CN1714811A - Radix bupleuri dripping pill and its preparing method - Google Patents
Radix bupleuri dripping pill and its preparing method Download PDFInfo
- Publication number
- CN1714811A CN1714811A CN 200410019826 CN200410019826A CN1714811A CN 1714811 A CN1714811 A CN 1714811A CN 200410019826 CN200410019826 CN 200410019826 CN 200410019826 A CN200410019826 A CN 200410019826A CN 1714811 A CN1714811 A CN 1714811A
- Authority
- CN
- China
- Prior art keywords
- radix bupleuri
- extractum
- water
- polyethylene glycol
- reflux
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
- 239000006187 pill Substances 0.000 title claims abstract description 103
- 238000000034 method Methods 0.000 title description 6
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims abstract description 100
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims abstract description 99
- 239000007788 liquid Substances 0.000 claims abstract description 72
- 239000003814 drug Substances 0.000 claims abstract description 49
- 238000002360 preparation method Methods 0.000 claims abstract description 46
- 238000010992 reflux Methods 0.000 claims description 87
- 229940057995 liquid paraffin Drugs 0.000 claims description 63
- 239000000203 mixture Substances 0.000 claims description 60
- 229940093429 polyethylene glycol 6000 Drugs 0.000 claims description 43
- 229940079593 drug Drugs 0.000 claims description 38
- TZBAVQKIEKDGFH-UHFFFAOYSA-N n-[2-(diethylamino)ethyl]-1-benzothiophene-2-carboxamide;hydrochloride Chemical compound [Cl-].C1=CC=C2SC(C(=O)NCC[NH+](CC)CC)=CC2=C1 TZBAVQKIEKDGFH-UHFFFAOYSA-N 0.000 claims description 37
- 238000012869 ethanol precipitation Methods 0.000 claims description 33
- 230000002262 irrigation Effects 0.000 claims description 28
- 238000003973 irrigation Methods 0.000 claims description 28
- 241000202726 Bupleurum Species 0.000 claims description 15
- 239000002671 adjuvant Substances 0.000 claims description 15
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 claims description 10
- 239000000284 extract Substances 0.000 claims description 8
- 238000010438 heat treatment Methods 0.000 claims description 8
- 239000000463 material Substances 0.000 claims description 6
- 239000001828 Gelatine Substances 0.000 claims description 5
- 229920000159 gelatin Polymers 0.000 claims description 5
- 235000019322 gelatine Nutrition 0.000 claims description 5
- 235000011187 glycerol Nutrition 0.000 claims description 5
- 239000012567 medical material Substances 0.000 claims description 5
- RYYKJJJTJZKILX-UHFFFAOYSA-M sodium octadecanoate Chemical compound [Na+].CCCCCCCCCCCCCCCCCC([O-])=O RYYKJJJTJZKILX-UHFFFAOYSA-M 0.000 claims description 5
- 239000012141 concentrate Substances 0.000 claims description 3
- 230000000144 pharmacologic effect Effects 0.000 abstract description 3
- 230000000694 effects Effects 0.000 description 16
- 229940057838 polyethylene glycol 4000 Drugs 0.000 description 10
- 239000004615 ingredient Substances 0.000 description 8
- 241000699666 Mus <mouse, genus> Species 0.000 description 7
- 102000030621 adenylate cyclase Human genes 0.000 description 7
- 108060000200 adenylate cyclase Proteins 0.000 description 7
- 238000010579 first pass effect Methods 0.000 description 7
- 238000002347 injection Methods 0.000 description 7
- 239000007924 injection Substances 0.000 description 7
- 210000004185 liver Anatomy 0.000 description 7
- NTYJJOPFIAHURM-UHFFFAOYSA-N Histamine Chemical compound NCCC1=CN=CN1 NTYJJOPFIAHURM-UHFFFAOYSA-N 0.000 description 6
- 238000011160 research Methods 0.000 description 6
- 239000000243 solution Substances 0.000 description 5
- 239000000341 volatile oil Substances 0.000 description 5
- BSYNRYMUTXBXSQ-UHFFFAOYSA-N Aspirin Chemical compound CC(=O)OC1=CC=CC=C1C(O)=O BSYNRYMUTXBXSQ-UHFFFAOYSA-N 0.000 description 4
- 241000699670 Mus sp. Species 0.000 description 4
- 102000004142 Trypsin Human genes 0.000 description 4
- 108090000631 Trypsin Proteins 0.000 description 4
- 229960001138 acetylsalicylic acid Drugs 0.000 description 4
- 230000002401 inhibitory effect Effects 0.000 description 4
- 230000007958 sleep Effects 0.000 description 4
- 239000007787 solid Substances 0.000 description 4
- 239000012588 trypsin Substances 0.000 description 4
- QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 description 3
- 241000282326 Felis catus Species 0.000 description 3
- 230000000202 analgesic effect Effects 0.000 description 3
- 238000002474 experimental method Methods 0.000 description 3
- 229960001340 histamine Drugs 0.000 description 3
- 239000001397 quillaja saponaria molina bark Substances 0.000 description 3
- 229930182490 saponin Natural products 0.000 description 3
- 150000007949 saponins Chemical class 0.000 description 3
- 101710095468 Cyclase Proteins 0.000 description 2
- OHCQJHSOBUTRHG-KGGHGJDLSA-N FORSKOLIN Chemical compound O=C([C@@]12O)C[C@](C)(C=C)O[C@]1(C)[C@@H](OC(=O)C)[C@@H](O)[C@@H]1[C@]2(C)[C@@H](O)CCC1(C)C OHCQJHSOBUTRHG-KGGHGJDLSA-N 0.000 description 2
- 208000022461 Glomerular disease Diseases 0.000 description 2
- 241001465754 Metazoa Species 0.000 description 2
- 206010033645 Pancreatitis Diseases 0.000 description 2
- 206010033647 Pancreatitis acute Diseases 0.000 description 2
- 206010037660 Pyrexia Diseases 0.000 description 2
- 102000019197 Superoxide Dismutase Human genes 0.000 description 2
- 108010012715 Superoxide dismutase Proteins 0.000 description 2
- 241000218636 Thuja Species 0.000 description 2
- 238000010521 absorption reaction Methods 0.000 description 2
- 239000002253 acid Substances 0.000 description 2
- 230000009471 action Effects 0.000 description 2
- 201000003229 acute pancreatitis Diseases 0.000 description 2
- 230000003110 anti-inflammatory effect Effects 0.000 description 2
- 230000008901 benefit Effects 0.000 description 2
- 230000037396 body weight Effects 0.000 description 2
- 239000002552 dosage form Substances 0.000 description 2
- 238000000605 extraction Methods 0.000 description 2
- 230000002496 gastric effect Effects 0.000 description 2
- 231100000852 glomerular disease Toxicity 0.000 description 2
- 241000411851 herbal medicine Species 0.000 description 2
- 238000000338 in vitro Methods 0.000 description 2
- 206010022000 influenza Diseases 0.000 description 2
- 239000002398 materia medica Substances 0.000 description 2
- 210000000496 pancreas Anatomy 0.000 description 2
- QLPRYZXNWYTFCI-UHFFFAOYSA-N saikosaponin D Natural products CC1OC(OC2CCC3(C)C(CCC4(C)C3C=CC56OCC7(CCC(C)(C)CC57)C(O)CC46C)C2(C)CO)C(O)C(O)C1OC8OC(CO)C(O)C(O)C8O QLPRYZXNWYTFCI-UHFFFAOYSA-N 0.000 description 2
- PQPVAGWUNWFCJE-UHFFFAOYSA-N saikosaponin a Natural products CC1OC(OC2CCC3(C)C(C2)C(C)(CO)CC4(C)C3C=CC56OCC7(CCC(C)(C)CC57)C(O)CC46C)C(O)C(OC8OC(CO)C(O)C(O)C8O)C1O PQPVAGWUNWFCJE-UHFFFAOYSA-N 0.000 description 2
- 238000000926 separation method Methods 0.000 description 2
- QZAYGJVTTNCVMB-UHFFFAOYSA-N serotonin Chemical compound C1=C(O)C=C2C(CCN)=CNC2=C1 QZAYGJVTTNCVMB-UHFFFAOYSA-N 0.000 description 2
- 239000007962 solid dispersion Substances 0.000 description 2
- 210000005090 tracheal smooth muscle Anatomy 0.000 description 2
- 206010001580 Albuminuria Diseases 0.000 description 1
- 230000003844 B-cell-activation Effects 0.000 description 1
- 241000510654 Bupleurum chinense Species 0.000 description 1
- 241000213015 Bupleurum scorzonerifolium Species 0.000 description 1
- 241000700199 Cavia porcellus Species 0.000 description 1
- 206010010904 Convulsion Diseases 0.000 description 1
- 206010011878 Deafness Diseases 0.000 description 1
