuvant drugs for adjuvant treatment of gynecological inflammation complications, and have effects of improving drug effect and accelerating healing. Not only can effectively kill germs, relieve itching and kill parasites, but also can maintain the acid-base balance of vagina, clear heat and remove dampness, kill parasites and relieve itching, and dissipate stagnation and detumescence. Is suitable for gynecological inflammation caused by bacteria, fungi, protozoa, etc.

2. The antibacterial gynecological external medicine composition provided by the invention has a strong inhibiting effect on escherichia coli, staphylococcus aureus, bacillus subtilis and candida albicans, the minimum inhibiting concentration on staphylococcus aureus is only 0.8mg/ml, the minimum inhibiting concentration on escherichia coli is only 1.6mg/ml, the minimum inhibiting concentration on bacillus subtilis is only 1.6mg/ml, and the minimum inhibiting concentration on candida albicans is only 0.8 mg/ml; the four components in the antibacterial gynecological external medicine composition provided by the invention are matched with each other and have synergistic interaction, so that the minimum inhibitory concentration of the antibacterial gynecological external medicine composition on escherichia coli, staphylococcus aureus, bacillus subtilis and candida albicans is greatly reduced, and the antibacterial rate is greatly increased.

3. The medicinal composition comprises 1-10 parts of taxus chinensis extract, 1-10 parts of scutellaria baicalensis extract, 0.5-5 parts of radix sophorae flavescentis extract and 0.5-5 parts of fructus cnidii extract, and the components in the formula are reasonably distributed: most gynecological inflammations are caused by dysbacteriosis, killing pathogenic bacteria and maintaining the balance of flora in vagina are the primary tasks, the inventor selects a taxus chinensis extract with good bacteriostasis as a main bacteriostatic agent, and selects scutellaria baicalensis with good escherichia coli inhibiting effect as an auxiliary bacteriostatic agent in consideration of poor inhibiting effect of the taxus chinensis extract on gram-negative bacteria represented by escherichia coli. The gynecological inflammation is also accompanied with complications such as pruritus vulvae and vagina, causalgia, redness and swelling, and the like, so that the fructus cnidii and the radix sophorae flavescentis are selected as auxiliary medicaments by the inventor to clear heat and dry dampness, kill parasites and relieve itching, detoxify and relieve pain, prevent corrosion and reduce swelling, and can greatly improve the quality of life.

4. According to the preparation method of the pharmaceutical composition provided by the invention, the effective components of the traditional Chinese medicine are extracted independently at first, different extraction temperatures and different extraction times can be set according to the performance of the traditional Chinese medicine, so that the effective components in the traditional Chinese medicine components are prevented from being excessively damaged during extraction, the extraction degree is maximized, the raw material consumption is reduced, and the cost is reduced. Secondly, the spray drying method is adopted, so that the extract can be uniformly dispersed, the effective components of different traditional Chinese medicines are fully mixed during preparation, the uniform dispersion of the effective components during preparation of the medicinal preparation is facilitated, and the antibacterial and anti-inflammatory effects of the medicinal composition are improved; the provided taxus extract is a water-soluble extract, and the extracted residue is still used for extracting paclitaxel, so that the utilization rate and the economic benefit of the taxus can be improved.

Detailed Description

EXAMPLE 1 formulation of antibacterial gynecological topical pharmaceutical composition

Discovery of components of antibacterial gynecological external-use medicine composition

(1) Preparation of extract of effective components of Chinese medicinal materials

The traditional Chinese medicine extract is prepared by the following steps: drying taxus chinensis, radix sophorae flavescentis, scutellaria baicalensis and fructus cnidii, and then respectively crushing by using a crusher to obtain traditional Chinese medicine powder, wherein the diameter of the powder is controlled to be 60-80 meshes; adding water with 5 times of the feeding amount into the Chinese medicinal powder for leaching; leaching for 3 times, each time for 5 hr to obtain Chinese medicinal material leaching solution, and adjusting the extraction temperature according to different Chinese medicinal materials; thirdly, pumping the Chinese medicinal material leaching liquor obtained in the step 2 into a circulating vacuum concentration tank for concentration, controlling the concentration temperature to be 80 ℃, controlling the vacuum degree to be 0.008MPa, and stopping concentration when the density of a concentrated solution reaches 1.0 g/mL; fourthly, spray drying the concentrated solution obtained in the step 3 at 120 ℃ to obtain the corresponding traditional Chinese medicine extract.

