Neostigmine bromide muhivescular liposome and preparation method thereof

A technology of polycystic liposomes and cystic lipids, which is applied in the field of neostigmine polyvesicular liposomes and its preparation, and can solve the problems that there are no research reports on polycystic liposomes of bromoneostigmine

Active Publication Date: 2013-07-10
CHONGQING MEDICAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

After consulting patents and literature, there is no research report on bromneostigmine multivesicular liposomes

Method used

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  • Neostigmine bromide muhivescular liposome and preparation method thereof
  • Neostigmine bromide muhivescular liposome and preparation method thereof
  • Neostigmine bromide muhivescular liposome and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0015] The composition ratio by weight of each component contained in the formula is: 2.3 parts of neostigmine bromide, 2 parts of lecithin, 1.4 parts of cholesterol, 2.2 parts of triolein, 3 parts of glucose in the inner aqueous phase, poloxamer F-685 parts, poloxamer F127

[0016] 22.5 parts, 100 parts of water in the inner water phase, 2 parts of L-lysine, 13 parts of glucose in the outer water phase, 300 parts of water in the outer water phase.

[0017] The preparation method comprises the following steps: (1) preparation of colostrum: get prescription amount of neostigmine bromide, poloxamer F-127, poloxamer F-68, glucose dissolved in the inner water phase of prescription amount Water is used as the inner water phase, and the prescribed amount of phospholipids, cholesterol, and triolein are dissolved in ether as the oil phase, and the inner water phase and the oil phase are mixed, and W / O colostrum is prepared under vortex conditions; (2) Double emulsion preparation: get...

Embodiment 2

[0019] The composition ratio by weight of each component contained in the formula is: 1.5 parts of neostigmine bromide, 3 parts of lecithin, 1 part of cholesterol, 1.5 parts of triolein, 2 parts of glucose in the inner aqueous phase, poloxamer F-684 parts, poloxamer F12720 parts, 85 parts of water in the inner water phase, 1.5 parts of L-lysine, 11 parts of glucose in the outer water phase, 300 parts of water in the outer water phase.

[0020] The preparation method is basically the same as in Example 1.

Embodiment 3

[0022] The composition ratio by weight of each component contained in the formula is: 3 parts of neostigmine bromide, 2 parts of lecithin, 2 parts of cholesterol, 3 parts of triolein, 4 parts of glucose in the inner aqueous phase, poloxamer F-686 parts, poloxamer F12725 parts, 118 parts of water in the inner water phase, 2.5 parts of L-lysine, 16 parts of glucose in the outer water phase, 400 parts of water in the outer water phase.

[0023] The preparation method is basically the same as in Example 1.

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Abstract

The invention belongs to the field of a pharmaceutic preparation, and relates to a neostigmine bromide muhivescular liposome formula and a preparation method thereof. The neostigmine bromide muhivescular liposome prepared by the method can achieve slow release of a medicine, and prolongs the medicine effect time and the effective medicine duration.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to bromyostigmine polyvesicular liposomes and a preparation method thereof. Background technique [0002] Neostigmine bromide is a reversible anticholinesterase drug, which is mainly used in the treatment of myasthenia gravis, postoperative functional flatulence and urinary retention. But because its bioavailability is low, half-life is short (average plasma half-life is 0.87 hours), the patient needs long-term medication (the domestic market listing preparation is the common tablet of bromiostigmine, and specification is every 15mg, oral, and commonly used amount is 15mg once a day, several times a day, the dosage of patients with myasthenia gravis depends on the condition), which reduces the patient's compliance. In addition, the drug needs to be taken for a long time in clinical treatment, and frequent administration for a long time brings inconvenience to the patient. T...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K31/27A61K47/34A61P21/04A61P1/00A61P13/10A61K47/10A61K47/28
Inventor 张景勍罗文何丹赵春景
Owner CHONGQING MEDICAL UNIVERSITY
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