- SUZLHDUTVMZSEV-UHFFFAOYSA-N Deoxycoleonol Natural products C12C(=O)CC(C)(C=C)OC2(C)C(OC(=O)C)C(O)C2C1(C)C(O)CCC2(C)C SUZLHDUTVMZSEV-UHFFFAOYSA-N 0.000 description 1
- 102000004190 Enzymes Human genes 0.000 description 1
- 108090000790 Enzymes Proteins 0.000 description 1
- 206010019233 Headaches Diseases 0.000 description 1
- 241000167880 Hirundinidae Species 0.000 description 1
- 108010002352 Interleukin-1 Proteins 0.000 description 1
- 108010002350 Interleukin-2 Proteins 0.000 description 1
- 208000019255 Menstrual disease Diseases 0.000 description 1
- 208000012902 Nervous system disease Diseases 0.000 description 1
- 208000002193 Pain Diseases 0.000 description 1
- 206010068676 Pneumoretroperitoneum Diseases 0.000 description 1
- 206010057190 Respiratory tract infections Diseases 0.000 description 1
- 208000005727 Retropneumoperitoneum Diseases 0.000 description 1
- KYWSCMDFVARMPN-MSSMMRRTSA-N Saikosaponin A Chemical compound O([C@@H]1[C@@H](O)[C@H](O[C@@H]2[C@@]([C@H]3[C@]([C@@H]4[C@@]([C@@]5(C[C@H](O)[C@]67CO[C@]5([C@@H]6CC(C)(C)CC7)C=C4)C)(C)CC3)(C)CC2)(C)CO)O[C@@H]([C@@H]1O)C)[C@@H]1O[C@H](CO)[C@@H](O)[C@H](O)[C@H]1O KYWSCMDFVARMPN-MSSMMRRTSA-N 0.000 description 1
- SXILFEBNQCRWAL-UHFFFAOYSA-N Saikosaponin-f Natural products OC1C(O)C(O)C(C)OC1OC1C(O)C(O)C(OC2C(C3C(C4C(C5(CC(O)C6(CO)CCC(C)(C)CC6C5=CC4)C)(C)CC3)(C)CC2)(C)C)OC1COC1C(O)C(O)C(O)C(CO)O1 SXILFEBNQCRWAL-UHFFFAOYSA-N 0.000 description 1
- 206010046306 Upper respiratory tract infection Diseases 0.000 description 1
- 206010046814 Uterine prolapse Diseases 0.000 description 1
- 230000004913 activation Effects 0.000 description 1
- 230000036592 analgesia Effects 0.000 description 1
- 230000000954 anitussive effect Effects 0.000 description 1
- 230000008485 antagonism Effects 0.000 description 1
- 230000000702 anti-platelet effect Effects 0.000 description 1
- 230000000259 anti-tumor effect Effects 0.000 description 1
- 239000003146 anticoagulant agent Substances 0.000 description 1
- 229940124584 antitussives Drugs 0.000 description 1
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 description 1
- 230000009286 beneficial effect Effects 0.000 description 1
- 230000033228 biological regulation Effects 0.000 description 1
- 235000019658 bitter taste Nutrition 0.000 description 1
- 210000004369 blood Anatomy 0.000 description 1
- 239000008280 blood Substances 0.000 description 1
- 210000004556 brain Anatomy 0.000 description 1
- 210000004027 cell Anatomy 0.000 description 1
- 210000000170 cell membrane Anatomy 0.000 description 1
- 238000006243 chemical reaction Methods 0.000 description 1
- 229910052956 cinnabar Inorganic materials 0.000 description 1
- OHCQJHSOBUTRHG-UHFFFAOYSA-N colforsin Natural products OC12C(=O)CC(C)(C=C)OC1(C)C(OC(=O)C)C(O)C1C2(C)C(O)CCC1(C)C OHCQJHSOBUTRHG-UHFFFAOYSA-N 0.000 description 1
- 239000000470 constituent Substances 0.000 description 1
- 230000036461 convulsion Effects 0.000 description 1
- 238000001816 cooling Methods 0.000 description 1
- 230000001186 cumulative effect Effects 0.000 description 1
- 231100000895 deafness Toxicity 0.000 description 1
- 230000002950 deficient Effects 0.000 description 1
- 230000001419 dependent effect Effects 0.000 description 1
- 238000011161 development Methods 0.000 description 1
- ZZVUWRFHKOJYTH-UHFFFAOYSA-N diphenhydramine Chemical compound C=1C=CC=CC=1C(OCCN(C)C)C1=CC=CC=C1 ZZVUWRFHKOJYTH-UHFFFAOYSA-N 0.000 description 1
- 201000010099 disease Diseases 0.000 description 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 1
- 239000006185 dispersion Substances 0.000 description 1
- 239000012153 distilled water Substances 0.000 description 1
- 208000002173 dizziness Diseases 0.000 description 1
- 230000009977 dual effect Effects 0.000 description 1
- 230000005284 excitation Effects 0.000 description 1
- 239000000796 flavoring agent Substances 0.000 description 1
- 235000019634 flavors Nutrition 0.000 description 1
- 238000009472 formulation Methods 0.000 description 1
- 210000001035 gastrointestinal tract Anatomy 0.000 description 1
- 238000000227 grinding Methods 0.000 description 1
- 231100000869 headache Toxicity 0.000 description 1
- 208000016354 hearing loss disease Diseases 0.000 description 1
- 210000002443 helper t lymphocyte Anatomy 0.000 description 1
- 230000002443 hepatoprotective effect Effects 0.000 description 1
- 230000037111 immune power Effects 0.000 description 1
- 230000036039 immunity Effects 0.000 description 1
- 230000007365 immunoregulation Effects 0.000 description 1
- 230000005764 inhibitory process Effects 0.000 description 1
- -1 lipid peroxide Chemical class 0.000 description 1
- 210000004698 lymphocyte Anatomy 0.000 description 1
- 201000004792 malaria Diseases 0.000 description 1
- 238000004519 manufacturing process Methods 0.000 description 1
- 230000007246 mechanism Effects 0.000 description 1
- 230000004060 metabolic process Effects 0.000 description 1
- 239000000401 methanolic extract Substances 0.000 description 1
- 238000002156 mixing Methods 0.000 description 1
- 229930014626 natural product Natural products 0.000 description 1
- 201000008383 nephritis Diseases 0.000 description 1
- 230000036963 noncompetitive effect Effects 0.000 description 1
- 229940126701 oral medication Drugs 0.000 description 1
- 229910052760 oxygen Inorganic materials 0.000 description 1
- 239000001301 oxygen Substances 0.000 description 1
- 230000036407 pain Effects 0.000 description 1
- 230000001314 paroxysmal effect Effects 0.000 description 1
- 235000017807 phytochemicals Nutrition 0.000 description 1
- 229930000223 plant secondary metabolite Natural products 0.000 description 1
- 210000003240 portal vein Anatomy 0.000 description 1
- 239000013641 positive control Substances 0.000 description 1
- 238000001556 precipitation Methods 0.000 description 1
- 238000003672 processing method Methods 0.000 description 1
- 230000036385 rapid eye movement (rem) sleep Effects 0.000 description 1
- 230000009467 reduction Effects 0.000 description 1
- 238000012827 research and development Methods 0.000 description 1
- 230000033764 rhythmic process Effects 0.000 description 1
- 230000000630 rising effect Effects 0.000 description 1
- 239000000932 sedative agent Substances 0.000 description 1
- 230000001624 sedative effect Effects 0.000 description 1
- 239000011734 sodium Substances 0.000 description 1
- 210000000952 spleen Anatomy 0.000 description 1
- 208000010110 spontaneous platelet aggregation Diseases 0.000 description 1
- 230000000087 stabilizing effect Effects 0.000 description 1
- 239000000758 substrate Substances 0.000 description 1
- 239000000725 suspension Substances 0.000 description 1
- 238000012360 testing method Methods 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
- 230000002992 thymic effect Effects 0.000 description 1
- 210000003437 trachea Anatomy 0.000 description 1
- 230000009284 tracheal contraction Effects 0.000 description 1
- 230000008728 vascular permeability Effects 0.000 description 1
- 210000003462 vein Anatomy 0.000 description 1
- 238000005303 weighing Methods 0.000 description 1
Landscapes
- Medicines Containing Plant Substances (AREA)
- Medicinal Preparation (AREA)
Abstract
The present invention discloses a kind of Radix bupleuri dripping pill and its preparation process. Radix bupleuri is twice refluxed in water, the extracted liquid is merged, concentrated, alcohol deposited and filtered to recover alcohol and obtain Radix bupleuri extractum, and the Radix bupleuri extractum is mixed with supplementary material and prepared into the dripping pill. The present invention also discloses the pharmacological effect of the Chinese medicine.
