Basil volatile oil vaginal suppository and its preparation method and application

Abstract

The present invention discloses a basil volatile oil vaginal suppository, a preparation method, and an application thereof. The suppository is composed of a mixture of a water-soluble matrix, an oily matrix, basil volatile oil, and an emulsifier. The water-soluble matrix comprises distilled water, polyethylene glycol 4000, and polyethylene glycol 6000, and the oily matrix comprises mixed fatty acid glycerides (stearin). The ratio of the water-soluble matrix to the oily matrix is ​​8:8-10. The basil volatile oil vaginal suppository of the present invention has moderate hardness, is not easily deformed, has good plasticity and stability, and has a moderate dissolution time and good solubility. This prevents the drug from dissolving too quickly or too slowly in the human body, ensuring that the drug is absorbed in the body to achieve the desired effect. It can stably release the drug in the vagina while reducing irritation to the vaginal mucosa. It has a precise therapeutic effect and low side effects in the treatment of vaginitis caused by Candida albicans.

Description

Technical Field

[0001] The present invention relates to the technical field of biomedicine, and more particularly to a basil volatile oil vaginal suppository and a preparation method and application thereof. Background Art

[0002] Vulvovaginal candidiasis (VVC), also known as vulvovaginal candidiasis, is a vaginitis primarily caused by Candida species. Candida albicans is the most common pathogen in candidal vaginitis. When the vaginal microenvironment is altered, it can cause infection and inflammation. Candida vaginitis accounts for 20% to 25% of vaginitis infections. Infectious vaginitis is a common infection among women of childbearing age, and Candida species are the most common vaginal fungus. Clinical symptoms primarily include increased discharge that may appear shoddy or curd-like, accompanied by vulvar itching. Frequent episodes can even lead to cervicitis, infertility, and miscarriage. Extensive epidemiological data confirm that the widespread use of antibiotics in recent years has led to the emergence of drug-resistant strains. The incidence of vaginitis caused by Candida species, in particular, has increased significantly each year. The vast majority of women of childbearing age will experience at least one Candida infection in their lifetime, significantly impacting their health. Clinically, sexual transmission is a major route of infection for women of childbearing age, and a weakened vaginal defense system can also lead to the proliferation of Candida albicans. It is estimated that approximately 75% of women of childbearing age will be affected by Candida albicans, with approximately half experiencing further episodes. A small proportion (5%-8%) will develop recurrent vulvovaginal candidiasis (RVVC).

[0003] In recent years, the incidence of candidal vaginitis has increased significantly due to the overuse of antibiotics and immunosuppressants. Several strategies have been adopted clinically to prevent and treat vaginitis. However, most Candida species have been shown to be resistant to conventional antifungal drugs, posing a serious threat to patients' health. Compared with traditional antifungal drugs, traditional Chinese medicine (TCM) and TCM compound formulas offer advantages in the treatment of vaginitis, such as strong antifungal activity, stable efficacy, low toxicity, and resistance to drug resistance. Basil, a plant of the genus Ocimum basilicum in the family Labiatae, produces a light yellow to yellow transparent liquid containing compounds such as alcohols, alkenes, ketones, heterocyclic rings, alkanes, aromatic hydrocarbons, and amines. Amber K et al. studied the antifungal activity of holy basil essential oil and its active components, methylchavicol (44.63%) and linalool (21.84%), against Candida albicans and confirmed that holy basil essential oil and its main components, methylchavicol and linalool, can interfere with ergosterol synthesis in fungi, thereby damaging the fungal cell membrane and disrupting its integrity. Consequently, basil essential oil exhibits certain antibacterial activity. Furthermore, the article "Preparation and Antibacterial Activity of Basil Volatile Oil Inclusion Compounds" reported that basil essential oil extracted by steam distillation and then prepared with hydroxypropyl-β-cyclodextrin exhibited an inhibition zone and minimum inhibitory concentration of 1.12 cm and 3.79 mg / mL, respectively, against Candida albicans. Therefore, it is speculated that basil essential oil has a certain therapeutic effect on vaginitis caused by Candida albicans.