(2) In vitro bacterial inhibition experiment strain selection

Bacillus subtilis (ATCC 6633), Escherichia coli (ATCC 35218), Staphylococcus aureus (ATCC 29213), and Candida albicans (ATCC 10231).

(3) Preparation of bacteriostatic agent

Respectively and precisely weighing 512mg of extracts of the taxus chinensis, the scutellaria baicalensis, the fructus cnidii and the radix sophorae flavescentis, adding water for dissolving (a small amount of DMSO can be added for promoting dissolution), fixing the volume by using a 10mL volumetric flask, and shaking up to obtain a traditional Chinese medicine extracting solution with the concentration of 51.2mg/mL, wherein the bacteriostatic agent is only used on the same day.

(4) Preparation of bacterial suspension

Taking a small amount of 2-generation nutrient agar slant culture of experimental bacteria, inoculating the slant culture into 5mL of liquid culture medium to prepare suspension, culturing at 36 +/-1 ℃ for 18-24 h, diluting the suspension to 0.5 McLee ratio by a turbidimetric method, diluting the bacterial solution to 5 multiplied by 105-5 multiplied by 106cFu/mL by using the liquid culture medium with double concentration, and only using the bacterial solution for the same day.

(5) Detection of minimum inhibitory concentration

48 sterile test tubes were taken and divided equally into 4 groups of parallel tests, numbered. Taking 12 sterile test tubes (13 × 100mm) of the first group, arranging in a row, adding 51.2mg/mL Chinese yew extract into tubes No. 1 and No. 2, adding 1mL water into tube No. 2, mixing uniformly, sucking 1mL to tube No. 3, diluting sequentially according to the method, adding 1mL water into tube No. 11, and adding 51.2, 25.6, 12.8, 6.4, 3.2, 1.6, 0.8, 0.4, 0.2, 0.1 and 0mg/mL medicine into tubes No. 1 to No. 11 sequentially. Then, 1mL of each of the prepared bacterial suspensions was added to 11 tubes and shaken. The drug concentrations in the 1 st to 11 th tubes were 25.6, 12.8, 6.4, 3.2, 1.6, 0.8, 0.4, 0.2, 0.1, 0.05, 0mg/mL, respectively, and the 12 th tube was added with a blank broth as a negative control. And (3) culturing for 24h in a 37 ℃ incubator, observing the culture medium after the culture is finished, and recording the minimum bacteriostatic concentration of the liquid culture medium without turbidity, namely the minimum bacteriostatic concentration.

(6) The results of the measurement of the minimum inhibitory concentration of taxus chinensis, scutellaria baicalensis, fructus cnidii and radix sophorae flavescentis by the method

The results of the minimum inhibitory concentrations of taxus chinensis, scutellaria baicalensis, fructus cnidii and sophora flavescens on four bacteria are shown in the following table:

TABLE 1 minimum inhibitory concentration (mg/mL) of four herbal extracts

According to MIC experiments of the four traditional Chinese medicine extracts, the extracts of the taxus chinensis, the scutellaria baicalensis, the fructus cnidii and the radix sophorae flavescentis have certain antibacterial activity, but the antibacterial activity of the taxus chinensis and the scutellaria baicalensis is obviously higher than that of the fructus cnidii and the radix sophorae flavescentis. The taxus chinensis extract has very good bacteriostatic activity on staphylococcus aureus and candida albicans, but has poor inhibition effect on escherichia coli (gram negative bacteria), and the scutellaria baicalensis has good inhibition effect on escherichia coli.

