Voriconazole containing tablets

A voriconazole tablet and voriconazole technology, applied in the field of medicine, can solve the problems of tablet dissolution rate difference, low bioavailability, and hindering the treatment of patients, and achieve the effects of small dissolution fluctuation, small dissolution difference, and improved bioavailability

Active Publication Date: 2011-07-27
ZHEJIANG HUAHAI PHARMACEUTICAL CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to the low solubility of voriconazole in water (0.098mg/ml), its solubility is pH-dependent, and its solubility is large at low pH values, and its solubility decreases with the increase of pH value.
This may lead to differences in the...

Method used

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  • Voriconazole containing tablets
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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Embodiment 1 Voriconazole different particle size comparative experiments:

[0028]

[0029] * Voriconazole uses three particle sizes marked 1, 2, and 3 to show the difference. The particle size of voriconazole 1 used in prescription 1 is D (V，0.9) About 200 μm, the voriconazole particle size 2 used in prescription 2 is D (V，0.9) About 100 μm, the voriconazole particle size 3 used in prescription 3 is D (V，0.9) about 40 μm.

[0030] Preparation Process:

[0031] 1. Dissolve the prescribed amount of povidone in an appropriate amount of purified water to make an adhesive for later use;

[0032] 2. Put voriconazole, lactose monohydrate, pregelatinized starch, and croscarmellose sodium into a granulation pot and mix to obtain Mix A;

[0033] 3. Add the binder in step 1 into the granulation pot and granulate with the mixture A to obtain wet granules, granulate the wet granules and dry to obtain dry granules B;

[0034] 4. Add the prescribed amount of magnesium steara...

Embodiment 2

[0043] Embodiment 2 Comparative test of different disintegrant contents of voriconazole tablets

[0044]

[0045]

[0046]* Lactose monohydrate is the filler, and minor changes have little effect on the tablet. Therefore, the components of the excipients in prescriptions 4-6 are the same, and the changed amount of the disintegrant is supplemented by the filler lactose monohydrate accordingly. The preparation process is the same as in Example 1 Same, same control tablet disintegration time.

[0047] Table 3 Dissolution results of prescription 4-6 under pH1.0 dissolution medium

[0048] serial number

[0049] Result analysis: as seen from Table 3, along with the increase of disintegrant content in tablet, the stripping of tablet becomes faster. However, too few disintegrants prevent rapid dissolution, too many disintegrants, the tablet is more likely to absorb moisture, the dissolution is unstable after storage, and the quality of the drug cannot be guaranteed. ...

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Abstract

The invention relates to voriconazole tablets. The particle size of voriconazole in the tablets is controlled in a range of D(V, 0.9) <= 100 mu m, and the content of a disintegrant accounts for 2-6% of the total weight of the tablets. According to the method provided by the invention, voriconazole tablets with a high dissolution rate, small dissolution difference and small dissolution fluctuation among different batches under different pH conditions can be obtained, thus improving the quality and bioavailability of the voriconazole tablets. The invention adopts a conventional wet granulation process which is simple and suitable for commercial production to prepare the voriconazole tablets.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to an antifungal drug voriconazole tablet. Background technique [0002] In recent years, with the widespread development of transplantation and the extensive application of broad-spectrum antibiotics, glucocorticoids, antineoplastic drugs and immunosuppressants, the imbalance of flora and the reduction of the body's resistance to fungi have resulted in superficial and deep mycoses. incidence is increasing. Since fungi and human cells are both eukaryotic cells, they often have considerable toxicity to the host after long-term drug use. At the same time, with the application of antifungal drugs, the drug resistance of fungi is becoming stronger and stronger. Therefore, the research and development of antifungal drugs is particularly urgent, and antifungal drugs with high efficiency and low toxicity have become the guiding direction of research. [0003] Voriconazole (Voriconazole CA...

Claims

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Application Information

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IPC IPC(8): A61K9/20A61K9/28A61K31/505A61P31/10
Inventor 胡李斌肖利思彭俊清李巧霞胡功允
Owner ZHEJIANG HUAHAI PHARMACEUTICAL CO LTD
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