Octreotide acetate preparation and preparation method thereof

A technology for octreotide acetate and preparation, which is applied in the field of octreotide acetate proliposome preparation and preparation, and can solve the problems of difficulty in achieving high encapsulation efficiency and lack of visibility.

Inactive Publication Date: 2012-07-04
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, as a polypeptide drug, there are many difficulties in encapsulating octreotide acetate into liposomes, and it is difficult to achieve high encapsulation efficiency by using conventional preparation methods, so there is no proliposome, liposome or micelle about OCT so far of Chinese patents

Method used

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  • Octreotide acetate preparation and preparation method thereof
  • Octreotide acetate preparation and preparation method thereof
  • Octreotide acetate preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] Example 1 Preparation of octreotide acetate liposomes by tert-butanol-water co-solvent freeze-drying method (1:60)

[0041] prescription

[0042] SPC 300mg

[0043] DSPG 300mg

[0044] Preparation:

[0045] 1) Dissolution: Weigh the prescribed amount of SPC and DSPG into a container, add 8 mL of tert-butanol, dissolve in a water bath at 65°C, add 18 mL of octreotide acetate solution containing 10% sucrose (concentration: 0.33 mg / mL), and continue adding in a water bath Until it is completely dissolved, until the solution is clear and transparent, dispense it.

[0046] 2) Freeze-drying: The freeze-drying curve is as follows: Pre-freeze at -74°C for 8 hours → vacuumize at -35°C for 1 hour, and finally reach a vacuum of about 5 Pa → increase the temperature to -25°C and keep for 12 hours (sublimation drying) → The temperature was raised to 20°C and kept for 3 hours (analysis and drying) to obtain proliposomes.

[0047] 3) Reconstitution: Add 2.5 mL of 5% glucose solu...

Embodiment 2

[0049] Example 2 (1:15)

[0050] EPC 300mg

[0051] DPPG 66.7mg

[0052] Preparation:

[0053] 1) Dissolution: Weigh the prescribed amount of EPC and DPPG into a container, add 4 mL of tert-butanol, dissolve in a 65°C water bath, add 18 mL of acetic acid containing 5% sucrose (w / v) and 5% lactose (w / v) Octreotide solution (concentration: 0.33 mg / mL), continue to add in water bath until it is completely dissolved, until the solution is clear and transparent, then dispense it.

[0054] 2) Freeze-drying: The freeze-drying curve is as follows: Pre-freeze at -74°C for 8 hours → vacuumize at -35°C for 1 hour, and finally reach a vacuum of about 10 Pa → increase the temperature to -25°C and keep for 12 hours (sublimation drying) → The temperature was raised to 20°C and kept for 4 hours (analysis and drying) to obtain proliposomes.

[0055] 3) Reconstitution: Add 2.5 mL of 5% glucose solution to the precursor liposome, disperse and redissolve, and obtain the octreotide acetate l...

Embodiment 3

[0058] prescription

[0059] EPC 260mg

[0060] DPPG 30mg

[0061] DOPG 30mg

[0062] Preparation:

[0063] 1) Dissolution: Weigh the prescribed amount of EPC, DPPG and DOPG into a container, add 4 mL of tert-butanol, dissolve in a water bath at 65°C, add 18 mL of octreotide acetate solution containing 5% sucrose (w / v) (concentration: 0.33 mg / mL), continue to add in a water bath until completely dissolved, until the solution is clear and transparent, and dispense.

[0064] 2) Freeze-drying: The freeze-drying curve is as follows: Pre-freeze at -74°C for 8 hours → vacuumize at -35°C for 1 hour, and finally reach a vacuum of about 5 Pa → increase the temperature to -25°C and keep for 12 hours (sublimation drying) → The temperature was raised to 20°C and kept for 5 hours (analysis and drying) to obtain proliposomes.

[0065] 3) Reconstitution: Add 2.5 mL of 5% glucose solution to the precursor liposome, disperse and redissolve, and obtain the octreotide acetate liposome prep...

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Abstract

The invention belongs to the field of medicament preparations, and discloses an octreotide acetate lipidosome precursor and a preparation method thereof. The precursor lipidosome contains octreotide acetate, negatively-charged phospholipid and a cryoprotectant, and can contain an appropriate quantity of other lipids including phosphatidylchline and cholesterol; components such as an antioxidant, a pH regulating agent and the like can be added as required; the molar ratio of the octreotide acetate to the negatively-charged phospholipid is smaller than 1:1; and the mass ratio of the negatively-charged phospholipid to the cryoprotectant is 1:1-1:10. In the invention, a tert-butyl alcohol-water cosolvent freeze-drying method is adopted. The entrapment rate of an octreotide acetate lipidosome/micelle obtained by hydrating a freeze-dried product can be over 50 percent, an octreotide acetate lipidosome/micelle obtained by hydrating the freeze-dried product has high stability, and the problem of difficulty in entrapping a protein polypeptide medicament during preparation of a lipidosome/micelle preparation is solved. The preparation method is simple and practicable, and is suitable for industrial mass production.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular to an octreotide acetate proliposome preparation and a preparation method. Background technique [0002] Compared with traditional drugs, protein-polypeptide drugs not only have outstanding advantages such as small dosage, good curative effect, and low toxic and side effects, but also have some new characteristics different from traditional drugs, such as (1) protein has a spatial structure and is complete The spatial structure of protein drugs is often the basis for their activity; (2) protein drugs are unstable in vivo and in vitro. In vitro, factors such as high temperature, light, strong acid, and strong alkali in the environment can cause protein denaturation and inactivation; Low utilization; (3) Protein drugs have large molecular weight and poor ability to pass through biological barriers (such as cell membranes), which further affects their efficacy. Therefore, h...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K38/08A61K47/34A61P1/00A61P1/18A61P5/08A61P35/00
Inventor 邓意辉翟文君佘振南宋艳志
Owner SHENYANG PHARMA UNIVERSITY
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