In addition, the inventor also considers the bacteriostasis of more than ten gynecological traditional Chinese medicinal material extracts such as golden cypress, Chinese prickly ash, alum, rhizoma atractylodis and the like by taking an MIC value as an index, the bacteriostasis of other traditional Chinese medicinal materials except the Chinese prickly ash cannot reach the level of the extracts of the taxus chinensis and the scutellaria baicalensis, but when the Chinese prickly ash is taken as a combined medicament to carry out a rabbit vaginal mucosa irritation experiment, the Chinese prickly ash extract is found to have certain irritation, so the extracts of the taxus chinensis and the scutellaria baicalensis are taken as bacteriostasis components.

Second, exploration of content of antibacterial gynecological external-use medicine composition

TABLE 2

As can be seen from table 2, the optimal ratio of the experimental group 4 including 6 parts of yew extract, 4 parts of scutellaria extract, 2 parts of sophora flavescens extract and 2 parts of cnidium fruit extract is shown.

According to the selection and matching results of the medicinal composition, the four components in the antibacterial gynecological external medicinal composition provided by the invention are matched with each other and have synergistic interaction, so that the minimum inhibitory concentration of the antibacterial gynecological external medicinal composition on escherichia coli, staphylococcus aureus, bacillus subtilis and candida albicans is greatly reduced, and the antibacterial rate is greatly increased.

Most gynecological inflammations are caused by dysbacteriosis, killing pathogenic bacteria and maintaining the balance of flora in vagina are the primary tasks, the inventor selects a taxus chinensis extract with good bacteriostasis as a main bacteriostatic agent, and selects scutellaria baicalensis with good escherichia coli inhibiting effect as an auxiliary bacteriostatic agent in consideration of poor inhibiting effect of the taxus chinensis extract on gram-negative bacteria represented by escherichia coli.

The gynecological inflammation is also accompanied with complications such as pruritus vulvae and vagina, causalgia, redness and swelling, and the like, so that the fructus cnidii and the radix sophorae flavescentis are selected as auxiliary medicaments by the inventor to clear heat and dry dampness, kill parasites and relieve itching, detoxify and relieve pain, prevent corrosion and reduce swelling, and can greatly improve the quality of life.

Example 2: preparation of antibacterial gynecological external medicine composition

First, investigation of extraction Process

1. The inventor investigates the influence of the feed-liquid ratio (1:5, 1:10 and 1:15), the extraction temperature (50 ℃, 60 ℃, 70 ℃ and 80 ℃) and the extraction frequency (1, 2 and 3) on the extraction yield and the antibacterial activity of the extract through an orthogonal test, and provides an economic and efficient extraction process by combining the extraction cost, namely extracting for three times with the feed-liquid ratio of 1: 5; the extraction temperature is 60 ℃ for the taxus chinensis and 75 ℃ for the scutellaria baicalensis, the fructus cnidii and the radix sophorae flavescentis.

Secondly, the influence of single extraction and mixed extraction on bacteriostasis

1. The preparation method of the taxus chinensis, the radix sophorae flavescentis, the radix scutellariae and the fructus cnidii extract comprises the following steps: drying taxus chinensis, radix sophorae flavescentis, scutellaria baicalensis and fructus cnidii, and then respectively crushing by using a crusher to obtain traditional Chinese medicine powder, wherein the diameter of the powder is controlled to be 60-80 meshes; adding water with 5 times of the feeding amount into the Chinese medicinal powder for leaching; leaching for 3 times, each time for 5 hr to obtain Chinese medicinal material leaching solution, and adjusting the extraction temperature according to different Chinese medicinal materials; thirdly, pumping the Chinese medicinal material leaching liquor obtained in the step 2 into a circulating vacuum concentration tank for concentration, controlling the concentration temperature to be 80 ℃, controlling the vacuum degree to be 0.008MPa, and stopping concentration when the density of a concentrated solution reaches 1.0 g/mL; fourthly, spray drying the concentrated solution obtained in the step 3 at 120 ℃ to obtain a corresponding traditional Chinese medicine extract; then, the obtained traditional Chinese medicine extract is prepared according to the following steps of Chinese yew: flavescent sophora root: scutellaria baicalensis: fructus Cnidii (6:4:2:2) is mixed uniformly for use.