Description
Technical field
The present invention relates to a kind of Chinese medicine preparation and preparation method thereof, specifically the present invention relates to a kind of bupleurum root dropping pills preparation, the invention also discloses its pharmacological action and preparation method thereof.
Background technology
Radix Bupleuri is the dry root of umbelliferae bupleurum Bupleurum chinense DC. or Radix Bupeuri Scorzonerfolii. B.scorzonerifolium Willd., practises title " Radix Bupleuri " respectively by the character difference and reaches " Radix Bupleuri Scorzonerifolii ".The Radix Bupleuri nature and flavor are bitter cool, go into the liver and gall warp, and motherland's medical science is used for alternate attack of chill and fever, fullness in the chest costalgia, bitter taste deafness, headache and dizziness, malaria proctoptosis, menoxenia, the treatment of diseases such as uterine prolapse.
Radix Bupleuri has the use history of nearly one thousand years in China as medical material.This year, constantly perfect along with phytochemical development and extraction process, people have carried out comparatively deep research to the effective ingredient of Radix Bupleuri, wherein relate generally to saikoside and Radix Bupleuri volatile oil.
Saikoside
Saikoside was called saikoside in the past, was water solublity effective site representative in the Radix Bupleuri medical material.Studies show that it has calmness, analgesia, cooling, antitussive, antiinflammatory, protects the liver, antitumor, reduction Sanguis Leporis seu oryctolagi are pressed, suppress the effects such as vascular permeability increase that caused by histamine and 5-hydroxy tryptamine.Along with the continuous progress of research, people have had new understanding again to its pharmacological action:
Suppress trypsin acting: Radix Bupleuri is used for the treatment of acute pancreatitis clinically, but does not have report before its effective ingredient and the mechanisms of therapeutic action.Yang Tongcheng [Yang Tongcheng etc., the saikoside extract is to the trypsin inhibitory action, the Fujian Chinese medicine, 1990,21 (6): 44-45] in experiment in vitro research, find, from Radix Bupleuri, extract saikoside a, d, get the saponin solution and the trypsin 1.0ml mixing of various dose volume, the reaction back finds that saikoside has strong inhibitory action to trypsin, can infer that therefore saikoside is the effective site of treatment acute pancreatitis.
Inhibitory action to adenyl cyclase (AC): Lin Mingdong [Lin Mingdong etc., the Radix Bupleuri discrete group is to the influence (two) of pancreas thuja acid cyclase, Pharmacology and Clinics of Chinese Materia Medica, 1991,7 (4): 17-21] in vitro study finds that first Radix Bupleuri separation component CH-5 (kaikosides) can significantly suppress the activity that Mouse Liver prepares AC, has obvious dose-effect relationship in the finite concentration scope.
Immunoregulation effect: in the Radix Bupleuri root isolating Saikosaponin a, d, f and Saponin slightly carry mixture (CSM) to mouse peritoneal injection (1～10mg/kg), studies show that all group thymic weight/body weight have increase in first week, after this decrescence; It is cumulative to suppress cell (Th/Ts) ratio for the mouse lymphocyte subgroup t helper cell/T that organizes with f, is reaching summit the 3rd week and give with a, d and CSM group Th/Ts, lowers then; All group IL-2 levels raise, spleen weight/weight increase, and the B cell activation is by Zhou Zengjia and stimulate IL-1 to induce; Give with a, d group in, IgA, IgG and IgM increase.More than the explanation saikoside can strengthen mouse immune power.
Influence to treatment renal glomerular disease aspect: discover that (wherein remove and contain s-a, s-c, s-d still contain a certain amount of s-b to the kaikosides c-s that extracts from Radix Bupleuri
1, s-b
2) at daily dose 1.0mg/ks and 5.0ms/ks, can significantly suppress the albuminuria of anti-GBM (GBM) nephritis Mus and the rising of cholesterolemia during i.p, its histopathology is visible obviously to be improved.The effect that the prompting saikoside has antiinflammatory, enhance immunity, anti-platelet aggregation, inhibition oxygen-derived free radicals and a stabilizing cell membrane comprehensively onset alleviates glomerule and damages, and is very promising Treatment of Glomerular Disease medicine.
Influence to sleep: modern medicine study proves that saikoside has central inhibitory actions such as calmness, convulsion, clinically can be used for multiple nervous system disease.Sun Bing [Sun Bing etc., saikoside is to the synthetic experimental study of cat sleep rhythm electrical activity, Chinese herbal medicine, 1994,25 (2): 82-83] discover to cat lumbar injection saikoside injection 1ms/ks, the increase that can prolong the cat length of one's sleep, particularly S sleep II phase (IISWS) and REM sleep phase (REM) is remarkable, and its effect is better than classical Cinnabar Sedative Pill.
Radix Bupleuri volatile oil
Radix Bupleuri volatile oil is one of effective site of antipyretic-antalgic clinically, dual regulation effect to adenyl cyclase (AC): Lin Mingdong [Lin Mingdong etc., the Radix Bupleuri discrete group is to the influence (two) of pancreas thuja acid cyclase, Pharmacology and Clinics of Chinese Materia Medica, 1991,7 (4): 17-21] once report the Radix Bupleuri methanolic extract in 1989 and be concentration dependent activation AC effect.
Influence to the isolated tracheal contraction that causes by histamine: Teng Chuxing [Teng Chuxing etc., Radix Bupleuri component (CHC-6) and Forskolin are to the influence of brain adenylate cyclase enzyme activity, Chinese herbal medicine, 1996,27 (increasing): 123-126] discover CHC-6 on stripped guinea pig trachea spiral bar specimen, there is the noncompetitive antagonism histamine to shrink the tracheal smooth muscle effect.This is using the prospect that provides for Radix Bupleuri aspect diastole tracheal smooth muscle.
Anti-drunk effect: Qi Kaiqin [Qi Kaiqin, the research of Radix Bupleuri extract anti-drunk function, research and development of natural products, 1995,17 (3): 20-23] discover that Radix Bupleuri (Radix Bupleri) alcohol extract has the central nervous excitation of raising, induce the liver drug enzyme activity, improve liver homogenate superoxide dismutase (SOD) activity, reduce effects such as lipid peroxide (LPO) content, thereby have anti-drunk and hepatoprotective effect.
In recent years, along with people to the going deep into of Radix Bupleuri research, the Radix Bupleuri oral formulations of having developed has: Radix Bupleuri oral liquid, injection of Radix Bupleuri etc., but because dosage form itself, they all exist following problem:
● the first pass effect problem.First pass effect (First-pass Effect) claim the first pass effect again, is meant oral drugs after gastrointestinal absorption, at first arrives liver through portal vein, enters the body circulation again.By metabolism, this phenomenon becomes first pass effect to some medicine by liver the time.Radix Bupleuri oral liquid is because itself, and its effective ingredient major part of back of taking medicine absorbs in gastrointestinal tract, is easy to generate first pass effect, and its effective ingredient is reduced.
● the clinical effectiveness of upper respiratory tract infection such as Radix Bupleuri oral liquid and injection of Radix Bupleuri treatment flu, influenza is fine, has and steadily brings down a fever, and fall the heat back and do not have characteristics such as rise.But the effective ingredient of injection of Radix Bupleuri has only volatile oil, and other effective ingredient such as saikoside etc. all abandon.In addition, injection of Radix Bupleuri and Radix Bupleuri oral liquid use and carry inconvenience, make its clinical practice be subjected to restriction greatly.
At the problem of above existence, we need a kind of quick-acting, the oral administration solid bupleurum preparation to be to satisfy the needs of clinical practice efficiently.
Summary of the invention
Purpose of the present invention is providing a kind of efficient, quick-acting oral administration solid bupleurum preparation.
Another object of the present invention is to provide the preparation method of this oral administration solid bupleurum preparation.
The present invention is implemented by following scheme:
A. get the Radix Bupleuri medical material, through suitably being processed into extractum;
B. with behind above-mentioned extractum and the suitable adjuvant mix homogeneously, add the transconversion into heat material;
The extractum that c. will mix adjuvant moves into the dropping-pill machine jar, splashes in the cryogenic liquid paraffin, removes liquid paraffin, selects ball, promptly.
