Fluconazole capsule and its preparation method

Abstract

The application belongs to the field of pharmaceutical preparations, and particularly relates to a fluconazole capsule and a preparation method thereof. The fluconazole capsule comprises a hollow capsule and a filling in the hollow capsule, and the filling is a fluconazole composition. The fluconazole composition comprises the following components by weight per 1000 capsules: 50g of fluconazole, 10-20g of spirulina extract, 5-15g of micronized silica gel, 0.1-1g of sodium alginate and 1-10g of naked flower purple perilla extract. The fluconazole capsule composition of the application adds the spirulina extract and the naked flower purple perilla extract in the fluconazole medicine, and adds the micronized silica gel and the sodium alginate, so that the flowability of the prepared composition is greatly improved, the medicine is uniformly dispersed, and the fluconazole capsule is beneficial to be divided. The prepared fluconazole capsule is uniform in quality, and the stability is greatly improved, so that the fluconazole capsule provides a guarantee for clinical use.

Description

TECHNICAL FIELD

[0001] The present application belongs to the field of pharmaceutical preparation, and particularly relates to a fluconazole capsule and a preparation method thereof. BACKGROUND

[0002] Fluconazole is a medicine for treating fungal infection, and is a broad-spectrum antifungal drug. It is effective against fungal infection of human and various animals, such as candida infection (including systemic candidiasis of human and animals with normal or impaired immunity), cryptococcus neoformans infection (including intracranial infection), malassezia furfur, microsporum, trichophyton, epidermophyton, blastomyces dermatitidis, coccidioides immitis (including intracranial infection), and histoplasma capsulatum, cladosporium carrionii, and so on. Among them, fluconazole capsule is a commonly used dosage form in clinic. In order to ensure the bioavailability and stability of fluconazole capsule, the effect is often achieved through improvement of auxiliary materials or process, but there are still problems such as poor fluidity and poor stability, which seriously affect the clinical efficacy of fluconazole. SUMMARY

[0003] The present application provides a fluconazole capsule and a preparation method thereof, which can effectively improve the fluidity of fluconazole and the stability of the capsule, and lays a foundation for the clinical use of fluconazole.

[0004] The technical scheme of the present application is implemented as follows:

[0005] A fluconazole composition, including the following components by weight per 1000 capsules: 50g of fluconazole, 10-20g of spirulina extract, 5-15g of micronized silica gel, 0.1-1g of sodium alginate, and 1-10g of extract of naked flowered purple gem.

[0006] Further, the fluconazole composition includes the following components by weight per 1000 capsules: 50g of fluconazole, 15g of spirulina extract, 10g of micronized silica gel, 0.5g of sodium alginate, and 5g of extract of naked flowered purple gem.

[0007] Further, the preparation method of the spirulina extract is as follows:

[0008] Dry spirulina powder is taken, crushed, and then soaked in water at 3-4 times the weight of the spirulina at 80-90 DEG C for 1-2 hours. The precipitate is removed, and the medicinal liquid is dried to obtain the spirulina extract.

[0009] Further, the preparation method of the extract of naked flowered purple gem is as follows:

[0010] Dry naked flowered purple gem medicinal material is taken, crushed, and then soaked in water at 3-4 times the weight of the medicinal material at 80-100 DEG C for 1-2 hours. The precipitate is removed, and the medicinal liquid is dried to obtain the extract of naked flowered purple gem.

[0011] A preparation method of fluconazole composition, comprising the following steps:

[0012] (1) respectively take spirulina extract and naked flower purple pearl extract, crush and sieve;

[0013] (2) take the formula amount of fluconazole, micro powder silica gel, sodium alginate and the crushed spirulina extract and naked flower purple pearl extract, mix evenly.

[0014] Further, the spirulina extract and naked flower purple pearl extract are crushed and sieved through 40-60 mesh.

[0015] The above-mentioned fluconazole composition is applied to the preparation of fluconazole capsules.

[0016] A fluconazole capsule, comprising a hollow capsule and a filling material filled in the hollow capsule; the filling material is the above-mentioned fluconazole composition.

[0017] A preparation method of fluconazole capsule, comprising the following steps:

[0018] Take the fluconazole composition, and according to the dosage, pack into the hollow capsule.

