Oral megestrol acetate nano-suspension and preparation method thereof

A technology of megestrol acetate and nano-suspension, which is applied in the field of pharmaceuticals, can solve the problems of not improving the dissolution rate and bioavailability of megestrol acetate, and achieve small particle size, stable system and good taste. Good results

Inactive Publication Date: 2018-07-24
青岛国海生物制药有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] But above-mentioned 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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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0052] (1) Weigh 20.0000g megestrol acetate, 1.0000g lecithin, 10.0000g xanthan gum, 1.5000g sodium tartrate, 0.5000g malic acid, 0.1500g stevia, 1.0000g potassium sorbate, 2.0000g lemon essence, Purified water 963.85g, set aside.

[0053] (2) Add lecithin to part of the purified water, set the ultrasonic conditions as frequency 150Hz, temperature 35°C, time 15min, and conduct ultrasonic heating and dissolving;

[0054] (3) Add xanthan gum to part of the purified water, set the ultrasonic conditions as frequency 150Hz, temperature 35°C, time 15min, and carry out ultrasonic heating and dissolving;

[0055] (4) Add sodium tartrate, malic acid, and stevia into part of the purified water, set the ultrasonic conditions to frequency 150Hz, temperature 35°C, time 15min, and conduct ultrasonic heating and dissolving;

[0056] (5) Add potassium sorbate to the remaining purified water, set the ultrasonic conditions to frequency 150Hz, temperature 35°C, time 15min, and conduct ultrasoni...

Embodiment 2

[0066] (1) Weigh 40.0000g megestrol acetate, Tween-202.0000g, 15.0000g sodium alginate, 1.5000g sodium phosphate, 1.0000g acetic acid, 50.0000g sucrose, 1.5000g sorbic acid, 3.5000g lemon essence, purified water 885.50g, spare.

[0067] (2) Add Tween-20 to part of the purified water, set the ultrasonic conditions as frequency 200Hz, temperature 40°C, time 20min, and conduct ultrasonic heating and dissolving;

[0068] (3) Add sodium alginate to part of the purified water, set the ultrasonic conditions to frequency 200Hz, temperature 40°C, time 20min, and conduct ultrasonic heating and dissolving;

[0069] (4) Add sodium phosphate, acetic acid, and sucrose to part of the purified water, set the ultrasonic conditions to frequency 200Hz, temperature 40°C, time 20min, and conduct ultrasonic heating and dissolving;

[0070] (5) Add sorbic acid to the remaining purified water, set the ultrasonic conditions to frequency 200Hz, temperature 40°C, time 20min, and conduct ultrasonic heat...

Embodiment 3

[0080] (1) Weigh megestrol acetate 60.0000g, Tween-403.0000g, PEG400016.0000g, sodium carbonate 2.0000g, lactic acid 1.0000g, mogroside 0.4000g, nisin 1.5000g, lemon essence 5.0000g, purify 911.10g of water, set aside.

[0081] (2) Add Tween-40 to part of the purified water, set the ultrasonic conditions as frequency 250Hz, temperature 50°C, time 20min, and conduct ultrasonic heating and dissolving;

[0082] (3) Add PEG4000 to part of the purified water, set the ultrasonic conditions as frequency 250Hz, temperature 50°C, time 20min, and conduct ultrasonic heating and dissolving;

[0083] (4) Add sodium carbonate, lactic acid, and Luo Han Guo soap to part of the purified water, set the ultrasonic conditions to frequency 250Hz, temperature 50°C, time 20min, and conduct ultrasonic heating and dissolving;

[0084] (5) Add nisin to the remaining purified water, set the ultrasonic conditions to frequency 250Hz, temperature 50°C, time 20min, and conduct ultrasonic heating and dissol...

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Abstract

The invention discloses an oral megestrol acetate nano-suspension and a preparation method thereof. The oral megestrol acetate nano-suspension contains effective amounts of megestrol acetate, a wetting agent, a suspending aid, a deflocculating agent, a pH adjusting agent, a flavoring, a bacteriostatic agent, a perfume and purified water. The preparation method comprises the following steps: respectively dissolving above materials in a part of water, mixing the obtained solutions to prepare an initial suspension, performing high-speed shearing to prepare a crude suspension, and performing micro-jet high-pressure homogenization treatment to prepare the oral megestrol acetate suspension. The oral megestrol acetate nano-suspension has the characteristics of small particle size of solid particles, high bioavailability, uniformity in distribution, stable system and good mouthfeel, the average particle size is less than 500 nm, and the dispersiveness is small; and the preparation method of the product has the advantages of simple process and easiness in realization of industrial production.

Description

[0001] manual technical field [0002] The invention belongs to the technical field of medicines, and in particular relates to an oral megestrol acetate nanosuspension and a preparation method thereof. Background technique [0003] Megestrol Acetate (MA) is an important synthetic progesterone drug, mainly used in the treatment of advanced breast cancer and endometrial cancer, it can improve the appetite and cachexia of patients with advanced tumors, and has a beneficial effect on functional uterus. Bleeding, irregular menstruation, endometrial hyperplasia, endometriosis and other diseases also have a certain effect. The solubility of megestrol acetate in water at 37° C. is 2 mg / ml, and the solubility in blood is 24 μg / ml. Due to its low solubility, it has a relatively low bioavailability. Commonly used methods to improve the bioavailability of poorly soluble drugs include micronization technology and nanosuspension technology. After the drug is micronized, the surface free...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/10A61K31/57A61P35/00B01F11/02B01F15/06B01F1/00B01F5/02
CPCA61K9/0053A61K9/10A61K31/57B01F21/02B01F25/20B01F31/80B01F35/90B01F2035/99B01F2101/22
Inventor 邢燕孙雪燕李士广
Owner 青岛国海生物制药有限公司
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