Wherein, the Radix Bupleuri processing method is as follows among the step a:
The water reflux extraction: concrete steps are, Radix Bupleuri adds water reflux, extract, twice, and merge extractive liquid, concentrates, and adds ethanol precipitation, filters, concentrate and reclaim ethanol, Radix Bupleuri extractum.Wherein, extracting amount of water for the first time is 4～6 times, and be 1～3 hour heat time heating time, and amount of water is 2～3 times for the second time, and be 0.5～1.5 hour heat time heating time; Optimum condition is that amount of water is 5 times for the first time, and be 2 hours heat time heating time, and amount of water is 2.5 times for the second time, and be 1 hour heat time heating time; Concentrated extracting solution is 1: 1～0.6 to the crude drug amount with the extracting liquid volume ratio, and optimal proportion is 1: 0.8; Ethanol precipitation is 50～90% to containing the alcohol amount, and optimum condition is 70%; Filter, reclaiming ethanol to relative density is 1.3～1.4.
Adjuvant is a Macrogol 4000 among the step b of the present invention, perhaps polyethylene glycol 6000 is perhaps with Macrogol 4000 and polyethylene glycol 6000 mixture, perhaps with sodium stearate, perhaps with glycerin gelatine, the Radix Bupleuri extractum that obtains among the step a and the ratio of adjuvant are 1: 2～4; Preferred adjuvant is polyethylene glycol 6000 or Macrogol 4000, and the ratio of Radix Bupleuri extractum and adjuvant is 1: 2.5～3.5; Best adjuvant is a polyethylene glycol 6000, and the ratio of Radix Bupleuri extractum and adjuvant is 1: 3; The ratio of the mixture that wherein said Macrogol 4000 and polyethylene glycol 6000 are formed is 1: 0.01～99.9, and preferred proportion is 1: 1～5, and optimal proportion is 1: 1; Changing the material temperature is 85～95 ℃, and preferred temperature is 90 ℃.
Drip a jar temperature among the step c and remain between 65～75 ℃, preferred temperature is 70 ℃; The liquid paraffin temperature is preferably 8 ℃ for being lower than 10 ℃.
We derive from " Radix Bupleuri oral liquid " of 95 years versions of Pharmacopoeia of People's Republic of China.Compare with original technology, the present invention has following advantage:
● the present invention has adopted " solid dispersion technology ", medicine is dispersed in has formed the molecular dispersion system in the substrate.Sublingual administration, effective ingredient can have been avoided the first pass effect that brings because of gastrointestinal absorption by sublingual vein directly into blood.
● saikoside is one of effective site of antipyretic-antalgic clinically, Given this present invention has partly adopted two kinds of diverse ways in the Radix Bupleuri medicinal material extract, Radix Bupleuri volatile oil has been carried out keeping fully, use the water extract-alcohol precipitation technology simultaneously and taken into account the proposition of aqueous saponin constituents, thereby guaranteed the abundant separation of the various effective ingredient in the medical material.Remedied prior art---the defective that the Radix Bupleuri oral liquid saikoside is dropped.
● be convenient to take.The present invention has adopted drops, and the medicine grain is little, swallows conveniently, and the child that is more convenient for uses.
● easy to carry.The present invention has adopted solid dispersion technology, the fast characteristics of existing solution rate of release, and it is easy to carry to possess solid drugs again, and accumulating is advantage easily.
Below by zoopery, beneficial effect of the present invention is described.
Classical analgesic test model---the hot writhing method of mice is adopted in this experiment, with the positive contrast medicine of aspirin, has observed the analgesic activity of bupleurum root dropping pills and oral liquid.The result shows that two kinds of dosage forms of Radix Bupleuri all have tangible analgesic effect (P＜0.05) to these two kinds of models.Medicine:
Bupleurum root dropping pills: 3.125g crude drug/g drop pill, the time spent is mixed with 16% solution with distilled water, and redilution becomes 8% solution.This medicine is provided by Tianjin Tasly Pharmaceutical Co., Ltd, lot number: 20010415;
Radix Bupleuri oral liquid: 1g crude drug/ml, Bai Quan pharmaceutical factory in Henan produces, lot number: 20010502.Original liquid concentration is used for experiment.Aspirin: content is greater than 99%, by Shandong Xinhua Pharmaceutical Factory production, and lot number: 20010105.Be mixed with 2.5% suspension with preceding the grinding with 0.5%CMC-Na.
Animal:
180 of white mice, body weight 23.7 ± 2.1g, be female, available from Tianjin drug research institute animal center.
Equipment:
Balance, DZKW-C type water-bath, stopwatch, syringe etc.
Method and result:
Writhing method: get 160 of mices and divide 8 groups at random, animal fasting 12 hours, the administration according to the method described above of weighing.45 minutes pneumoretroperitoneums of administration are only injected 0.5% acetic acid 0.2ml/, observe mouse writhing number of times in 20 minutes, obtain and respectively organize mean, carry out two groups of mean t checks, the results are shown in following table.
Bupleurum root dropping pills is to paroxysmal pain effect (writhing method, the n=20 of mice; X ± s)
| Group | Dosage (g/kg) | Turn round the body number of times (inferior/20min) |
| Matched group | —— | 27.6±21.6 |
| Bupleurum root dropping pills | 4.0 | 10.8±7.8* |
| Radix Bupleuri oral liquid | 4.0 | 12.3±10.2* |
| Aspirin | 0.2 | 5.0±8.1* |
Annotate: have significant difference, * P＜0.01 with the matched group ratio.
The result shows that the present invention's " a kind of bupleurum root dropping pills " all has the effect (comparing P＜0.01 with matched group) that reduces the mouse writhing number of times significantly with the positive control drug aspirin.
Specific embodiment
The present invention is further illustrated below in conjunction with specific embodiment, and following this embodiment only is used to the present invention is described and to the present invention without limits.
Embodiment 1
A. get Radix Bupleuri 1.25kg, add water and reflux 2 times, add the water of 5 times of amounts for the first time, reflux 2 hours; The water that adds for the second time 2.5 times of amounts, reflux 1 hour, merge extractive liquid,, the ratio that is concentrated into crude drug and extracting liquid volume is 1: 0.8, adds 95% ethanol precipitation and makes and contain the alcohol amount to 70%, leaves standstill, filter, concentrating and reclaiming ethanol to relative density is 1.35, gets Radix Bupleuri extractum;
B. get above-mentioned Radix Bupleuri extractum and mix with polyethylene glycol 6000, ratio is 1: 3;
C. the preparation of product: get above-mentioned Radix Bupleuri extractum and polyethylene glycol 6000 and be heated to 90 ℃, the drip irrigation that moves into the drop pill machine remains on 70 ℃, drips to 8 ℃ liquid paraffin, takes out drop pill, removes liquid paraffin, selects ball, makes 1000 of drop pill.
Embodiment 2
A. get Radix Bupleuri 1.25kg, add water and reflux 2 times, add the water of 4 times of amounts for the first time, reflux 1 hour; The water that adds for the second time 2 times of amounts, reflux 1 hour, merge extractive liquid,, the ratio that is concentrated into crude drug and extracting liquid volume is 1: 0.6, adds 95% ethanol precipitation and makes and contain the alcohol amount to 50%, leaves standstill, filter, concentrating and reclaiming ethanol to relative density is 1.35, gets Radix Bupleuri extractum;
B. get above-mentioned Radix Bupleuri extractum and mix with polyethylene glycol 6000, ratio is 1: 3;
C. the preparation of product: get above-mentioned Radix Bupleuri extractum and polyethylene glycol 6000 and be heated to 85 ℃, the drip irrigation that moves into the drop pill machine remains on 70 ℃, drips to 8 ℃ liquid paraffin, takes out drop pill, removes liquid paraffin, selects ball, makes 1000 of drop pill.
Embodiment 3
A. get Radix Bupleuri 1.25kg, add water and reflux 2 times, add the water of 6 times of amounts for the first time, reflux 1 hour; The water that adds for the second time 2 times of amounts, reflux 1 hour, merge extractive liquid,, the ratio that is concentrated into crude drug and extracting liquid volume is 1: 0.7, adds 95% ethanol precipitation and makes and contain the alcohol amount to 60%, leaves standstill, filter, concentrating and reclaiming ethanol to relative density is 1.35, gets Radix Bupleuri extractum;
B. get above-mentioned Radix Bupleuri extractum and mix with polyethylene glycol 6000, ratio is 1: 3;
C. the preparation of product: get above-mentioned Radix Bupleuri extractum and polyethylene glycol 6000 and be heated to 95 ℃, the drip irrigation that moves into the drop pill machine remains on 65 ℃, drips to 8 ℃ liquid paraffin, takes out drop pill, removes liquid paraffin, selects ball, makes 1000 of drop pill.
