CN101168057A - Dopamine agonist preparation - Google Patents
Dopamine agonist preparation Download PDFInfo
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- CN101168057A CN101168057A CNA200610048754XA CN200610048754A CN101168057A CN 101168057 A CN101168057 A CN 101168057A CN A200610048754X A CNA200610048754X A CN A200610048754XA CN 200610048754 A CN200610048754 A CN 200610048754A CN 101168057 A CN101168057 A CN 101168057A
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- crude drug
- receptor
- agonist
- stimulating agent
- dopamine
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- 238000002360 preparation method Methods 0.000 title claims abstract description 20
- 239000003136 dopamine receptor stimulating agent Substances 0.000 title claims abstract description 11
- VYFYYTLLBUKUHU-UHFFFAOYSA-N dopamine Chemical compound NCCC1=CC=C(O)C(O)=C1 VYFYYTLLBUKUHU-UHFFFAOYSA-N 0.000 claims abstract description 414
- 239000003814 drug Substances 0.000 claims abstract description 221
- 229960003638 dopamine Drugs 0.000 claims abstract description 208
- 229940079593 drug Drugs 0.000 claims abstract description 205
- 238000002347 injection Methods 0.000 claims abstract description 28
- 239000007924 injection Substances 0.000 claims abstract description 28
- 239000000243 solution Substances 0.000 claims abstract description 19
- 239000000843 powder Substances 0.000 claims abstract description 17
- 239000006188 syrup Substances 0.000 claims abstract description 12
- 235000020357 syrup Nutrition 0.000 claims abstract description 12
- 239000000839 emulsion Substances 0.000 claims abstract description 10
- 239000000725 suspension Substances 0.000 claims abstract description 10
- 239000006187 pill Substances 0.000 claims abstract description 9
- 239000000829 suppository Substances 0.000 claims abstract description 9
- 238000007796 conventional method Methods 0.000 claims abstract description 3
- 239000002269 analeptic agent Substances 0.000 claims description 96
- 229960003692 gamma aminobutyric acid Drugs 0.000 claims description 60
- BTCSSZJGUNDROE-UHFFFAOYSA-N gamma-aminobutyric acid Chemical compound NCCCC(O)=O BTCSSZJGUNDROE-UHFFFAOYSA-N 0.000 claims description 60
- 239000000556 agonist Substances 0.000 claims description 55
- 239000002671 adjuvant Substances 0.000 claims description 16
- 239000003795 chemical substances by application Substances 0.000 claims description 16
- 238000013270 controlled release Methods 0.000 claims description 8
- -1 micropill Substances 0.000 claims description 2
- 206010013663 drug dependence Diseases 0.000 abstract description 14
- 230000000694 effects Effects 0.000 abstract description 14
- 208000011117 substance-related disease Diseases 0.000 abstract description 11
- 231100000331 toxic Toxicity 0.000 abstract description 8
- 230000002588 toxic effect Effects 0.000 abstract description 8
- 206010012335 Dependence Diseases 0.000 abstract description 6
- 239000000018 receptor agonist Substances 0.000 abstract description 4
- 229940044601 receptor agonist Drugs 0.000 abstract description 4
- 238000001784 detoxification Methods 0.000 abstract description 2
- 238000004904 shortening Methods 0.000 abstract description 2
- 238000004500 asepsis Methods 0.000 abstract 1
- 239000008187 granular material Substances 0.000 abstract 1
- 239000000546 pharmaceutical excipient Substances 0.000 abstract 1
- 102000005962 receptors Human genes 0.000 description 148
- 108020003175 receptors Proteins 0.000 description 148
- 238000000034 method Methods 0.000 description 65
- DHSSDEDRBUKTQY-UHFFFAOYSA-N 6-prop-2-enyl-4,5,7,8-tetrahydrothiazolo[4,5-d]azepin-2-amine Chemical compound C1CN(CC=C)CCC2=C1N=C(N)S2 DHSSDEDRBUKTQY-UHFFFAOYSA-N 0.000 description 30
- ZXRVKCBLGJOCEE-UHFFFAOYSA-N Gaboxadol Chemical compound C1NCCC2=C1ONC2=O ZXRVKCBLGJOCEE-UHFFFAOYSA-N 0.000 description 30
- BKRGVLQUQGGVSM-KBXCAEBGSA-N Revanil Chemical compound C1=CC(C=2[C@H](N(C)C[C@H](C=2)NC(=O)N(CC)CC)C2)=C3C2=CNC3=C1 BKRGVLQUQGGVSM-KBXCAEBGSA-N 0.000 description 30
- 229950004346 gaboxadol Drugs 0.000 description 30
- 229960003587 lisuride Drugs 0.000 description 30
- 229960001511 pergolide mesylate Drugs 0.000 description 30
- UWCVGPLTGZWHGS-ZORIOUSZSA-N pergolide mesylate Chemical compound CS(O)(=O)=O.C1=CC([C@H]2C[C@@H](CSC)CN([C@@H]2C2)CCC)=C3C2=CNC3=C1 UWCVGPLTGZWHGS-ZORIOUSZSA-N 0.000 description 30
- 229960003089 pramipexole Drugs 0.000 description 30
- FASDKYOPVNHBLU-ZETCQYMHSA-N pramipexole Chemical compound C1[C@@H](NCCC)CCC2=C1SC(N)=N2 FASDKYOPVNHBLU-ZETCQYMHSA-N 0.000 description 30
- 229960001879 ropinirole Drugs 0.000 description 30
- UHSKFQJFRQCDBE-UHFFFAOYSA-N ropinirole Chemical compound CCCN(CCC)CCC1=CC=CC2=C1CC(=O)N2 UHSKFQJFRQCDBE-UHFFFAOYSA-N 0.000 description 30
- 229950008418 talipexole Drugs 0.000 description 30
- 229960001475 zolpidem Drugs 0.000 description 30
- ZAFYATHCZYHLPB-UHFFFAOYSA-N zolpidem Chemical compound N1=C2C=CC(C)=CN2C(CC(=O)N(C)C)=C1C1=CC=C(C)C=C1 ZAFYATHCZYHLPB-UHFFFAOYSA-N 0.000 description 30
- 239000000654 additive Substances 0.000 description 22
- NOJMTMIRQRDZMT-GSPXQYRGSA-N bromocriptine methanesulfonate Chemical compound CS(O)(=O)=O.C1=CC(C=2[C@H](N(C)C[C@@H](C=2)C(=O)N[C@]2(C(=O)N3[C@H](C(N4CCC[C@H]4[C@]3(O)O2)=O)CC(C)C)C(C)C)C2)=C3C2=C(Br)NC3=C1 NOJMTMIRQRDZMT-GSPXQYRGSA-N 0.000 description 16
