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Alprostadil freeze-dried microemulsion, raw material composition and preparation method of alprostadil freeze-dried microemulsion

A raw material composition, the technology of alprostadil is applied in the directions of pharmaceutical formulations, emulsion delivery, medical preparations containing active ingredients, etc. problems, to achieve the effect of reducing the risk of blood embolism, convenient storage and transportation, and stable quality

Inactive Publication Date: 2016-12-07
SHANGHAI MODERN PHARMA ENG INVESTIGATION CENT
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0012] The technical problem to be solved by the present invention is to overcome the large particle size of the existing alprostadil freeze-dried emulsion, the large fluctuation range of encapsulation efficiency and particle size between batches, poor stability and the need to adopt high-pressure homogenization during preparation. Machine shearing homogeneity, not only the preparation process is cumbersome, but also causes the defect of alprostadil drug degradation, provides a kind of drug with small particle size, high encapsulation efficiency, stability, safety, high efficiency, targeting, irritation and other side effects Alprostadil freeze-dried microemulsion, raw material composition and preparation method thereof

Method used

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  • Alprostadil freeze-dried microemulsion, raw material composition and preparation method of alprostadil freeze-dried microemulsion
  • Alprostadil freeze-dried microemulsion, raw material composition and preparation method of alprostadil freeze-dried microemulsion
  • Alprostadil freeze-dried microemulsion, raw material composition and preparation method of alprostadil freeze-dried microemulsion

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Embodiment 1

[0051] A kind of raw material composition of alprostadil freeze-dried microemulsion, its component and content are as follows:

[0052]

[0053] The preparation method of the alprostadil freeze-dried microemulsion of the present embodiment comprises the steps:

[0054] (1) Under nitrogen atmosphere, mix soybean oil, MCT, Solutol HS 15, egg yolk lecithin, glycerin and oleic acid according to the above formula, heat and dissolve at 40°C, then add alprostadil to it, dissolve and mix to obtain oil phase; mix lactose with 80mL water for injection, stir and dissolve to obtain the water phase;

[0055] (2) Under a nitrogen atmosphere, add the obtained water phase dropwise into the oil phase at a rate of 0.5 mL / min, and emulsify at 50-60° C. using Fluko shear conditions to obtain a microemulsion;

[0056] (3) Under a nitrogen atmosphere, adjust the pH of the obtained microemulsion to 4.5 with citric acid, then dilute it to 100 mL with water for injection, then perform sterile filt...

Embodiment 2

[0058] A kind of raw material composition of alprostadil freeze-dried microemulsion, its component and content are as follows:

[0059]

[0060] The preparation method of the alprostadil freeze-dried microemulsion of the present embodiment comprises the steps:

[0061] (1) Under nitrogen atmosphere, mix soybean oil, MCT, Solutol HS 15, egg yolk lecithin, glycerin and oleic acid according to the above formula, heat and dissolve at 25°C, then add alprostadil to it, dissolve and mix to obtain oil phase; glucose was mixed with 60mL water for injection, stirred and dissolved to obtain the aqueous phase;

[0062] (2) Under a nitrogen atmosphere, add the obtained water phase dropwise into the oil phase at a rate of 1.0 mL / min, emulsify at 40-45° C. using Fluko shear conditions to obtain a microemulsion;

[0063] (3) Under a nitrogen atmosphere, adjust the pH of the obtained microemulsion to 5.0 with citrate buffered salt, then dilute it to 100 mL with water for injection, and the...

Embodiment 3

[0065] A kind of raw material composition of alprostadil freeze-dried microemulsion, its component and content are as follows:

[0066]

[0067] The preparation method of the alprostadil freeze-dried microemulsion of the present embodiment comprises the steps:

[0068] (1) Under a nitrogen atmosphere, mix soybean oil, MCT, Solutol HS 15, egg yolk lecithin, glycerin and sodium oleate according to the above formula, heat and dissolve at 50°C, then add alprostadil to it, dissolve and mix to obtain Oil phase; mix sucrose with 80mL water for injection, stir and dissolve to obtain the water phase;

[0069] (2) Under a nitrogen atmosphere, the obtained water phase was added dropwise to the oil phase at a rate of 1.5 mL / min, and emulsified at 30-50° C. using Fluko shear conditions to obtain a microemulsion;

[0070] (3) Under a nitrogen atmosphere, adjust the pH of the obtained microemulsion to 5.2 with citrate buffered salt, then dilute it to 100 mL with water for injection, then p...

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Abstract

0.1-10mg / 100mL of alprostadil, 0.5-20g / 100mL of oil, 0.5-30g / 100mL of an emulsifier, 0.5-2g / 100mL of co-emulsifier, 5-40mg / 100mL of a stabilizer, 5-20g / 100mL of a cryoprotectant, 0.5-500mg / 100mL of a pH regulator and the balance of water. The preparation method comprises the following steps: preparing an oil phase and an aqueous phase in an inert atmosphere, dropping the aqueous phase to the oil phase at a dropping speed of 0.5-5mL / min, and conducting shearing and emulsifying at 30-50 DEG C, so that a micro-emulsion is obtained; and then, regulating the pH value of the micro-emulsion to 3.0-6.0, and conducting sterile filtration and freeze-drying, so that the alprostadil freeze-dried microemulsion is obtained. The alprostadil freeze-dried microemulsion disclosed by the invention is small in grain size, high in encapsulation efficiency, stable and safe and is efficient in targeting.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular to an alprostadil freeze-dried microemulsion, a raw material composition and a preparation method thereof. Background technique [0002] Alprostadil, also known as prostaglandin E1 (PGE 1 ), its water solubility is poor, unstable in aqueous solution, and the clinical irritation of alprostadil has direct connection with its free concentration, and its pH environment directly affects the degradation of alprostadil, thereby to the preparation of alprostadil Put forward higher technical requirements. According to current research, improving the encapsulation efficiency of alprostadil emulsion can effectively reduce the free concentration of alprostadil, slow down the degradation of alprostadil, and then reduce its clinical irritation. The following tables 1 and 2 are the oil-water phase distribution of alprostadil under different pHs studied in the prior art and the degradat...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K31/5575A61K47/34
Inventor 何军刘洁柳帅李晓燕
Owner SHANGHAI MODERN PHARMA ENG INVESTIGATION CENT
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