Embodiment 4
A. get Radix Bupleuri 1.25kg, add water and reflux 2 times, add the water of 4 times of amounts for the first time, reflux 1 hour; The water that adds for the second time 2 times of amounts, reflux 1 hour, merge extractive liquid,, the ratio that is concentrated into crude drug and extracting liquid volume is 1: 0.6, adds 95% ethanol precipitation and makes and contain the alcohol amount to 50%, leaves standstill, filter, concentrating and reclaiming ethanol to relative density is 1.35, gets Radix Bupleuri extractum;
B. get above-mentioned Radix Bupleuri extractum and mix with Macrogol 4000, ratio is 1: 3;
C. the preparation of product: get above-mentioned Radix Bupleuri extractum and Macrogol 4000 and be heated to 85 ℃, the drip irrigation that moves into the drop pill machine remains on 70 ℃, drips to 8 ℃ liquid paraffin, takes out drop pill, removes liquid paraffin, selects ball, makes 1000 of drop pill.
Embodiment 5
A. get Radix Bupleuri 1.25kg, add water and reflux 2 times, add the water of 5 times of amounts for the first time, reflux 1 hour; The water that adds for the second time 2 times of amounts, reflux 1 hour, merge extractive liquid,, the ratio that is concentrated into crude drug and extracting liquid volume is 1: 0.9, adds 95% ethanol precipitation and makes and contain the alcohol amount to 50%, leaves standstill, and filters, concentrating and reclaiming ethanol to relative density is 1.4, Radix Bupleuri extractum;
B. get above-mentioned Radix Bupleuri extractum and mix with Macrogol 4000, ratio is 1: 3;
C. the preparation of product: get above-mentioned Radix Bupleuri extractum and Macrogol 4000 and be heated to 85 ℃, the drip irrigation that moves into the drop pill machine remains on 70 ℃, drips to 8 ℃ liquid paraffin, takes out drop pill, removes liquid paraffin, selects ball, makes 1000 of drop pill.
Embodiment 6
A. get Radix Bupleuri 1.25kg, add water and reflux 2 times, add the water of 4 times of amounts for the first time, reflux 1 hour; The water that adds for the second time 2 times of amounts, reflux 1 hour, merge extractive liquid,, the ratio that is concentrated into crude drug and extracting liquid volume is 1: 0.6, adds 95% ethanol precipitation and makes and contain the alcohol amount to 85%, leaves standstill, filter, concentrating and reclaiming ethanol to relative density is 1.39, gets Radix Bupleuri extractum;
B. get above-mentioned Radix Bupleuri extractum and mix with Macrogol 4000, ratio is 1: 2;
C. the preparation of product: get above-mentioned Radix Bupleuri extractum and Macrogol 4000 and be heated to 85 ℃, the drip irrigation that moves into the drop pill machine remains on 70 ℃, drips to 8 ℃ liquid paraffin, takes out drop pill, removes liquid paraffin, selects ball, makes 1000 of drop pill.
Embodiment 7
A. get Radix Bupleuri 1.25kg, add water and reflux 2 times, add the water of 4 times of amounts for the first time, reflux 1 hour; The water that adds for the second time 2 times of amounts, reflux 1 hour, merge extractive liquid,, the ratio that is concentrated into crude drug and extracting liquid volume is 1: 0.6, adds 95% ethanol precipitation and makes and contain the alcohol amount to 50%, leaves standstill, filter, concentrating and reclaiming ethanol to relative density is 1.35, gets Radix Bupleuri extractum;
B. get above-mentioned Radix Bupleuri extractum and mix with polyethylene glycol 6000, ratio is 1: 2;
C. the preparation of product: get above-mentioned Radix Bupleuri extractum and polyethylene glycol 6000 and be heated to 85 ℃, the drip irrigation that moves into the drop pill machine remains on 70 ℃, drips to 8 ℃ liquid paraffin, takes out drop pill, removes liquid paraffin, selects ball, makes 1000 of drop pill.
Embodiment 8
A. get Radix Bupleuri 1.25kg, add water and reflux 2 times, add the water of 4 times of amounts for the first time, reflux 1 hour; The water that adds for the second time 2 times of amounts, reflux 1 hour, merge extractive liquid,, the ratio that is concentrated into crude drug and extracting liquid volume is 1: 0.6, adds 95% ethanol precipitation and makes and contain the alcohol amount to 50%, leaves standstill, filter, concentrating and reclaiming ethanol to relative density is 1.35, gets Radix Bupleuri extractum;
B. get above-mentioned Radix Bupleuri extractum and mix with polyethylene glycol 6000, ratio is 1: 2.5;
C. the preparation of product: get above-mentioned Radix Bupleuri extractum and polyethylene glycol 6000 and be heated to 85 ℃, the drip irrigation that moves into the drop pill machine remains on 70 ℃, drips to 8 ℃ liquid paraffin, takes out drop pill, removes liquid paraffin, selects ball, makes 1000 of drop pill.
Embodiment 9
A. get Radix Bupleuri 1.25kg, add water and reflux 2 times, add the water of 4 times of amounts for the first time, reflux 1 hour; The water that adds for the second time 2 times of amounts, reflux 1 hour, merge extractive liquid,, the ratio that is concentrated into crude drug and extracting liquid volume is 1: 0.6, adds 95% ethanol precipitation and makes and contain the alcohol amount to 90%, leaves standstill, filter, concentrating and reclaiming ethanol to relative density is 1.31, gets Radix Bupleuri extractum;
B. get above-mentioned Radix Bupleuri extractum and mix with polyethylene glycol 6000, ratio is 1: 3.5;
C. the preparation of product: get above-mentioned Radix Bupleuri extractum and polyethylene glycol 6000 and be heated to 85 ℃, the drip irrigation that moves into the drop pill machine remains on 75 ℃, drips to 8 ℃ liquid paraffin, takes out drop pill, removes liquid paraffin, selects ball, makes 1000 of drop pill.
Embodiment 10
A. get Radix Bupleuri 1.25kg, add water and reflux 2 times, add the water of 4 times of amounts for the first time, reflux 1 hour; The water that adds for the second time 2 times of amounts, reflux 1 hour, merge extractive liquid,, the ratio that is concentrated into crude drug and extracting liquid volume is 1: 1, adds 95% ethanol precipitation and makes and contain the alcohol amount to 80%, leaves standstill, and filters, concentrating and reclaiming ethanol to relative density is 1.33, Radix Bupleuri extractum;
B. get above-mentioned Radix Bupleuri extractum and mix with polyethylene glycol 6000, ratio is 1: 4;
C. the preparation of product: get above-mentioned Radix Bupleuri extractum and polyethylene glycol 6000 and be heated to 85 ℃, the drip irrigation that moves into the drop pill machine remains on 65 ℃, drips to 8 ℃ liquid paraffin, takes out drop pill, removes liquid paraffin, selects ball, makes 1000 of drop pill.
Embodiment 11
A. get Radix Bupleuri 1.25kg, add water and reflux 2 times, add the water of 6 times of amounts for the first time, reflux 1 hour; The water that adds for the second time 2 times of amounts, reflux 1 hour, merge extractive liquid,, the ratio that is concentrated into crude drug and extracting liquid volume is 1: 0.9, adds 95% ethanol precipitation and makes and contain the alcohol amount to 80%, leaves standstill, filter, concentrating and reclaiming ethanol to relative density is 1.36, gets Radix Bupleuri extractum;
B. get above-mentioned Radix Bupleuri extractum and mix with Macrogol 4000, ratio is 1: 2;
C. the preparation of product: get above-mentioned Radix Bupleuri extractum and Macrogol 4000 and be heated to 85 ℃, the drip irrigation that moves into the drop pill machine remains on 75 ℃, drips to 8 ℃ liquid paraffin, takes out drop pill, removes liquid paraffin, selects ball, makes 1000 of drop pill.
Embodiment 12
A. get Radix Bupleuri 1.25kg, add water and reflux 2 times, add the water of 4 times of amounts for the first time, reflux 1 hour; The water that adds for the second time 2 times of amounts, reflux 1 hour, merge extractive liquid,, the ratio that is concentrated into crude drug and extracting liquid volume is 1: 0.6, adds 95% ethanol precipitation and makes and contain the alcohol amount to 50%, leaves standstill, filter, concentrating and reclaiming ethanol to relative density is 1.35, gets Radix Bupleuri extractum;
B. get above-mentioned Radix Bupleuri extractum and mix with Macrogol 4000, ratio is 1: 2.5;
C. the preparation of product: get above-mentioned Radix Bupleuri extractum and Macrogol 4000 and be heated to 95 ℃, the drip irrigation that moves into the drop pill machine remains on 70 ℃, drips to 9 ℃ liquid paraffin, takes out drop pill, removes liquid paraffin, selects ball, makes 1000 of drop pill.