[0004] In the treatment of gynecological diseases, in addition to oral preparations and various lotions, traditional Chinese medicine vaginal suppositories are also a gynecological preparation with significant therapeutic effects. Because traditional Chinese medicine suppositories have the advantage of avoiding interactions with the gastrointestinal tract, such as the stomach and intestines, that could inactivate drugs or irritate them, as well as the "first-pass effect" on the liver, a variety of new suppositories have been developed to achieve combined drug administration, rapid release, and sustained release, thus being applied clinically to alleviate patients' pain. Traditional Chinese medicine suppositories and vaginal suppositories not only have local and systemic therapeutic effects, but also have the advantages of simple operation, definite efficacy, and easy patient acceptance. They are widely used in clinical practice and have achieved certain economic and social benefits. For example, patent CN107334727A discloses a eugenol / clove oil suppository for urethra or anus and a preparation method thereof. The suppository, whose main ingredient is eugenol / clove oil, can effectively inhibit Staphylococcus aureus, Escherichia coli, and Shigella dysenteriae, which are common bacteria in the urinary and digestive systems. However, the long-term stability and shelf life of the suppository prepared in this patent still need to be improved. Due to the different properties of different drugs, the choice of suppository base may vary. Currently, there are no reports on the use of basil volatile oil as a single antibacterial ingredient to prepare a long-term stable, effective, soluble, and releasable vaginal suppository for the treatment of vaginitis caused by Candida albicans. Summary of the Invention

[0005] The purpose of the present invention is to overcome the above-mentioned defects and deficiencies in the prior art and to provide a basil volatile oil vaginal suppository.

[0006] The second object of the present invention is to provide a method for preparing a basil volatile oil vaginal suppository.

[0007] The third object of the present invention is to provide an application of a basil volatile oil vaginal suppository in preparing a product for treating vaginitis.

[0008] The above-mentioned object of the present invention is achieved through the following technical solutions:

[0009] The invention provides a basil volatile vaginal oil suppository. The suppository is composed of a mixture of a water-soluble base, an oily base, basil volatile oil and an emulsifier; the water-soluble base is distilled water, polyethylene glycol 4000 and polyethylene glycol 6000; the oily base is mixed fatty acid glyceride (stearin); and the mass ratio of the water-soluble base to the oily base in the suppository is 8:8-10.

[0010] Because the vaginal environment is relatively moist and the vaginal mucosa is relatively delicate, it is required to be able to soften and slowly dissolve and release drugs at body temperature, and to play a role locally and continuously. In the selection of the matrix, it is necessary to avoid using highly irritating materials. In order to explore the vaginal suppository matrix suitable for coating basil oil, the present invention has found that the long-term stability and shelf life of suppositories using only water-soluble matrix are poor, while suppositories using only oleaginous matrix not only irritate the vaginal mucosa but also release time is too fast. Only by using a specific water-soluble matrix and an oleaginous matrix and mixing the two in a specific ratio to prepare a basil volatile oil vaginal suppository can the suppository be formed and have moderate hardness, are not easy to deform, have good plasticity and stability, have moderate dissolution time, and have good solubility, prevent the drug from being absorbed too quickly or too slowly in the human body, ensure that the absorption of the drug in the body reaches the desired effect, can stably release the drug in the vagina, and can reduce the irritation to the vaginal mucosa. It has an accurate therapeutic effect in the treatment of vaginitis caused by Candida albicans and can be directly applied to the affected area to quickly relieve symptoms; relative to oral medications, the concentration and absorption of the suppository in the body are low, and the side effects are low. The oily matrix is ​​a mixed fatty acid glyceride (stearin), which is a mixture of monoglycerides, diesters and triesters of C8 to C18 saturated fatty acids. It has a relatively suitable melting point and can gradually soften at body temperature, thereby releasing the drug.

[0011] Furthermore, the mixed fatty acid glyceride (hard fat) is type 36, and has a melting point of 35-37°C. 35-37°C is within the standard body temperature range of the human body, and this melting point is conducive to melting in the body and drug release when the suppository is used.

[0012] Furthermore, the mass ratio of the water-soluble matrix, the oily matrix, the basil volatile oil and the emulsifier is 8:8-10:1-2:1-2.

[0013] Furthermore, the mass ratio of the water-soluble matrix, the oily matrix, the basil volatile oil and the emulsifier is 8:9:1.6:1.8.

[0014] Furthermore, the mass ratio of distilled water, polyethylene glycol 4000, and polyethylene glycol 6000 in the water-soluble matrix is ​​1-2:2-3:3-5.

