External preparation containing phentolamine and preparation method thereof

Abstract

The invention belongs to the preparation field of western medicines and particularly relates to a high-efficiency and quick-acting phentolamine external preparation which takes natural plant naphtha and the extraction elaboration product thereof as a transdermal sorbefacient and a preparation method thereof. The invention selects the transdermal sorbefacient of natural volatile oils, takes phentolamine as the main active substance which plays a role in treatment in the preparation and is added with the accessories necessary in pharmacy, so as to prepare the phentolamine external transdermal preparation. Proved by experimentation on animals, the preparation can largely reduce the medication dosage and lower the systemic side effect and use cost when simultaneously maintaining the effectiveness of drugs. Compared with the prior art, the preparation can significantly improve the transdermal drug absorption amount of phentolamine, and shorten latent period of onset, has good medication safety and can offer patients more satisfactory curative effect.

Description

technical field [0001] The invention belongs to the field of western medicine preparations, and relates to an external preparation containing phentolamine, in particular to a high-efficiency and quick-acting phentolamine external preparation using natural plant volatile oil and its extracted 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-selectiv...

AI Technical Summary

Problems solved by technology

Practice has shown that the prior art still has serious deficiencies in the effectiveness and safety of the accelerator, especially in the speed of onset, and there are also unreasonable problems in the dosage form of the preparation: the patent CN1113757 uses propylene glycol as a solvent, and at the same time Absorption promoting effect, yet the external application concentration of propylene glycol should generally not exceed 30%, and excessive concentration will produce local stimulation and allergic reaction; All select dimethyl sulfoxide (DMSO) as transdermal absorption accelerator in patent WO0108659 and CA1320442, and it has stench , long-term or large-scale use can cause severe irritation to the skin, and may even cause liver damage and neurotoxicity; the dosage form used in patents CN1380061 and CN2497789 is a transdermal patch, which has the disadvantage of high production cost, and more importantly, the lack of flexibility of the patch Sex, it cannot be in close contact with the skin of the penis and scrotum, which affects the therapeutic effect to a certain extent; on the other hand, since the total area of ​​the patch needs to be 70cm 2 , the patch still cannot be removed during use, and the user may cause discomfort and inconvenience due to foreign body sensation, and the compliance is poor; patent CN1383820 introduces phentolamine cream. Compared with the patch, the cream is more convenient to use. Uniform, reduce foreign body sensation, more acceptable to patients

But same as CN1380061, all selected laurocapram as transdermal absorption accelerator in the described technical scheme, although laurocaprazine is widely used in transdermal preparations, its promoting effect on phentolamine mesylate The penetration effect is relatively limited, which is not enough to exert the therapeutic effect of the drug in a short time, and the onset time is as long as 45 minutes, which is difficult to meet the needs of ED patients for rapid onset of effect

[0005] In addition, patents KR20010045152, WO9965303, EP0346297 and CN1113757 respectively introduced compound external preparations containing phentolamine, and the patents involved containing phentolamine, prostaglandins, prazosin, papaverine, nitroglycerin and some traditional Chinese medicines (such as Ligusticum chuanxiong But there are also defects such as unsatisfactory selection of absorption enhancers, long onset time, etc.

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