[0019] Beneficial effects:

[0020] The fluconazole capsule composition disclosed in the application adds spirulina extract and naked flower purple pearl extract to fluconazole medicine, and adds micro powder silica gel and sodium alginate, so that the prepared composition has greatly improved flowability, the medicine is uniformly dispersed, and the filling of the fluconazole capsule is facilitated. The prepared fluconazole capsule has uniform quality and greatly improved stability, which provides guarantee for the clinical use of fluconazole. DETAILED DESCRIPTION

[0021] The application will be further described below in combination with specific implementation modes, so that the application can be better understood.

[0022] Example 1

[0023] A fluconazole composition, 1000 capsules comprising the following components by weight: fluconazole 50g, spirulina extract 10g, micro powder silica gel 5g, sodium alginate 0.1g, naked flower purple pearl extract 10g.

[0024] A preparation method of fluconazole composition, comprising the following steps:

[0025] (1) respectively take spirulina extract and naked flower purple pearl extract, crush and sieve through 40 mesh respectively;

[0026] (2) take the formula amount of fluconazole, micro powder silica gel, sodium alginate and the crushed spirulina extract and naked flower purple pearl extract, mix evenly.

[0027] Example 2

[0028] A fluconazole composition, including the following components by weight per 1000 capsules: fluconazole 50g, spirulina extract 15g, micro-silica 10g, sodium alginate 0.5g, and naked flower-lavender extract 5g.

[0029] A method for preparing a fluconazole composition, comprising the following steps:

[0030] (1) separately taking spirulina extract and naked flower-lavender extract, crushing and then passing through a 60-mesh sieve;

[0031] (2) taking the formula amount of fluconazole, micro-silica, sodium alginate, and the crushed spirulina extract and naked flower-lavender extract, mixing uniformly to obtain.

[0032] Example 3

[0033] A fluconazole composition, including the following components by weight per 1000 capsules: fluconazole 50g, spirulina extract 20g, micro-silica 15g, sodium alginate 1g, and naked flower-lavender extract 1g.

[0034] A method for preparing a fluconazole composition, comprising the following steps:

[0035] (1) separately taking spirulina extract and naked flower-lavender extract, crushing and then passing through a 40-mesh sieve;

[0036] (2) taking the formula amount of fluconazole, micro-silica, sodium alginate, and the crushed spirulina extract and naked flower-lavender extract, mixing uniformly to obtain.

[0037] In the above examples, the preparation method of the spirulina extract is:

[0038] Take spirulina dry powder, crush, add water 3-4 times the weight of spirulina, heat to 80-90℃, hot soak for 1-2h, remove the precipitate, and dry the liquid to obtain the spirulina extract.

[0039] The preparation method of the naked flower-lavender extract is:

[0040] Take dried naked flower-lavender medicinal material, crush, add water 3-4 times the weight of the medicinal material, heat to 80-100℃, hot soak for 1-2h, remove the precipitate, and dry the liquid to obtain the naked flower-lavender extract.

[0041] Example 4

[0042] A fluconazole capsule, including a hollow capsule and a filling material filled in the hollow capsule; the filling material is the fluconazole composition according to any one of examples 1-3.

[0043] A preparation method of fluconazole capsules, comprising the following steps:

[0044] The fluconazole composition is divided into empty capsules according to the dosage.

[0045] The fluconazole composition described in the present application is investigated in quality

[0046] The rest angle is the largest angle formed by the free inclined plane of the powder accumulation layer and the horizontal plane, and is the simplest method for testing the flowability of the powder. The compression degree reflects the cohesiveness and soft state of the powder, and is an important indicator of the flowability of the powder. Therefore, the rest angle and the compression degree of the fluconazole compositions prepared by different methods are measured respectively, and the flowability differences of the fluconazole compositions are compared. The rest angle is measured by the fixed cone method, the powder is introduced into the funnel, the powder is allowed to fall freely from the funnel, and a cone with a height of h and a radius of r is formed on the disc. The rest angle is calculated by measuring the height h and the radius r of the powder layer. When measuring the compression degree, the weighed powder is loaded into the measuring cylinder, and the initial volume is measured. Then, the measuring cylinder is tapped until the volume of the powder no longer changes, which is the final volume. The compression degree is calculated according to the volume change.

[0047] The experiment is divided into 5 groups, of which 3 are example groups and 2 are control groups. When measuring, the rest angle and the compression degree of the fluconazole compositions prepared by the 3 examples and the 2 control groups are measured respectively. The compositions of the 2 control groups are as follows: control group 1: fluconazole 50g, micro-powder silica gel 10g, sodium alginate 0.5g, and naked flower purple gem extract 5g; control group 2: fluconazole 50g, micro-powder silica gel 10g, and sodium alginate 0.5g. The preparation method of the compositions of the 2 control groups is according to example 2. The measurement results are shown in table 1.