- CBIAWPMZSFFRGN-UHFFFAOYSA-N Indiplon Chemical compound CC(=O)N(C)C1=CC=CC(C=2N3N=CC(=C3N=CC=2)C(=O)C=2SC=CC=2)=C1 CBIAWPMZSFFRGN-UHFFFAOYSA-N 0.000 description 15
- 229950003867 indiplon Drugs 0.000 description 15
- 238000010255 intramuscular injection Methods 0.000 description 9
- 239000007927 intramuscular injection Substances 0.000 description 9
- 238000001990 intravenous administration Methods 0.000 description 6
- 239000000203 mixture Substances 0.000 description 6
- 208000007271 Substance Withdrawal Syndrome Diseases 0.000 description 5
- 230000035479 physiological effects, processes and functions Effects 0.000 description 5
- UGJMXCAKCUNAIE-UHFFFAOYSA-N Gabapentin Chemical compound OC(=O)CC1(CN)CCCCC1 UGJMXCAKCUNAIE-UHFFFAOYSA-N 0.000 description 4
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- 239000003995 emulsifying agent Substances 0.000 description 3
- 230000003203 everyday effect Effects 0.000 description 3
- 238000010253 intravenous injection Methods 0.000 description 3
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- 210000002569 neuron Anatomy 0.000 description 3
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- KORNTPPJEAJQIU-KJXAQDMKSA-N Cabaser Chemical compound C1=CC([C@H]2C[C@H](CN(CC=C)[C@@H]2C2)C(=O)N(CCCN(C)C)C(=O)NCC)=C3C2=CNC3=C1 KORNTPPJEAJQIU-KJXAQDMKSA-N 0.000 description 2
- WHUUTDBJXJRKMK-UHFFFAOYSA-N Glutamic acid Natural products OC(=O)C(N)CCC(O)=O WHUUTDBJXJRKMK-UHFFFAOYSA-N 0.000 description 2
- GMZVRMREEHBGGF-UHFFFAOYSA-N Piracetam Chemical compound NC(=O)CN1CCCC1=O GMZVRMREEHBGGF-UHFFFAOYSA-N 0.000 description 2
- 206010070834 Sensitisation Diseases 0.000 description 2
- KJADKKWYZYXHBB-XBWDGYHZSA-N Topiramic acid Chemical compound C1O[C@@]2(COS(N)(=O)=O)OC(C)(C)O[C@H]2[C@@H]2OC(C)(C)O[C@@H]21 KJADKKWYZYXHBB-XBWDGYHZSA-N 0.000 description 2
- 229960000793 aniracetam Drugs 0.000 description 2
- ZXNRTKGTQJPIJK-UHFFFAOYSA-N aniracetam Chemical compound C1=CC(OC)=CC=C1C(=O)N1C(=O)CCC1 ZXNRTKGTQJPIJK-UHFFFAOYSA-N 0.000 description 2
- 229960004596 cabergoline Drugs 0.000 description 2
- 238000002474 experimental method Methods 0.000 description 2
- 229960002870 gabapentin Drugs 0.000 description 2
- 235000013922 glutamic acid Nutrition 0.000 description 2
- 239000004220 glutamic acid Substances 0.000 description 2
- CEXBONHIOKGWNU-NTISSMGPSA-N hydron;(6s)-6-[propyl(2-thiophen-2-ylethyl)amino]-5,6,7,8-tetrahydronaphthalen-1-ol;chloride Chemical compound [Cl-].CCC[NH+]([C@@H]1CC2=CC=CC(O)=C2CC1)CCC1=CC=CS1 CEXBONHIOKGWNU-NTISSMGPSA-N 0.000 description 2
- 239000004615 ingredient Substances 0.000 description 2
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- 210000000056 organ Anatomy 0.000 description 2
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- AYXYPKUFHZROOJ-ZETCQYMHSA-N pregabalin Chemical compound CC(C)C[C@H](CN)CC(O)=O AYXYPKUFHZROOJ-ZETCQYMHSA-N 0.000 description 2
- 238000012827 research and development Methods 0.000 description 2
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- 238000012360 testing method Methods 0.000 description 2
- 229960004394 topiramate Drugs 0.000 description 2
- 229960004010 zaleplon Drugs 0.000 description 2
- HUNXMJYCHXQEGX-UHFFFAOYSA-N zaleplon Chemical compound CCN(C(C)=O)C1=CC=CC(C=2N3N=CC(=C3N=CC=2)C#N)=C1 HUNXMJYCHXQEGX-UHFFFAOYSA-N 0.000 description 2
- SFLSHLFXELFNJZ-QMMMGPOBSA-N (-)-norepinephrine Chemical compound NC[C@H](O)C1=CC=C(O)C(O)=C1 SFLSHLFXELFNJZ-QMMMGPOBSA-N 0.000 description 1
- RKUNBYITZUJHSG-FXUDXRNXSA-N (S)-atropine Chemical compound C1([C@@H](CO)C(=O)O[C@H]2C[C@H]3CC[C@@H](C2)N3C)=CC=CC=C1 RKUNBYITZUJHSG-FXUDXRNXSA-N 0.000 description 1
- USSIQXCVUWKGNF-UHFFFAOYSA-N 6-(dimethylamino)-4,4-diphenylheptan-3-one Chemical compound C=1C=CC=CC=1C(CC(C)N(C)C)(C(=O)CC)C1=CC=CC=C1 USSIQXCVUWKGNF-UHFFFAOYSA-N 0.000 description 1
- 208000012639 Balance disease Diseases 0.000 description 1
- 208000014644 Brain disease Diseases 0.000 description 1
- OMFXVFTZEKFJBZ-UHFFFAOYSA-N Corticosterone Natural products O=C1CCC2(C)C3C(O)CC(C)(C(CC4)C(=O)CO)C4C3CCC2=C1 OMFXVFTZEKFJBZ-UHFFFAOYSA-N 0.000 description 1
- 229920001353 Dextrin Polymers 0.000 description 1
- 239000004375 Dextrin Substances 0.000 description 1
- 206010013754 Drug withdrawal syndrome Diseases 0.000 description 1
- 102000005915 GABA Receptors Human genes 0.000 description 1
- 108010005551 GABA Receptors Proteins 0.000 description 1
- RKUNBYITZUJHSG-UHFFFAOYSA-N Hyosciamin-hydrochlorid Natural products CN1C(C2)CCC1CC2OC(=O)C(CO)C1=CC=CC=C1 RKUNBYITZUJHSG-UHFFFAOYSA-N 0.000 description 1
- AFVFQIVMOAPDHO-UHFFFAOYSA-N Methanesulfonic acid Chemical compound CS(O)(=O)=O AFVFQIVMOAPDHO-UHFFFAOYSA-N 0.000 description 1
- 241001597008 Nomeidae Species 0.000 description 1
- 102000003840 Opioid Receptors Human genes 0.000 description 1
- 108090000137 Opioid Receptors Proteins 0.000 description 1
- 229920002472 Starch Polymers 0.000 description 1
- 230000001154 acute effect Effects 0.000 description 1
- 229960002802 bromocriptine Drugs 0.000 description 1
- ZPEIMTDSQAKGNT-UHFFFAOYSA-N chlorpromazine Chemical compound C1=C(Cl)C=C2N(CCCN(C)C)C3=CC=CC=C3SC2=C1 ZPEIMTDSQAKGNT-UHFFFAOYSA-N 0.000 description 1
- 229960001076 chlorpromazine Drugs 0.000 description 1
- 239000011248 coating agent Substances 0.000 description 1
- 238000000576 coating method Methods 0.000 description 1
- 150000001875 compounds Chemical class 0.000 description 1
