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Title:  Asafetida extract as medicine for abstinence of drugs
United States Patent: 
7,288,269
Issued: 
October 30, 2007

Inventors:
 Wang; Zemin (Qionglai, CN)
Assignee: 
Wang; Yanding (Quionglai, P.R., CN)
Appl. No.: 
10/965,698
Filed: 
October 13, 2004


 

Executive MBA in Pharmaceutical Management, U. Colorado


Abstract

An asafetida extract in the preparation of medicine for abstinence of drugs. A method for abstinence of drugs, which comprises administering a therapeutically effective amount of asafetida extract to subjects. The asafetida extract may be extracted from factice resin of Ferula sinkiangensis K. M. Shen or Ferula fukanensis K.M. Shen, and consists essentially of .alpha.-pinene, .alpha.-terpinene, 2-borneol, terpin-4-ol, D-fenchyl alcohol, pinocarveol, .beta.-ocimene A, .beta.-ocimene B, di-sec-butyl disulfide, sec-butyl-trans-1-butenyl disulfide, sec-butyl-cis-propenyl disulfide, sec-butyl-cis-1-butenyl disulfide, sec-butyl-trans-2-butenyl disulfide and thio-sec-butyl-trans-methylethenyl disulfide. The asafetida extract may also be extracted from factice resin of F. assafoetida L from Iran and Afghanistan and the like, and consists essentially of .alpha.-pinene, 2-borneol, terpin-4-ol, D-fenchyl alcohol, pinocarveol, dimethyl disulfide, dimethyl trisulfide, methylpropenyl disulfide, 2,2-dimethylthiopropane, 1,2-diethylthiopropane, N,N-dimethylthioformamide and propenylbutyl disulfide. The medicine for abstinence of drugs prepared with asafetida extract is suitable for the use in the abstinence treatment of subjects addicted to opioid, morphine, marijuana, diamorphine and the like.

Description of the Invention

FIELD OF THE INVENTION

The present invention relates to the use of asafetida extract as a medicine for abstinence of drugs.

BACKGROUND OF THE INVENTION

Asafetida is a secretion of natural plant. According to "Pharmacopoeia of the People's Republic of China", edited in 2000, page 148, Part I, the asafetida is described as: bitter in taste, pungent, warm, going through spleen and stomach channel; eliminating stagnated food, dispelling cold, destroying intestinal worms and used for stagnated meat food, gore lump, abdomen lump, abdominal pain due to enterositosis. According to "National Chinese herbal medicine compilation", published by Renmin Sanitation Press, 1978, Vol. 2, p. 318 the asafetida is described as: bitter in taste, tepefaction, eliminating stagnated food, destroying intestinal worms and dispelling cold; effective in the treatment of malnutrition due to parasitic infestation, abdominal mass, distending pain in stomach and abdomen, malaria and diarrhea, and also effective in preventing measles. Asafetida is conventionally used as water decoction or pill, wherein the special strong odor of asafetida is difficult to be covered up and therefore limits its application. Use of modern preparation technology may cover up or weaken the special odor of asafetida. Therefore, there has been asafetida extract prepared by conventional methods from Chinese asafetida or asafetida from other countries, the extract being volatile oil or supersaturated aqueous solution of volatile oil.

Addictive drugs impair health of human body, seriously influence the stability of family and society, and is one of the sources of plunder, violence, degeneration and homicide. The drug abuse is a serious worldwide problem endangering human being. Some chemical drugs have been used as medicine for abstinence of drugs for a long time, e.g., phenoxyimidazoline hydrochloride (clonidine), methadone, barbiturates and other sedative hypnotics. These pharmaceutical chemicals are also narcotics or psychotropics, and may result in drug dependence. In addition, these chemicals may bring about many side effects in case of long-term use.

SUMMARY OF THE INVENTION

The present invention provides the use of asafetida extract in the preparation of medicine for abstinence of drugs. The medicine for abstinence of drugs is in a form selected from the group consisted of injection, capsule, drop pill, tablet, granule, powder, oral liquid and the like.

The present invention further provides a method for abstinence of drugs, which comprises administering a therapeutically effective amount of asafetida extract to subjects. In the present invention, the asafetida extract may be administrated in a form selected from the group consisted of injection, capsule, drop pill, tablet, granule, powder, oral liquid and the like.

In the present invention, the term "therapeutically effective amount of asafetida extract" refers to the amount of asafetida extract sufficient for producing an effect of abstinence of morphine. Commonly, the effective amount of asafetida extract is 0.1-20 g, preferably 1-3 g (equivalent to the amount of original crude material).

The asafetida extract according to the present invention may be extracted from factice resin of Ferula sinkiangensis K. M. Shen or Ferula fukanensis K. M. Shen, and consisted essentially of .alpha.-pinene, .alpha.-terpinene, 2-borneol, terpin-4-ol, D-fenchyl alcohol, pinocarveol, .beta.-ocimene A, .beta.-ocimene B, di-sec-butyl disulfide, sec-butyl-trans-1-butenyl disulfide, sec-butyl-cis-propenyl disulfide, sec-butyl-cis-1-butenyl disulfide, sec-butyl-trans-2-butenyl disulfide and thio-sec-butyl-trans-methylethenyl disulfide.