[0048] Table 1: Difference in rest angle and compression degree of different fluconazole compositions

[0049]

[0050]

[0051] As can be seen from table 1, the rest angle of examples 1-3 is between 30-35°, and the rest angle of the 2 control examples is higher than that of the 3 examples; the compression degree of examples 1-3 is maintained at 11-19%, which is also much lower than that of the 2 control examples. Therefore, the powder flowability of examples 1-3 is better, and the powder flowability of the 2 control examples is significantly reduced by changing the composition of the composition, which is significantly lower than that of the 3 examples.

[0052] The stability of the fluconazole composition described in the present application is investigated

[0053] Fluconazole capsules were prepared according to the method of Example 4, with the component allocation ratio of Examples 1-3 and Control Groups 1-2, and were packaged in aluminum plastic according to the market standard. The samples were taken at the end of the 0th, 1st, 2nd, 3rd, and 6th months, respectively, for content determination, and the content changes of the active ingredient in the fluconazole capsules prepared by different preparation methods were compared.

[0054] Table 2 Content change determination of fluconazole in fluconazole capsules with different component allocation ratios (%)

[0055] 0 months 1 month 2 months 3 months 6 months Example 1 99.51 100.32 100.13 99.46 99.75 Example 2 99.16 99.78 100.22 100.09 99.03 Example 3 99.95 99.89 100.08 100.10 99.43 Control 1 100.01 101.15 90.13 81.76 75.32 Control 2 99.57 99.48 100.19 89.26 80.17

[0056] As shown in Table 2, through the accelerated stability experiment, the content of fluconazole in the capsules prepared according to the material allocation ratios of the three examples of the present application can be kept relatively stable during the experiment. The content of fluconazole in Control Group 1 significantly decreased at the 2nd month, and the content of fluconazole in Control Group 2 significantly decreased at the 3rd month, until the end of the 6th month experiment, the content of fluconazole in the two control groups decreased more significantly. It shows that the stability of the fluconazole capsules described in the present application is higher than that of the two control groups.

[0057] The above describes the specific examples of the present application in detail, but it is only as an example, the present application is not limited to the specific examples described above. For those skilled in the art, any equivalent modification and substitution to the present application are also within the scope of the present application. Therefore, any equivalent transformation and modification without departing from the spirit and scope of the present application should be covered within the scope of the present application.

Claims

1. A fluconazole composition, characterized in that, Each 1000 capsules contains the following components by weight: 50g fluconazole, 10-20g spirulina extract, 5-15g micronized silica gel, 0.1-1g sodium alginate, and 1-10g Callicarpa nudiflora extract. The preparation method of the spirulina extract is as follows: Take spirulina powder, pulverize it, add 3-4 times the weight of water to spirulina, heat to 80-90℃ and soak for 1-2 hours, remove the precipitate, and dry the liquid to obtain spirulina extract. The preparation method of the extract of Callicarpa nudiflora is as follows: Take dried Callicarpa nudiflora, pulverize it, add 3-4 times its weight of water and heat to 80-100℃ for 1-2 hours to soak. Remove the precipitate and dry the liquid to obtain Callicarpa nudiflora extract.

2. The fluconazole composition according to claim 1, characterized in that, Each 1000 capsules contains the following components by weight: 50g fluconazole, 15g spirulina extract, 10g micronized silica gel, 0.5g sodium alginate, and 5g Callicarpa nudiflora extract.

3. A method for preparing a fluconazole composition as described in claim 1 or 2, characterized in that, Includes the following steps: (1) Take Spirulina extract and Callicarpa nudiflora extract respectively, pulverize them and then sieve them; (2) Take the prescribed amounts of fluconazole, micronized silica gel, sodium alginate, and pulverized spirulina extract and Naked Flower Purple Beauty extract, and mix them well to obtain the final product.

4. The method for preparing a fluconazole composition as described in claim 3, characterized in that, The spirulina extract and the Naked Flower Purple Beauty extract were pulverized and passed through a 40-60 mesh sieve.

5. The use of the fluconazole composition as described in claim 1 or 2 in the preparation of fluconazole capsules.

6. A fluconazole capsule, characterized in that: It includes empty capsules and fillers filled within the empty capsules; said filler is the fluconazole composition of claim 1 or 2.

7. A method for preparing fluconazole capsules, characterized in that, Includes the following steps: The fluconazole composition according to claim 1 or 2 can be dispensed into empty capsules according to the dosage.

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