[0015] Furthermore, the mass ratio of distilled water, polyethylene glycol 4000, and polyethylene glycol 6000 in the water-soluble matrix is ​​1.6:2.4:4.

[0016] Furthermore, the mass ratio of the water-soluble base to the oily base in the suppository is 8:9. The amount of the oily base and the water-soluble base has a significant impact on the formability and hardness of the suppository. When the water-soluble base:oily base = 8:9, the suppository has good formability and moderate hardness.

[0017] Preferably, the suppository is made from the following ingredients in the following weight ratio: 1.6 parts distilled water, 2.4 parts polyethylene glycol 4000, 4 parts polyethylene glycol 6000, 1.8 parts emulsifier, 1.6 parts basil essential oil, and 9 parts mixed fatty acid glycerides (stearin). This results in optimal suppository plasticity, solubility, and stability, as well as good release characteristics.

[0018] Furthermore, the emulsifier in the suppository is Tween-80.

[0019] The present invention provides a method for preparing the basil volatile oil vaginal suppository, comprising the following steps:

[0020] S1. Distilled water, polyethylene glycol 4000, and polyethylene glycol 6000 were mixed and heated to melt to obtain a water-soluble matrix;

[0021] S2. The mixed fatty acid glycerides (stearin) are heated and melted to obtain an oily matrix;

[0022] S3. injecting the oily matrix into the water-soluble matrix, adding an emulsifier and basil essential oil to mix, and demoulding to obtain the basil essential oil vaginal suppository.

[0023] Furthermore, the heating temperature is 65-70° C. According to the properties of the main drug, a water bath melting temperature of 65-70° C. is selected to prevent the drug from being oxidized during the preparation process and causing a decrease in content.

[0024] Furthermore, the preparation method of basil volatile oil in step S3 is to mix basil with distilled water, heat and distill to extract.

[0025] Preferably, dried basil plants are crushed, distilled water is added at a feed ratio of 1.0:30.0 (g:mL), and the mixture is thoroughly mixed. The mixture is then refluxed in a volatile oil extractor for 4-5 hours until the amount of oil in the measuring vessel no longer increases. Heating is then stopped to obtain the volatile oil, which is then dried to obtain a yellow oily liquid with an aromatic odor, namely, basil volatile oil. The average extraction yield of the prepared basil volatile oil is 0.607%.

[0026] Furthermore, the demoulding method in step S3 is to apply a lubricant of detergent: glycerin: 95% ethanol = 1: 0.5-1.5: 4-6 to the mold.

[0027] Furthermore, in order to facilitate demoulding in step S3, the lubricant applied to the mold is detergent: glycerol: 95% ethanol = 1:1:5.

[0028] The present invention uses steam distillation to extract volatile oil components from the herbal medicinal plant basil based on their volatility. Based on the volatile oil extraction rate and the oral medication dosage, the mass of the main drug contained in the corresponding number of suppositories is obtained. During the preparation process, the mass of the oily matrix is ​​greater than the mass of the water-soluble matrix. At a certain temperature, the oily matrix is ​​slowly injected into the water-soluble matrix and stirred to mix evenly, ensuring that the suppository matrix has good formability, a smooth surface, good stability, and substantially uniform quality, meeting quality standard requirements. This ensures both patient comfort and convenience during use, as well as the ability of the suppository to remain stably in the body and evenly release the drug. Secondly, to ensure smooth demoulding, a lubricant needs to be applied to the mold. The lubricant is a 1:1:5 ratio of detergent: glycerol: 95% ethanol.

[0029] The present invention also provides an application of a basil volatile oil vaginal suppository in preparing a product for treating vaginitis.

[0030] Furthermore, the vaginitis is candidal vaginitis.

[0031] Furthermore, the candidal vaginitis is candida albicans vaginitis.

