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Ketoconazole vaginal tablet and preparation method thereof

A technology of ketoconazole and vaginal tablets, which is applied in the direction of pharmaceutical formulas, medical preparations containing active ingredients, and pill delivery, which can solve problems such as unstable product quality, easy deformation, and unqualified effervescent tablets, and improve retention Time and effective concentration, overcoming the effect of easy drug loss and overcoming pollution of clothes

Inactive Publication Date: 2009-11-11
SHANGHAI PUKANG PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] Vaginal suppositories are easy to lead to drug loss and contamination of underwear, and have strict requirements on storage conditions. They need to be stored in airtight storage below 30°C, and they are easily deformed, moldy, and deteriorated when exposed to heat and moisture.
Effervescent tablets have looser temperature requirements and are more convenient to use, but are prone to moisture and have high requirements on production conditions such as temperature and humidity, are not easy to operate, and easily lead to unstable product quality. Qualified report, in addition, effervescent tablets have two parts of acid source and alkali source, ketoconazole is easy to oxidize and change color when it encounters common organic acids, and the stability of effervescent tablets made is poor

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] A preparation method of ketoconazole vaginal tablet, the method comprises the following steps:

[0039] (1) Prepare materials according to the following components and content (weight):

[0040] Ketoconazole 500g

[0041] Sodium carboxymethyl starch 50g

[0042] Sodium bisulfite 50g

[0043] Lactose 680g

[0044] Polysorbate 80 4g

[0045] Povidone K30 20g

[0046] Magnesium stearate 0.5g

[0047] Talc powder 50g

[0048] (2) Preparation of adhesive:

[0049] Dissolving polysorbate 80 and povidone K30 prepared in step (1) with dehydrated alcohol as adhesive, for subsequent use;

[0050] (3) preparation of ketoconazole vaginal tablet

[0051] Fully mix the ketoconazole, sodium bisulfite and lactose prepared in step (1) and pass through an 80-mesh sieve, add the adhesive obtained in step (2) to make a suitable soft material, and granulate with an 18-mesh sieve , dried at 60°C for 5 hours, granulated with a 16-mesh sieve, added sodium carboxymethyl starch, magnes...

Embodiment 2

[0053] A preparation method of ketoconazole vaginal tablet, the method comprises the following steps:

[0054] (1) Prepare materials according to the following components and content (weight):

[0055] Ketoconazole 500g

[0056] Sodium carboxymethyl starch 5g

[0057] Sodium bisulfite 100g

[0058] Lactose 50g

[0059] Polysorbate 80 10g

[0060] Povidone K30 0.5g

[0061] Magnesium Stearate 50g

[0062] Talc powder 0.5g

[0063] (2) Preparation of adhesive:

[0064] Dissolving polysorbate 80 and povidone K30 prepared in step (1) with dehydrated alcohol as adhesive, for subsequent use;

[0065] (3) preparation of ketoconazole vaginal tablet

[0066] Fully mix the ketoconazole, sodium bisulfite and lactose prepared in step (1) and pass through an 80-mesh sieve, add the adhesive obtained in step (2) to make a suitable soft material, and granulate with an 18-mesh sieve , dried at 10°C for 10 hours, sieved with a 16-mesh sieve, added sodium carboxymethyl starch, magnesiu...

Embodiment 3

[0068] A preparation method of ketoconazole vaginal tablet, the method comprises the following steps:

[0069] (1) Prepare materials according to the following components and content (weight):

[0070] Ketoconazole 500g

[0071] Sodium carboxymethyl starch 100g

[0072] Sodium bisulfite 5g

[0073] Lactose 1000g

[0074] Polysorbate 80 0.5g

[0075] Povidone K30 100g

[0076] Magnesium Stearate 25g

[0077] Talc powder 25g

[0078] (2) Preparation of adhesive:

[0079] Dissolving polysorbate 80 and povidone K30 prepared in step (1) with dehydrated alcohol as adhesive, for subsequent use;

[0080] (3) preparation of ketoconazole vaginal tablet

[0081] Fully mix the ketoconazole, sodium bisulfite and lactose prepared in step (1) and pass through an 80-mesh sieve, add the adhesive obtained in step (2) to make a suitable soft material, and granulate with an 18-mesh sieve , dried at 100°C for 1 hour, sized with a 16-mesh sieve, added sodium carboxymethyl starch, magnesiu...

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PUM

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Abstract

The invention relates to a ketoconazole vaginal tablet and a preparation method thereof. The prescription of the vaginal tablet comprises the following components according to the parts by weight: 1 of ketoconazole, 0.01-0.2 of carboxyrnethyl starch sodium, 0.01-0.2 of sodium bisulfite, 0.1-2 of lactose; 0.001-0.02 of polysorbate 80, 0.001-0.2 of polyvidone K30; 0.001-0.1 of magnesium stearate and 0.001-0.1 of talcum powder. Compared with the prior art, the ketoconazole vaginal tablet not only overcomes the defects of easy loss and clothing pollution of pessary, but also avoids the defects of demanding production conditions, inconvenient storage, and the like which are caused by a vaginal effervescent tablet using special accessories. Meanwhile, the ketoconazole vaginal tablet improves the cure effect in using ketoconazole to cure colpitis, reduces toxic and side effects, provides more choices for clinical doctors and patients and is one of ideal ketoconazole partial-vagina administration medicament forms.

Description

technical field [0001] The invention relates to antifungal drugs, in particular to ketoconazole vaginal tablets and a preparation method thereof. Background technique [0002] Ketoconazole is the first oral azole antifungal drug developed in the United States in 1981. It inhibits the synthesis of ergosterol by interfering with the demethylation of ergosterol precursors, resulting in the lack of ergosterol on the fungal cell membrane. , the increased permeability of the membrane cannot maintain normal functions; and the specific activity of the enzymes located on the membrane also changes, and finally inhibits the growth of fungi or causes the death of fungal bacteria. Ketoconazole is clinically used for the treatment of systemic fungal infections, yeast infections of the gastrointestinal tract, chronic and recurrent vaginal candidiasis that is ineffective for topical treatment, and for the prevention and treatment of fungal infections caused by decreased immune function. As...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K31/496A61P15/02A61P31/10
Inventor 倪宏曹济宁
Owner SHANGHAI PUKANG PHARMA
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