Teriparatide sustained-release microsphere and preparation method thereof

A technology of slow-release microspheres and teriparatide, applied in the field of medicine, can solve the problems of injection site damage, lack of sustained release, low patient compliance, etc., achieve high encapsulation rate, reduce the probability of infection, The effect of reducing the frequency of administration

Active Publication Date: 2013-06-19
HYBIO PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] However, the existing teriparatide drug does not have sustained-release properties and needs to be injected subcutaneously every day. For patients, such frequent injections for a long time will bring gre

Method used

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  • Teriparatide sustained-release microsphere and preparation method thereof
  • Teriparatide sustained-release microsphere and preparation method thereof
  • Teriparatide sustained-release microsphere and preparation method thereof

Examples

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preparation example Construction

[0050] The preparation method of the teriparatide sustained-release microspheres provided by the present invention comprises the following steps: taking a carrier and teriparatide and dissolving them in an organic solvent, mixing them with an aqueous solution of a surfactant, and emulsifying to obtain an emulsion; taking the emulsion and surfactant The aqueous solution of the agent is mixed, the organic solvent is removed, purified and dried.

[0051] The organic solvent is one or a mixture of two or more of dichloromethane, acetone, ethyl acetate, acetonitrile, methyl acetate, 1,4-dioxane, ethanol, and dimethylformamide.

[0052] In the preparation method of the teriparatide sustained-release microspheres provided by the present invention, the mass volume concentration of the surfactant in the aqueous solution of the surfactant mixed with the organic solvent containing the carrier and the teriparatide is 1% to 10%.

[0053] The surfactant in the aqueous solution of the surfac...

Embodiment 1

[0080] Example 1 Preparation of Teriparatide Sustained-release Microspheres by Emulsion Solvent Evaporation Method

[0081] Accurately weigh 2g of lactic acid-glycolic acid copolymer (85:15, Mw=15000) and 200mg of teriparatide, dissolve in 40mL of dichloromethane as the dispersed phase; add the above dispersed phase slowly in a water bath at 10°C Put it into 200mL aqueous solution containing 1% polyvinyl alcohol, emulsify for 1 hour, the emulsification condition is 1000 rpm, stir while adding; add the obtained emulsion into 500mL aqueous solution containing 0.1% polyvinyl alcohol, the temperature is 25 ℃, stir The organic solvent was volatilized in 4 hours to form solidified microspheres; the solution obtained above was collected by centrifugation at 3000 rpm, washed three times with purified water to remove the drug and polyvinyl alcohol on the surface of the microspheres, and dried in vacuum for two days to obtain Teriparatide extended-release microspheres.

Embodiment 2

[0082] Example 2 Preparation of Teriparatide Sustained Release Microspheres by Emulsion Solvent Evaporation Method

[0083] Accurately weigh 10g of lactic acid-glycolic acid copolymer (75:25, Mw=15000) and 200mg of teriparatide, dissolve it in 40mL of dichloromethane as the dispersed phase; slowly add the above dispersed phase in a water bath at 10°C Put it into 200mL aqueous solution containing 2% polyvinyl alcohol, emulsify for 1 hour, the emulsification condition is 1000 rpm, stir while adding; add the obtained emulsion into 500mL aqueous solution containing 0.2% polyvinyl alcohol, the temperature is 25 ℃, stir The organic solvent was volatilized in 4 hours to form solidified microspheres; the solution obtained above was collected by centrifugation at 3000 rpm, washed three times with purified water to remove the drug and polyvinyl alcohol on the surface of the microspheres, and dried in vacuum for two days to obtain Teriparatide extended-release microspheres.

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Abstract

The invention relates to the technical field of medicines, and in particular relates to a teriparatide sustained-release microsphere and a preparation method thereof. The teriparatide sustained-release microsphere comprises a teriparatide and a carrier, wherein the particle size of the teriparatide is 30 micrometers-50 micrometers; and the carrier is a mixture of one or two of polyester, starch, gelatin, Arabic gum, albumin, alginate and chitosan. The teriparatide microsphere is prepared by adjusting the constitution and molecular weight of the carrier and the medicine-loading rate and particle size of the microsphere according to the properties of the teriparatide. The prepared microsphere is stable in releasing and small in sudden releasing, the dose administration times can be reduced, the probability of infection is decreased, patients can conveniently take the microsphere, and the compliance of the patients is improved. Experiments show that the teriparatide has uniform particle size distribution, high encapsulation efficiency and large medicine-loading capacity. The sustained-release microsphere can be externally released for 10 days.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a teriparatide sustained-release microsphere and a preparation method thereof. Background technique [0002] Teriparatide, English name Teriparatide, is the biologically active N-terminal region of the human parathyroid hormone (PTH) peptide sequence. The complete human parathyroid hormone contains 84 amino acids, and teriparatide is a polypeptide fragment composed of 1 to 34 amino acids located in the N-terminal region. The molecular formula is C 181 h 291 N 55 o 51 S 2 , the molecular weight is 4177.77. [0003] Endogenous parathyroid hormone is a major regulator of calcium and phosphorus metabolism in bone and kidney. PTH increases the calcium concentration in serum, and with the increase of calcium concentration, the absorption of calcium by bone also partially increases. Long-term elevation of PTH will deplete bone stores. But intermittent exposure to PTH activates ...

Claims

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Application Information

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IPC IPC(8): A61K38/29A61K9/16A61K9/10A61K47/42A61K47/36A61K47/34A61P5/18
Inventor 徐春莲郑春莲马亚平袁建成
Owner HYBIO PHARMA
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