2. The preparation method of the taxus chinensis, radix sophorae flavescentis, scutellaria baicalensis and fructus cnidii compound extract comprises the following steps: firstly, mixing taxus chinensis, radix sophorae flavescentis, scutellaria baicalensis and fructus cnidii according to a ratio of 6:4:2:2, and crushing by using a crusher to obtain traditional Chinese medicine powder, wherein the diameter of the powder is controlled to be 60-80 meshes; adding water with 5 times of the feeding amount into the Chinese medicinal powder for leaching; leaching for 3 times, each time for 5 hr to obtain Chinese medicinal material leaching solution, and extracting at 80 deg.C; thirdly, pumping the Chinese medicinal material leaching liquor obtained in the step 2 into a circulating vacuum concentration tank for concentration, controlling the concentration temperature to be 80 ℃, controlling the vacuum degree to be 0.008MPa, and stopping concentration when the density of a concentrated solution reaches 1.0 g/mL; and fourthly, spray drying the concentrated solution obtained in the step 3 at the temperature of 120 ℃ to obtain the compound traditional Chinese medicine extract.

3. The minimum inhibitory concentrations of the two extracts against bacillus subtilis (ATCC 6633), escherichia coli (ATCC 35218), staphylococcus aureus (ATCC 29213) and candida albicans (ATCC 10231) were determined by MIC test method shown in example 1 using the extracts obtained from the two processes, and the results were as follows:

TABLE 3 minimum inhibitory concentration (mg/mL) of two kinds of compound Chinese medicinal extracts

According to the test results, the antibacterial activity of the extracts obtained by respectively extracting the traditional Chinese medicines and then mixing the traditional Chinese medicines is obviously higher than that of the extracts obtained by mixing the traditional Chinese medicines, so that the mode of respectively extracting the traditional Chinese medicines and then mixing the traditional Chinese medicines is selected. The antibacterial performance of the traditional Chinese medicine extract is superior to that of the traditional Chinese medicine extract obtained by mixing and leaching the raw materials after extracting different traditional Chinese medicine components respectively, mainly because the content of various traditional Chinese medicine components can be controlled more accurately by means of respective leaching, the compatibility effect among the traditional Chinese medicines is remarkable, and the efficacy of the traditional Chinese medicines is improved. In addition, due to the existence of compatibility of the traditional Chinese medicines, the prepared antibacterial gynecological external medicine composition can also exert respective unique performances of different traditional Chinese medicines, such as clearing heat and removing dampness, relieving itching and killing parasites, and can treat complications caused by gynecological diseases.

EXAMPLE 3 preparation of lotion

Preparing the extract of the effective components of the traditional Chinese medicine, 8 to 15 parts of the pharmaceutical composition, 0.1 to 0.5 part of menthol, 0.1 to 0.5 part of borneol and 1 to 3 parts of ethanol.

In one embodiment, the pharmaceutical composition comprises 14 parts (6 parts of yew extract, 4 parts of scutellaria extract, 2 parts of cnidium fruit extract and 2 parts of sophora flavescens extract), 0.1 part of menthol, 0.1 part of borneol and 2 parts of ethanol.

The method comprises the following steps:

(1) drying Taxus chinensis, Scutellariae radix, radix Sophorae Flavescentis and fructus Cnidii, pulverizing respectively with pulverizer to obtain Chinese medicinal powder with particle size of 60-80 mesh;

(2) respectively taking 10 parts of Chinese medicinal powder, and adding water with 5 times of the feeding amount to carry out leaching; leaching for 3 times, each for 5 hr, to obtain Chinese medicinal material leaching solution, wherein the temperature for extracting Taxus chinensis is 60 deg.C, and the temperature for extracting Scutellariae radix, radix Sophorae Flavescentis and fructus Cnidii is 80 deg.C;

(3) pumping the corresponding Chinese medicinal material leaching liquor obtained in the step (2) into a circulating vacuum concentration tank for concentration, controlling the concentration temperature to be 80 ℃ (the temperature of the Chinese yew is 60 ℃), controlling the vacuum degree to be 0.008MPa, and stopping concentration when the density of a concentrated solution reaches 1.0 g/mL;

(4) and (4) spray drying the corresponding Chinese medicinal material concentrated solution obtained in the step (3) at 120 ℃ to obtain a corresponding Chinese medicinal extract.

