Preparation method of tacrolimus solid dispersion, quick-release pharmaceutical composition and application

A technology of solid dispersion and tacrolimus, which is applied in the field of medicine, can solve the problems of many steps and inconvenient operation, and achieve the effect of stable quality and good uniformity of release

Pending Publication Date: 2021-11-02
SINOPHARM CHUANKANG PHARMACEUTICAL CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The patented production method has many steps, the operation is not easy, and secondary granulation is required

Method used

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  • Preparation method of tacrolimus solid dispersion, quick-release pharmaceutical composition and application
  • Preparation method of tacrolimus solid dispersion, quick-release pharmaceutical composition and application
  • Preparation method of tacrolimus solid dispersion, quick-release pharmaceutical composition and application

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preparation example Construction

[0028] In the first aspect, an embodiment of the present invention provides a method for preparing a tacrolimus solid dispersion, comprising the following steps: using a fluidized bed one-step forming process, using a carrier material as a substrate, and spraying a tacrolimus solution After the granulation is completed, continue to dry in the fluidized bed to obtain a dried solid dispersion, wherein the tacrolimus solid dispersion contains 1-3 parts by mass of tacrolimus and 5- 10 parts by mass.

[0029] In an optional embodiment, the spray granulation parameters are: the air inlet temperature of the fluidized bed is 50°C-55°C, the material temperature is 20°C-35°C, and the air inlet temperature is a key parameter. If the temperature is too high, then Related substances will increase significantly; the air intake volume and atomization pressure will affect the size and uniformity of the prepared particles, which need to be adjusted in real time during the preparation process t...

Embodiment 1

[0042] The batch size is 15,000 capsules, and the capsule weight is 65mg / capsule.

[0043] prescription composition

[0044] Tacrolimus 15g Absolute ethanol 300g Hypromellose 615 45g Croscarmellose Sodium 6g lactose 900g Magnesium stearate 9.75g

[0045] The preparation method is as follows:

[0046] Dissolve tacrolimus in absolute ethanol, stir until clear and free of foreign matter; add hypromellose into the fluidized bed, set the air volume to 5m 3 / h, the air inlet temperature is 50°C, the material temperature is controlled at about 25°C, the atomization pressure is 0.05MPa, the backflush pressure is 0.06MPa, the peristaltic pump speed is 20r / min, the spray granulation is started, and the liquid medicine is dried at 50°C for 1 The weight loss on drying of the solid dispersion is less than 3% after 1 hour; add croscarmellose sodium, lactose, and magnesium stearate, mix well, and then fill the capsules, the capsule capacity is 6...

Embodiment 2

[0049] The batch size is 15,000 capsules, and the capsule weight is 65mg / capsule.

[0050] prescription composition

[0051] Tacrolimus 18g Absolute ethanol 360g Hypromellose 615 42g Croscarmellose Sodium 6g lactose 909.3g Magnesium stearate 9.75g

[0052] The preparation method and stripping method are the same as in Example 1.

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Abstract

The invention discloses a preparation method of a tacrolimus solid dispersion, a quick-release pharmaceutical composition and application, and the preparation method of the tacrolimus solid dispersion comprises the following steps: adopting a fluidized bed one-step forming process, taking a carrier material as a substrate, carrying out spray granulation by using a tacrolimus solution, and after the granulation is completed, continuously drying in the fluidized bed to obtain the dried solid dispersion. The prepared solid and split particles are sieved and then directly mixed with other auxiliary materials to be filled into capsules to prepare the quick-release capsules, the problems of acetone solvents and residues are solved, the temperature in the whole preparation process is controlled to be not higher than 50 DEG C, the increase of related substances can be effectively controlled, and compared with original commercially-available products, the product has the same release behavior, and is good in release uniformity, stable in quality, lower in production cost and beneficial to industrial production.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a preparation method of tacrolimus solid dispersion, an immediate-release pharmaceutical composition and application. Background technique [0002] In 1984, Japan Astellas Pharmaceutical Co., Ltd., originally Fujisawa Pharmaceutical Co., Ltd., extracted a new type of macrolide immunosuppressant from the fermentation product of Streptomyces, named it FK506, and then officially named it Tacrolimus (tacrolimus). Tacrolimus has a strong immunosuppressive effect, and its immunosuppressive effect is about 10 to 100 times that of cyclosporine. In 1989, Starzl et al first applied it to liver transplantation and achieved good results. [0003] In 1993, tacrolimus capsules and injections produced by Japan Astellas Pharmaceuticals Co., Ltd. were launched, and the trade name was Prograf (Prograf), which was used to prevent or treat liver, kidney, and heart transplants in patients after tr...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K9/20A61K9/48A61K31/436A61K47/38A61K47/10A61P37/06
CPCA61K9/1652A61K9/1641A61K9/2054A61K9/2031A61K9/4866A61K31/436A61P37/06
Inventor 苏辉樊永庆向雪梅刘光海张媛媛
Owner SINOPHARM CHUANKANG PHARMACEUTICAL CO LTD
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