- OMFXVFTZEKFJBZ-HJTSIMOOSA-N corticosterone Chemical compound O=C1CC[C@]2(C)[C@H]3[C@@H](O)C[C@](C)([C@H](CC4)C(=O)CO)[C@@H]4[C@@H]3CCC2=C1 OMFXVFTZEKFJBZ-HJTSIMOOSA-N 0.000 description 1
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Landscapes
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Provided is a preparation of dopamine agonist, belonging to the technical field of addiction medicines and neurobiology. The invention is prepared by receptor agonist raw medicine of ergot dopamine (DA), receptor agonist raw medicine of gamma-propalanine A receptor (GABAA), receptor agonist raw medicine of gamma- propalanine B receptor (GABAB) and excipients which are dispensed according to the conventional method. The preparation is Pulvis, drop pills, micro-granules, suppository, solution type injection, suspension type injection, and emulsion type injection, asepsis powder for injection, solution, syrup, emulsion, suspensions or controlled released preparation. The invention has the advantages of low costs, safety, reliability, little toxic and side effects, obvious shortening of withdrawal time, obvious alleviation or partially relief of psychological drug craving and the like, being adaptable to detoxification medicines for curing various drug addictions.
Description
Technical field:
The present invention relates to dopamine agonist preparation and application thereof, belong to addiction medicine and neurobiology technical field.
Background technology:
The drug addict that China registers on the books at present surpasses 1,170,000.Drug abuse employee in payroll and 1: 10 ratio of drug addict in the recommendation of drug control organ of the United Nations, China drug addict has broken through 1,100 ten thousand, the existence of this specific group, serious threat is to the social stability and the sustainable development of China, and drug issue has become the main threat that China builds a harmonious society.Want to obtain the triumph of prohibiting drug and fighting drug struggle, must rely on the solution for giving up addiction of drug addict biological medicine technology, the research and development application paces of strengthening this technical field make a breakthrough to banning drugs work and play an important role within a short period of time.
Current, banning drugs work is all paid much attention in countries in the world, and anti-additive medicament is treated as important measures.But, because a series of physiologic derangement phenomenon withdrawal symptoms that the addict is shown when stopping using the opiates medicine suddenly make that they are reluctant to accept drug rehabilitation and the control oneself reverts to take drugs.International drug control organ and academia have been noted that: whether can be smoothly, the physiology drug addiction and the drugs of the genuine withdrawal junkie of people crave for degree, and be that can junkie be accepted to quit drug abuse and prolong the key factor of personal integrity.According to actual in recent years anti-additive medicament research and development of China and applicable cases analysis, though domestic existing anti-additive medicament has kind more than ten, if but these withdrawal and treatment drug mains rely on folk prescription among the people or adding that dependent ingredient is arranged, toxic and side effects is big, lacks scientific basis.The drug rehabilitation quasi drugs of relatively being taken a fancy in the past, treatment principle are " with mild toxicities for big poison ".Lack in the acute detoxification phase under the background of specific drug, methadone helplessly becomes the first-use drug in the current drug addiction treatment, but its dependency is strong, side effect is big, and relapse rate reaches more than 98% after reaching 70%, one year after the January of giving up taking addictive drugs by force.At present China does not also find the ideal physiology that does not contain hyoscyamine, chlorpromazine or do not have the dependence effect to give up or alleviates the medicine that drugs are craved for degree.And in the vigilance addiction or eliminate drugs and crave for and be still blank at present aspect the degree medicine.
Studies have shown that the addict has suffered from disease of brain.Painful main two parts that divide that drugs bring to them, the one, physiology is given up the withdrawal symptoms in the process, this process generally continues 10-15 days, the outbreak of withdrawal symptoms makes junkie very painful, and usually cause their injure himself or make himself disabled behavior, in order to alleviate these miseries, their drugs of reverting to take drugs again; The 2nd, psychological withdrawal, they can't forget that drugs bring their pleasant sensation and lack the possessiveness of quitting drug abuse, and madness is pursued the sort of pleasant sensation at all adventures throughout one's life, and this madness is not can prove effective by education.Prevent to revert to take drugs, shortening or alleviation withdrawal symptoms, elimination simultaneously or reduction addict just become a kind of ideal drug rehabilitation method to the degree of craving for of drugs.
Summary of the invention:
The object of the present invention is to provide a kind of cost low, safe in utilization, scientific strong, reliability height, the mixture preparation that is used for the treatment of drug addiction that toxic and side effects is little.
