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Long-acting injection capable of inhibiting abrupt release effect

An injection, long-acting technology, used in medical preparations containing active ingredients, endocrine system diseases, peptide/protein components, etc. Fast speed and other problems, to achieve a smooth and long-lasting release effect, avoid loss of protein activity, and smooth blood drug concentration

Inactive Publication Date: 2004-09-08
SHANGHAI PHARMCO RES +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The delivery system does not require surgical implantation, and a sustained-release effect of several weeks and high bioavailability can be achieved with one administration, which significantly improves patient compliance, but the disadvantage is that the microspheres have an obvious burst-release effect , usually reaching or exceeding 20% ​​of the administered dose (Advanced Drug Delivery Reviews, 1997(28): 85-96), seriously affecting the safety and effectiveness of preparations, especially hormone preparations with strong drug effects
However, there are two obvious deficiencies in this type of delivery system: first, water or aqueous media are used as solvents, which can easily affect the stability of protein drugs during storage and use; The rate of erosion or degradation is fast, and the effect of delayed release is not ideal

Method used

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  • Long-acting injection capable of inhibiting abrupt release effect
  • Long-acting injection capable of inhibiting abrupt release effect

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Take 3 g of poloxamer 407, 7.5 g of poloxamer 188, 75 μl of phenol, 19.5 g of 10 mM sterile sodium citrate buffer solution (pH 6.0), and 0.264 g of sodium chloride. Sodium chloride and phenol were dissolved in sodium citrate buffer solution, and poloxamer was slowly added to the above solution under ice bath and stirring conditions, and stored in low temperature refrigeration until a clear solution was formed. Packaged in single doses after autoclaving.

[0035] 0.6g recombinant human growth hormone (rhGH)-Zn 2+ The compound and 0.035g of zinc carbonate were added to 30ml of dichloromethane solution containing 6g of PLGA (75:25, MW 15kD), ultrasonicated for 1 minute to disperse the solid particles evenly, and then the polymer solution was added to 300ml of polyvinyl alcohol solution (6% g / ml), stirred at 2000rpm for 1min, poured the solution into 2L of distilled water and continued to stir at a lower speed for 4h to completely volatilize the organic solvent to obtain P...

Embodiment 2

[0041] Take 4.5 g of poloxamer 407, 4.5 g of poloxamer 188, 300 μl of benzyl alcohol, 19.65 g of 10 mM sterile phosphate buffer solution (pH 6.8), and 1.35 g of mannitol. Mannitol and benzyl alcohol were dissolved in phosphate buffer solution, and poloxamer was slowly added to the above solution under the conditions of ice bath and stirring, and kept in cold storage until a clear solution was formed. Packaged in single doses after autoclaving.

[0042] Dissolve 0.12g leuprolide and 0.2g mannitol in 1.5ml buffer solution, and gradually add this solution dropwise to 30ml dichloromethane solution containing 6g PLGA (50:50, MW 10kD), emulsify at 5000rpm for 1min Immediately, the suspension was sprayed into a frozen ethanol solution through an ultrasonic nozzle, and the interface of the latter was sealed with liquid nitrogen. At -70°C, use ethanol to continuously extract dichloromethane from the microspheres, and remove the ethanol by filtration to obtain microspheres with good fl...

Embodiment 3

[0045] Take 4.5 g of poloxamer 407, 4.5 g of poloxamer 188, 75 μl of phenol, 20.74 g of 10 mM sterile sodium citrate buffer solution (pH 6.0), and 0.26 g of sodium chloride. Sodium chloride and phenol were dissolved in sodium citrate buffer solution, and poloxamer was slowly added to the above solution under ice bath and stirring conditions, and stored in low temperature refrigeration until a clear solution was formed.

[0046] Weigh 60mg of sodium alginate and a certain amount of folic acid-dextran complex (LFY) and dissolve them in 3ml of distilled water to make a mixed solution, and add them dropwise to 50ml of rapeseed oil (containing a certain amount of Span80) at a stirring speed of 1400rpm. Stir and emulsify for half an hour, slowly pour the emulsion into 200ml containing 0.5% CaCl 2 Cured in a mixture of acetone and ethanol (1:1) for 2 hours. The precipitate was washed once with ethanol, and finally cleaned with acetone.

[0047] release test : Precisely weigh 5 mg...

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Abstract

The present invention belongs to the field of medicinal preparation, relates to one kind of long-acting injection, and is especially one kind of long-acting medicine injection capable of inhibiting abrupt release effect. The present invention contains blank or medicated temperature-sensitive polymer solution and medicine-carrying biodegradable microsphere or particle, which is dispersed into the polymer solution just before use. The two components are mixed before use and injected into body, and medicine preparation will have its medicine on the surface and inside the microsphere or particle released smoothly and slowly. The present invention can raise the safety and effectiveness of available preparation.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations and relates to a long-acting injection of medicine, in particular to a long-acting injection of medicine capable of suppressing the burst release effect. Background technique [0002] In drug therapy, administration by injection is the most important route of administration besides oral administration. Many drugs are administered by injection because they are not easily absorbed or easily destroyed in the gastrointestinal tract. However, for some drugs that require long-term use, the physical damage and mental stress caused by frequent injections are often unbearable for patients. Unless the disease affects life, many patients may eventually choose to give up treatment. In recent years, with the rapid development of life-related disciplines, a large number of protein and peptide drugs have emerged. Such drugs usually have the characteristics of low oral bioavailability, poor physical a...

Claims

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Application Information

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IPC IPC(8): A61K9/10A61K38/27A61P5/06
Inventor 魏刚陆丽芳陆伟跃
Owner SHANGHAI PHARMCO RES
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