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Phentolamine external-applied preparation and its preparation method

A technology of phentolamine and phentolamine mesylate, which is applied in the field of quick-acting phentolamine external preparations and its preparation, high-efficiency, and phentolamine external preparations, which can solve the problem of different effects and onset time To achieve the effects of avoiding hepatic first-pass effect, good drug safety and reasonable design

Inactive Publication Date: 2008-03-19
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Overall, the effect and onset time of phentolamine transdermal preparations are not satisfactory at present

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] Add 5mL eucalyptus oil into 35mL Tween-80, stir well and set aside. Take an appropriate amount of distilled water, add 5g of phentolamine mesylate, 100mL of propylene glycol, 150mL of glycerin, and 0.2g of chlorhexidine acetate, and stir to dissolve it completely. Slowly inject this solution into the mixed solution of eucalyptus oil and Tween, add distilled water to 1000mL, and obtain a clear and uniform solution after stirring, adjust the pH to 3.5-4.5 with hydrochloric acid, filter, and pack in special spray bottles, namely Get topical sprays.

Embodiment 2

[0032] Take 10mL of clove oil and add 10mL of oleic acid, mix evenly, preheat to 55°C as the oil phase, and set aside; add 6g of lecithin into 100mL of distilled water to disperse, add 60mL of glycerin, 10g of tragacanth, and 1g of ethylparaben, and stir to make Dissolve, heat to 55°C, and continue to stir, while slowly adding the oil phase, homogenize at high speed for 8 minutes to obtain colostrum, pass the colostrum through the high-pressure homogenizer for 6 times, add phentolamine mesylate under low-speed stirring 5g, add distilled water to 1000mL, filter, and pack in special spray bottles to obtain the external spray.

Embodiment 3

[0034] Take an appropriate amount of distilled water, add 50mL Tween-80, fully dissolve, add 50mL peppermint oil, ultrasonic emulsification for 5 minutes, add 150mL glycerin, 0.2g chlorhexidine acetate, 1g phentolamine mesylate, add distilled water after fully dissolving to 1000mL, mix well. The pH is adjusted to 3.5-4.5 with hydrochloric acid, and the mixture is divided into special spray bottles to obtain the external spray.

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Abstract

The invention belongs to the western medicine preparation field and concretely relates to an efficient and quick effective external preparation of phentolamine which considers the volatile oil of natural plant and the extracted finished product of the volatile oil of the natural plant as a percutaneous sorbefacient and the preparation method of the external preparation. The invention selects the percutaneous sorbefacient of the natural volatile oil to prepare an external percutaneous preparation of the phentolamine of the invention by considering the phentolamine as the only curative active matter of the preparation and adding the necessary medicinal auxiliary materials. The animal experiment testifies that the invention can keep the drug usability and synchronously reduce the medicament dosage greatly and reduce the side effect to the whole body and the use cost. Compared with the prior art, the preparation can improve the percutaneous absorption of the drug dosage of the phentolamine very obviously and shortens the latent period of effecting, and the preparation has good medicament safety and can provide the patient with more satisfying curative effect.

Description

technical field [0001] The invention belongs to the field of western medicine preparations, and relates to an external preparation of phentolamine, in particular to a high-efficiency and quick-acting external preparation of phentolamine using natural plant volatile oil and its extracted and refined product as a transdermal absorption accelerator and a preparation method thereof. Background technique [0002] Erectile dysfunction (erectile dysfunction, ED) is a common and important sexual dysfunction. Epidemiological data suggest that the occurrence of male ED is more common, and there is a close relationship with increasing age and diseases such as dyslipidemia, hypertension, coronary artery disease, and diabetes. At present, there are about 152 million men in the world suffering from ED. With the aging of human society, it is predicted that by 2025, there will be 322 million men in the world suffering from this sexual dysfunction. [0003] Phentolamine is a non-selective a...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K9/70A61K31/4164A61P15/10
Inventor 蒋新国陶炜兴
Owner FUDAN UNIV
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