Principle of the present invention is: medicine can act on different target spots and different neurotransmitteies in the different addiction stages of giving up targetedly, reaches the effect that ideal physiology withdrawal and treatment and auxiliary treatment drugs are craved for degree by acting on opiate system, norepinephrine system, dopamine system, glutamic acid system, corticosterone, GABA system.
Studies show that: the available DA of addict's brain is less than the normal person far away, and its drugs suck the level that has just in time improved DA.Improve level or the exciting DA receptor (D1-D4) of addict's brain DA and don't can produce the direction that new drug dependence is various countries' scientists study always.Ergota class dopamine (DA) receptor stimulating agent and non-Ergota class dopamine (DA) receptor stimulating agent can carry out selectivity to the DA system (D1-D4) of brain cortex limbic lobe to be regulated, improve level or the exciting DA receptor (D1-D4) of addict's brain DA, play drug treatment function.
Studies show that: γ-An Jidingsuan (GABA) serotonergic neuron of midbrain ventral tegmental area (VTA) can suppress the neuronic transmembrane potential of DA, reduces the release of DA, and drugs and other opioid receptor agonists increase the release of DA just by suppressing the GABA neuron.GABA can suppress the release of DA, has to experimental results show that injecting gaba agonist in the VTA separately can reduce the DA release that drugs cause, and can cause the drugs withdrawal symptom.γ-An Jidingsuan A receptor (GABA
A) agonist or and γ-An Jidingsuan B receptor (GABA
B) agonist can be by to GABA receptor (GABA
AAnd GABA
B) selectivity regulate, control DA discharges, thereby plays the drug rehabilitation effect.
It is also closely related with behavior sensitization to revert to take drugs.Behavior sensitization may be relevant with glutamic acid serotonergic neuron adaptability dysequilibrium with dopaminergic between drug-induced ventral tegmental nucleus, nucleus accumbens septi, frontal cortex, the corpus amygdaloideum.Therefore Ergota class dopamine (DA) receptor stimulating agent and non-Ergota class dopamine (DA) receptor stimulating agent, γ-An Jidingsuan A receptor (GABA
A) agonist or and γ-An Jidingsuan B receptor (GABA
B) agonist is by synergism, plays the effect that ideal physiology withdrawal and treatment and auxiliary treatment drugs are craved for degree jointly.
Because drugs infringements, drug addict's physical difference is bigger, therefore selects suitable route of administration, is in time to bring into play drug effect, reduce the drug addict and give up painful effective ways, and we develop different pharmaceutical dosage forms for this reason.
Dopamine agonist preparation of the present invention is by Ergota class dopamine (DA) receptor stimulating agent crude drug, non-Ergota class dopamine (DA) receptor stimulating agent crude drug, γ-An Jidingsuan A receptor (GABA
A) agonist crude drug, γ-An Jidingsuan B receptor (GABA
B) agonist crude drug and adjuvant be prepared into powder, drop pill, micropill, suppository, solution type injection agent, suspension type injection, emulsion-type injection, injectable sterile powder, solution, syrup, Emulsion, suspensoid, controlled release agent according to a conventional method.Wherein:
The effective ingredient weight ratio of raw material is: Ergota class dopamine (DA) receptor stimulating agent crude drug and non-Ergota class dopamine (DA) receptor stimulating agent crude drug are 0.001%～30%, γ-An Jidingsuan A receptor (GABA
A) agonist crude drug or γ-An Jidingsuan B receptor (GABA
B) the agonist crude drug is 99.009%～65%, all the other are adjuvant (conventional with).
Ergota class dopamine (DA) receptor stimulating agent crude drug is: bromocriptine methanesulfonate (BromocriptineMesilate), pergolide mesylate (Pergolide Mesylate), lisuride (Lisuride), cabergoline (Cabergoline), alpha-DHEC mesylate (Cripar), Trastal (Trastal) etc.
Non-Ergota class dopamine (DA) receptor stimulating agent crude drug is: and ropinirole (Ropinirole), pramipexole (Pramipexole), talipexole (Talipexole), rotigotine hydrochloride (N-0923, SPM-962) etc.
γ-An Jidingsuan A receptor (GABA
A) the agonist crude drug is: because of ground general grand (indiplon), zolpidem (Zolpidem), gaboxadol (gaboxadol), topiramate (topiramate), Zaleplon (Zaleplon) etc.
γ-An Jidingsuan B receptor (GABA
B) the agonist crude drug is: the derivant of C-34647 Ba (Beclofen), gabapentin (Gabapentin), lyrica (Pregabalin), other γ-An Jidingsuan (as piracetam Piracetam, aniracetam Aniracetam).
Dopamine agonist preparation of the present invention is as the application of the anti-additive medicament of treatment drug addiction.
Dopamine agonist preparation of the present invention method is routinely carried out animal experiment and has been confirmed its effect, its result of the test unanimity.
Dopamine agonist preparation of the present invention shows through animal test results: mixture preparation has very obvious suppression effect to the addiction animal, statistical result showed has significance in 1-5 days after the morphine of stopping using, show that this mixture preparation has the obvious suppression effect to the behavior that morphine class drug dependence causes.
Dopamine agonist preparation of the present invention method is routinely carried out the dependency animal experiment, and the result shows no any drug dependence.
Dopamine agonist preparation of the present invention has that cost is low, safe, reliable, scientific strong, toxic and side effects is little, can obviously shorten the time of giving up and alleviation or part and remove advantage to the drugs drug craving.
The specific embodiment:
In following examples: adjuvant is starch, dextrin, compound coating material etc.
Embodiment 1:
Select Ergota class dopamine (DA) receptor stimulating agent bromocriptine methanesulfonate crude drug and non-Ergota class dopamine (DA) receptor stimulating agent ropinirole (Ropinirole) crude drug, γ-An Jidingsuan A receptor (GABA
A) agonist because of general grand (indiplon) crude drug in ground, adopt different amounts routinely technology make different dosage forms.
A. powder: select Ergota class dopamine (DA) receptor stimulating agent bromocriptine methanesulfonate crude drug 0.0005%, non-Ergota class dopamine (DA) receptor stimulating agent ropinirole (Ropinirole) crude drug 0.0005%, γ-An Jidingsuan A receptor (GABA
A) agonist is because of general grand (indiplon) crude drug 89.999% in ground, adjuvant is 10%, adopts common process to make powder.