[0032] Compared with the prior art, the present invention has the following beneficial effects:

[0033] The present invention provides a basil volatile oil vaginal suppository, which is composed of a water-soluble base, an oily base, basil volatile oil, and an emulsifier. By using a specific water-soluble base and an oily base mixed in a specific ratio to prepare the basil volatile oil vaginal suppository, the basil volatile oil vaginal suppository can be formed with moderate hardness, is not easily deformed, has good plasticity and stability, and has a moderate dissolution time and good solubility. This prevents the drug from being absorbed too quickly or too slowly in the human body, ensuring that the drug is absorbed in the body to achieve the desired effect. It can both stably release the drug in the vagina and reduce irritation to the vaginal mucosa. It has a precise therapeutic effect in treating vaginitis caused by Candida albicans and can be directly applied to the affected area to quickly relieve symptoms. Compared with oral medications, the suppository has a lower concentration and absorption in the body and has fewer side effects. Furthermore, the vaginal suppository of the present invention avoids the use of multiple processes, specialized equipment, and high-quality raw materials, resulting in low production costs. The sole basil volatile oil component serves as the active ingredient, making it easy to collect and statistically analyze the efficacy evaluation and adverse reactions of the vaginal suppository during use. BRIEF DESCRIPTION OF THE DRAWINGS

[0034] Figure 1 The invention discloses a preparation process of basil essential oil vaginal suppository. DETAILED DESCRIPTION

[0035] The present invention will be further described below with reference to the accompanying drawings and specific examples, but the examples do not limit the present invention in any way. Unless otherwise specified, the reagents, methods and equipment used in the present invention are conventional reagents, methods and equipment in the art.

[0036] Unless otherwise specified, the reagents and materials used in the following examples were commercially available.

[0037] The mixed fatty acid glyceride (stearin) is type 36, has a melting point of 35 to 37 degrees Celsius, and is purchased from Shandong Ruisheng Pharmaceutical Excipients Co., Ltd.

[0038] Example 1 Extraction of basil essential oil

[0039] Dried basil plants were pulverized using a YB-1000A high-speed multifunctional pulverizer (Yongkang Sufeng Industry and Trade Co., Ltd.). Distilled water was added at a ratio of 1.0:30.0 (g:mL), and the mixture was shaken. The extract was then refluxed in a volatile oil extractor for 4–5 hours until the oil level in the analyzer ceased to increase. Heating was then stopped to obtain the volatile oil. The extract was dried over anhydrous sodium sulfate to obtain a yellow oily liquid with an aromatic odor. The extract was sealed in a suitable EP tube and stored for later use.

[0040] After multiple extraction experiments, the average extraction rate of volatile oil was 0.607%.

[0041] Example 2 Inhibitory Effect of Basil Volatile Oil on Candida albicans

[0042] The drug sensitivity test was used to conduct antibacterial experiments on different concentrations of basil essential oil. Candida albicans liquid (10 6 ~10 7 200 μL (100 CFU / mL) of the test strain suspension was added to the solid culture medium and evenly spread using a spreader. Basil essential oil was diluted with acetone to five concentrations of 100%, 50%, 25%, 12.5%, and 6.25%. Sterilized blank antimicrobial susceptibility strips were picked up with sterile tweezers and soaked in each of the five concentrations of basil essential oil. After soaking for 20 minutes, the strips were removed and allowed to dry slightly. The antimicrobial susceptibility strips were then applied to plates coated with Candida albicans. Three antimicrobial susceptibility strips were applied to each plate, forming a regular triangle: a positive control, a blank control, and the test essential oil. The positive control was a 2% chlorhexidine solution (diluted according to the above concentration gradient), and the blank control was acetone. The plates were incubated in an inverted, electrically heated, water-tight incubator at 28°C for 48 hours. The diameters of the inhibition zones were measured and the average values ​​were used for analysis. The experiment was repeated three times.

[0043] The results are shown in Table 1. Essential oil concentrations of 100%, 50%, 25%, 12.5%, and 6.25% showed antibacterial activity against Candida albicans. At a 100% volatile oil concentration, the average inhibition zone diameter was 17.00 mm, indicating high sensitivity. At a 50% volatile oil concentration, the average inhibition zone diameter was 14.20 mm; at a 25% volatile oil concentration, the average inhibition zone diameter was 12.33 mm; and at a 12.5% ​​volatile oil concentration, the average inhibition zone diameter was 10.67 mm, indicating moderate sensitivity. At a 6.25% volatile oil concentration, the average inhibition zone diameter was 7.67 mm, indicating low sensitivity. The blank control showed no inhibition zone. The inhibition zones produced at different concentrations of the positive control are shown in Table 1.

