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Alprostadil hydroxypropyl-alpha-cyclodextrin inclusion compound injection

A technology of alprostadil and hydroxypropyl, which is applied in the field of medicine, can solve problems such as existing deficiencies, and achieve the effects of low toxicity, high bioavailability, and good stability

Inactive Publication Date: 2015-08-26
海南路易丹尼生物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, through further studies, it was found that the stability and bioavailability of the alprostadil inclusion complexes obtained by β-cyclodextrin and its analogues still have deficiencies after a period of time.

Method used

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  • Alprostadil hydroxypropyl-alpha-cyclodextrin inclusion compound injection
  • Alprostadil hydroxypropyl-alpha-cyclodextrin inclusion compound injection
  • Alprostadil hydroxypropyl-alpha-cyclodextrin inclusion compound injection

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] Example 1 Alprostadil Hydroxypropyl-α-Cyclodextrin Inclusion Complex for Injection

[0040] prescription:

[0041]

[0042] Preparation Process

[0043] (1) Weigh 20g of hydroxypropyl-α-cyclodextrin, add 1500g of water for injection, stir and dissolve completely, and prepare solution A;

[0044] (2) Take by weighing 20mg alprostadil, add 20g ethanol and make dissolving completely, make solution B;

[0045] (3) Combine solution A and solution B, adjust the pH to 4.9 with disodium hydrogen phosphate and sodium dihydrogen phosphate buffer solution at pH 5.0, stir for 5 hours until completely dissolved, and become a clear and uniform solution;

[0046] (4) Weigh 20 g of dextran, stir to dissolve completely, concentrate under reduced pressure at 45° C., and remove ethanol and part of water;

[0047] (5) Add 0.75g of activated carbon, stir and adsorb for 20 minutes, filter for decarbonization, and sterilize and filter;

[0048] (6) Filling; 1.5g / bottle.

[0049] (7) Fre...

Embodiment 2

[0050] Example 2 Alprostadil Hydroxypropyl-α-Cyclodextrin Inclusion Complex for Injection

[0051] prescription:

[0052]

[0053] Preparation Process

[0054] (1) Weigh 80g of hydroxypropyl-α-cyclodextrin, add 2400g of water for injection, stir and dissolve completely, and prepare solution A;

[0055] (2) Take by weighing 100mg alprostadil, add 50g ethanol and make dissolving completely, make solution B;

[0056] (3) Combine solution A and solution B, adjust the pH to 4.8 with disodium hydrogen phosphate and sodium dihydrogen phosphate buffer solution at pH 5.0, stir for 3 hours until completely dissolved, and become a clear and uniform solution;

[0057] (4) Weigh 32g lactose, stir to dissolve completely, concentrate under reduced pressure at 40°C, remove ethanol and part of water;

[0058] (5) Add 1.2g of activated carbon, stir and adsorb for 30 minutes, filter for decarbonization, and sterilize and filter;

[0059] (6) Filling; 2.4g / bottle.

[0060] (7) Freeze-dryi...

Embodiment 3

[0061] Example 3 Alprostadil Hydroxypropyl-α-Cyclodextrin Inclusion Complex for Injection

[0062] prescription:

[0063]

[0064] Preparation Process

[0065] (1) Weigh 300g of hydroxypropyl-α-cyclodextrin, add 6000g of water for injection, stir and dissolve completely, and prepare solution A;

[0066] (2) Take by weighing 200mg alprostadil, add 150g ethanol and make dissolving completely, make solution B;

[0067] (3) Combine solution A and solution B, adjust the pH to 5.1 with disodium hydrogen phosphate and sodium dihydrogen phosphate buffer solution at pH 5.0, stir for 4 hours until completely dissolved, and become a clear and uniform solution;

[0068] (4) Weigh 100g of mannitol, stir to dissolve completely, concentrate under reduced pressure at 50°C, and remove ethanol and part of water;

[0069] (5) Add 3g of activated carbon, stir and adsorb for 25 minutes, filter for decarbonization, and sterilize and filter;

[0070] (6) Filling; 6g / bottle.

[0071] (7) Free...

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PUM

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Abstract

The invention provides an alprostadil hydroxypropyl-alpha-cyclodextrin inclusion compound injection. The inclusion compound injection is prepared through inclusion of alprostadil with hydroxypropyl-alpha-cyclodextrin, and the solubility of the alprostadil and the stability of the injection are greatly improved.

Description

technical field [0001] The invention relates to a pharmaceutical preparation of alprostadil, in particular to a hydroxypropyl-alpha-cyclodextrin inclusion complex injection of alprostadil, which belongs to the technical field of medicine. Background technique [0002] Alprostadil, also known as prostaglandin E1, is one of the natural prostaglandins. Prostaglandins exist in most mammalian tissues, and their basic structure is a 20-carbon fatty acid containing a cyclopentane and two fatty side chains. According to the double bond position and substituent on cyclopentane, it can be divided into several types, among which there are mainly four types such as E / F / A / B. Each class has different subtypes with a wide range of biological effects. [0003] Alprostadil is a high-efficiency biologically active substance with a chemical name of 11a, 15(S)-dihydroxy-9-carbonyl-13-reprostenic acid, molecular formula C 20 h 34 o 5 , molecular weight 354.48, structural formula: [0004] ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/08A61K47/40A61K31/5575A61P7/02A61P9/10
Inventor 王平曹仕霞
Owner 海南路易丹尼生物科技有限公司