Instructions of taking: three times on the one, one time one bag; 5 days is a course of treatment.
B. drop pill: select Ergota class dopamine (DA) receptor stimulating agent bromocriptine methanesulfonate crude drug 0.5%, non-Ergota class dopamine (DA) receptor stimulating agent ropinirole (Ropinirole) crude drug 1%, γ-An Jidingsuan A receptor (GABA
A) agonist is because of general grand (indiplon) crude drug 97.9% in ground, adjuvant is 0.6%, adopts common process to make drop pill.
Instructions of taking: three times on the one, one time 8; 6 days is a course of treatment.
C. micropill: select Ergota class dopamine (DA) receptor stimulating agent bromocriptine methanesulfonate crude drug 0.5%, non-Ergota class dopamine (DA) receptor stimulating agent ropinirole (Ropinirole) crude drug 1%, γ-An Jidingsuan A receptor (GABA
A) agonist is because of general grand (indiplon) crude drug 97.9% in ground, adjuvant is 0.6%, adopts common process to make micropill.
Instructions of taking: three times on the one, one time 3 ball, 5 days is a course of treatment.
D. suppository: select Ergota class dopamine (DA) receptor stimulating agent bromocriptine methanesulfonate crude drug 0.015%, non-Ergota class dopamine (DA) receptor stimulating agent ropinirole (Ropinirole) crude drug 0.005%, γ-An Jidingsuan A receptor (GABA
A) agonist is because of general grand (indiplon) crude drug 65% substrate 34.998% in ground, the employing common process is made suppository.
Using method: fill in apart from anus 2cm place, each 1 piece, twice on the one; 6 days is a course of treatment.
E. solution type injection agent: select Ergota class dopamine (DA) receptor stimulating agent bromocriptine methanesulfonate crude drug 5.53%, non-Ergota class dopamine (DA) receptor stimulating agent ropinirole (Ropinirole) crude drug 6.46%, γ-An Jidingsuan A receptor (GABA
A) agonist is because of general grand (indiplon) crude drug 88% in ground, additives 0.01% adopt common process to make solution type injection agent.
Using method: every day 10～30mg, intramuscular injection is at twice; Intravenous drip, medicine adds in the 200ml normal saline, drips off in 40 minutes.4 days is a course of treatment.
F. suspension type injection: select Ergota class dopamine (DA) receptor stimulating agent bromocriptine methanesulfonate crude drug 2.61%, non-Ergota class dopamine (DA) receptor stimulating agent ropinirole (Ropinirole) crude drug 2.39%, γ-An Jidingsuan A receptor (GABA
A) agonist is because of general grand (indiplon) crude drug 94.85% in ground, additives 0.15% adopt common process to make the suspension type injection.
Using method: intramuscular injection, 20～60mg/ day, divide 2～3 times.5 days is a course of treatment.
G. emulsion-type injection: select Ergota class dopamine (DA) receptor stimulating agent bromocriptine methanesulfonate crude drug 10%, non-Ergota class dopamine (DA) receptor stimulating agent ropinirole (Ropinirole) crude drug 4.79%, γ-An Jidingsuan A receptor (GABA
A) agonist is because of general grand (indiplon) crude drug 83.21% in ground, additives 2.0% adopt common process to make the emulsion-type injection.
Using method: intravenous injection, 20～40mg/ day, once-a-day, 4 days is a course of treatment.
H injectable sterile powder: select Ergota class dopamine (DA) receptor stimulating agent bromocriptine methanesulfonate crude drug 11.65%, non-Ergota class dopamine (DA) receptor stimulating agent ropinirole (Ropinirole) (Trastal) crude drug 14.03%, γ-An Jidingsuan A receptor (GABA
A) agonist is because of general grand (indiplon) crude drug 74.3% in ground, additives 0.2% adopt common process to make injectable sterile powder.
Using method: face and use preceding wiring solution-forming, 10～30mg/ day, intramuscular injection to divide 2 times.Intravenous drip 1 time.4 days is a course of treatment.
I. solution: select Ergota class dopamine (DA) receptor stimulating agent bromocriptine methanesulfonate crude drug 1.6%, non-Ergota class dopamine (DA) receptor stimulating agent ropinirole (Ropinirole) crude drug 3.2%, γ-An Jidingsuan A receptor (GABA
A) agonist is because of general grand (indiplon) crude drug 83.2% in ground, additives 12% adopt common process to make solution.
Instructions of taking: three times on the one, one time one, 8 days is a course of treatment.
J. syrup: select Ergota class dopamine (DA) receptor stimulating agent bromocriptine methanesulfonate crude drug 0.0005%, non-Ergota class dopamine (DA) receptor stimulating agent ropinirole (Ropinirole) crude drug 0.0005%, γ-An Jidingsuan A receptor (GABA
A) agonist is because of general grand (indiplon) crude drug 65% in ground, syrup 34.999% adopts common process to make syrup.
Instructions of taking: three times on the one, one time one, 8 days is a course of treatment.
K. Emulsion: select Ergota class dopamine (DA) receptor stimulating agent bromocriptine methanesulfonate crude drug 10%, non-Ergota class dopamine (DA) receptor stimulating agent ropinirole (Ropinirole) (Trastal) crude drug 1.65%, γ-An Jidingsuan A receptor (GABA
A) agonist is because of general grand (indiplon) crude drug 76.35% in ground, emulsifying agent 12% adopts common process to make Emulsion.
Instructions of taking: three times on the one, a 10ml, 7 days is a course of treatment.
L suspensoid: select Ergota class dopamine (DA) receptor stimulating agent bromocriptine methanesulfonate crude drug 6.33%, non-Ergota class dopamine (DA) receptor stimulating agent ropinirole (Ropinirole) crude drug 3.62%, γ-An Jidingsuan A receptor (GABA
A) agonist is because of general grand (indiplon) crude drug 70.05% in ground, additives 20% adopt common process to make suspensoid.
Using method; Face with preceding and be made into debita spissitudo with eliminating cold for resuscitation water, oral, 5g/ day, divide 2 times.5 days is a course of treatment.
