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Octreotide acetate freeze-dried combination for injection and preparation method thereof

A technology for octreotide acetate and a composition, which is applied in the field of pharmacy, can solve problems such as long half-life, hidden danger, microbial contamination, etc., and achieves the effects of improving stability, overcoming local irritation, good shelf-life stability and compatibility stability

Active Publication Date: 2014-08-06
西藏嘉信景天药业有限公司 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0015] (2) Long half-life: the half-life of subcutaneous injection is 2 hours
[0020] In the patent application number 200910074427.5, in order to overcome the above shortcomings of octreotide acetate injection, Tween-80 and citric acid were added to the prescription to improve the stability of the solution, but the injection described in this invention has not been terminally extinguished. Bacteria, although there is a sterilization and filtration process, there is also a hidden danger of microbial contamination during the liquid storage process, and the product has not taken effective protective measures against oxidation

Method used

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  • Octreotide acetate freeze-dried combination for injection and preparation method thereof
  • Octreotide acetate freeze-dried combination for injection and preparation method thereof
  • Octreotide acetate freeze-dried combination for injection and preparation method thereof

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Embodiment 1 Pre-experiment

[0032] 1. During the preparation of octreotide acetate solution, the optimal pH of the solution was determined by examining the stability of solutions with different pH values, and at the same time, different pH buffer pairs were investigated to examine whether they were suitable for the prescription.

[0033] Table 1 Stability investigation of octreotide acetate solutions with different pHs (the index is the content of related substances, 20°C)

[0034] pH 0h 1h 2h 4h 8h 3.5 0.52% 0.60% 0.67% 0.78% 0.90% 4.0 0.48% 0.57% 0.64% 0.74% 0.88% 4.5 0.40% 0.42% 0.42% 0.44% 0.49% 5.0 0.47% 0.40% 0.43% 0.45% 0.48% 5.5 0.55% 0.62% 0.73% 0.80% 0.94% 6.0 0.58% 0.69% 0.80% 0.94% 1.15%

[0035] The study found that the octreotide acetate solution had better stability in the pH range of 4.5 to 5.0. In the investigation of different buffer systems, we found that lactic acid / sodium bic...

Embodiment 2

[0048] The pH of the solution does not fall into the optimal pH range, the temperature of the solution preparation is not controlled at a low level, and the freezing and pre-freezing method is medium freezing

[0049] prescription

[0050] Octreotide Acetate

[0051] (C 49 h 66 N 10 o 10 S 2 ) 0.1g

[0052] Mannitol 45g

[0053] Lactic acid 3.4g

[0054] Sodium bicarbonate to adjust pH to 3.5

[0055] Add water for injection to 1000ml

[0056]

[0057] Makes 1000 bottles

[0058] Take the prescribed amount of mannitol, lactic acid and water for injection about 800ml, stir to dissolve, add 0.1% activated carbon, heat to 80°C and stir for 30 minutes, decarbonize through titanium rod circulation, cool the filtrate to 30°C, add the prescribed amount of octreotide acetate After stirring and dissolving, add sodium bicarbonate to adjust the pH to 3.5, and add water for injection to 1000ml. Send it to a sterile room by a peristaltic pump, filter it through a 0.22 μm mic...

Embodiment 3

[0061] The pH of the solution does not fall within the optimal pH range, the solution preparation temperature is not controlled at a low level, and the freezing and pre-freezing are prescribed in the middle freezing method

[0062] Octreotide Acetate

[0063] (C 49 h 66 N 10 o 10 S 2 ) 0.1g

[0064] Mannitol 45g

[0065] Tartaric acid 3.0g

[0066] Sodium tartrate Adjust pH to 4.0

[0067] Add water for injection to 1000ml

[0068]

[0069] Makes 1000 bottles

[0070] Take the prescribed amount of mannitol, tartaric acid and water for injection about 800ml, stir to dissolve, add 0.1% activated carbon, heat to 80°C and stir for 30 minutes, decarbonize through titanium rod circulation, cool the filtrate to 30°C, add the prescribed amount of octreotide acetate After stirring and dissolving, add sodium tartrate to adjust the pH to 4.0, and add water for injection to 1000ml. Send it to a sterile room by a peristaltic pump, filter it through a 0.22 μm microporous membr...

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PUM

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Abstract

The invention provides an octreotide acetate freeze-dried combination for injection, which comprises octreotide acetate, mannitol and a proper amount of buffer substances, wherein the mass ratio of the octreotide acetate to the mannitol is 1:(450-500); and the buffer substances are lactic acid and sodium bicarbonate and can be tartaric acid and sodium tartrate. The invention also provides a preparation method of the composition. The composition provided by the invention is produced by adopting an aseptic technique; by striving to make the technological breakthrough in optimal pH range and optimal preparation temperature in a liquid medicine preparation process, the product stability is improved; and finally, a freeze-dried product is prepared. By adopting a quick-freezing mode for pre-freezing, a finished product has low related substance content and good re-solubility, can be preserved at room temperature for two months and can be refrigerated for two years, thereby facilitating the product transportation and delivery. By clinically matching with a solution, the combination has good stability and low local injection irritation. The invention provides a safe and effective octreotide acetate freeze-dried combination for injection, which has good and controllable quality, for clinics.

Description

technical field [0001] The present invention relates to the field of pharmacy. Background technique [0002] Octreotide acetate chemical name: L-cysteinyl, D-phenylalanyl-L-cysteinyl-L-phenylalanyl-D-tryptophanyl-L-lysyl-L-threonyl -N-[2-Hydroxy-1-(hydroxymethyl)propyl]-cyclo(2→7)-disulfide [R-(R*,R*)]acetate [0003] L-Cysteinamide,D-phenylalanyl-L-cysteinyl-L-phenylalanyl-D-tryptophyl-L-lysyl-L-threonyl-N-[2-hydroxy-1-(hydroxymethyl)propyl]-,cyclic(2→7) -disulfide;[R-(R*,R*)]acetate salt [0004] Its structural formula is [0005] : [0006] Molecular formula: C 49 h 66 N 10 o 10 S 2 · x CH 3 COOH (x=1.4~2.5) [0007] Molecular weight: 1019.24 (calculated as octreotide) [0008] CAS: 83150-76-9 [0009] Since Brazeau et al. isolated somatostatin (Somatostatin, ST) from sheep hypothalamus in 1973, a lot of research has been done on the production, distribution and biological activity of ST, and its primary structure has been determined. [0010] With the dev...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K38/08A61P1/00A61P1/18A61P5/08A61P35/00A61P35/04
Inventor 叶东赵卉唐建华
Owner 西藏嘉信景天药业有限公司
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