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Hypocrellin liposome preparation and preparation method thereof

A technology of liposome preparation and hypocretin, which is applied in the direction of liposome delivery, pharmaceutical formulation, medical preparation of non-active ingredients, etc., can solve the problems affecting the monodisperse shape stability of liposome solid powder, The quality of batch finished products is not easy to control, and the bilayer phospholipid film is damaged, etc., to achieve the effect of good monodispersity, increased yield, and stable shape

Active Publication Date: 2009-02-25
INST OF CHEM CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, Tween series surfactants (4.30-6.50%) are added to the formula without exception. At present, the State Food and Drug Administration has made stricter restrictions on Tween-type excipients, and its injection concentration is currently limited to 100 μg / ml Below, the concentration of Tween after the original solid powder is redissolved is 10mg / ml, 100 times beyond the limit; the maximum drug loading concentration is 0.5mg / ml, and the drug loading is on the low side; Scale uniformity and liposome morphology are determined by the strength of the ultrasonic field, and the quality of the finished product between batches is not easy to control; in the patented freeze-drying process, the step-by-step pre-freezing method is used, and large ice crystals may destroy the bilayer phospholipid membrane. Affecting the stability of liposome solid powder monodispersity and morphology after reconstitution

Method used

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  • Hypocrellin liposome preparation and preparation method thereof
  • Hypocrellin liposome preparation and preparation method thereof
  • Hypocrellin liposome preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] 100mg hypocrellin A, 4g lecithin, 240mg cholesterol and 97.7mL water were emulsified to make multilamellar liposomes with a particle size below 1000nm. Pour it into a high-pressure homogenizer at 10MPa for initial homogenization, then pressurize to 180MPa for high-pressure homogenization, and keep the system temperature at 15 0C, cycled 5 times to obtain single-lamellar liposomes with a particle size distribution of 46-140 nm. Add 4g of sucrose, shake and dissolve, sterilize by ultrafiltration through a filter membrane with a pore size of 220nm, put it in a -80°C refrigerator for rapid pre-freezing, and freeze-dry the obtained freeze-dried liposome powder. The content is 1.20%.

[0032] Among them, the particle size distribution of multilamellar liposomes is shown in figure 1 Shown; the particle size distribution of liposomes before freeze-drying and liposomes after reconstitution image 3 Shown; The transmission electron micrograph of liposome diluted to 0.05mg / ml b...

Embodiment 2

[0035] 200mg Hypocretin A, 6g hydrogenated soybean lecithin, 480mg cholesterol and 195.4mL water were emulsified to make multilamellar liposomes with a particle size below 1000nm. Pour it into a high-pressure homogenizer at 15MPa for initial homogenization, then pressurize to 200MPa for high-pressure homogenization, and keep the system temperature at 10 0 C, cycled twice to obtain single-lamellar liposomes with a particle size distribution of 40-129 nm. Add 8g of mannose, shake and dissolve, sterilize by ultrafiltration through a 220nm filter membrane, put it in a -60°C refrigerator for rapid pre-freezing, freeze-dry the obtained freeze-dried liposome powder and store it in an inert gas seal. The drug content is 1.36%.

Embodiment 3

[0037] 500mg Hypocretin A, 20g hydrogenated lecithin, 1.2g cholesterol and 488.5mL water were emulsified to make multilamellar liposomes with a particle size below 1000nm. Pour it into a high-pressure homogenizer at 20MPa for initial homogenization, then pressurize to 130MPa for high-pressure homogenization, and keep the system temperature at 5 0 C, cycled 7 times to obtain unilamellar liposomes with a particle size distribution of 49-162 nm. Add 10g of sucrose, shake and dissolve, sterilize by ultrafiltration through a filter membrane with a pore size of 220nm, put it in a -70°C refrigerator for rapid pre-freezing, and freeze-dry the obtained freeze-dried liposome powder. The content is 1.58%.

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Abstract

The invention discloses a hypocrellin liposome preparation and a preparation method thereof. The hypocrellin liposome preparation comprises the following components according to parts by weight: 1-5 parts of hypocrellin, 40-200 parts of phospholipids, 2.4-12 parts of cholesterol and 50-100 parts of protective agent for freeze drying. The hypocrellin liposome preparation prepared by the high pressure homogenization is characterized in that: the preparation contains no surfactant of Tween; the drug content of the preparation can be increased to more than 1.2 percent from 0.6 percent; the drug concentration of redissolution reaches 1mg / ml, an increase of 100 percent. The invention substitutes the high pressure homogenization for the ultrasonic method so that the quality of the hypocrellin liposome preparation can be assured and the yield greatly increased which meets dual requirements of the industrial production and clinical application of drugs of hypocrellin liposome; meanwhile, the invention substitutes rapid pre-freezing for steady pre-freezing, which can ensure that solid powder of hypocrellin liposome with good monodispersity and more stable morphology after the redissolution is obtained.

Description

technical field [0001] The invention relates to a hypocretin liposome preparation and a preparation method thereof. Background technique [0002] Microvascular diseases, including port wine stains, macular degeneration, etc., belong to the category of common diseases in clinical medicine. Patients are considered to be the primary cause of blindness in the elderly. According to statistics, such patients are as high as one million in the United States alone. At present, it has been proved that photodynamic therapy is the only effective or preferred therapy for treating microvascular diseases. However, photodynamic drugs for microvascular diseases are currently the bottleneck of clinical application of such diseases. [0003] For many years, photodynamic therapy has mainly aimed at anti-tumor. Therefore, photodynamic drugs are also mainly evaluated on the anti-tumor function. The tissue penetration depth of light in the wavelength range (3-10 mm) is beneficial to the curative...

Claims

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Application Information

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IPC IPC(8): A61K31/122A61K9/127A61K47/28A61P43/00A61P27/02
Inventor 赵井泉张杨谢杰
Owner INST OF CHEM CHINESE ACAD OF SCI
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