Fluoxetine hydrochloride liposome solid preparation

A technology of fluoxetine hydrochloride and fluoxetine hydrochloride, applied in the field of medicine, can solve the problems of low bioavailability, influence on treatment effect, long dissolution time, etc., and achieve high bioavailability, good sustained release effect, and dissolution Excellent effect

Inactive Publication Date: 2013-09-25
HAINAN MEIDA PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

There are common compressed tablets of fluoxetine hydrochloride in domestic and foreign marketed drugs at present, but this dosage form has the following problems: due to reasons such as preparation technology, the oral preparations of most drugs all exist after taking the dissolution time is long, the dissolution rate is low, Poor absorption, many times of taking medicine, uncontrollable drug release, low bioavailability and other problems, which affect the efficacy of the drug and directly affect the therapeutic effect, so its bioavailability is low
[0011] Fluoxetine hydrochloride liposome and its solid preparations designed for oral application are not disclosed in the prior art

Method used

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  • Fluoxetine hydrochloride liposome solid preparation
  • Fluoxetine hydrochloride liposome solid preparation
  • Fluoxetine hydrochloride liposome solid preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0069] Example 1 Fluoxetine Hydrochloride Liposome Tablets

[0070]

[0071]

[0072] The following production process is used to prepare fluoxetine hydrochloride liposome tablets:

[0073] (1) Accurately weigh out 10g fluoxetine hydrochloride (calculated as fluoxetine), 200g egg yolk phosphatidylglycerol, 100g dimyristoylphosphatidylcholine, 50g cholesterol succinate, 40g Span 40, and dissolve in 2000ml volume ratio In a 2:1 mixed solvent of ethanol and acetone, stir to dissolve;

[0074] (2) Put the above solution in an eggplant-shaped bottle, remove the ethanol and acetone under reduced pressure in a 45℃ water bath, and form a uniform transparent film on the bottle wall;

[0075] (3) Add 2000ml of phosphate buffer solution with pH value of 6.8 to the eggplant-shaped bottle, and continue to rotate in a water bath at 45℃ under normal pressure to swell and hydrate the film;

[0076] (4) Filter the above solution with a 0.45μm microporous filter membrane, freeze the filtrate overnight ...

Embodiment 2

[0080] Example 2 Fluoxetine Hydrochloride Liposome Capsules

[0081] The raw materials used are as follows:

[0082]

[0083] The following production process is used to prepare fluoxetine hydrochloride liposome tablets:

[0084] (1) Accurately weigh 20g fluoxetine hydrochloride (calculated as fluoxetine), 400g egg yolk phosphatidylglycerol, 200g dimyristoylphosphatidylcholine, 300g cholesterol succinate, 70g Span 40, and dissolve in 5000ml volume ratio In a 2:1 mixed solvent of ethanol and acetone, stir to dissolve;

[0085] (2) Put the above solution in an eggplant-shaped bottle, remove the ethanol and acetone under reduced pressure in a 45℃ water bath, and form a uniform transparent film on the bottle wall;

[0086] (3) Add 5000ml of phosphate buffer solution with pH value of 6.8 to the eggplant-shaped bottle, and continue to rotate at 45℃ in a water bath at atmospheric pressure to swell and hydrate the film;

[0087] (4) Filter the above solution with a 0.45μm microporous filter me...

Embodiment 3

[0091] Example 3 Fluoxetine Hydrochloride Liposome Tablets

[0092] The raw materials used are as follows:

[0093]

[0094] The following production process is used to prepare fluoxetine hydrochloride liposome tablets:

[0095] (1) Accurately weigh 90g fluoxetine hydrochloride (calculated as fluoxetine), 600g egg yolk phosphatidylglycerol, 300g dimyristoylphosphatidylcholine, 450g cholesterol succinate, 200g Span 40 and dissolve in 8000ml volume ratio as In a 2:1 mixed solvent of ethanol and acetone, stir to dissolve;

[0096] (2) Put the above solution in an eggplant-shaped bottle, remove the ethanol and acetone under reduced pressure in a 45℃ water bath, and form a uniform transparent film on the bottle wall;

[0097] (3) Add 8000ml of phosphate buffer solution with pH value of 6.8 to the eggplant-shaped bottle, and continue to rotate in a water bath at 45℃ under normal pressure to swell and hydrate the film;

[0098] (4) Filter the above solution with a 0.45μm microporous filter me...

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Abstract

The invention discloses a fluoxetine hydrochloride liposome solid preparation and a preparation method of the fluoxetine hydrochloride liposome solid preparation. Active ingredients fluoxetine hydrochloride and egg yolk phosphatidyl glycerol, dimyristoyl phosphatidyl choline, cholesterol succinate and span 40 in specific combination are prepared into lipidosome, the stability, the dissolvability and the bioavailability of medicine are greatly improved, in addition, the effect is stable and durable, and the curative effect is obvious. The preparation disclosed by the invention has the advantages that the product quality of the preparation is improved, and the toxic or side effect is reduced.

Description

Technical field [0001] The invention relates to a new preparation of fluoxetine hydrochloride, in particular to fluoxetine hydrochloride liposomes and solid preparations and preparation methods thereof, and belongs to the technical field of medicine. Background technique [0002] Depression is a common mental illness, which is mainly manifested as low mood, decreased interest, pessimism, slow thinking, lack of initiative, self-crimination, poor diet and sleep, and mainly worrying about suffering from various diseases. Discomfort, severe suicidal thoughts and behavior may occur. Depression is mainly composed of depressed mood, slow thinking and decreased volition, and most cases still have various physical symptoms. These include sleep disorders (difficulty falling asleep, light sleep, waking up early, or others think he is sleeping well, but I don’t feel asleep at all), lack or energy loss, loss of appetite, loss of sexual function, weight loss, constipation, Non-specific physi...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/127A61K9/20A61K9/48A61K31/138A61K47/28A61K47/24A61P25/24
Inventor 廖爱国
Owner HAINAN MEIDA PHARMA
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