Self-assembling proliposome soft capsule and preparation method thereof

A proliposome and self-assembly technology, which is applied in capsule delivery, drug combination, pharmaceutical formulation, etc., can solve the problems of patients' blood vessel stimulation, inconvenient clinical application, poor stability, etc., achieve low cost and solve complex production process , the effect of improving compliance

Inactive Publication Date: 2010-07-21
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Nimodipine is almost insoluble in water and has poor absorption in the gastrointestinal tract. Compared with oral administration, the route of injection can significantly improve its bioavailability, but nimodipine injection is sensitive to light and has poor stability. Adjuvant oral medication required
In addition, because the drug is insoluble in water, a large amount of organic solvents such as ethanol must be added as a solvent for intravenous injection, which is easy to cause irritation to the blood vessels of patients, and there is a possibility of drug precipitation, which brings great inconvenience to clinical application.

Method used

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  • Self-assembling proliposome soft capsule and preparation method thereof
  • Self-assembling proliposome soft capsule and preparation method thereof
  • Self-assembling proliposome soft capsule and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] The composition of the prescription is as follows: Nimodipine 8g

[0042] Egg phospholipids 200g

[0043] Macrogol 400 220g

[0044] Poloxamer 188 (trade name F-68) 80g

[0045] Cholesterol 16g

[0046] A total of 1000 soft capsules were made, and the average particle diameters of liposomes formed after disintegration and hydration in artificial gastric juice and water were 468.2nm and 447.8nm respectively; the encapsulation efficiency was 81.77%

[0047] Preparation process: Put the prescribed amount of drugs, phospholipids, and PEG into a vial, add an appropriate amount of absolute ethanol, and dissolve it by ultrasonication, then add cholesterol and poloxamer, and dissolve it by ultrasonication, and then prepare a self-assembled proliposome. Quantitative filling is then filled in the soft capsule, and the nimodipine self-assembled proliposome soft capsule is formed.

Embodiment 2

[0049] The composition of the prescription is as follows: Nimodipine 8g

[0050] Soy Lecithin 180g

[0051] Macrogol 400 200g

[0052] Polyoxyethylene castor oil 80g

[0053] Sodium deoxycholate 8g

[0054] A total of 1000 soft capsules were made, and the average particle diameters of the liposomes formed after disintegration and hydration in artificial gastric juice and water were 516.5nm and 503.4nm respectively; the encapsulation efficiency was 80.2%

[0055] Preparation method: with embodiment 1.

Embodiment 3

[0057] The composition of the prescription is as follows: Nimodipine 6g

[0058] Hydrogenated Phospholipids 100g

[0059] Macrogol 600 200g

[0060] Tween 80 150g

[0061] Sodium deoxycholate 10g

[0062] Anhydrous ethanol amount

[0063] A total of 1,000 soft capsules were made, and the average particle diameters of liposomes formed after disintegration and hydration in artificial gastric juice and water were 537.3nm and 521.8nm respectively; the encapsulation efficiency was 80.43%

[0064] Preparation method: with embodiment 1.

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Abstract

The invention relates to the field of pharmaceutical preparations, in particular to a nimodipine self-assembling proliposome soft capsule and a preparation method thereof. The invention is characterized in that self-assembling proliposome liquid medicine which is composed by medicine, phospholipids, dispersion medium and polyethylene glycol modifier is wrapped by a soft capsule. The invention fills the self-assembling proliposome liquid medicine into the soft capsule, then self-assembling proliposome is completely wrapped by a capsule shell, and thereby the soft capsule not only can play the role of isolating oxygen, moisture and the like, but also can cover up bad taste and bring convenience to oral administration. After being disintegrated by gastric juice, the soft capsule can quickly hydrate and self-assemble to form liposome with high entrapment rate and uniform particle size.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a nimodipine self-assembled proliposome soft capsule and a preparation method thereof. Background technique [0002] Liposomes have unique advantages such as good biocompatibility, improved absorption of insoluble drugs, sustained release and long-acting effect. At present, liposomes are mainly administered in the form of intravenous injection. In the gastrointestinal tract, liposomes will encounter problems such as gastric acid and gastrointestinal enzyme degradation, aggregation and agglomeration under different pH conditions, and particle size growth or drug degradation. Difficult to administer orally. To a certain extent, proliposomes can solve the problems of liposome dispersion instability in direct storage and gastrointestinal degradation of oral liposomes. Slow, incomplete local dissolution, uneven dispersion and other shortcomings, resulting in low drug encap...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/48A61K47/34A61K47/44A61K31/4422A61P9/10A61K47/10A61K47/28
Inventor 刘建平邱璐
Owner CHINA PHARM UNIV
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