The asafetida extract according to the present invention may also be extracted from factice resin of F. assafoetida L from Iran, Afghanistan and the like, and consisted essentially of .alpha.-pinene, 2-borneol, terpin-4-ol, D-fenchyl alcohol, pinocarveol, dimethyl disulfide, dimethyl trisulfide, methylpropenyl disulfide, 2,2-dimethylthiopropane, 1,2-diethylthiopropane, N,N-dimethylthioformamide and propenylbutyl disulfide.

DETAILED DESCRIPTION OF THE PREFERRED EMBODIMENT

When drugs and narcotics enter human body, they bind with morphine receptor existing in some domains inside human brain and produce a series of euphoria sensations. Once the drugs are quitted, a series of abstinence syndromes are produced in the same manner. The inventors have conducted intensive experimental study and found asafetida extract has a regulatory effect on central nervous system. The effective ingredients in asafetida extract enter into human body and then combine with morphine receptor existing in human brain to maintain normal function of nerve cells, thereby resulting in the remission and even disappearance of abstinence syndrome, stopping drug addiction. Asafetida extract therefore can be used in the preparation of medicine for abstinence of drugs.

Asafetida extract may be prepared by conventional methods from the factice resin of Ferula sinkiangensis K. M. Shen or Ferula fukanensis K. M. Shen, the extract being volatile oil or supersaturated aqueous solution of volatile oil, pH 4-5.7. Above asafetida extracts were analyzed by GC-MS detection at Chengdu Analytic and Test Center of Chinese Academy of Sciences. The results demonstrated all of these asafetida extracts consisted essentially of .alpha.-pinene, .alpha.-terpinene, 2-borneol, terpin-4-ol, D-fenchyl alcohol, pinocarveol, .beta.-ocimene A, .beta.-ocimene B, di-sec-butyl disulfide, sec-butyl-trans-1-butenyl disulfide, sec-butyl-cis-propenyl disulfide, sec-butyl-cis-1-butenyl disulfide, sec-butyl-trans-2-butenyl disulfide and thio-sec-butyl-trans-methylethenyl disulfide.

Asafetida extract may also be prepared by conventional methods from the factice resin of F. assafoetida L from Iran, Afghanistan and the like, the extract being volatile oil or supersaturated aqueous solution of volatile oil, pH 4-5.7. Above asafetida extracts was analyzed by GC-MS detection at Chengdu Analytic and Test Center of Chinese Academy of Sciences. The results demonstrated all of these asafetida extracts consisted essentially of .alpha.-pinene, 2-borneol, terpin-4-ol, D-fenchyl alcohol, pinocarveol, dimethyl disulfide, dimethyl trisulfide, methylpropenyl disulfide, 2,2-dimethylthiopropane, 1,2-diethylthiopropane, N,N-dimethylthioformamide and propenylbutyl disulfide.

Asafetida extract may be prepared by conventional oil-water separation, water vapor distillation, azeotropic distillation, vacuum distillation or solvent extraction.

With regard to the oil-water separation, azeotropic distillation or water vapor distillation may be applied and volatile oil is separated by oil-water separator. 0.1-80 parts by weight of purified water is added to 0.1-20 parts by weight of asafetida and the azeotropic distillation or water vapor distillation is performed at 105-108.degree. C. 0.012-2.4 parts by weight of volatile oil is collected after oil-water separation (assuming average content of volatile oil in crude material is 12%).

With regard to the water vapor distillation, 0.1-80 parts by weight of purified water is added to 0.1-20 parts by weight of asafetida and the water vapor distillation is performed at 105-108.degree. C. 0.2-240 parts by weight of forerunning liquid is collected and redistillation is performed. 0.1-200 parts by weight of redistillation liquid, i.e. asafetida extract, is obtained after collection.

With regard to the azeotropic distillation, 0.5-400 parts by weight of purified water is added to 0.1-20 parts by weight of asafetida and the azeotropic distillation is performed at 105-108.degree. C. 0.2-240 parts by weight of forerunning liquid is collected and redistillation is performed. 0.1-200 parts by weight of redistillation liquid, i.e. asafetida extract, is obtained after collection.

With regard to the vacuum distillation, 0.5-400 parts by weight of purified water is added to 0.1-20 parts by weight of asafetida and the vacuum distillation is performed at 104-107.degree. C. and pressure of 1300-1400 Pa. 0.2-240 parts by weight of forerunning liquid is collected and redistillation is performed. 0.1-200 parts by weight of redistillation liquid, i.e. asafetida extract, is obtained after collection.

