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Pharmaceutical composition containing butylphthalide and novel solubilizer

A technology of solubilizer and composition, which is applied in the field of medicine, can solve the problems of large safety hazards in intravenous use, complex prescription composition and preparation process, difficulty in consistent or constant curative effect, etc., so as to improve bioavailability and facilitate dissolution And absorption, resistance to moist heat sterilization effect

Inactive Publication Date: 2016-06-22
SICHUAN MANSAISI MEDICINE TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Chinese patent CN200510102355.2 discloses the prescription and preparation method of butylphthalide intravenous emulsion, which can solve the insoluble problem of butylphthalide in water, but the emulsifier soybean lecithin is used in the prescription, and soybean lecithin is easily oxidized into lysophospholipid. There are serious potential safety hazards; and the preparation process of the emulsion is relatively complicated, and it is difficult to control the product quality in industry
Chinese patent CN200410012533.8 discloses a freeze-dried powder injection of butylphthalide, which can also solve the insoluble problem of butylphthalide in water, but a large amount of emulsifiers and co-emulsifiers need to be used in the prescription, and the composition of the prescription and the preparation process are uniform. It is more complicated, and there is also the problem that the quality of industrial products is difficult to control
Chinese patent CN200410075068.2 discloses a butylphthalide self-emulsifying drug delivery system, which can also solve the problem of butylphthalide being insoluble in water, but the self-emulsifying drug delivery system needs to be in the gastrointestinal tract or at a body temperature of 37°C and under gentle stirring The oil-in-water emulsion can be formed spontaneously, and the individual variation of patients after medication is large, so it is difficult to ensure the consistency or constant of the curative effect in the body
Chinese patent CN200610081440.X discloses a concentrated solution of butylphthalide for injection. In the prescription, a non-aqueous solvent, a solubilizer and a cosolvent must be used at the same time to solve the problem of water insolubility of butylphthalide. Big security risk

Method used

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  • Pharmaceutical composition containing butylphthalide and novel solubilizer
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  • Pharmaceutical composition containing butylphthalide and novel solubilizer

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1-6

[0037] Embodiment 1-6 Butylphthalide injection and preparation method thereof

[0038]

[0039] The preparation method of Examples 1 and 4 is as follows: mix the prescription ingredients except water for injection, and heat to 60°C; then heat the water for injection to the same temperature, and add the water for injection into the above molten liquid under sufficient stirring to obtain Clarify the solution; add activated carbon, keep warm at 60°C for 20 minutes, decarbonize, and filter; add osmotic pressure regulator, mix well, add activated carbon, keep warm, decarbonize, filter; use pH regulator to adjust the pH of the liquid to 4.0-9.0, and fill , sterilized, packaged.

[0040] The preparation methods of Examples 2 and 5 are as follows: (1) Mix all the prescription ingredients, heat to 60°C, and stir thoroughly to obtain a clear solution; add osmotic pressure regulator, mix well, add activated carbon, keep warm, decarbonize, and filter ; Use a pH regulator to adjust the...

Embodiment 7-12

[0042] Embodiment 7-12 Butylphthalide injection and preparation method thereof

[0043]

[0044] The preparation method is as follows: take the prescribed amount of excipients except the main drug butylphthalide and heat to 55°C to melt, add butylphthalide and stir to dissolve; then heat the water for injection to the same temperature, and dissolve the water for injection under sufficient stirring Add to the above molten liquid to obtain a clear solution; add activated carbon, keep warm at 60°C for 30 minutes, decarbonize, filter; add osmotic pressure regulator, and replenish the volume to 1000ml, adjust the pH of the liquid to 4.0-9.0, fill, 121°C Sterilize for 20min, pack.

Embodiment 13

[0045] Embodiment 13 butylphthalide capsules and preparation method thereof

[0046] Take 20g of polyethylene glycol 15-hydroxystearate and heat it to 55°C to melt it, add 40g of butylphthalide, stir; keep the above temperature, add 100g of SyloidFP244, stir well, take it out, cool to room temperature, mix with 80g of mannitol 200SD, 26g of microcrystalline cellulose, mixed evenly, adding an appropriate amount of 2% HPMC aqueous solution, granulated, dried, granulated, added 4g of magnesium stearate, mixed evenly, filled into 0.35g / capsule capsules, and ready.

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PUM

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Abstract

The invention relates to the field of medicine, in particular to a pharmaceutical composition containing butylphthalide and a novel solubilizer to improve the water solubility of butylphthalide by means of the novel solubilizer, clinically required solid form, or semisolid form or liquid form of butylphthalide is developed, so that the treatment effect of butylphthalide can be better realized. The composition can be used for preparing various drug forms such as tablets, capsules, particles, powder, ointment, cream, gel, infusion, squirt cut, powder filling and oral liquid. Compared with the prior art, the pharmaceutical composition is better in safety performance and water solubility of butylphthalide.

Description

technical field [0001] The invention relates to the field of medicine, in particular to a pharmaceutical composition containing butylphthalide and a novel solubilizer. Background technique [0002] Butylphthalide is the main component of celery and its seeds. It can be extracted directly from natural plant celery seed oil or obtained through synthesis. Butylphthalide contains a chiral carbon atom, so it has two optical isomers, namely L-butylphthalide and D-butylphthalide, whose structural formula is as follows: [0003] [0004] Butylphthalide is a water-insoluble oily liquid with a strong celery fragrance. Butylphthalide has been clinically used in the treatment of ischemic cerebrovascular disease, which can improve the symptoms of neurological deficit after stroke and promote the functional recovery of patients. At present, the marketed preparations of butylphthalide include butylphthalide soft capsules for oral use and butylphthalide sodium chloride injection for in...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/34A61K31/365A61P9/10A61P25/00
CPCA61K9/0019A61K9/0095A61K9/08A61K9/146A61K9/1641A61K9/2031A61K9/28A61K9/4866A61K31/365A61K47/14
Inventor 不公告发明人
Owner SICHUAN MANSAISI MEDICINE TECH CO LTD
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