Lanreotide long-acting injection microsphere preparation and preparation method thereof

A technology of lanreotide and microspheres, which is applied in the field of long-acting lanreotide injection microsphere preparations and its preparation, can solve the problems of complex process of long-acting sustained-release preparations, difficulties in comprehensive clinical promotion, poor compliance of treatment, etc., and achieve Improve medication compliance, reduce treatment burden, and reduce production costs

Inactive Publication Date: 2011-01-12
蚌埠丰原涂山制药有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] Both acromegaly and growth hormone-type pituitary adenoma require long-term treatment, but long-term injection administration makes patients miserable, and the compliance of treatment is very poor. Although approved by the US FDA, there is long-acting lanreotide abroad Sustained-

Method used

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  • Lanreotide long-acting injection microsphere preparation and preparation method thereof
  • Lanreotide long-acting injection microsphere preparation and preparation method thereof
  • Lanreotide long-acting injection microsphere preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] 1. Dissolve gelatin with water to make a 7.5% gelatin solution, add 80g of lanreotide hydrochloride to 200mL of the above gelatin solution, heat on a water bath at 40°C to completely dissolve the drug, and use it as the inner water phase for later use;

[0039] 2. Dissolve 800g polylactic acid-glycolic acid copolymer (the molar ratio of lactide to glycolide monomer is 85 / 15) in 1000mL acetone, as the organic phase, and set aside;

[0040] 3. Add the organic phase of step 2 to the inner water phase of step 1, mix the inner water phase and the organic phase, and ultrasonically emulsify at 45°C to obtain colostrum;

[0041] 4. Cool the above-mentioned colostrum to 12°C, add it to 4000mL of 4% polyvinyl alcohol that has been cooled to 12°C, and stir at a high speed of 7500r / min for 2min to obtain double emulsion;

[0042] 5. Add the double emulsion to 2000mL 0.1% polyvinyl alcohol solution, heat in a water bath at 30°C, stir at a low speed of 75r / min for 3h, then evaporate ...

Embodiment 2

[0046] 1. Dissolve gelatin with water to make a 7.5% gelatin solution, add 100g of lanreotide acetate to 250mL of the above gelatin solution, heat on a water bath at 55°C to completely dissolve the drug, and use it as the inner water phase for later use;

[0047] 2. Dissolve 1000g of polylactic acid-glycolic acid copolymer (the molar ratio of lactide to glycolide monomer is 85 / 15) in 1500mL of acetone, as the organic phase, and set aside;

[0048] 3. Add the organic phase of step 2 to the inner water phase of step 1, mix the inner water phase and the organic phase, and ultrasonically emulsify at 40°C to obtain colostrum;

[0049] 4. Cool the above-mentioned colostrum to 16°C, add it to 4000mL of 4% polyvinyl alcohol that has been cooled to 16°C, and stir at a high speed of 5000r / min for 2min to obtain double emulsion;

[0050] 5. Add the double emulsion to 2000mL 0.1% polyvinyl alcohol solution, heat in a water bath at 30°C, stir at a low speed of 50r / min for 3h, then evaporat...

Embodiment 3

[0054] 1. Dissolve hydroxypropyl cellulose with water to make a 5% hydroxypropyl cellulose solution, add 150g of lanreotide acetate to 400mL of the above hydroxypropyl cellulose solution, and heat on a water bath at 70°C to make the drug completely Dissolved, as the inner water phase, for subsequent use;

[0055] 2. Dissolve 1500g of polylactic acid-glycolic acid copolymer (the molar ratio of lactide to glycolide monomer is 85 / 15) in 2000mL of acetone, as the organic phase, and set aside;

[0056] 3. Add the organic phase of step 2 to the inner water phase of step 1, mix the inner water phase and the organic phase, and ultrasonically emulsify at 35°C to obtain colostrum;

[0057] 4. Cool the above-mentioned colostrum to 14°C, add it to 4000mL of 4% polyvinyl alcohol that has been cooled to 14°C, and stir at a high speed of 6500r / min for 2min to obtain double emulsion;

[0058] 5. Add the double emulsion to 2000mL 0.1% polyvinyl alcohol solution, heat in a water bath at 30°C, ...

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Abstract

The invention provides a lanreotide long-acting injection microsphere preparation, which is prepared from the following raw materials in part by weight: 10 to 400 parts of lanreotide or salt thereof, 100 to 4,000 parts of polylactic acid-glycolic acid copolymer, 0.1 to 50 parts of stabilizer, 50 to 5,000 parts of excipient and 0.1 to 200 parts of surfactant. The invention also provides a preparation method for the lanreotide long-acting injection microsphere preparation. The lanreotide long-acting injection sustained-release microsphere preparation is subjected to subcutaneous injection once every two months, one conventional treatment course only needs two times of medication, and the preparation greatly relieves the treatment burden of patients, improves the medication compliance and reduces the treatment cost; and the preparation method has the advantages of simple process, low production cost and easy popularization.

Description

technical field [0001] The invention relates to a long-acting lanreotide injection microsphere preparation and a preparation method thereof. Background technique [0002] Acromegaly is a rare disease due to overproduction of growth hormone, which is clinically progressive and characterized by weakness and weakness, usually due to growth hormone (GH)-secreting pituitary cell adenomas. If GH overproduction occurs before puberty, gigantism results; if it occurs after puberty, the disease appears more insidious. The easily seen disease is characterized by progressive bone growth, enlarged hands and feet, thickened skin, and roughened face. Life-threatening conditions such as cardiac hypertrophy, high blood pressure, and malignant sleep apnea are relatively difficult to observe. [0003] Pituitary adenoma is a tumor that occurs on the pituitary gland. It is one of the common neuroendocrine tumors, accounting for about 10-15% of central nervous system tumors. The vast majority ...

Claims

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Application Information

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IPC IPC(8): A61K38/31A61K9/16A61K47/34A61P35/00A61K47/10A61K47/26
Inventor 李士桥汪洪湖
Owner 蚌埠丰原涂山制药有限公司
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