With regard to the solvent extraction, 0.1-20 parts by weight of asafetida is added to 0.6-120 parts by weight of organic solvents such as ethanol and chloroform. Weight ratio of ethanol and chloroform is 2:1. Reflux extraction is performed at 65-70.degree. C. for 2 hours. When the temperature of refluxing liquid drops to room temperature, the refluxing liquid is discharged and organic solvents are recovered. 0.1-80 parts by weight of purified water is added to obtained crude volatile oil and water vapor distillation is conducted at 105-108.degree. C. 0.2-240 parts by weight of forerunning liquid is collected and then subjected to redistillation. 0.1-200 parts by weight of redistillation liquid, i.e. asafetida extract, is obtained after collection.

Above medicine for abstinence of drugs may be in a form selected from the group consisting of injection, capsule, drop pill, tablet, granule, powder, oral liquid and the like. The injection may be administrated intramuscularly or intravenously.

In order to understand the essence of present invention, the asafetida injection, asafetida capsule, asafetida tablet, and asafetida granule for abstinence of drugs are prepared from asafetida extract. The use of asafetida extract as a medicine for abstinence of drugs is demonstrated by animal experiment and clinical trial.

The medicine for abstinence of drugs prepared with asafetida extract: asafetida injection. Solubilizer such as 2,3-HP, .beta.-CD (2,3-hydroxypropyl-.beta.-cyclodextrin) is added to asafetida extract with agitation and isotonic adjusting agent NaCl (NaCl for injection) is then added. Water for injection is added to a defined amount and agitation is continued. After pH adjustment, resulting solution is filtered through membrane filter, filled into ampules and sealed. Asafetida injection is obtained after sterilization.

The medicine for abstinence of drugs prepared with asafetida extract: asafetida capsule. The weight ratio of asafetida volatile oil and excipient is 1: 3-20, wherein the excipient is at least one selected from starch, compressible starch, hydroxypropyl cellulose with low substitution degree (L-HPC), microcrystalline cellulose, carboxymethyl starch sodium (CMS-Na). Excipients are placed into agitator and agitated for 5 min, then volatile oil is sprayed uniformly into excipients and agitation is continued for 5 min. 5% starch slurry is added to make a soft material, which is placed into a granulator and filtered through stainless steel sieve to form wet granules. The wet granules are dried below 60.degree. C. and obtained dry granules are put into granulator again and filtered through stainless steel sieve to adjust the granules. In order to filling the capsule uniformly and smoothly, lubricant such as magnesium stearate is added and the weight ratio of excipient and lubricant is 1: 0.002-0.01. Dry granules after adjustment are put into agitator and lubricant is added to mix for 5 min, then asafetida capsules are made in a full automatic capsule filling machine. Asafetida extract in each asafetida capsule is equivalent to 0.1-1 g asafetida crude material.

The medicine for abstinence of drugs prepared with asafetida extract: asafetida tablet. The weight ratio of asafetida volatile oil and excipient is 1: 3-20, wherein the excipient is at least one selected from starch, compressible starch, L-HPC, microcrystalline cellulose, CMS-Na. Excipients are placed into agitator and agitated for 5 min, then volatile oil is sprayed uniformly into excipients and agitation is continued for 5 min. 5% starch slurry is added to make a soft material, which is placed into a granulator and filtered through stainless steel sieve to form wet granules. The wet granules are dried below 60.degree. C. and obtained dry granules are put into granulator again and filtered through stainless steel sieve to adjust the granules. In order to tabletting uniformly and smoothly, lubricant such as magnesium stearate is added and the weight ratio of excipient and lubricant is 1:0.002-0.01. Dry granules after adjustment are put into agitator and lubricant is added to mix for 5 min, then asafetida tablets are made in a tablet machine. The asafetida tablets are then sent to a coating machine to form film coating. Asafetida extract in each asafetida tablet is equivalent to 0.1-1 g asafetida crude material.

The medicine for abstinence of drugs prepared with asafetida extract: asafetida granule. The weight ratio of asafetida volatile oil and excipient is 1:10-100, wherein the excipient is sucrose powder and dextrin. Excipients are placed into agitator and agitated for 5 min, then volatile oil is sprayed uniformly into adjuvant and agitation is continued for 5 min. 2% starch slurry is added to make a soft material, which is placed into a granulator and filtered through stainless steel sieve to form wet granules. The wet granules are dried below 60.degree. C. and obtained dry granules are put into granulator again and filtered through stainless steel sieve to adjust the granules. Dry granules after adjustment are sent to a granule racking machine for packaging. Asafetida extract in each package of asafetida is equivalent to 0.1-2 g asafetida crude material.
 


Claim 1 of 4 Claims

1. A method for abstinence of drugs which bind with morphine receptor, which comprises administering a therapeutically effective amount of asafetida extract to a subject in need thereof, wherein the asafetida extract is a volatile oil extracted by distillation from factice resin of Ferula sinkiangensis K. M. Shen, Ferula fukanensis K. M. Shen, or Ferula assafoetida L. from Iran and Afghanistan.

 

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