(5) Preparing the antibacterial gynecological external medicine composition of the lotion: dissolving the Chinese medicinal extract with appropriate amount of water, dissolving Borneolum Syntheticum and Mentholum in appropriate amount of ethanol, mixing, adding water to the solution, adjusting to 100mL, adjusting pH to 5.5-6.5 with lactic acid, standing, filtering, sterilizing, and packaging.

EXAMPLE 4 preparation of gels

1. By adopting the procedure of preparing the extract of the effective ingredients of the traditional Chinese medicine in example 3, the taxus chinensis extract, the scutellaria baicalensis extract, the sophora flavescens extract and the cnidium monnieri fruit extract are prepared.

2. Preparation of gel formulations

The raw materials of the gel preparation comprise 0.5-1.4 parts of pharmaceutical composition, 0.05-0.2 part of menthol, 0.05-0.2 part of borneol, 0.5-1 part of gel matrix and 1-5 parts of ethanol.

As one of the above embodiments, 0.6 parts of taxus chinensis extract, 0.4 parts of scutellaria baicalensis extract, 0.2 parts of sophora flavescens extract, 0.2 parts of fructus cnidii extract, 0.05 parts of borneol, 0.05 parts of menthol, 0.5 parts of carbomer 940 (gel matrix) and 2 parts of ethanol. The specific method comprises the following steps: swelling carbomer 940 with appropriate amount of water to form colloid, and adjusting pH to 2.3-2.5 with hydrochloric acid; adding the four Chinese medicinal extracts, Borneolum Syntheticum, and ethanol, stirring, draining the sodium hydroxide solution to pH 5.5-6.5, adjusting total liquid amount to 100mL, stirring, sterilizing, and packaging.

EXAMPLE 5 preparation of effervescent

The operation of preparing the extracts of the effective ingredients of the traditional Chinese medicine in example 3 is adopted to prepare the taxus chinensis extract, the scutellaria baicalensis extract, the sophora flavescens extract and the fructus cnidii extract.

The vaginal effervescent tablet comprises the following substances in parts by weight: 5-10 parts of the pharmaceutical composition, 25-35 parts of effervescent disintegrant, 20-30 parts of filler, 1-5 parts of glidant, 0.2-0.6 part of lubricant and 24-32 parts of adhesive.

The effervescent disintegrant consists of organic acid and alkali, specifically one or more of citric acid, tartaric acid and fumaric acid, and sodium carbonate or sodium bicarbonate.

The common fillers of the vaginal effervescent tablets include starch, microcrystalline cellulose, dextrin and the like.

The common adhesive comprises lubricants such as hydroxypropyl methylcellulose (with foaming function) aqueous solution and mannitol, which are divided into water-soluble lubricants and water-insoluble lubricants, wherein the common water-soluble lubricants comprise polyethylene glycol 4000 or 6000, sodium dodecyl sulfate, magnesium dodecyl sulfate, L-leucine, sodium benzoate, sodium oleate, sodium chloride, sodium acetate, boric acid and the like; commonly used water-insoluble lubricants include magnesium stearate, talc, aerosil, sucrose fatty acid esters, sodium stearyl fumarate, and the like.

The antibacterial gynecological external medicine composition comprises 3 parts of taxus chinensis extract, 2 parts of scutellaria baicalensis extract, 1 part of sophora flavescens extract, 1 part of fructus cnidii extract, 30 parts of microcrystalline cellulose (filler), 25.5 parts of mannitol (adhesive), 10 parts of citric acid (effervescent disintegrant), 20 parts of sodium bicarbonate (effervescent disintegrant), 5 parts of povidone (glidant) and 0.5 part of magnesium stearate (lubricant). Uniformly mixing the traditional Chinese medicine extract, mannitol and sodium bicarbonate to obtain a mixture 1, and uniformly mixing microcrystalline cellulose and citric acid to obtain a mixture 2; adding polyvidone water solution into the mixture 1 and the mixture 2 respectively, and granulating; drying and granulating; mixing the two groups of dry granules, adding magnesium stearate, mixing, and tabletting.

