Octreotide acetate dry powder inhalation preparation and preparation method thereof

A technology for inhalation of octreotide acetate and dry powder, which is applied in powder delivery, pharmaceutical formulations, peptide/protein components, etc. It can solve the problems of easy adhesion, aggregation, dispersion, etc., and achieve high-efficiency preparation, high emptying rate and deposition rate, and fluidity Good results

Active Publication Date: 2020-10-13
GUANGZHOU NEWORLD PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] Based on this, it is necessary to provide a preparation method of octreotide acetate dry powder inhalation preparation, so that patients are more acceptable and convenient to use, while improving the dispersibility, inhalation performance, emptying rate and deposition rate of the dry powder, and solving the problem of common spray-dried powder. The problem of poor dispersion of adhesion and aggregation can improve the relative bioavailability

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  • Octreotide acetate dry powder inhalation preparation and preparation method thereof
  • Octreotide acetate dry powder inhalation preparation and preparation method thereof
  • Octreotide acetate dry powder inhalation preparation and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0038] Example 1 Preparation and in vitro evaluation of octreotide acetate dry powder inhalation preparation

[0039] Mannitol is used as a drug carrier, ammonium carbonate is used as a porogen, the mass ratio of mannitol to ammonium carbonate is 8:2, the solid content is 1%, the drug content is 1%, and the spray drying solvent is water. Its preparation method comprises the following steps:

[0040]Weigh 0.8g of mannitol and 0.2g of ammonium carbonate, and dissolve them in 98ml of distilled water; weigh 1.0g of octreotide acetate, dissolve them in the above solution, and prepare a spray drying solution. During the spray drying process, water is used as the spray drying solvent, the inlet temperature (inlet air temperature) is 100°C, and the compressed air flow rate is 0.8m 3 / min, the atomization pressure is 150kPa, and the liquid supply rate is 1.5mL / min to obtain octreotide acetate fractal powder. The drug powder is packed into capsules and packed into a dry powder inhalat...

Embodiment 2

[0053] Example 2 Pharmacokinetic evaluation of octreotide acetate dry powder inhalation preparation

[0054] Mannitol is used as a drug carrier, ammonium carbonate is used as a porogen, the mass ratio of mannitol to ammonium carbonate is 1:1, the solid content is 3%, the drug content is 1%, and the spray drying solvent is water. Its preparation method comprises the following steps:

[0055] Weigh 1.5g of mannitol and 1.5g of ammonium carbonate, and dissolve them in 96ml of distilled water; weigh 1.0g of octreotide acetate, dissolve them in the above solution, and prepare a spray drying solution. During the spray drying process, water is used as the spray drying solvent, the inlet temperature is 110°C, and the air flow is 0.7m 3 / min, the atomization pressure is 165kPa, and the liquid supply rate is 1.8mL / min to obtain octreotide acetate fractal powder. The medicine powder is packed into a capsule and packed into a dry powder inhalation device to obtain the octreotide acetate...

Embodiment 3

[0063] With mannitol as the drug carrier and ammonium carbonate as the porogen, the mass ratio of mannitol:ammonium carbonate is 10:0, 9:1, 8:2, 7:3, 6:4, 5:5. Take 2.0g of mannitol and ammonium carbonate, dissolve in 97ml of distilled water; weigh 1.0g of octreotide acetate, and prepare a spray-dried solution according to the ratio of solid content 2% and drug content 1%. During the spray drying process, water is used as the spray drying solvent, the inlet temperature (inlet air temperature) is 120°C, and the compressed air flow rate is 0.6m 3 / min, the atomization pressure is 155kPa, and the liquid supply rate is 2.0mL / min to obtain octreotide acetate fractal powder. The drug powder is put into capsules and put into a dry powder inhalation device to obtain dry powder prescriptions of different ratios of mannitol and porogen ammonium carbonate.

[0064] The two parameters of powder yield and aerodynamic diameter were selected as the investigation index, and the results of ea...

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Abstract

The invention relates to an octreotide acetate dry powder inhalation preparation and a preparation method thereof. The preparation method comprises the following steps of dissolving a medicine carrier and a hole forming agent into a proper amount of distilled water to obtain a mixed solution; weighing a proper amount of octreotide acetate to be mixed with the obtained mixed solution; preparing a spraying drying solution, wherein the chemical content in the spraying drying solution is 0.5 percent to 1.5 percent; performing spraying drying; obtaining the octreotide acetate fragment powder. The prepared dry powder inhalation preparation has the advantages that the recipe is simple; the safety is high; the one-step efficient preparation is realized; the relative bioavailability is high.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to an octreotide acetate dry powder inhalation preparation and a preparation method thereof. Background technique [0002] Octreotide acetate is a synthetic octapeptide compound, which is an analogue of fourteen-peptide human somatostatin. The pharmacological effects of octreotide are similar to natural hormones, but its inhibitory effect on growth hormone, glucagon and insulin is stronger. Due to the structural modification of the 1st, 4th, and 8th amino acids, it is not easily destroyed by proteases in the body, so it has a stronger inhibitory effect on hormone secretion and a longer half-life in the body, about 2 hours. Its mechanism of action includes: inhibition of the secretion and release of growth hormone; as an important hormone-regulating peptide for cell proliferation and differentiation, it indirectly inhibits tumor cell proliferation by inhibiting the secreti...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/72A61K47/26A61K47/02A61K38/08
CPCA61K9/0075A61K9/143A61K9/145A61K38/08
Inventor 吴传斌侯嫒琳潘昕权桂兰黄莹李露陈航平
Owner GUANGZHOU NEWORLD PHARMA CO LTD
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