Preparation of tamoxifen citrate microcapsule prepared by complex coacervation method

A technology of tamoxifen and complex coagulation method is applied in the field of preparation of tamoxifen citrate microcapsules, which can solve the problems of large gastrointestinal irritation and short drug release time, and achieves prolonged release time and convenient source of raw materials. , the effect of facilitating industrialization

Inactive Publication Date: 2008-07-02
DONGHUA UNIV
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Problems solved by technology

But so far, the dosage form of tamoxifen citrate is mainly tablets, which have th

Method used

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  • Preparation of tamoxifen citrate microcapsule prepared by complex coacervation method
  • Preparation of tamoxifen citrate microcapsule prepared by complex coacervation method
  • Preparation of tamoxifen citrate microcapsule prepared by complex coacervation method

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[0030] Example 1

[0031] (1) Preparation of tamoxifen citrate microcapsules

[0032] Weigh 500 mg of tamoxifen citrate, dissolve it in 20 mL of 95% ethanol by ultrasonic, add 40 mL of 3% aqueous gum arabic solution, and stir at 40°C to 45°C under temperature control, with a stirring speed of 400 rpm, and then add 40 mL of 3% of gelatin solution. During the stirring process, slowly add 10% glacial acetic acid dropwise to adjust the pH to 4.22, then add 100 mL of distilled water at about 35°C, stir at a high speed, and stir at a speed of 3000 rpm. When the solution is naturally cooled to below 30°C, set the ice bath quickly After dropping to 10 °C, add 2 mL of 37% formaldehyde, solidify for 0.5 h, adjust to pH 8-9 with 20% NaOH, continue stirring in an ice bath, solidify for 3 h, centrifuge, wash with water until formaldehyde-free, freeze-dried under reduced pressure, The finished microcapsules are obtained.

[0033] (2) Morphology and particle size of microcapsules

[0034...

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Abstract

The invention relates to a complex coacervation method for preparing the tamoxifen citrate microcapsule, the steps include: (1) the capsule core tamoxifen citrate is weighed and dissolved in 95 percent of ethanol for ultrasonic dissolution, Arab gum solution is added, the mixture is treated ultrasonically in a water bath, then the gel water solution is added, and the water bathing and stirring are carried out to control the weight ratio of the capsule core and the capsule material; (2) 10 percent of glacial acetic acid is added to adjust the pH value to 4.0 to 4.3 during the stirring process, distilled water is added for dilution, the high-speed stirring is carried out, then the mixture is arranged in an ice bath for rapid temperature-decreasing to 0 to 10 DEG C, and crosslinker is added for curing; (3) 20 percent of NaOH solution is used for adjusting the pH value, the high-speed stirring is carried out at 0 to 10 DEG C, and the tamoxifen citrate microcapsule can be obtained by curing, centrifugalizing, washing, freezing, decompression and drying. The method is simple, safe and good in reproducibility, and the prepared microcapsule is proved to have the better sustained-release function by transdermal and in vitro dissolution results, so the invention can be taken as the drug sustained-release formulation for the prevention and treatment of breast cancer.

Description

technical field [0001] The invention belongs to the field of preparing pharmaceutical preparations for preventing and treating breast cancer, in particular to a preparation method of tamoxifen citrate microcapsules. Background technique [0002] In recent years, the incidence of breast cancer has increased dramatically. In Western countries, breast cancer has become the number one cause of death among women. In recent years, the incidence of breast cancer in my country has also been on the rise. According to the latest report from the health department, the incidence of breast cancer has become the No. It still ranks 9th among tumor diseases. In recent years, there are about 1.6 million to 1.8 million new cancer patients in my country every year, and the total number of cancer patients is about 4.5 million to 6 million. [0003] At present, the main means of breast cancer treatment include: surgery, radiotherapy, chemotherapy and endocrine therapy. Among them, endocrine...

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Application Information

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IPC IPC(8): A61K9/50A61K31/138A61P35/00
Inventor 朱利民马宗会张晓飞樊在霞
Owner DONGHUA UNIV
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