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Mixed snuff prepn. for reducing side effect of Apomorphinum

A nasal administration preparation and preparation technology, applied in the field of new compound preparations, can solve problems such as abnormal taste and dizziness

Inactive Publication Date: 2002-10-23
ZHEJIANG ACAD OF MEDICAL SCI +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, some patients may experience side effects such as nausea, vomiting, dizziness and abnormal taste

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0015] Example 1 Apomorphine hydrochloride 1.4g granisetron hydrochloride 1.4g sodium carboxymethylcellulose 0.5g sodium bisulfite 0.5g distilled water Add to 100ml

[0016] The antiemetic effects of the above preparations were observed through animal experiments. The 8 dogs were divided into two groups, 4 in each group, half male and half male. The first group received intranasal instillation of preparations containing granisetron hydrochloride, and the second group received intranasal instillation of preparations without granisetron hydrochloride. The other ingredients of the two preparations were the same. Nasally drop 0.2ml for each dog, and observe the vomiting at the specified time. The results showed that none of the four dogs in the first group vomited, while two dogs in the second group experienced nausea and vomiting. (See Table 1) Table 1 Data comparison of vomiting in dogs after intranasal administration of apomorphine Treatment dose (mg) Vomiting incidence rate ...

Embodiment 2

[0018] Example 2 Apomorphine hydrochloride 1.4g menthol 0.7g hydroxypropyl β-cyclodextrin 10g sodium metabisulfite 0.3g EDTA-2Na 0.05g distilled water Add to 100ml

[0019] The effect of menthol on the incidence of vomiting after intranasal administration of apomorphine was studied in dogs. The 8 dogs were divided into two groups, 4 dogs in each group, half male and half male. The first group received a menthol-containing formulation and the second a menthol-free formulation. The other ingredients of the two preparations are the same, and 0.2ml is instilled into the nasal cavity of each dog.

[0020] The result is basically similar to Example 2. No vomiting occurred in the first group. In Group 2, two rats vomited.

[0021] Dogs are known to be suitable models for studying the emetic response to apomorphine. And dogs are 5-10 times more sensitive to apomorphine-induced vomiting than humans. If the apomorphine preparation does not cause vomiting after being used in dogs, ...

Embodiment 3

[0022] Example 3 Apomorphine Hydrochloride 1.4g Nicotine 1g Glycerin 5g Carbopol 940 1g Sodium Lauryl Sulfate 1g Sodium Hydroxide 0.4g Ethylparaben 0.1g Distilled water Add to 100g

[0023] Preparation method: mix carbopol with sodium lauryl sulfate and 30ml distilled water, then add ethylparaben aqueous solution and apomorphine hydrochloride, stir well to dissolve the drug completely, and finally dissolve sodium hydroxide in 10ml Add water and stir to obtain a transparent gel containing apomorphine hydrochloride.

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Abstract

An apomorphine preparation compound of nasal cavity feeding used for curing Parkinson syndrom, male erection disturbance and female sexual disturbance can eliminate or decrease the side effects of bad feeling, dizziness, vomiting and abnormal taste sense occured in the treatment of apomarphine through using preparation compound adding with the vomiting stop medicine. The aromatic substance is added in order to let the nasal cavity have feelings of refreshing and comfort after the medicine is fed and the natural or synthetic high polymer compound is added to liquid preparation in order to delay the retaining period of medicine in nasal cavity. The preparation has the advantage of transmitting the medicine towards the brain and furthermore can be used with convenience, safety, effectivenessand good compliance.

Description

technical field [0001] The invention is a novel compound preparation, especially a compound nasal administration preparation for treating Parkinson's syndrome, male erectile dysfunction and female sexual dysfunction and reducing the side effects of apomorphine. Background technique [0002] Apomorphine is a dopamine receptor agonist and acts on the central drug, and its action site is in the hypothalamus. Apomorphine has a good effect in the treatment of Parkinson's syndrome, and there have been extensive studies and reports on the treatment of impotence or sexual dysfunction. U.S. Patent Nos. 5,888,534 and 5,994,363 etc. have been disclosed for improving male erectile dysfunction. US Patent No. 5,945,117 also discloses the use of apomorphine to improve female sexual dysfunction. WO 99 / 27905 discloses the treatment of erectile dysfunction with nasal administration of apomorphine. Sublingual apomorphine tablets (usually containing 2.5-10 mg of apomorp...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/485A61P15/08A61P25/16
Inventor 陈国神蒋新国张望刚陆伟郑高利陈钧
Owner ZHEJIANG ACAD OF MEDICAL SCI
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