[0044] Table 1 Antibacterial effect of different concentrations of basil essential oil on Candida albicans

[0045]

[0046] Example 3 Optimization of the prescription of basil essential oil vaginal suppository

[0047] 1. Determination of volatile oil content in basil

[0048] The oral dosage of the medicinal plant basil, or decoction, is approximately 10-15g. The suppository dosage is at least equivalent to the oral dosage. Based on the extraction rate of basil volatile oil, the initial dosage per suppository is 0.08g. The dosage is one suppository once daily. This product is primarily intended for adults. To meet the drug loading and molding requirements of the suppository, the designed suppository size (weight) is approximately 1.0g.

[0049] 2. Preparation of suppositories

[0050] The preparation flow chart of suppositories is as follows Figure 1 As shown:

[0051] Take the prescribed amount of PEG4000 (polyethylene glycol 4000) and PEG6000 (polyethylene glycol 6000) and place them in an evaporating dish. Take the prescribed amount of distilled water and add the distilled water to the evaporating dish containing polyethylene glycol. Heat it in a water bath at 65-70°C. Stop heating when 2 / 3 of the matrix is ​​melted and stir to dissolve it completely to obtain a water-soluble matrix.

[0052] Take the prescribed amount of mixed fatty acid glycerides (stearin) in an evaporating dish and heat it in a water bath at 65-70°C. Stop heating when 2 / 3 of the matrix is ​​melted and stir until it is completely dissolved to obtain the oily matrix.

[0053] Slowly pour the oily base into the water-soluble base and stir evenly. Add the prescribed amount of Tween-80 and basil essential oil and stir evenly. When the mixture becomes viscous, cool it slightly and pour it into a suppository mold coated with a lubricant (the prescription is: detergent: glycerin: 95% ethanol = 1:1:5). After cooling and solidification, cut off the overflowing part of the mold and demold it to obtain a vaginal suppository containing basil essential oil.

[0054] 3. Determination of the ratio of water-soluble base to oily base in suppositories

[0055] The matrix and drug dosage ratio selected for a suppository formulation must be rationally designed, possessing appropriate properties such as plasticity, solubility, and stability to ensure smooth vaginal suppository preparation and optimal release characteristics. The ratio of the water-soluble matrix to the oily matrix is ​​a key factor. Therefore, different ratios of water-soluble matrix to oily matrix were used to investigate their effects on the appearance of vaginal suppositories.

[0056] The results, as shown in Tables 2 and 3, show that when the ratio of the water-soluble matrix to the oily matrix is ​​8:9, the water-soluble matrix comprises PEG6000 and PEG4000, and the oily matrix is ​​a mixed fatty acid glyceride (stearin), the suppositories can be formed and have a moderate hardness. Therefore, to achieve the objectives of the present invention, the present invention adopts the following formulation: 0.80g of distilled water, 1.20g of PEG4000 (polyethylene glycol 4000), 2.00g of PEG6000 (polyethylene glycol 6000), 0.90g of Tween-80, 0.80g of basil essential oil, and 4.50g of mixed fatty acid glyceride (stearin) to prepare 10 basil essential oil vaginal suppositories that inhibit Candida albicans.

[0057] Table 2 Screening of suppository prescriptions combining water-soluble base and oily base

[0058]

[0059] Table 3 Effects of different oily bases on water-soluble bases and oily base combined suppositories

[0060]

[0061] 4. Comparison of different matrix suppository prescriptions

[0062] In order to screen out suppositories with the best plasticity, solubility and stability, the present invention performs prescription optimization:

[0063] Prescription 1: Ten basil essential oil vaginal suppositories were prepared using only a water-soluble matrix: distilled water 1.70 g, PEG 4000 (polyethylene glycol 4000) 2.55 g, PEG 6000 (polyethylene glycol 6000) 4.25 g, Tween-80 0.90 g, and basil essential oil 0.80 g. The water-soluble matrix was a 5:3:2 ratio of PEG 6000:PEG 4000:distilled water. The hot-melt method was used to prepare these 10 vaginal suppositories.

[0064] Prescription 2: Only an oily matrix, i.e., 0.80 g of basil essential oil, 0.90 g of Tween-80, and 8.50 g of mixed fatty acid glycerides (stearin), was used to prepare 10 basil essential oil vaginal suppositories by the hot melt method.

