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Megestrol acetate nanosuspension and preparation method and application thereof

A technology of megestrol acetate and nanosuspension, applied in the field of medicine, can solve the problems such as the dissolution rate and bioavailability of megestrol acetate are not well improved, and achieve the improvement of oral bioavailability and preparation method. Simple and easy to transport

Inactive Publication Date: 2016-07-20
西安远大德天药业股份有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] But said method does not improve the dissolution rate and the bioavailability of megestrol acetate well yet, still need a kind of method to further improve the dissolution rate and the bioavailability of megestrol acetate at present

Method used

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  • Megestrol acetate nanosuspension and preparation method and application thereof

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Embodiment 1

[0030] The nano-suspension of megestrol acetate of the present embodiment is made after mixing megestrol acetate and a stabilizer solution through a nano-grinding machine, and the stabilizer is a cellulose derivative and an anionic surfactant according to 10 : the mixture that the mass ratio of 1 mixes; Described cellulose derivative is hydroxypropyl methylcellulose and hydroxypropyl cellulose, and the mass ratio of hydroxypropyl methyl cellulose and hydroxypropyl cellulose is 10:1, so Described anion surfactant is sodium lauryl sulfate and sodium deoxycholate, and the mass ratio of sodium lauryl sulfate and sodium deoxycholate is 10:1; In the described megestrol acetate nanosuspension, acetic acid The concentration of megestrol is 400 mg / mL; the mass ratio of megestrol acetate and stabilizer in the megestrol acetate suspension is 50:1.

[0031] The preparation method of the megestrol acetate nanosuspension of the present embodiment may further comprise the steps:

[0032] St...

Embodiment 2

[0037]This embodiment is the same as Example 1, except that the filler is starch, dextrin, lactose or mannitol, or at least two of starch, dextrin, lactose, mannitol and microcrystalline cellulose , the disintegrant is cross-linked polyvinylpyrrolidone, cross-linked sodium carboxymethylcellulose or sodium carboxymethyl starch, or cross-linked polyvinylpyrrolidone, cross-linked sodium carboxymethylcellulose, sodium carboxymethyl starch and low Substituting at least two of hypromellose, the lubricant is magnesium stearate, micropowder silica gel or polyethylene glycol, or at least two of magnesium stearate, micropowder silica gel, talc and polyethylene glycol .

Embodiment 3

[0039] The nano-suspension of megestrol acetate of the present embodiment is made after mixing megestrol acetate and a stabilizer solution through a nano-grinding machine, and the stabilizer is a cellulose derivative and an anionic surfactant according to 10 : the mass ratio mixing mixture of 1.2; Described cellulose derivative is hydroxypropyl methylcellulose and hydroxypropyl cellulose, and the mass ratio of hydroxypropyl methyl cellulose and hydroxypropyl cellulose is 10:5, so Described anionic surfactant is sodium lauryl sulfate and sodium deoxycholate, and the mass ratio of sodium lauryl sulfate and sodium deoxycholate is 10:4; In the described megestrol acetate nanosuspension, acetic acid The concentration of megestrol is 200mg / mL; the mass ratio of megestrol acetate and stabilizer in the megestrol acetate suspension is 50:2.

[0040] The preparation method of the megestrol acetate nanosuspension of the present embodiment may further comprise the steps:

[0041] Step 1....

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Abstract

The invention discloses a megestrol acetate nanosuspension.The megestrol acetate nanosuspension is prepared by mixing megestrol acetate and a stabilizer solution and then grinding the mixture through a nanometer grinder.The stabilizer is a mixture obtained by mixing cellulose derivatives and anionic surfactants according to the mass ratio of 10: (1-2); the cellulose derivatives are hydroxypropyl methyl cellulose and hydroxyl propyl cellulose, and the mass ratio of hydroxypropyl methyl cellulose to hydroxyl propyl cellulose is 10: (1-10); the anionic surfactants are lauryl sodium sulfate and sodium deoxycholate, and the mass ratio of lauryl sodium sulfate to sodium deoxycholate is 10: (1-5).The invention further discloses a preparation method and application of the megestrol acetate nanosuspension.According to the megestrol acetate nanosuspension, the average grain diameter of megestrol acetate is below 1,000 nm, the dissolution rate of megestrol acetate is remarkably increased, and then the oral bioavailability of megestrol acetate is improved.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a megestrol acetate nanosuspension and its preparation method and application. Background technique [0002] Megestrol acetate (megestrolacetate, MA) is a progestogen drug, mainly used in the treatment of advanced breast cancer and advanced endometrial cancer, it can improve the appetite and cachexia of patients with advanced tumors, and it is effective for kidney cancer, prostate cancer and ovarian cancer. Cancer also has a certain curative effect. Megestrol acetate is a poorly soluble drug, and dissolution is the main step that limits the absorption of the drug in the body. Therefore, increasing the dissolution rate of the drug can significantly improve the absorption of the drug, thereby increasing the bioavailability. [0003] Various approaches are available to increase the bioavailability of megestrol acetate, as described in the following literature: [0004...

Claims

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Application Information

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IPC IPC(8): A61K9/10A61K9/20A61K31/57A61K47/38A61K47/28A61K47/20A61P35/00
CPCA61K47/20A61K47/28A61K47/38A61K9/10A61K9/2059A61K31/57
Inventor 李成胜王亚轩
Owner 西安远大德天药业股份有限公司
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