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Lyophilized emulsion preparation for injection of levo-gossypol and acetate of levo-gossypol

A technology of L-gossypol and acetate, which is applied in the direction of freeze-drying transportation, emulsion transportation, active ingredients of aldehydes, etc., can solve the problems of poor stability and achieve strong stability, good safety in vivo, and good stability Effect

Active Publication Date: 2012-07-04
山东肽莱生物制药有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, except for the oral tablet of gossypol, there is no report on the preparation of L-gossypol or L-gossypol acetate with stronger pharmacological effects but poorer stability.

Method used

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  • Lyophilized emulsion preparation for injection of levo-gossypol and acetate of levo-gossypol
  • Lyophilized emulsion preparation for injection of levo-gossypol and acetate of levo-gossypol

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Example 1 Preparation of lyophilized milk preparation for L-gossypol injection

[0035] The formula is as follows:

[0036] L-Gossypol 10mg

[0037] Oleic acid 980mg

[0038] Glycerin 4.8g

[0039] Soy Lecithin 31.2mg

[0040] Span 80 7.8mg

[0041] Trehalose 14mg

[0042] Human Albumin 14mg

[0043] Sodium sulfite 0.21mg

[0044] Soybean oil for injection 17.2g

[0045] Water for injection 10L

[0046] The preparation method is as follows:

[0047] 1) mixing L-gossypol, soybean oil for injection, soybean lecithin, Span 80, and sodium sulfite to make an oil phase;

[0048] 2) Mix water for injection, glycerin and oleic acid, add sodium hydroxide to adjust the pH to 9.0-10.5;

[0049] 3) Pour the oil phase into the water phase to prepare colostrum;

[0050] 4) Use a high-pressure homogenizer to homogenize the colostrum to make final milk;

[0051] 5) Add treha...

Embodiment 2

[0056] Example 2 Preparation of lyophilized milk preparation for L-gossypol acetate injection

[0057] The formula is as follows:

[0058] L-Gossypol Acetate 10mg

[0059] Oleic acid 1200mg

[0060] Glycerin 4.5g

[0061] Soy Lecithin 27.2mg

[0062] Span 80 6.8mg

[0063] Trehalose 9.5mg

[0064] Human Albumin 9.5mg

[0065] Sodium sulfite 0.26mg

[0066] Soybean oil for injection 19.7g

[0067] Water for injection 10L

[0068] The preparation method is as follows:

[0069] 1) mixing L-gossypol acetate, soybean oil for injection, soybean lecithin, Span 80, and sodium sulfite to make an oil phase;

[0070] 2) Mix water for injection, glycerin and oleic acid, add sodium hydroxide to adjust the pH to 9.0-10.5;

[0071] 3) Pour the oil phase into the water phase to prepare colostrum;

[0072] 4) Use a high-pressure homogenizer to homogenize the colostrum to make final...

Embodiment 3

[0078] Example 3 Preparation of lyophilized milk preparation for L-gossypol injection

[0079] The formula is as follows:

[0080] L-Gossypol 10mg

[0081] Oleic acid 1300mg

[0082] Glycerin 4.2g

[0083] Soy Lecithin 25.6mg

[0084] Span 80 6.4mg

[0085] Trehalose 12mg

[0086] Human Albumin 12mg

[0087] Sodium sulfite 0.22mg

[0088] Soybean oil for injection 14.1g

[0089] Water for injection 10L

[0090] The preparation method is as follows:

[0091] 1) mixing L-gossypol, soybean oil for injection, soybean lecithin, Span 80, and sodium sulfite to make an oil phase;

[0092] 2) Mix water for injection, glycerin and oleic acid, add sodium hydroxide to adjust the pH to 9.0-10.5;

[0093] 3) Pour the oil phase into the water phase to prepare colostrum;

[0094] 4) Use a high-pressure homogenizer to homogenize the colostrum to make final milk;

[0095] 5) Add tr...

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Abstract

The invention discloses lyophilized emulsion preparation for injection of levo-gossypol and acetate of the levo-gossypol and a preparation method thereof. The lyophilized emulsion preparation for the injection of the levo-gossypol and the acetate of the levo-gossypol consists of levo-gossypol or levo gossypol acetate, oleic acid, glycerol, emulsifying agent, cryoprotectant, oil for injection, potential of hydrogen (pH) conditioning agent, antioxidant and water for injection. Mixture of granulesten and Span 80 serves as the emulsifying agent, mixture of trehalose and human serum albumin servesas the cryoprotectant, and the prepared lyophilized emulsion preparation is strong in salability and high in bioavailability.

Description

technical field [0001] The invention relates to a pharmaceutical preparation of L-gossypol and its acetate, in particular to a freeze-dried milk preparation for injection of L-gossypol and its acetate. Background technique [0002] Gossypol (Gossypol), CAS No. 303-45-7, is a yellow phenolic compound composed of two optical isomers, L-gossypol and D-gossypol. Natural gossypol exists in the seeds, leaves, stems and roots of the Malvaceae cotton plant. [0003] Gossypol is known for its spermicidal properties and can be used as a male birth control. At present, gossypol acetate oral preparations have been marketed as male contraceptives or for the treatment of gynecological diseases, including endometriosis, menorrhagia or disorders. Chinese patent 200510022777.9 (applicant: Shenyang Pharmaceutical University, publication number CN1827117, publication date: September 06, 2006, date of authorization announcement: December 16, 2009) discloses a gossypol acetate slow for the tre...

Claims

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Application Information

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IPC IPC(8): A61K9/19A61K31/11A61K47/44A61P15/00A61P15/16A61P35/00A61K9/107
Inventor 厉保秋厉凌子高继友
Owner 山东肽莱生物制药有限公司
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