Embodiment 12
A. get Radix Bupleuri 1.25kg, add water and reflux 2 times, add the water of 4 times of amounts for the first time, reflux 1 hour; The water that adds for the second time 2 times of amounts, reflux 1 hour, merge extractive liquid,, the ratio that is concentrated into crude drug and extracting liquid volume is 1: 0.9, adds 95% ethanol precipitation and makes and contain the alcohol amount to 85%, leaves standstill, filter, concentrating and reclaiming ethanol to relative density is 1.34, gets Radix Bupleuri extractum;
B. get above-mentioned Radix Bupleuri extractum and mix with Macrogol 4000, ratio is 1: 3.5;
C. the preparation of product: get above-mentioned Radix Bupleuri extractum and Macrogol 4000 and be heated to 90 ℃, the drip irrigation that moves into the drop pill machine remains on 65 ℃, drips to 6 ℃ liquid paraffin, takes out drop pill, removes liquid paraffin, selects ball, makes 1000 of drop pill.
Embodiment 13
A. get Radix Bupleuri 1.25kg, add water and reflux 2 times, add the water of 4 times of amounts for the first time, reflux 1 hour; The water that adds for the second time 2 times of amounts, reflux 1 hour, merge extractive liquid,, the ratio that is concentrated into crude drug and extracting liquid volume is 1: 0.6, adds 95% ethanol precipitation and makes and contain the alcohol amount to 50%, leaves standstill, filter, concentrating and reclaiming ethanol to relative density is 1.35, gets Radix Bupleuri extractum;
B. get above-mentioned Radix Bupleuri extractum and mix with Macrogol 4000, ratio is 1: 4;
C. the preparation of product: get above-mentioned Radix Bupleuri extractum and Macrogol 4000 and be heated to 95 ℃, the drip irrigation that moves into the drop pill machine remains on 75 ℃, drips to 8 ℃ liquid paraffin, takes out drop pill, removes liquid paraffin, selects ball, makes 1000 of drop pill.
Embodiment 14
A. get Radix Bupleuri 1.25kg, add water and reflux 2 times, add the water of 4 times of amounts for the first time, reflux 1 hour; The water that adds for the second time 2 times of amounts, reflux 1 hour, merge extractive liquid,, the ratio that is concentrated into crude drug and extracting liquid volume is 1: 0.8, adds 95% ethanol precipitation and makes and contain the alcohol amount to 80%, leaves standstill, filter, concentrating and reclaiming ethanol to relative density is 1.38, gets Radix Bupleuri extractum;
B. get above-mentioned Radix Bupleuri extractum and mix with polyethylene glycol 6000, ratio is 1: 2;
C. the preparation of product: get above-mentioned Radix Bupleuri extractum and polyethylene glycol 6000 and be heated to 85 ℃, the drip irrigation that moves into the drop pill machine remains on 70 ℃, drips to 8 ℃ liquid paraffin, takes out drop pill, removes liquid paraffin, selects ball, makes 1000 of drop pill.
Embodiment 15
A. get Radix Bupleuri 1.25kg, add water and reflux 2 times, add the water of 4 times of amounts for the first time, reflux 1 hour; The water that adds for the second time 2 times of amounts, reflux 1 hour, merge extractive liquid,, the ratio that is concentrated into crude drug and extracting liquid volume is 1: 0.8, adds 95% ethanol precipitation and makes and contain the alcohol amount to 80%, leaves standstill, filter, concentrating and reclaiming ethanol to relative density is 1.38, gets Radix Bupleuri extractum;
B. get above-mentioned Radix Bupleuri extractum and mix with the mixture (ratio is 1: 1) of polyethylene glycol 6000 and 4000, ratio is 1: 3;
C. the preparation of product: get the mixture heated to 85 ℃ of above-mentioned Radix Bupleuri extractum and polyethylene glycol 6000 and 4000, the drip irrigation that moves into the drop pill machine remains on 70 ℃, drips to 8 ℃ liquid paraffin, takes out drop pill, removes liquid paraffin, selects ball, makes 1000 of drop pill.
Embodiment 16
A. get Radix Bupleuri 1.25kg, add water and reflux 2 times, add the water of 4 times of amounts for the first time, reflux 1 hour; The water that adds for the second time 2 times of amounts, reflux 1 hour, merge extractive liquid,, the ratio that is concentrated into crude drug and extracting liquid volume is 1: 0.8, adds 95% ethanol precipitation and makes and contain the alcohol amount to 80%, leaves standstill, filter, concentrating and reclaiming ethanol to relative density is 1.38, gets Radix Bupleuri extractum;
B. get above-mentioned Radix Bupleuri extractum and mix with the mixture (ratio is 1: 1) of polyethylene glycol 6000 and 4000, ratio is 1: 2;
C. the preparation of product: the mixture of getting above-mentioned Radix Bupleuri extractum and polyethylene glycol 6000 and 4000 is mixed and heated to 85 ℃, and the drip irrigation that moves into the drop pill machine remains on 70 ℃, drips to 8 ℃ liquid paraffin, take out drop pill, remove liquid paraffin, select ball, make 1000 of drop pill.
Embodiment 17
A. get Radix Bupleuri 1.25kg, add water and reflux 2 times, add the water of 4 times of amounts for the first time, reflux 1 hour; The water that adds for the second time 2 times of amounts, reflux 1 hour, merge extractive liquid,, the ratio that is concentrated into crude drug and extracting liquid volume is 1: 0.8, adds 95% ethanol precipitation and makes and contain the alcohol amount to 80%, leaves standstill, filter, concentrating and reclaiming ethanol to relative density is 1.38, gets Radix Bupleuri extractum;
B. get above-mentioned Radix Bupleuri extractum and mix with the mixture (ratio is 1: 1) of polyethylene glycol 6000 and 4000, ratio is 1: 2.5;
C. the preparation of product: the mixture of getting above-mentioned Radix Bupleuri extractum and polyethylene glycol 6000 and 4000 is mixed and heated to 85 ℃, and the drip irrigation that moves into the drop pill machine remains on 70 ℃, drips to 8 ℃ liquid paraffin, take out drop pill, remove liquid paraffin, select ball, make 1000 of drop pill.
Embodiment 18
A. get Radix Bupleuri 1.25kg, add water and reflux 2 times, add the water of 4 times of amounts for the first time, reflux 1 hour; The water that adds for the second time 2 times of amounts, reflux 1 hour, merge extractive liquid,, the ratio that is concentrated into crude drug and extracting liquid volume is 1: 0.8, adds 95% ethanol precipitation and makes and contain the alcohol amount to 80%, leaves standstill, filter, concentrating and reclaiming ethanol to relative density is 1.38, gets Radix Bupleuri extractum;
B. get above-mentioned Radix Bupleuri extractum and mix with the mixture (ratio is 1: 1) of polyethylene glycol 6000 and 4000, ratio is 1: 3.5;
C. the preparation of product: the mixture of getting above-mentioned Radix Bupleuri extractum and polyethylene glycol 6000 and 4000 is mixed and heated to 85 ℃, and the drip irrigation that moves into the drop pill machine remains on 70 ℃, drips to 8 ℃ liquid paraffin, take out drop pill, remove liquid paraffin, select ball, make 1000 of drop pill.
Embodiment 19
D. get Radix Bupleuri 1.25kg, add water and reflux 2 times, add the water of 5 times of amounts for the first time, reflux 1 hour; The water that adds for the second time 3 times of amounts, reflux 1 hour, merge extractive liquid,, the ratio that is concentrated into crude drug and extracting liquid volume is 1: 0.9, adds 95% ethanol precipitation and makes and contain the alcohol amount to 90%, leaves standstill, filter, concentrating and reclaiming ethanol to relative density is 1.40, gets Radix Bupleuri extractum;
E. get above-mentioned Radix Bupleuri extractum and mix with the mixture (ratio is 1: 1) of polyethylene glycol 6000 and 4000, ratio is 1: 4; The preparation of product: the mixture of getting above-mentioned Radix Bupleuri extractum and polyethylene glycol 6000 and 4000 is mixed and heated to 85 ℃, and the drip irrigation that moves into the drop pill machine remains on 70 ℃, drips to 8 ℃ liquid paraffin, takes out drop pill, removes liquid paraffin, selects ball, makes 1000 of drop pill.