Experimental example 1 antibacterial function test of antibacterial gynecological external drug composition

(1) Selection of strains

The strains selected in the in vitro bacteriostasis test are respectively as follows: escherichia coli (ATCC 35218), Staphylococcus aureus (ATCC 29213) and Candida albicans (ATCC 10231). The Escherichia coli, the staphylococcus aureus and the Candida albicans in the invention are purchased from China pharmaceutical and biological product institute.

(2) Experiment of quantitative sterilization of carrier

According to the requirements of quantitative sterilization test of carriers in the technical Specification for disinfection (2002 edition), the prepared antibacterial gynecological external medicine composition is taken to act for 5min, 10min and 60min, and the results are shown in the following table:

TABLE 4

From the test results in table 4, it can be seen that the formulations prepared in the present invention (the lotion of example 3, the gel of example 4, the vaginal effervescent tablet of example 5) have rapid bactericidal properties, can be sterilized efficiently in a short time, and can be bacteriostatic for a long time. It should be noted that other embodiments (not shown) within the formulation range of examples 3 to 5 of the present invention can achieve the same or similar technical effects, and are not described herein again.

Experimental example 2 toxicological test

1. Toxicology experiments were performed on experimental animals using the formulations of examples 3-5, and the results were as follows:

TABLE 5

2. As can be seen from the experimental results in Table 5, the preparations of examples 3 to 5 have high safety to experimental animals and good application prospects.

The invention is not to be considered as limited to the particular embodiments shown, but is to be accorded the widest scope consistent with the principles and novel features disclosed herein.

Claims

1. The antibacterial gynecological external medicine composition is characterized by comprising the following substances in parts by weight: 4-8 parts of a taxus chinensis extract, 2-6 parts of a scutellaria baicalensis extract, 1-3 parts of a sophora flavescens extract and 1-3 parts of a fructus cnidii extract;

the preparation method of the antibacterial gynecological external medicine composition comprises the following steps:

step 1, drying and crushing taxus chinensis, scutellaria baicalensis, radix sophorae flavescentis and fructus cnidii respectively;

2. The antibacterial gynecological topical pharmaceutical composition according to claim 1, characterized in that the pharmaceutical composition consists of the following substances in parts by weight: 6 parts of taxus chinensis extract, 4 parts of scutellaria baicalensis extract, 2 parts of sophora flavescens extract and 2 parts of fructus cnidii extract.

3. The antibacterial gynecological topical pharmaceutical composition according to claim 1, wherein in the step 2, the addition amount of the leaching hot water is 5-15 times of the batch amount; leaching for more than 1 time; the leaching temperature is 60-100 ℃; the leaching time is more than 1h each time.

4. The antibacterial gynecological topical pharmaceutical composition according to claim 1, wherein the concentration in the step 3 is performed until the density of the concentrated solution reaches 0.9-1.1 g/mL; the spray drying temperature is 100-150 ℃.

5. A formulation prepared from the pharmaceutical composition of any one of claims 1-4, wherein: the pharmaceutical composition consists of the pharmaceutical composition of any one of claims 1 to 4 and a pharmaceutically acceptable carrier, and the preparation is lotion, gel, vaginal effervescent tablet, emulsion, cream, tincture, lotion, liniment, plastics or spray.

6. The formulation of claim 5, wherein the lotion is comprised of the following parts by weight: the pharmaceutical composition of any one of claims 1-4, 8-15 parts, 0.1-0.5 part of menthol, 0.1-0.5 part of borneol, and 1-3 parts of ethanol.

7. The formulation of claim 5, wherein the gelling agent is comprised of the following parts by weight: the pharmaceutical composition of any one of claims 1-4, 0.5-1.4 parts, menthol 0.05-0.2 parts, borneol 0.05-0.2 parts, gel matrix 0.5-1 parts, and ethanol 1-5 parts.

8. The formulation of claim 5, wherein the vaginal effervescent tablet is comprised of the following parts by weight: 5-10 parts of the pharmaceutical composition of any one of claims 1-4, 25-35 parts of effervescent disintegrant, 20-30 parts of filler, 1-5 parts of glidant, 0.2-0.6 part of lubricant and 24-32 parts of adhesive.