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Slow-release microsphere containing venenum bufonis lipoclastic substances as well as preparation method and application thereof

A technology of toad venom fat-soluble matter and sustained-release microspheres, which is applied in the field of sustained-release preparations of toad venom, can solve problems such as easy demulsification and deterioration, and achieve the effects of prolonging the drug effect time, high encapsulation rate, and reducing the number of administrations

Inactive Publication Date: 2012-07-04
SOUTH CHINA AGRI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

All three preparations can effectively reduce the toxicity and irritation of the fat-soluble extract of Bufoni Bufoni or its monomers, but the lipid nanoparticle and lipid microsphere injection of Bufoni Bufoni are injection emulsions, which are easy to demulsify and deteriorate after being left for a period of time; Cinobufaffir-based albumin nanoparticles are a new dosage form limited to the monomer of Cinobufaffir-based

Method used

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  • Slow-release microsphere containing venenum bufonis lipoclastic substances as well as preparation method and application thereof
  • Slow-release microsphere containing venenum bufonis lipoclastic substances as well as preparation method and application thereof
  • Slow-release microsphere containing venenum bufonis lipoclastic substances as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0047] The emulsification solvent evaporation method prepares the polylactic acid sustained-release microspheres of the bufo fat-soluble substance, including the following steps:

[0048] After the toad cake is pulverized, it is extracted with dichloromethane, the solvent is distilled off under reduced pressure, and dried in vacuum to obtain a fat-soluble substance of toad venom. Weigh 0.50g of Bufoni fat-soluble matter and 2.85g of polylactic acid with an average molecular weight of 30,000Da, dissolve them in 33mL of dichloromethane, and after they are completely dissolved, add the above solution dropwise to 667mL of 1% (w / v) polyvinyl alcohol (PVA-224) aqueous solution (1% content means that the amount of polyvinyl alcohol is 6.67g), at the same time, under low temperature (ice bath) high-speed (1200r / min) stirring for 8min, the obtained emulsion was stirred at low speed (200r / min) for 6h , centrifuged at 15000r / min for 10min, the precipitate was taken, washed 3 times, and v...

Embodiment 2

[0061] The method of emulsifying solvent evaporation to prepare cinobufaction-based polylactic acid-glycolic acid sustained-release microspheres includes the following steps:

[0062] Weigh 25mg of cinobufaction base and 4.00g of polylactic acid-glycolic acid copolymer with an average molecular weight of 30000Da, dissolve them in 40mL of dichloromethane, and after they are completely dissolved, add the above solution dropwise to 800mL of 1% (w / v) In the aqueous solution of polyvinyl alcohol (PVA-224), at the same time, stir at high speed (1200r / min) at low temperature (ice bath) for 8min, stir the obtained emulsion at low speed (200r / min) for 6h, centrifuge at 15000r / min for 10min, take the precipitate and wash it for 3 3.62 g of cinobufaction-based polylactic-glycolic acid sustained-release microspheres were obtained by vacuum drying.

[0063] According to the method for determining the drug loading in Example 1, the content of the cinobufaction base in the slow-release micro...

Embodiment 3

[0065] The spray-drying method prepares the polylactic acid sustained-release microspheres of the bufo fat-soluble substance, comprising the following steps:

[0066] After the toad cake is powdered, it is extracted with ethyl acetate, the solvent is removed by distillation under reduced pressure, and the toad venom is dried in vacuum to obtain a fat soluble substance of toad venom. Weigh 10.00 g of bufo bufo fat solution and 90.00 g of polylactic acid with an average molecular weight of 30,000 Da, dissolve them in 800 mL of ethyl acetate, shake the solution well and spray dry to prepare drug-loaded microspheres. The inlet temperature of the spray dryer was controlled at 50°C, the outlet temperature at 30°C, and the liquid flow rate at 5mL / min. The dry micropowder was collected and weighed 83.50 g.

[0067] In this example, the content of the bufo bufo solubles in the sustained-release microspheres was 9.92%. Observing the microspheres with a scanning electron microscope, it...

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Abstract

The invention discloses a slow-release microsphere containing venenum bufonis lipoclastic substances as well as a preparation method and application of the slow-release microsphere. The slow-release microsphere is prepared from 0.5 to 30.6 percent of venenum bufonis lipoclastic substances and 69.4 to 99.5 percent of packing materials, wherein the venenum bufonis lipoclastic substances are venenum bufonis extracts using ethanol, ethyl acetate or dichloromethane as solvents, or are bufadienolide monomers obtained from the venenum bufonis lipoclastic substances, and the pakcing materials are preferably selected from polylactic acid or polylactic acid-glycolic acid copolymers. The venenum bufonis lipoclastic substance slow-release microsphere obtained by the invention has the advantages that the medicine loading capability and the encapsulation rate are high, the stability is good, the slow-release effect is obvious, the medicine toxicity can be reduced, the medicine irritation is reduced, the medicine effect time is prolonged, and the medicine administration times are decreased. Various modes such as intravenous injection, intramuscular injection, oral administration and the like are adopted for medicine administration, the slow-release microsphere can be directly used for treating tumor in the medical clinical aspect, or is used for treating various diseases through being matched with other traditional Chinese medicine; and in the veterinary clinical aspect, the slow-release microsphere can be used for treating inflammation or can be used for treating infectious diseases through the combined application with chemotherapy medicine.

Description

technical field [0001] The invention relates to a slow-release preparation of toad venom, in particular to a sustained-release microsphere containing toad venom fat-soluble matter, a preparation method and application thereof. Background technique [0002] Venenum Bufonis, also known as Toad Meizhi ("Medicinal Properties"), Toad Meisu ("Rihuazi Materia Medica"), is a white substance secreted by the back ear glands and skin glands of Bufodae animals such as Bufo bufo or Bufo black orbit. Serum, processed and dried, has sweet, spicy, warm and poisonous properties, and has the functions of detoxification, swelling, refreshment, resuscitation, heart strengthening and pain relief, etc. It is widely used clinically to treat various cancers, tuberculosis, heart Disease, malignant blood disease, periodic facial paralysis, acute pharyngitis and chronic hepatitis B and other infectious diseases, can also be used for local anesthesia. Modern pharmacological studies have shown that toa...

Claims

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Application Information

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IPC IPC(8): A61K35/56A61K31/585A61K47/34A61K9/16A61P35/00A61P29/00A61P11/00A61P1/00A61P31/00A61K35/65
Inventor 陈建新王文佳刘雅红曾振灵方炳虎张晓丽杨耀智
Owner SOUTH CHINA AGRI UNIV
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