[0065] Prescription 3: A combination of a water-soluble matrix and an oily matrix was used. The optimal ratio of the water-soluble matrix to the oily matrix was adjusted and screened. The final composition was 0.80g distilled water, 1.20g PEG4000 (polyethylene glycol 4000), 2.00g PEG6000 (polyethylene glycol 6000), 0.90g Tween-80, 0.80g basil essential oil, and 4.50g type 34 mixed fatty acid glycerides (stearin). Ten basil essential oil vaginal suppositories were prepared using the hot melt method at a ratio of 8:9.

[0066] Prescription 4: A combination of a water-soluble matrix and an oily matrix was used. The optimal ratio of the water-soluble matrix to the oily matrix was adjusted and screened. The final composition was 0.80g distilled water, 1.20g PEG4000 (polyethylene glycol 4000), 2.00g PEG6000 (polyethylene glycol 6000), 0.90g Tween-80, 0.80g basil essential oil, and 4.50g type 36 mixed fatty acid glycerides (stearin). Ten basil essential oil vaginal suppositories were prepared using the hot melt method at a ratio of 8:9.

[0067] Prescription 5: A combination of a water-soluble matrix and an oily matrix was used. The optimal ratio of the water-soluble matrix to the oily matrix was adjusted and screened. The final composition was 0.80g distilled water, 1.20g PEG4000 (polyethylene glycol 4000), 2.00g PEG6000 (polyethylene glycol 6000), 0.90g Tween-80, 0.80g basil essential oil, and 4.50g type 38 mixed fatty acid glycerides (stearin). Ten basil essential oil vaginal suppositories were prepared using the hot melt method at a ratio of 8:9.

[0068] Prescription 6: A combination of a water-soluble matrix and an oily matrix was used. The optimal ratio of the water-soluble matrix to the oily matrix was adjusted and screened. The final composition was 0.80g distilled water, 1.20g PEG4000 (polyethylene glycol 4000), 2.00g PEG6000 (polyethylene glycol 6000), 0.90g Tween-80, 0.80g basil essential oil, and 4.50g type 40 mixed fatty acid glycerides (stearin). Ten basil essential oil vaginal suppositories were prepared using the hot melt method at a ratio of 8:9.

[0069] Prescription 7: A combination of a water-soluble matrix and an oily matrix was used. The optimal ratio of the water-soluble matrix to the oily matrix was adjusted and screened. The final composition was 0.80g distilled water, 1.20g PEG4000 (polyethylene glycol 4000), 2.00g PEG6000 (polyethylene glycol 6000), 0.90g Tween-80, 0.80g basil essential oil, and 4.50g glyceryl monostearate. Ten basil essential oil vaginal suppositories were prepared using the hot melt method at a ratio of 8:9.

[0070] Referring to the quality standards under the Suppository column in Part 4, General Chapter 0107 of the 2020 edition of the "Chinese Pharmacopoeia", the appearance properties and melting time differences of the three prescription suppositories were screened to obtain the prescription with the best plasticity, solubility and stability.

[0071] The results are shown in Table 4. The combined water-soluble and oleaginous matrix of Prescription 3 had a complete and smooth appearance, moderate hardness, and good plasticity. The pure water-soluble matrix of Prescription 1 had a melting time of over 40 minutes, while the pure oleaginous matrix of Prescription 2 had a melting time of 23 minutes and 13 seconds. Comparing the water-soluble matrix and the combined oleaginous matrix, the pure water-soluble matrix had an excessively long dissolution time, while the pure oleaginous matrix had an excessively short dissolution time. The combination of a water-soluble matrix and an oleaginous matrix provides a moderate dissolution time and good solubility, preventing the drug from being absorbed too quickly or too slowly in the human body and ensuring optimal absorption within the body. Furthermore, the pure water-soluble matrix suppository exhibited slight dissolution after being placed at room temperature for 1 hour. Compared to the pure oleaginous matrix, the water-soluble matrix, and the combined oleaginous matrix, the pure water-soluble matrix suppository had poor stability. In summary, the combined water-soluble and oleaginous matrix suppository formulation was optimal. At the same time, different types of mixed fatty acid glycerides (stearin) and monostearate glyceryl (formula 4-formula 7) were compared, and it was found that the stability and solubility of mixed fatty acid glycerides (stearin) were better than those of monostearate glyceryl. Since different types of mixed fatty acid glycerides (stearin) have different dissolution temperatures, type 36 mixed fatty acid glyceride (stearin) was comprehensively selected as the oily base in the suppository of the present invention.

