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Blank and topotecan hydrochloride containing polycystin liposome and preparation method thereof

A multivesicular liposome and blank technology, applied in the field of sustained-release preparations, can solve the problems that the sustained-release drug effect of topotecan in vivo cannot be achieved, the sustained-release effect is unsatisfactory, and the application cannot be applied.

Inactive Publication Date: 2010-06-23
SHANGHAI INST OF PHARMA IND
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But its sustained-release effect is not ideal, basically can not reach the effect of topotecan sustained-release drug in vivo
At present, although the multivesicular liposome preparations of certain drugs have been successfully developed, because different drugs have different physical and chemical properties and mechanisms of action, the prescription and preparation process of its multivesicular liposomes have no effect on other drugs. generally not applicable
Therefore, for topotecan hydrochloride, a specific drug, in order to achieve the purpose of sustained release and targeted delivery in vivo, there are still the following problems: it is necessary to find a specific prescription and preparation process according to the requirements of its clinical application before it can be prepared. multivesicular liposome formulation

Method used

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  • Blank and topotecan hydrochloride containing polycystin liposome and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0062] Step 1: In a clean glass vessel add 1 mL containing 19.8mM (14.85mg) lecithin, 4.2mM (3.13mg) dipalmitoylphosphatidylglycerol, 30mM (11.61mg) cholesterol and 3.75mM (3.32mg) trioleic acid Chloroform solution of glycerides. This solution is called the lipid phase.

[0063] Step 2: Add 1mL of the internal water phase of the aqueous solution of 120mM (15.86mg) ammonium sulfate into the above-mentioned glass container containing the lipid phase, and stir at a speed of 10,000rpm for 10 minutes with a high-speed shearer to obtain W / O type colostrum.

[0064] Step 3: 5 mL of a solution containing 5% (w / v) (250 mg) glucose and 40 mM (29.36 mg) lysine was placed on the colostrum layer, and then mixed at a speed of 7500 rpm for 10 seconds to obtain W / O / W type double milk.

[0065] Step 4: Transfer the double emulsion to a 250mL Erlenmeyer flask containing 7mL containing 5% (w / v) (350mg) glucose and 40mM (40.93mg) lysine, in a constant temperature water bath at 37°C, and make ...

Embodiment 2

[0070] Step 1: Add 1 mL of 5 mM (3.96 mg) Hydrogenated Soy Lecithin, 0.5 mM (0.38 mg) Dipalmitate Phosphatidylserine, 10 mM (3.87 mg) Cholesterol and 0.155 mM (0.073 mg) Tricaprylic Glycerin to a clean glass container Esters in chloroform-ether solution. This solution is called the lipid phase.

[0071] Step 2: Add 0.5mL of the inner water phase of the aqueous solution of 10mM manganese sulfate (0.845mg) and 6% (w / v) (600mg) sucrose into the above-mentioned glass container containing the lipid phase, and use a high-speed shearing machine to Stir at a speed of 10,000 rpm for 10 minutes to obtain W / O colostrum.

[0072] Step 3: 7.5 mL of a solution containing 0.5% (w / v) (37.5 mg) mannitol and 80 mM (87.71 mg) lysine was placed on the colostrum layer, and then mixed at a speed of 4500 rpm for 40 seconds to obtain W / O / W type double emulsion.

[0073] Step 4: Transfer the double emulsion to a 250mL Erlenmeyer flask containing 9mL containing 0.5% (w / v) (45mg) mannitol and 80mM (...

Embodiment 3

[0078] Step 1: Add 1 mL of a dichloromethane solution containing 100 mM (75 mg) lecithin, 20 mM (8.49 mg) phosphatidic acid, 10 mM (3.87 mg) cholesterol and 13 mM (11.51 mg) triolein into a clean glass container. This solution is called the lipid phase.

[0079] Step 2: Add 1mL of the inner water phase of the aqueous solution with 1000mM (192.1mg) citric acid into the above-mentioned glass container containing the lipid phase, and stir at a speed of 10,000rpm for 10 minutes with a high-speed shearer to obtain a W / O type colostrum.

[0080] Step 3: 20 mL of a solution containing 10% (w / v) (2000 mg) mannitol and 20 mM (58.48 mg) lysine was placed on the colostrum layer, and then mixed at a speed of 7500 rpm for 20 seconds to obtain W / O / W type double milk.

[0081] Step 4: Transfer the double emulsion to a 1000mL Erlenmeyer flask containing 22mL containing 10% (w / v) (2200mg) mannitol and 20mM (64.32mg) lysine. Flow through the suspension in the Erlenmeyer flask, slowly evapor...

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Abstract

The invention discloses a blank polycystin liposome and a topotecan hydrochloride containing polycystin liposome and a preparation method thereof; the blank polycystin liposome comprises the following ingredients by mass parts: 1 part of lipid ingredient and 0.1-50 parts of ion gradient regulator, wherein the lipid ingredient comprises amphipathy lipid and neutral lipid which have 5-36:1 molar ratio. The topotecan hydrochloride containing polycystin liposome comprises drug active ingredient-topotecan hydrochloride and the blank liposome which is used as a carrier; in the invention, the blank polycystin liposome which is encapsulated with the encapsulate is prepared firstly, and then the topotecan hydrochloride is led to penetrate through a phospholipid membrane to be loaded in liposome internal water phase by adopting a transmembrane gradient active medicine carrying method, so as to obtain the topotecan hydrochloride containing polycystin liposome. In the invention, the utilization rate of the raw materials is high, the medicine carrying concentration is high, and the polycystin liposome has good slow release function in in-vivo and in-vitro experiments and has better anti-tumor effect.

Description

technical field [0001] The invention relates to the field of sustained-release preparations, in particular to a blank multivesicular liposome, a topotecan hydrochloride multivesicular liposome and a preparation method thereof. Background technique [0002] Topotecan (Topotecan, TPT) was first developed by Smithkline Beecham in 1990. It is a semi-synthetic water-soluble derivative of camptothecin. It was approved by the FDA in 1996 for the treatment of progressive drug-resistant ovarian cancer and has been approved successively. For the treatment of lobular cell lung cancer. Topotecan has a good effect on recurrent or drug-resistant neurocytoma, non-small cell lung cancer, small cell lung cancer, ovarian cancer, breast cancer, colon cancer and esophageal cancer. [0003] Topotecan is clinically available as an injection. Due to the short biological half-life of topotecan hydrochloride, multiple administrations are required in clinical application, and the patient's complian...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K47/24A61K47/02A61K31/4745A61P35/00
Inventor 陈亭亭陆伟根王培全李军虞丽芳王莉莉
Owner SHANGHAI INST OF PHARMA IND
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