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Uncaria alkaloid temperature-sensitive gel nasal delivery preparation and preparation method thereof

A technology of sensitive gel nasal cavity and temperature-sensitive gel matrix, which is applied in the direction of pharmaceutical formulation, drug combination, drug delivery, etc., and can solve problems such as poor water solubility of rhynchophylline, reduced clearance rate of nasal cilia, and short stagnation time

Pending Publication Date: 2022-02-11
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The object of the present invention is to provide a new dosage form of rhynchophylline for the problems that rhynchophylline is poor in water solubility and difficult to enter the central nervous system through the blood-brain barrier, and the stagnation time of the drug in the nasal cavity is short after nasal administration. , that is rhynchophylline thermosensitive gel nasal administration preparation, this new dosage form changes from a liquid state to a semi-solid state with higher viscosity through the nasal administration route, so as to achieve tight adhesion with the nasal mucosa and reduce the clearance rate of nasal cilia. The slow release of the drug allows the drug to be fully absorbed by the nasal mucosa and quickly acts on the nervous system to achieve brain targeting

Method used

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  • Uncaria alkaloid temperature-sensitive gel nasal delivery preparation and preparation method thereof
  • Uncaria alkaloid temperature-sensitive gel nasal delivery preparation and preparation method thereof
  • Uncaria alkaloid temperature-sensitive gel nasal delivery preparation and preparation method thereof

Examples

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Embodiment 1

[0062] The formulation of rhynchophylline thermosensitive gel nasal administration preparation: rhynchophylline: 1.6g, poloxamer 407: 20g, poloxamer 188: 1g, PEG-6000: 1g, HP-β-CD: 2g, plus Purified water to 100 mL.

[0063] Preparation of Rhynchophylline Thermosensitive Gel Nasal Administration by Cold Melting Method:

[0064] Prepare the aqueous solution of hydroxypropyl-β-cyclodextrin (HP-β-CD), disperse rhynchophylline in the aqueous solution of hydroxypropyl-β-cyclodextrin, add hydrochloric acid with an appropriate concentration of 0.1mol / L, and make Uncaria Fully dissolve the alkali, adjust the pH to 6 with L sodium hydroxide at a concentration of 0.1mol / , form a rhynchophylline solution, store at 4°C; mix Poloxamer 407, Poloxamer 188, and polyethylene glycol 6000 , add purified water to the mixture to make the mixture wet with water, put it in the refrigerator, and store it at 4°C for more than 24 hours until a clear, lump-free, uniformly dispersed blank thermosensitiv...

Embodiment 2

[0072] The formulation of rhynchophylline thermosensitive gel nasal administration preparation: rhynchophylline: 1.6g, poloxamer 407: 21g, poloxamer 188: 1.5g, PEG-6000: 2g, HP-β-CD: 2g, Add purified water to 100mL.

[0073] The preparation method is the same as in Example 1, and rhynchophylline thermosensitive gel nasal cavity administration preparation is prepared.

[0074] The rhynchophylline thermosensitive gel nasal administration preparation is translucent uniform and delicate viscous colloid in appearance, with a pH value of 6.2 and a gelling temperature of 33.8°C. Adopt transmission electron microscope to observe rhynchophylline temperature-sensitive gel nasal administration preparation of this embodiment, such as Figure 8 As shown, micelles and micellar aggregates can be observed, compared with Example 1, by Figure 9 It can be seen from the TEM images that as the content of poloxamer 407 increases, the ratio of micelles to micellar aggregates also increases.

[0...

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Abstract

The invention belongs to the field of pharmaceutical preparations, and discloses a rhynchophylline temperature-sensitive gel nasal delivery preparation which is formed by dispersing a rhynchophylline solution in a temperature-sensitive gel matrix, every 100 mL of the rhynchophylline temperature-sensitive gel nasal delivery preparation contains 1 to 6 g of rhynchophylline, 17 to 22 g of poloxamer 407, 0.5 to 4 g of poloxamer 188, 0.5 to 3 g of polyethylene glycol 6000, 1 to 4 g of hydroxypropyl-beta-cyclodextrin and the balance of water. The rhynchophylline temperature-sensitive gel nasal delivery preparation is in a liquid state when the environment temperature does not reach the phase-change temperature, and can be changed into a semi-solid gel state from the liquid state within a short time after entering the nasal cavity, so that administration can be facilitated, and the medicine can be fully absorbed. The rhynchophylline temperature-sensitive gel nasal delivery preparation has a slow release property during drug release, can bypass a blood brain barrier, has a certain brain targeting property, and can improve the concentration of the drug in the brain.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to a rhynchophylline thermosensitive gel nasal administration preparation and a preparation method. Background technique [0002] Rhyncholphylline is an alkaloid extracted from the hooked branches of the Chinese folk plant Uncaria, and its molecular formula is C 22 h 28 N 2 o 4 , with a molecular weight of 384.46, is a white or off-white crystalline powder. Rhynchophylline, whether used as an active ingredient alone or in combination with other drugs, has protective effects on the degenerative nervous system, including sedative, anti-convulsant, anti-epilepsy, anti-anxiety, and brain neuron protection. It relieves symptoms of patients and helps It is used in the treatment of degenerative nervous system diseases such as Parkinson's disease and Alzheimer's disease, so it has high medicinal value. The overall clinical safety of rhynchophylline was good, and there was no ab...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/06A61K47/10A61K47/40A61K47/02A61K31/438A61P25/16A61P25/28
CPCA61K9/06A61K9/0043A61K47/10A61K47/40A61K47/02A61K31/438A61P25/16A61P25/28
Inventor 柳文媛韩凌飞林红蕾冯锋刘富垒曲玮
Owner CHINA PHARM UNIV
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