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Timolol liposome and preparation method thereof

A technology of timolol fat and timolol, which is applied in the field of timolol liposome and its preparation, can solve the problems of no preparation on the market, no timolol liposome, etc., and achieve stability Good, broad industrialization prospects, and the effect of reducing fluctuations

Inactive Publication Date: 2009-04-08
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] The present invention makes timolol into liposome for the first time. At present, there are no reports of timolol liposome at home and abroad, and there is no listing of related preparations. Therefore, the present invention has a remarkable practical application prospect and potential economic value

Method used

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  • Timolol liposome and preparation method thereof
  • Timolol liposome and preparation method thereof
  • Timolol liposome and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0060] Timolol 25mg

[0061] Phosphatidylcholine 170mg

[0062] Preparation method: Take the prescribed amount of phosphatidylcholine, dissolve it in 10mL ether, add 4mL200mmol·L -1 Ammonium sulfate solution, mixed evenly, and ultrasonicated for 5 minutes to form a stable W / O emulsion, which was placed in a 50mL beaker. Under constant temperature electromagnetic stirring at 40°C, add 200mmol·L when the colloidal state is reached -1 6 mL of ammonium sulfate solution, and continued to stir at constant temperature for 1 h to distill off the ether to obtain blank liposomes. After the dialyzed blank liposome was dissolved by adding timolol, add 1mol·L - 1 Adjust the pH of the NaOH solution to 9.2, place it in a water bath at 40°C and incubate it for 30 minutes, then dialyze it with 0.9% NaCl for 24 hours, adjust the volume to 10 mL, and obtain timolol liposomes.

Embodiment 2

[0064] Timolol 25mg

[0065] Phosphatidylcholine 170mg

[0066] Cholesterol 34mg

[0067] Preparation method: Take the prescribed amount of phosphatidylcholine and cholesterol, dissolve them in 10mL ether, add 4mL 200mmol·L -1 Ammonium sulfate solution, mixed evenly, and ultrasonicated for 5 minutes to form a stable W / O emulsion, which was placed in a 50mL beaker. Under constant temperature electromagnetic stirring at 40°C, add 200mmol·L when the colloidal state is reached -1 6 mL of ammonium sulfate solution, and continued to stir at constant temperature for 1 h to distill off the ether to obtain blank liposomes. After the dialyzed blank liposome was dissolved by adding timolol, add 1mol·L -1 Adjust the pH of the NaOH solution to 9.2, place it in a water bath at 40°C and incubate it for 30 minutes, then dialyze it with 0.9% NaCl for 24 hours, adjust the volume to 10 mL, and obtain timolol liposomes.

Embodiment 3

[0069] Timolol 50mg

[0070] Phosphatidylcholine 340mg

[0071] Cholesterol 68mg

[0072] Vitamin E 10mg

[0073] Preparation method: Take the prescribed amount of phosphatidylcholine, cholesterol and vitamin E, dissolve them in 10mL ether, add 4mL 200mmol·L -1 ammonium sulfate solution, mix well, and ultrasonicate for 5 minutes to form a stable W / O emulsion, and place the emulsion in a 50mL beaker. Under constant temperature electromagnetic stirring at 40°C, add 200mmol·L when the colloidal state is reached -1 6 mL of ammonium sulfate solution, and continued to stir at constant temperature for 1 h to distill off the ether to obtain blank liposomes. After the dialyzed blank liposome was dissolved by adding timolol, add 1mol·L -1 Adjust the pH of the NaOH solution to 9.2, place it in a water bath at 40° C. and incubate for 30 minutes, then dialyze it with 0.9% NaCl for 24 hours, and adjust the volume to 10 mL to obtain timolol liposomes.

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Abstract

The invention relates to the technical field of pharmaceutical preparation, and particularly discloses a timolol liposome and a method for preparing the same. The timolol liposome comprises timolol, phospholipid, cholesterol, antioxidant and the like, wherein the weight percentages of various composition are as follows: 0.01 to 60.00 percent of the timolol, 10.00 to 99.99 percent of the phospholipid, 0.00 to 68.00 percent of the cholesterol, 0.00 to 50.00 percent of the antioxidant, and 0.00 to 89.99 percent of osmotic pressure regulator. A gel matrix can be further added into the timolol liposome to prepare a gel. The timolol liposome has the advantages of high envelop rate, good stability, and excellent biocompatibility, bio-adhesion property and biodegradability, can form very good storage effect in a cornea, and can realize the aims of improving bioavailability, reduce toxicity, and reduce pungency, thus the timolol liposome is particularly suitable for eye instillation to better play the effect of the timolol to reduce the intraocular pressure and resist glaucoma.

Description

Technical field: [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to timolol liposomes and a preparation method thereof. Background technique: [0002] Timolol (timolol) is a β-adrenergic blocker, according to the classification of receptor subtypes and intrinsic sympathetic activity, it belongs to the second category, that is, it is non-selective, has no obvious intrinsic sympathomimetic activity and membrane stabilizing effect. By blocking the beta of the heart 1 Receptors slow down the heart rate, weaken the contractility of the heart, decrease the cardiac output, decrease the myocardial oxygen consumption, and decrease the blood pressure. [0003] With the continuous deepening of its pharmacological research, the clinical application of Timolol is also becoming more and more extensive. Such as: treatment of high blood pressure, anti-angina pectoris, anti-myocardial infarction, etc. In recent years, it has discovered ...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K31/5377A61P9/12A61P9/10A61P27/06
Inventor 聂淑芳张慧慧潘卫三李想关津
Owner SHENYANG PHARMA UNIVERSITY
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