Tacrolimus sustained-release tablets and preparation method thereof
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A technology for tacrolimus and sustained-release tablets, applied in the field of water-insoluble drug tacrolimus sustained-release tablets and its preparation, can solve problems such as complex processes, achieve simple prescription processes, low production costs, and maintain blood drug concentrations Effect
Active Publication Date: 2017-01-11
SHENYANG PHARMA UNIVERSITY
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Embodiment 1
[0049] Embodiment 1: Tacrolimus solid dispersion
[0050] Prescription 1:
[0051] Tacrolimus 10mg
[0052] Glyceryl Behenate 150mg
[0053] Weigh glyceryl behenate, heat and stir in a water bath at 80°C to melt, then lower the temperature to 70°C, add tacrolimus, continue stirring for 3 hours, slowly cool to room temperature, crush, pass through a 60-mesh sieve, and place at 40°C Put it down for 24h. 4h dissolution rate was 95%. After being placed at 40°C for 10 days, the dissolution rate in 4 hours was 80%. It shows that the physical stability of the prescription is not good, and the dissolution rate obviously decreases after being placed.
Embodiment 2
[0054] Embodiment 2: tacrolimus solid dispersion
[0055] Prescription 2:
[0056] Tacrolimus 10mg
[0057] Glyceryl Behenate 75mg
[0058] Macrogol Glyceryl Stearate 75mg
[0059] Weigh glyceryl behenate and polyethylene glycol stearate, heat and stir in a water bath at 80°C to melt, then lower the temperature to 70°C, add tacrolimus, continue stirring for 3 hours, slowly cool to room temperature, and pulverize , passed through a 60-mesh sieve, and placed at 40°C for 24 hours. The dissolution rate in 0.5h is 98%; after 10 days at 40°C, the dissolution rate in 0.5h is 20%. It shows that the physical stability of the prescription is not good, and the dissolution rate obviously decreases after being placed.
Embodiment 3
[0060] Embodiment 3: tacrolimus solid dispersion
[0061] Prescription 3:
[0062] Tacrolimus 10mg
[0063] Glyceryl Behenate 125mg
[0064] Stearic acid 25mg
[0065] Weigh glyceryl behenate and stearic acid, heat, stir and melt in a water bath at 80°C, lower the temperature to 70°C, add tacrolimus, continue stirring for 3 hours, slowly cool to room temperature, pulverize, pass through a 60-mesh sieve, Place it at 40°C for 24h. 4h dissolution rate was 90%.
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Abstract
The invention relates to a water-insoluble drug, namely, tacrolimus sustained-release tablets. The tacrolimus sustained-release tablets take a lipid material, a water-soluble material, a stabilizer and the like as a carrier, and are prepared by adopting a melting method to prepare a solid dispersion which is stable in properties and is capable of obviously improving the dissolution rate of tacrolimus, blending the prepared solid dispersion with a sustained-release material, a diluent and other pharmaceutical necessities, and tabletting the mixture. The tacrolimus sustained-release tablets have the unique advantages that (1) the sustained-release tablets are simple in formulation and technology, and can be formed by directly tabletting powder without adding auxiliary materials such as a lubricating agent and a binding agent; (2) the low-melting-point lipid material is used, the medicine can be directly dissolved in the molten lipid material and is then cooled and cured, and a volatile organic solvent does not need to be treated, so that the production safety is greatly improved, and the environmental pollution is reduced; (3) the quaternary solid dispersion formed by the medicine, the lipid material, the water-soluble material and the stabilizer is good in stability, so that the dissolution rate of the tacrolimus sustained-release tablets does not change significantly after the tacrolimus sustained-release tablets are placed for a period of time; (4) the tacrolimus sustained-release tablets can reduce the times of administration, thus reducing the fluctuation of plasma concentration.
Description
technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and relates to a water-insoluble drug tacrolimus sustained-release tablet and a preparation method thereof. Background technique [0002] At present, improving the dissolution rate and bioavailability of poorly water-soluble drugs is a difficult problem in the field of pharmaceutical preparation research and pharmaceutical production. [0003] Tacrolimus (tacrolimus; FK 506) is a non-dissociative hydrophobic macrolide antibiotic that was first isolated from the fermentation broth of Streptomyces tsukubaensis by Fujisawa Company in Japan. Its molecular formula is C 44 h 69 NO 12 , relative molecular mass is 804.02, melting point is 127-129°C, soluble in methanol, ethanol, acetonitrile and other organic reagents, insoluble in water. [0004] Tacrolimus belongs to the BCS class II drugs, and the main absorption sites of oral administration are in the jejunum and ileum, and the...
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