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Preparation method and application of tanshinone II A solid dispersion pellets

A solid dispersion, tanshinone technology, applied in the field of medicine, can solve the problems of heat-sensitive drug stability, unfavorable reproducibility and controllability, loss of raw materials and excipients, etc. Simple and feasible, the effect of improving solubility and dissolution rate

Inactive Publication Date: 2011-07-27
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Chinese patent 200510039106.3 discloses a Tanshinone IIA dripping pill, which uses solid dispersion technology to improve the dissolution characteristics of the drug. However, the higher temperature required in the high-temperature melting preparation process will greatly affect the stability of the heat-sensitive drug Tanshinone IIA.
The method has many steps, and the preparation process involves many process parameters, which is not conducive to the reproducibility and controllability of industrial production, and will cause a large loss of raw materials and auxiliary materials, increasing production costs

Method used

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  • Preparation method and application of tanshinone II A solid dispersion pellets
  • Preparation method and application of tanshinone II A solid dispersion pellets
  • Preparation method and application of tanshinone II A solid dispersion pellets

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] Weigh 1.3g of Tanshinone IIA and 6.5g of PVPK30 and dissolve them in 95ml of ethanol, stir until completely dissolved, and wait for the medicine to be applied. Weigh 50g of blank ball cores and add them to the hopper, turn on the fan and heating device, preheat the balls in a fluidized state for a period of time, and start adding medicine. The preparation process parameters of the fluidized bed one-step molding are coating temperature 45°C, blast frequency 30Hz, spray gun spray pressure 0.3MPa, liquid spray rate 5ml / min. After the drug application is completed, the drug-loaded pellets are kept boiling for a period of time in a fluidized state to obtain the final product.

[0031] Fill the solid dispersion pellets into capsules to obtain tanshinone IIA quick-release pellets capsules.

Embodiment 2

[0033] Weigh 1.3g of tanshinone IIA and 10g of PEG4000 and PEG6000 and dissolve them in 75ml of ethanol and 25ml of acetone respectively, heat the acetone solution of polyethylene glycol to dissolve, then add it dropwise into the ethanol solution of tanshinone IIA, stir until completely dissolved, and then apply the medicine. Weigh 50g of blank ball cores and add them to the hopper, turn on the fan and heating device, preheat the balls in a fluidized state for a period of time, and start adding medicine. The preparation process parameters of the fluidized bed one-step molding are coating temperature 35°C, blast frequency 27Hz, spray gun spray pressure 0.25MPa, liquid spray rate 4ml / min. After the drug application is completed, the drug-loaded pellets are kept boiling for a period of time in a fluidized state to obtain the final product.

[0034] The solid dispersion pellets are uniformly mixed with microcrystalline cellulose, pregelatinized starch and magnesium stearate, and t...

Embodiment 3

[0036]Weigh 1.3g of tanshinone IIA and 7.5g of citric acid and dissolve them in 60ml of ethyl acetate and 10ml of 95% ethanol respectively, add the citric acid ethanol solution dropwise into the tanshinone IIA ethyl acetate solution, stir until completely dissolved, and wait for the medicine . Weigh 50g of blank ball cores and add them to the hopper, turn on the fan and heating device, preheat the balls in a fluidized state for a period of time, and start adding medicine. The preparation process parameters of the fluidized bed one-step molding are coating temperature 32°C, blast frequency 25Hz, spray gun spray pressure 0.3MPa, liquid spray rate 3ml / min. After the drug application is completed, the drug-loaded pellets are kept boiling for a period of time in a fluidized state to obtain the final product.

[0037] The solid dispersion pellets are coated with an aqueous dispersion of ethyl cellulose, and the obtained sustained-release pellets are filled in capsules to obtain tan...

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Abstract

The invention belongs to the technical field of medicine, and relates to a preparation method and application of tanshinone II A solid dispersion pellets. The in-vitro dissolution rate of the tanshinone II A solid dispersion pellets prepared by a fluidized bed one-step molding process is remarkably increased, and bioavailability is remarkably improved; and the process is convenient to operate, feasible, high in production efficiency and low in cost, and industrial production is easy to realize.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a method for preparing tanshinone IIA solid dispersion pellets by a fluidized bed one-step molding process and an application thereof. Background technique [0002] Tanshinone IIA is the active ingredient with a relatively high content in the fat-soluble components of Danshen, and it exhibits various pharmacological effects in vivo, such as dilating blood vessels, reducing blood viscosity, anti-platelet aggregation, improving microcirculation and antagonizing angiotensin II, protecting Cardiomyocytes and anti-infection, anti-cancer and other functions. However, the solubility of tanshinone II A in water is only 2.8ng / ml, and the absolute bioavailability of oral administration is lower than 3.5%, which greatly limits its pharmacological effects. Increasing the solubility and dissolution rate of tanshinone IIA by means of pharmacy is one of the ways to improve its oral bioavailab...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K9/22A61K9/52A61K31/58A61P7/02A61P9/10A61P31/00A61P35/00
Inventor 刘建平刘盼李瑾
Owner CHINA PHARM UNIV
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