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Anastrozole dispersed tablet formulation

A technology of anastrozole and dispersible tablets, applied in the field of pharmaceutical preparations, can solve the problems of decreased compliance, low bioavailability, low toxicity, etc., and achieve the effects of low production packaging cost, simple production process, and convenient administration

Inactive Publication Date: 2005-07-06
LUNAN PHARMA GROUP CORPORATION
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Anastrozole is of great significance to the vast number of breast cancer patients in our country. After a lot of investigations on the clinical application of anastrozole, we found that the only common tablets and other dosage forms on the market are far from satisfying the majority of patients. Especially for those patients with severe cancer who are difficult to take, and patients with decreased gastrointestinal absorption function after taking antineoplastic drugs for a long time, there is currently no ideal clinical medication method for administering anastrozole
Ordinary anastrozole tablets are inconvenient for patients to take, have low bioavailability, and are highly irritating to the gastrointestinal tract, which leads to a decrease in drug compliance of tumor patients after long-term medication, which largely limits the ability of anastrozole to resist drug resistance. Tumor activity, and anastrozole has poor water solubility, and it is not suitable for making injections for patients
Since anastrozole has the above-mentioned excellent anti-tumor activity and low toxicity, further developing a variety of dosage forms suitable for patients’ needs has been the goal of pharmaceutical companies for many years. However, due to some specific physical and chemical properties of anastrozole , it is difficult to develop, and now there are only some common tablets for patients to use

Method used

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  • Anastrozole dispersed tablet formulation
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Examples

Experimental program
Comparison scheme
Effect test

Embodiment

[0015] Embodiment (prescription quantity is 1000):

[0016] Eight specific prescriptions:

[0017] Prescription A:

[0018] Anastrozole 0.1g

[0019] Microcrystalline cellulose (disintegrant) 49g

[0020] Preparation process: The main drug is passed through a 100-mesh sieve, and the disintegrant is passed through a 80-mesh sieve. Weigh the prescribed amount of the disintegrant and mix evenly. , granulated, dried and pressed into tablets. Dispersible tablet dispersion time limit is 2.8min.

[0021] Prescription B:

[0022] Anastrozole 0.5g

[0023] Lactose (filler) 92g

[0024] Sodium carboxymethyl starch (disintegrant) 5g

[0025] 4% PVP K30 Aqueous solution (adhesive) 50g

[0026] Magnesium stearate (lubricant) 0.5g

[0027] Preparation process: the main drug is passed through a 100-mesh sieve, the filler and disintegrant are passed through a 80-mesh sieve, the prescribed amount of filler and disintegrant is weighed and mixed evenly, and then the prescribed amount ...

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PUM

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Abstract

The invention belongs to medical technology, in particular to a dispersible tablet form of anastrozole. Through a large number of clinical investigations, we have overcome the technical prejudice that anastrozole does not need to be developed into dispersible tablets in the prior art, and obtained the present invention. Clinical experiments have confirmed that the adverse reactions of the present invention are significantly reduced, and the compliance of medication is significantly improved. Obtained unexpected clinical efficacy. It has the characteristics of low production cost, stable preparation, fast absorption and high bioavailability. The invention is suitable for treating advanced breast cancer of postmenopausal women, and provides a good therapeutic drug dosage form for breast cancer patients.

Description

technical field [0001] The invention belongs to the technology of pharmaceutical preparations, in particular to a clinical dosage form of anastrozole. Background technique [0002] Cancer is a large class of diseases that seriously endanger human health. The mortality rate caused by tumors in my country ranks second among all causes, reaching 128.58 / 100,000 in 1995, and the incidence rate is on the rise. [0003] Breast cancer is a common malignant tumor, ranking fifth in the incidence of cancer. In 1995, the mortality rate was 3.14 / 100,000, and the incidence rate increased every year. Anastrozole, developed by Zeneca, is a third-generation aromatase inhibitor for the treatment of advanced breast cancer in postmenopausal women. It is also effective for patients who have failed tamoxifen treatment; it has stronger effects and fewer side effects than the first-generation and second-generation aromatase inhibitors. Anastrozole has a highly specific selection effect, so it doe...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K31/4196A61P35/00
Inventor 赵志全
Owner LUNAN PHARMA GROUP CORPORATION
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