[0072] Table 4 Screening of different matrix suppository prescriptions

[0073]

[0074] Example 4 Quality Inspection of the Optimal Prescription of Basil Volatile Oil Vaginal Suppositories

[0075] According to the preparation method and preferred prescription in Example 3, 10 complete basil volatile oil vaginal suppositories were prepared, weighed, and their properties were observed. The quality evaluation was performed with reference to the quality standards under the general chapter 0107 suppositories in Part IV of the 2020 edition of the Chinese Pharmacopoeia.

[0076] 1. Appearance inspection

[0077] All three batches of suppositories were white, conical in shape, with a smooth, intact appearance. They were well-formed, possessed moderate hardness, were not easily deformed, and exhibited good plasticity. After standing at room temperature for 1 hour, no surface dissolution was observed, demonstrating excellent stability.

[0078] 2. Weight difference check

[0079] Take 10 test sample pellets and accurately weigh them on a BT125D 1 / 100,000 analytical balance (Shanghai Tianmei Balance Instrument Co., Ltd.). After calculating the average pellet weight, accurately weigh each pellet separately. Compare the weight of each pellet with the average pellet weight. According to the Chinese Pharmacopoeia (2020 edition), no more than one pellet should exceed the weight difference limit, and the difference should not exceed 100% of the limit.

[0080] The results are shown in Tables 5 to 7. According to the requirements of the 2020 edition of the Chinese Pharmacopoeia, the average particle weight is above 1.0g and below 3.0g, and the weight difference limit is ±7.5%. After inspection of the three batches of suppositories, there were 0 suppositories exceeding the weight difference limit, and 0 suppositories exceeding the limit by 1 times, which proves that the weight difference inspection of the three batches of suppositories complies with the regulations.

[0081] Table 5 Batch 1 weight difference limit check

[0082]

[0083] Table 6 Batch 2 weight difference limit check

[0084]

[0085] Table 7 Batch 3 weight difference limit check

[0086]

[0087] 3. Melting time limit inspection

[0088] Take three pellets of the test sample and, after standing at room temperature for one hour, place them on the lower circular plates of the three metal racks of an RBY-4A automatic melting time detector (Tianjin Tianda Tianfa Technology Co., Ltd.), insert them into their respective sleeves, and secure them with hooks. Each of these devices should be vertically immersed in a container containing at least 4 L of water at 37.0°C ± 0.5°C, with the top position 90 mm below the water surface. A rotator should be installed in the container to flip the device in the solution every 10 minutes, and the dissolution time should be recorded.

[0089] The results are shown in Table 8. According to the melting time data of three batches of suppositories, the suppositories can be completely dissolved within 24 minutes to 32 minutes, and the solubility is good.

[0090] Table 8 Results of the melting time limit inspection of each batch of suppositories

[0091] .

Claims

1. A basil volatile oil vaginal suppository, characterized in that: The suppository is composed of a mixture of a water-soluble base, an oily base, basil volatile oil, and an emulsifier; the water-soluble base is distilled water, polyethylene glycol 4000, and polyethylene glycol 6000; the oily base is mixed fatty acid glycerides; the suppository is made of the following raw materials in the following weight ratio: 1.6 parts of distilled water, 2.4 parts of polyethylene glycol 4000, 4 parts of polyethylene glycol 6000, 1.8 parts of emulsifier, 1.6 parts of basil volatile oil, and 9 parts of mixed fatty acid glycerides; the emulsifier is Tween-80.

2. The method for preparing the basil volatile oil vaginal suppository according to claim 1, wherein The following steps are involved: S1. Distilled water, polyethylene glycol 4000, and polyethylene glycol 6000 were mixed and heated to melt to obtain a water-soluble matrix; S2. The mixed fatty acid glycerides were heated and melted to obtain an oily matrix; S3. injecting the oily matrix into the water-soluble matrix, adding an emulsifier and basil essential oil to mix, and demoulding to obtain the basil essential oil vaginal suppository.

3. The preparation method according to claim 2, characterized in that: The heating temperature is 65-70°C.

4. The preparation method according to claim 2, characterized in that The preparation method of the basil essential oil in step S3 is to mix basil with distilled water, heat and perform distillation extraction.

5. Use of the basil volatile oil vaginal suppository according to claim 1 in preparing a medicament for treating vaginitis.

6. The application according to claim 5, characterized in that The vaginitis is candidal vaginitis.

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