M. controlled release agent: select Ergota class dopamine (DA) receptor stimulating agent bromocriptine methanesulfonate crude drug 5.32%, non-Ergota class dopamine (DA) receptor stimulating agent ropinirole (Ropinirole) crude drug 3.355%, γ-An Jidingsuan A receptor (GABA
A) agonist is because of general grand (indiplon) crude drug 81.625% in ground, adjuvant 11.25% adopts common process to make controlled release agent.
Using method: once-a-day, once two, 5 days is a course of treatment.
After experimenter person takes 2-5 course of treatment mixture preparation, all can obviously shorten the time of giving up and alleviation or part and remove drug craving, and toxic and side effects is little drugs.
Embodiment 2:
Select Ergota class dopamine (DA) receptor stimulating agent pergolide mesylate (Pergolide Mesylate) crude drug and non-Ergota class dopamine (DA) receptor stimulating agent pramipexole (Pramipexole) crude drug, γ-An Jidingsuan B receptor (GABA
B) agonist C-34647 Ba (Beclofen) crude drug, employing different amounts technology is routinely made different dosage forms.
A. powder: select Ergota class dopamine (DA) receptor stimulating agent pergolide mesylate (Pergolide Mesylate) crude drug 0.0005%, non-Ergota class dopamine (DA) receptor stimulating agent pramipexole (Pramipexole) crude drug 0.0005%, γ-An Jidingsuan B receptor (GABA
B) agonist C-34647 Ba (Beclofen) crude drug 89.999%, adjuvant is 10%, adopts common process to make powder.
Instructions of taking: three times on the one, one time one bag; 5 days is a course of treatment.
B. drop pill: select Ergota class dopamine (DA) receptor stimulating agent pergolide mesylate (Pergolide Mesylate) crude drug 0.5%, non-Ergota class dopamine (DA) receptor stimulating agent pramipexole (Pramipexole) crude drug 1%, γ-An Jidingsuan B receptor (GABA
B) agonist C-34647 Ba (Beclofen) crude drug 97.9%, adjuvant is 0.6%, adopts common process to make drop pill.
Instructions of taking: three times on the one, one time 8; 6 days is a course of treatment.
C. micropill: select Ergota class dopamine (DA) receptor stimulating agent pergolide mesylate (Pergolide Mesylate) crude drug 0.5%, non-Ergota class dopamine (DA) receptor stimulating agent pramipexole (Pramipexole) crude drug 1%, γ-An Jidingsuan B receptor (GABA
B) agonist C-34647 Ba (Beclofen) crude drug 97.9%, adjuvant is 0.6%, adopts common process to make micropill.
Instructions of taking: three times on the one, one time 3 ball, 5 days is a course of treatment.
D. suppository: select Ergota class dopamine (DA) receptor stimulating agent pergolide mesylate (Pergolide Mesylate) crude drug 0.015%, non-Ergota class dopamine (DA) receptor stimulating agent pramipexole (Pramipexole) crude drug 0.005%, γ-An Jidingsuan B receptor (GABA
B) agonist C-34647 Ba (Beclofen) crude drug 65%, substrate 34.998%, adopt common process to make suppository.
Using method: fill in apart from anus 2cm place, each 1 piece, twice on the one; 6 days is a course of treatment.
E. solution type injection agent: select Ergota class dopamine (DA) receptor stimulating agent pergolide mesylate (PergolideMesylate) crude drug 5.53%, non-Ergota class dopamine (DA) receptor stimulating agent pramipexole (Pramipexole) crude drug 6.46%, γ-An Jidingsuan B receptor (GABA
B) agonist C-34647 Ba (Beclofen) crude drug 88%, additives 0.01% adopt common process to make solution type injection agent.
Using method: every day 10～30mg, intramuscular injection is at twice; Intravenous drip, medicine adds in the 200ml normal saline, drips off in 40 minutes.4 days is a course of treatment.
F. suspension type injection: select Ergota class dopamine (DA) receptor stimulating agent pergolide mesylate (PergolideMesylate) crude drug 2.61%, non-Ergota class dopamine (DA) receptor stimulating agent pramipexole (Pramipexole) crude drug 2.39%, γ-An Jidingsuan B receptor (GABA
B) agonist C-34647 Ba (Beclofen) crude drug 94.85%, additives 0.15% adopt common process to make the suspension type injection.
Using method: intramuscular injection, 20～60mg/ day, divide 2～3 times.5 days is a course of treatment.
G. emulsion-type injection: select Ergota class dopamine (DA) receptor stimulating agent pergolide mesylate (PergolideMesylate) crude drug 10%, non-Ergota class dopamine (DA) receptor stimulating agent pramipexole (Pramipexole) crude drug 4.79%, γ-An Jidingsuan B receptor (GABA
B) agonist C-34647 Ba (Beclofen) crude drug 83.21%, additives 2.0% adopt common process to make the emulsion-type injection.
Using method: intravenous injection, 20～40mg/ day, once-a-day, 4 days is a course of treatment.
H. injectable sterile powder: select Ergota class dopamine (DA) receptor stimulating agent pergolide mesylate (PergolideMesylate) crude drug 11.65%, non-Ergota class dopamine (DA) receptor stimulating agent pramipexole (Pramipexole) crude drug 14.03%, γ-An Jidingsuan B receptor (GABA
B) agonist C-34647 Ba (Beclofen) crude drug 74.3%, additives 0.2% adopt common process to make injectable sterile powder.
Using method: face and use preceding wiring solution-forming, 10～30mg/ day, intramuscular injection to divide 2 times.Intravenous drip 1 time.4 days is a course of treatment.
I. solution: select Ergota class dopamine (DA) receptor stimulating agent pergolide mesylate (Pergolide Mesylate) crude drug 1.6%, non-Ergota class dopamine (DA) receptor stimulating agent pramipexole (Pramipexole) crude drug 3.2%, γ-An Jidingsuan B receptor (GABA
B) agonist C-34647 Ba (Beclofen) crude drug 83.2%, additives 12% adopt common process to make solution.
Instructions of taking: three times on the one, one time one, 8 days is a course of treatment.
J. syrup: select Ergota class dopamine (DA) receptor stimulating agent pergolide mesylate (Pergolide Mesylate) crude drug 0.0005%, non-Ergota class dopamine (DA) receptor stimulating agent pramipexole (Pramipexole) crude drug 0.0005%, γ-An Jidingsuan B receptor (GABA
B) agonist C-34647 Ba (Beclofen) crude drug 65%, syrup 34.999% adopts common process to make syrup.