Embodiment 20
A. get Radix Bupleuri 1.25kg, add water and reflux 2 times, add the water of 4 times of amounts for the first time, reflux 1 hour; The water that adds for the second time 2 times of amounts, reflux 1 hour, merge extractive liquid,, the ratio that is concentrated into crude drug and extracting liquid volume is 1: 0.8, adds 95% ethanol precipitation and makes and contain the alcohol amount to 80%, leaves standstill, filter, concentrating and reclaiming ethanol to relative density is 1.38, gets Radix Bupleuri extractum;
B. get above-mentioned Radix Bupleuri extractum and mix with the mixture (ratio is 1: 0.01) of Macrogol 4000 and 6000, ratio is 1: 2.5;
C. the preparation of product: get the mixture heated to 85 ℃ of above-mentioned Radix Bupleuri extractum and Macrogol 4000 and 6000, the drip irrigation that moves into the drop pill machine remains on 70 ℃, drips to 8 ℃ liquid paraffin, takes out drop pill, removes liquid paraffin, selects ball, makes 1000 of drop pill.
Embodiment 21
A. get Radix Bupleuri 1.25kg, add water and reflux 2 times, add the water of 5 times of amounts for the first time, reflux 1 hour; The water that adds for the second time 2 times of amounts, reflux 1 hour, merge extractive liquid,, the ratio that is concentrated into crude drug and extracting liquid volume is 1: 0.8, adds 95% ethanol precipitation and makes and contain the alcohol amount to 80%, leaves standstill, filter, concentrating and reclaiming ethanol to relative density is 1.38, gets Radix Bupleuri extractum;
B. get above-mentioned Radix Bupleuri extractum and mix with the mixture (ratio is 1: 0.01) of Macrogol 4000 and 6000, ratio is 1: 3;
C. the preparation of product: get the mixture heated to 90 ℃ of above-mentioned Radix Bupleuri extractum and Macrogol 4000 and 6000, the drip irrigation that moves into the drop pill machine remains on 70 ℃, drips to 8 ℃ liquid paraffin, takes out drop pill, removes liquid paraffin, selects ball, makes 1000 of drop pill.
Embodiment 22
A. get Radix Bupleuri 1.25kg, add water and reflux 2 times, add the water of 4 times of amounts for the first time, reflux 1 hour; The water that adds for the second time 2 times of amounts, reflux 1 hour, merge extractive liquid,, the ratio that is concentrated into crude drug and extracting liquid volume is 1: 0.9, adds 95% ethanol precipitation and makes and contain the alcohol amount to 70%, leaves standstill, filter, concentrating and reclaiming ethanol to relative density is 1.38, gets Radix Bupleuri extractum;
B. get above-mentioned Radix Bupleuri extractum and mix with the mixture (ratio is 1: 0.01) of Macrogol 4000 and 6000, ratio is 1: 3.5;
C. the preparation of product: get the mixture heated to 85 ℃ of above-mentioned Radix Bupleuri extractum and Macrogol 4000 and 6000, the drip irrigation that moves into the drop pill machine remains on 75 ℃, drips to 8 ℃ liquid paraffin, takes out drop pill, removes liquid paraffin, selects ball, makes 1000 of drop pill.
Embodiment 23
A. get Radix Bupleuri 1.25kg, add water and reflux 2 times, add the water of 4 times of amounts for the first time, reflux 1 hour; The water that adds for the second time 2 times of amounts, reflux 1 hour, merge extractive liquid,, the ratio that is concentrated into crude drug and extracting liquid volume is 1: 0.8, adds 95% ethanol precipitation and makes and contain the alcohol amount to 80%, leaves standstill, filter, concentrating and reclaiming ethanol to relative density is 1.38, gets Radix Bupleuri extractum;
B. get above-mentioned Radix Bupleuri extractum and mix with the mixture (ratio is 1: 99.9) of Macrogol 4000 and 6000, ratio is 1: 3:
C. the preparation of product: get the mixture heated to 85 ℃ of above-mentioned Radix Bupleuri extractum and Macrogol 4000 and 6000, the drip irrigation that moves into the drop pill machine remains on 70 ℃, drips to 8 ℃ liquid paraffin, takes out drop pill, removes liquid paraffin, selects ball, makes 1000 of drop pill.
Embodiment 24
A. get Radix Bupleuri 1.25kg, add water and reflux 2 times, add the water of 4 times of amounts for the first time, reflux 1 hour; The water that adds for the second time 2 times of amounts, reflux 1 hour, merge extractive liquid,, the ratio that is concentrated into crude drug and extracting liquid volume is 1: 0.8, adds 95% ethanol precipitation and makes and contain the alcohol amount to 80%, leaves standstill, filter, concentrating and reclaiming ethanol to relative density is 1.38, gets Radix Bupleuri extractum;
B. get above-mentioned Radix Bupleuri extractum and mix with the mixture (ratio is 1: 0.01) of Macrogol 4000 and 6000, ratio is 1: 2.5;
C. the preparation of product: get the mixture heated to 85 ℃ of above-mentioned Radix Bupleuri extractum and Macrogol 4000 and 6000, the drip irrigation that moves into the drop pill machine remains on 70 ℃, drips to 8 ℃ liquid paraffin, takes out drop pill, removes liquid paraffin, selects ball, makes 1000 of drop pill.
Embodiment 25
A. get Radix Bupleuri 1.25kg, add water and reflux 2 times, add the water of 4 times of amounts for the first time, reflux 1 hour; The water that adds for the second time 2 times of amounts, reflux 1 hour, merge extractive liquid,, the ratio that is concentrated into crude drug and extracting liquid volume is 1: 0.8, adds 95% ethanol precipitation and makes and contain the alcohol amount to 80%, leaves standstill, filter, concentrating and reclaiming ethanol to relative density is 1.38, gets Radix Bupleuri extractum;
B. get above-mentioned Radix Bupleuri extractum and mix with glycerin gelatine, ratio is 1: 3;
C. the preparation of product: get above-mentioned Radix Bupleuri extractum and glycerin gelatine and be heated to 85 ℃, the drip irrigation that moves into the drop pill machine remains on 70 ℃, drips to 8 ℃ liquid paraffin, takes out drop pill, removes liquid paraffin, selects ball, makes 1000 of drop pill.
Embodiment 26
A. get Radix Bupleuri 1.25kg, add water and reflux 2 times, add the water of 4 times of amounts for the first time, reflux 1 hour; The water that adds for the second time 2 times of amounts, reflux 1 hour, merge extractive liquid,, the ratio that is concentrated into crude drug and extracting liquid volume is 1: 0.8, adds 95% ethanol precipitation and makes and contain the alcohol amount to 80%, leaves standstill, filter, concentrating and reclaiming ethanol to relative density is 1.38, gets Radix Bupleuri extractum;
B. get above-mentioned Radix Bupleuri extractum and mix with sodium stearate, ratio is 1: 3;
C. the preparation of product: get above-mentioned Radix Bupleuri extractum and sodium stearate and be heated to 85 ℃, the drip irrigation that moves into the drop pill machine remains on 70 ℃, drips to 8 ℃ liquid paraffin, takes out drop pill, removes liquid paraffin, selects ball, makes 1000 of drop pill.
Claims (13)
1. bupleurum root dropping pills, it is characterized in that Radix Bupleuri extractum and adjuvant Macrogol 4000, perhaps with polyethylene glycol 6000, perhaps with Macrogol 4000 and polyethylene glycol 6000 mixture, perhaps with sodium stearate, perhaps the weight ratio with glycerin gelatine is 1: 2～4.
2. a kind of bupleurum root dropping pills according to claim 1 is characterized in that Radix Bupleuri extractum and Macrogol 4000 and polyethylene glycol 6000 weight ratio are 1: 2.5～3.5.
3. a kind of bupleurum root dropping pills according to claim 1, the weight ratio that it is characterized in that described Macrogol 4000 and polyethylene glycol 6000 is 1: 0.5～1.5.
4. a kind of bupleurum root dropping pills according to claim 1, the weight ratio that it is characterized in that described Macrogol 4000 and polyethylene glycol 6000 is 1: 1.
5. a kind of bupleurum root dropping pills according to claim 1 is characterized in that Radix Bupleuri and Macrogol 4000 and polyethylene glycol 6000 mixture weight ratio are 1: 3, and wherein the weight ratio of Macrogol 4000 and polyethylene glycol 6000 is 1: 1 in the mixture.
6. the preparation method of the described drop pill of claim 1 comprises the following steps:
A. get the Radix Bupleuri medical material, add water reflux, extract, twice, merge extractive liquid,, concentrated, add ethanol precipitation, filter, concentrate and reclaim ethanol, get Radix Bupleuri extractum.Through suitably being processed into extractum;
B. with behind above-mentioned extractum and the suitable adjuvant mix homogeneously, add the transconversion into heat material;
The extractum that c. will mix adjuvant moves into the dropping-pill machine jar, splashes in the cryogenic liquid paraffin, removes liquid paraffin, selects ball, promptly.