Instructions of taking: three times on the one, one time one, 8 days is a course of treatment.
K. Emulsion: select Ergota class dopamine (DA) receptor stimulating agent pergolide mesylate (Pergolide Mesylate) crude drug 10%, non-Ergota class dopamine (DA) receptor stimulating agent pramipexole (Pramipexole) crude drug 1.65%, γ-An Jidingsuan B receptor (GABA
B) agonist C-34647 Ba (Beclofen) crude drug 76.35%, emulsifying agent 12% adopts common process to make Emulsion.
Instructions of taking: three times on the one, a 10ml, 7 days is a course of treatment.
L. suspensoid: select Ergota class dopamine (DA) receptor stimulating agent pergolide mesylate (Pergolide Mesylate) crude drug 6.33%, non-Ergota class dopamine (DA) receptor stimulating agent pramipexole (Pramipexole) crude drug 3.62%, γ-An Jidingsuan B receptor (GABA
B) agonist C-34647 Ba (Beclofen) crude drug 70.05%, additives 20% adopt common process to make suspensoid.
Using method; Face with preceding and be made into debita spissitudo with eliminating cold for resuscitation water, oral, 5g/ day, divide 2 times.5 days is a course of treatment.
M. controlled release agent: select Ergota class dopamine (DA) receptor stimulating agent pergolide mesylate (Pergolide Mesylate) crude drug 5.32%, non-Ergota class dopamine (DA) receptor stimulating agent pramipexole (Pramipexole) crude drug 3.355%, γ-An Jidingsuan B receptor (GABA
B) agonist C-34647 Ba (Beclofen) crude drug 81.625%, adjuvant 11.25% adopts common process to make controlled release agent.
Using method: once-a-day, once two, 5 days is a course of treatment.
After experimenter person takes 2-5 course of treatment mixture preparation, all can obviously shorten the time of giving up and alleviation or part and remove drug craving, and toxic and side effects is little drugs.
Embodiment 3:
Select Ergota class dopamine (DA) receptor stimulating agent lisuride (Lisuride) crude drug and non-Ergota class dopamine (DA) receptor stimulating agent talipexole (Talipexole) crude drug, γ-An Jidingsuan A receptor (GABA
A) agonist zolpidem (Zolpidem) crude drug and gaboxadol (gaboxadol) crude drug, employing different amounts technology is routinely made different dosage forms.
A. powder: select Ergota class dopamine (DA) receptor stimulating agent lisuride (Lisuride) crude drug 0.0005%, non-Ergota class dopamine (DA) receptor stimulating agent talipexole (Talipexole) crude drug 0.0005%, γ-An Jidingsuan A receptor (GABA
A) agonist zolpidem (Zolpidem) crude drug 11.23% and gaboxadol (gaboxadol) crude drug 78.769%, adjuvant is 10%, adopts common process to make powder.
Instructions of taking: three times on the one, one time one bag; 5 days is a course of treatment.
B. drop pill: select Ergota class dopamine (DA) receptor stimulating agent lisuride (Lisuride) crude drug 0.5%, non-Ergota class dopamine (DA) receptor stimulating agent talipexole (Talipexole) crude drug 1%, γ-An Jidingsuan A receptor (GABA
A) agonist zolpidem (Zolpidem) crude drug 53.56% and gaboxadol (gaboxadol) crude drug 44.34%, adjuvant is 0.6%, adopts common process to make drop pill.
Instructions of taking: three times on the one, one time 8; 6 days is a course of treatment.
C. micropill: select Ergota class dopamine (DA) receptor stimulating agent lisuride (Lisuride) crude drug 0.5%, non-Ergota class dopamine (DA) receptor stimulating agent talipexole (Talipexole) crude drug 1%, γ-An Jidingsuan A receptor (GABA
A) agonist zolpidem (Zolpidem) crude drug 53.56% and gaboxadol (gaboxadol) crude drug 44.34%, adjuvant is 0.6%, adopts common process to make micropill.
Instructions of taking: three times on the one, one time 3 ball, 5 days is a course of treatment.
D. suppository: select Ergota class dopamine (DA) receptor stimulating agent lisuride (Lisuride) crude drug 0.015%, non-Ergota class dopamine (DA) receptor stimulating agent talipexole (Talipexole) crude drug 0.005%, γ-An Jidingsuan A receptor (GABA
A) agonist zolpidem (Zolpidem) crude drug 30% and gaboxadol (gaboxadol) crude drug 35%, substrate 34.998%, adopt common process to make suppository.
Using method: fill in apart from anus 2cm place, each 1 piece, twice on the one; 6 days is a course of treatment.
E. solution type injection agent: select Ergota class dopamine (DA) receptor stimulating agent lisuride (Lisuride) crude drug 5.53%, non-Ergota class dopamine (DA) receptor stimulating agent talipexole (Talipexole) crude drug 6.46%, γ-An Jidingsuan A receptor (GABA
A) agonist zolpidem (Zolpidem) crude drug 53.64% and gaboxadol (gaboxadol) crude drug 34.36%, additives 0.01% adopt common process to make solution type injection agent.
Using method: every day 10～30mg, intramuscular injection is at twice; Intravenous drip, medicine adds in the 200ml normal saline, drips off in 40 minutes.4 days is a course of treatment.
F. suspension type injection: select Ergota class dopamine (DA) receptor stimulating agent lisuride (Lisuride) crude drug 2.61%, non-Ergota class dopamine (DA) receptor stimulating agent talipexole (Talipexole) crude drug 2.39%, γ-An Jidingsuan A receptor (GABA
A) agonist zolpidem (Zolpidem) crude drug 69.35% and gaboxadol (gaboxadol) crude drug 25.5%, additives 0.15% adopt common process to make the suspension type injection.
Using method: intramuscular injection, 20～60mg/ day, divide 2～3 times.5 days is a course of treatment.
G. emulsion-type injection: select Ergota class dopamine (DA) receptor stimulating agent lisuride (Lisuride) crude drug 10%, non-Ergota class dopamine (DA) receptor stimulating agent talipexole (Talipexole) crude drug 4.79%, γ-An Jidingsuan A receptor (GABA
A) agonist zolpidem (Zolpidem) crude drug 33.26% and gaboxadol (gaboxadol) crude drug 49.95%, additives 2.0% adopt common process to make the emulsion-type injection.
Using method: intravenous injection, 20～40mg/ day, once-a-day, 4 days is a course of treatment.
H. injectable sterile powder: select Ergota class dopamine (DA) receptor stimulating agent lisuride (Lisuride) crude drug 11.65%, non-Ergota class dopamine (DA) receptor stimulating agent talipexole (Talipexole) crude drug 14.03%, γ-An Jidingsuan A receptor (GABA
A) agonist zolpidem (Zolpidem) crude drug 35.6% and gaboxadol (gaboxadol) crude drug 38.7%, additives 0.2% adopt common process to make injectable sterile powder.
Using method: face and use preceding wiring solution-forming, 10～30mg/ day, intramuscular injection to divide 2 times.Intravenous drip 1 time.4 days is a course of treatment.
I. solution: select Ergota class dopamine (DA) receptor stimulating agent lisuride (Lisuride) crude drug 1.6%, non-Ergota class dopamine (DA) receptor stimulating agent talipexole (Talipexole) crude drug 3.2%, γ-An Jidingsuan A receptor (GABA
A) agonist zolpidem (Zolpidem) crude drug 39.89% and gaboxadol (gaboxadol) crude drug 43.31%, additives 12% adopt common process to make solution.
Instructions of taking: three times on the one, one time one, 8 days is a course of treatment.
J. syrup: select Ergota class dopamine (DA) receptor stimulating agent lisuride (Lisuride) crude drug 0.0005%, non-Ergota class dopamine (DA) receptor stimulating agent talipexole (Talipexole) crude drug 0.0005%, γ-An Jidingsuan A receptor (GABA
A) agonist zolpidem (Zolpidem) crude drug 23% and gaboxadol (gaboxadol) crude drug 42%, syrup 34.999% adopts common process to make syrup.
Instructions of taking: three times on the one, one time one, 8 days is a course of treatment.
K. Emulsion: select Ergota class dopamine (DA) receptor stimulating agent lisuride (Lisuride) crude drug 10%, non-Ergota class dopamine (DA) receptor stimulating agent talipexole (Talipexole) crude drug 1.65%, γ-An Jidingsuan A receptor (GABA
A) agonist zolpidem (Zolpidem) crude drug 63.1% and gaboxadol (gaboxadol) crude drug 13.25%, emulsifying agent 12% adopts common process to make Emulsion.
Instructions of taking: three times on the one, a 10ml, 7 days is a course of treatment.
L. suspensoid: select Ergota class dopamine (DA) receptor stimulating agent lisuride (Lisuride) crude drug 6.33%, non-Ergota class dopamine (DA) receptor stimulating agent talipexole (Talipexole) crude drug 3.62%, γ-An Jidingsuan A receptor (GABA
A) agonist zolpidem (Zolpidem) crude drug 30.05% and gaboxadol (gaboxadol) crude drug 40%, additives 20% adopt common process to make suspensoid.
Using method; Face with preceding and be made into debita spissitudo with eliminating cold for resuscitation water, oral, 5g/ day, divide 2 times.5 days is a course of treatment.
M. controlled release agent: select Ergota class dopamine (DA) receptor stimulating agent lisuride (Lisuride) crude drug 5.32%, non-Ergota class dopamine (DA) receptor stimulating agent talipexole (Talipexole) crude drug 3.355%, γ-An Jidingsuan A receptor (GABA
A) agonist zolpidem (Zolpidem) crude drug 69.45% and gaboxadol (gaboxadol) crude drug 12.175%, adjuvant 11.25% adopts common process to make controlled release agent.
Using method: once-a-day, once two, 5 days is a course of treatment.
After experimenter person takes 2-5 course of treatment mixture preparation, all can obviously shorten the time of giving up and alleviation or part and remove drug craving drugs, and the little drug craving to drugs of toxic and side effects, and toxic and side effects is little.
Claims (1)
1. dopamine agonist preparation is by Ergota class dopamine (DA) receptor stimulating agent crude drug, non-Ergota class dopamine (DA) receptor stimulating agent crude drug, γ-An Jidingsuan A receptor (GABA
A) agonist crude drug, γ-An Jidingsuan B receptor (GABA
B) agonist crude drug and adjuvant prepare according to a conventional method, it is characterized in that said preparation is powder, drop pill, micropill, suppository, solution type injection agent, suspension type injection, emulsion-type injection, injectable sterile powder, solution, syrup, Emulsion, suspensoid or controlled release agent.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA200610048754XA CN101168057A (en) | 2006-10-26 | 2006-10-26 | Dopamine agonist preparation |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA200610048754XA CN101168057A (en) | 2006-10-26 | 2006-10-26 | Dopamine agonist preparation |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN101168057A true CN101168057A (en) | 2008-04-30 |
Family
ID=39388910
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CNA200610048754XA Pending CN101168057A (en) | 2006-10-26 | 2006-10-26 | Dopamine agonist preparation |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN101168057A (en) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102600090A (en) * | 2012-03-16 | 2012-07-25 | 北京阜康仁生物制药科技有限公司 | Dropping pill adopting zolpidem as major active ingredients and preparation method of dropping pill |
| JP2021521103A (en) * | 2018-04-06 | 2021-08-26 | オービッド・セラピューティクス・インコーポレイテッドＯｖｉｄ Ｔｈｅｒａｐｅｕｔｉｃｓ Ｉｎｃ． | Use of gaboxadol in the treatment of substance use disorders |
-
2006
- 2006-10-26 CN CNA200610048754XA patent/CN101168057A/en active Pending
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102600090A (en) * | 2012-03-16 | 2012-07-25 | 北京阜康仁生物制药科技有限公司 | Dropping pill adopting zolpidem as major active ingredients and preparation method of dropping pill |
| JP2021521103A (en) * | 2018-04-06 | 2021-08-26 | オービッド・セラピューティクス・インコーポレイテッドＯｖｉｄ Ｔｈｅｒａｐｅｕｔｉｃｓ Ｉｎｃ． | Use of gaboxadol in the treatment of substance use disorders |
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Open date: 20080430 |