7. the preparation method of claim 6, wherein for the first time extracting amount of water among the step a is 4～6 times, and be 1～3 hour heat time heating time, and amount of water is 2～3 times for the second time, and be 0.5～1.5 hour heat time heating time; Concentrated extracting solution is 1: 1～0.6 to the crude drug amount with the extracting liquid volume ratio, and ethanol precipitation is 50～90% to containing the alcohol amount, and reclaiming ethanol to relative density is 1.3～1.4.
8. claim 6 or 7 preparation method, wherein amount of water is 5 times for the first time, and be 2 hours heat time heating time, and amount of water is 2.5 times for the second time, and be 1 hour heat time heating time; Concentrated extracting solution to crude drug amount is 1: 0.8 with the extracting liquid volume ratio; Ethanol precipitation is 70% to containing the alcohol amount, and reclaiming ethanol to relative density is 1.3～1.4.
9. the preparation method of claim 6, wherein the adjuvant among the step b is a Macrogol 4000, perhaps polyethylene glycol 6000, perhaps Macrogol 4000 and polyethylene glycol 6000 mixture, perhaps sodium stearate, perhaps glycerin gelatine; The weight ratio of extractum and adjuvant is 1: 2～4.
10. claim 6 or 9 preparation method, wherein adjuvant is a polyethylene glycol 6000; The weight ratio of extractum and adjuvant is 1: 3.
11. according to the preparation method of claim 6, wherein the change material temperature among the step c is 85～95 ℃; Dripping the system temperature is 70～80 ℃; Low 10 ℃ of liquid paraffin temperature.
12. according to the preparation method of claim 6 or 11, change material temperature wherein is 90 ℃; Dripping the system temperature is 75 ℃; The liquid paraffin temperature is lower than 10 ℃.
13. preparation method according to claim 6 comprises the following steps:
A. get Radix Bupleuri, add water and reflux 2 times, add the water of 5 times of amounts for the first time, reflux 2 hours; The water that adds for the second time 2.5 times of amounts, reflux 1 hour, merge extractive liquid,, the ratio that is concentrated into crude drug and extracting liquid volume is 1: 0.8, adds 95% ethanol precipitation and makes and contain the alcohol amount to 70%, leaves standstill, filter, concentrating and reclaiming ethanol to relative density is 1.35, gets Radix Bupleuri extractum;
B. get above-mentioned Radix Bupleuri extractum and mix with polyethylene glycol 6000, ratio is 1: 3;
C. the preparation of product: get above-mentioned Radix Bupleuri extractum and polyethylene glycol 6000 and be heated to 90 ℃, the drip irrigation that moves into the drop pill machine remains on 70 ℃, drips to 8 ℃ liquid paraffin, takes out drop pill, removes liquid paraffin, selects ball, promptly.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNB2004100198269A CN100430045C (en) | 2004-06-30 | 2004-06-30 | Radix bupleuri dripping pill and its preparing method |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNB2004100198269A CN100430045C (en) | 2004-06-30 | 2004-06-30 | Radix bupleuri dripping pill and its preparing method |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN1714811A true CN1714811A (en) | 2006-01-04 |
| CN100430045C CN100430045C (en) | 2008-11-05 |
Family
ID=35821170
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CNB2004100198269A Active CN100430045C (en) | 2004-06-30 | 2004-06-30 | Radix bupleuri dripping pill and its preparing method |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN100430045C (en) |
Cited By (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101015575B (en) * | 2006-02-08 | 2011-10-05 | 天津天士力制药股份有限公司 | Process for preparing bupleurum root dropping pills |
| CN102631386A (en) * | 2012-05-10 | 2012-08-15 | 四川德培源中药科技开发有限公司 | Bupleurum antipyretic and analgesic preparation and technology for preparing same |
| CN103364496A (en) * | 2012-04-09 | 2013-10-23 | 天士力制药集团股份有限公司 | Method for simultaneously measuring content of four types of saikoside in bupleurum extract |
| CN104840496A (en) * | 2014-02-17 | 2015-08-19 | 天士力制药集团股份有限公司 | Radix bupleuri dripping pills and preparation method thereof |
| CN101810654B (en) * | 2009-02-24 | 2015-12-16 | 上海医药工业研究院 | Vinegar-prepared radix bupleuri solvent extract is preparing the application in anticholesteremic agent |
| CN109745348A (en) * | 2019-03-04 | 2019-05-14 | 河南福森药业有限公司 | A kind of preparation method of bupleurum formulation particle |
Family Cites Families (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1436554A (en) * | 2002-02-08 | 2003-08-20 | 上海华拓医药科技发展有限公司 | Bupleurum-skullcap dripping pills |
-
2004
- 2004-06-30 CN CNB2004100198269A patent/CN100430045C/en active Active
Cited By (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101015575B (en) * | 2006-02-08 | 2011-10-05 | 天津天士力制药股份有限公司 | Process for preparing bupleurum root dropping pills |
| CN101810654B (en) * | 2009-02-24 | 2015-12-16 | 上海医药工业研究院 | Vinegar-prepared radix bupleuri solvent extract is preparing the application in anticholesteremic agent |
| CN103364496A (en) * | 2012-04-09 | 2013-10-23 | 天士力制药集团股份有限公司 | Method for simultaneously measuring content of four types of saikoside in bupleurum extract |
| CN103364496B (en) * | 2012-04-09 | 2016-07-06 | 天士力制药集团股份有限公司 | Measure the method for four kinds of saikoside content in Radix Bupleuri extractum simultaneously |
| CN102631386A (en) * | 2012-05-10 | 2012-08-15 | 四川德培源中药科技开发有限公司 | Bupleurum antipyretic and analgesic preparation and technology for preparing same |
| CN104840496A (en) * | 2014-02-17 | 2015-08-19 | 天士力制药集团股份有限公司 | Radix bupleuri dripping pills and preparation method thereof |
| CN104840496B (en) * | 2014-02-17 | 2019-03-22 | 天士力医药集团股份有限公司 | A kind of bupleurum root dropping pills and preparation method thereof |
| CN109745348A (en) * | 2019-03-04 | 2019-05-14 | 河南福森药业有限公司 | A kind of preparation method of bupleurum formulation particle |
Also Published As
| Publication number | Publication date |
|---|---|
| CN100430045C (en) | 2008-11-05 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| CN1840166A (en) | Modern Chinese medicinal oral liquid of 'Wen Dan Tang' and preparation method thereof | |
| CN1857562A (en) | Kidney invigorating hair restorer preparation its preparing process | |
| CN1857654A (en) | Trachaitis treating preparation and its preparing process | |
| CN1775276A (en) | Fushu Preparation and new preparing method | |
| CN1883638A (en) | Compound medicine for treating depression and method for preparing same | |
| CN1748783A (en) | Dismenorrhea preparation and new preparing method | |
| CN1714811A (en) | Radix bupleuri dripping pill and its preparing method | |
| CN1775279A (en) | Gynaecologic formulation and new preparing method | |
| CN1628662A (en) | Medicine with abirritation | |
| CN100341540C (en) | Angelica root mistletoe granules and its preparation method | |
| CN1748748A (en) | Little leaf deervetch herb preparation for pregnant woman and new preparing method | |
| CN100344315C (en) | Medicinal composition for promoting bone fracture healing and its preparing method | |
| CN1850264A (en) | Safflower preparation for treating wound and new preparing method | |
| CN1282470C (en) | Traditional Chinese medicine for anti depression | |
| CN1616060A (en) | Chinese medicine drippling pill preparation for promoting blood circulation and removing blood stasis, promoting Qi circulation and rilieving pain | |
| CN1660259A (en) | Chinese traditional medicine for treating imitable bowel syndrome and preparation method | |
| CN1640436A (en) | Chinese medicine composition for treating menstrual period syndrome | |
| CN1943694A (en) | A Chinese traditional medicinal composition for treating renal deficiency, edema, lumbago and gonalgia, etc. | |
| CN1650895A (en) | Method of extracting medicamout having memory strengthening function from natural plant compound preparation | |
| CN1772122A (en) | Indian stringbush prepn with antiphlogistic and detoxicating functions | |
| CN1824113A (en) | Postpartum laonurus medicinal preparation and its new preparation method | |
| CN1824241A (en) | Medicinal preparation and its new preparation method | |
| CN1748741A (en) | Little leaf deervetch herb acne removing preparation and new preparing method | |
| CN1709329A (en) | Composition for treating female algomenorrhea and its preparing method | |
| CN1651017A (en) | Medicinal composition for treating cervical vertebra disease and its preparation method |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| C14 | Grant of patent or utility model | ||
| GR01 | Patent grant | ||
| EE01 | Entry into force of recordation of patent licensing contract |
Assignee: Tianjin Tasly Modern Chinese Medicine Resource Co., Ltd. Assignor: Tianjin Tianshili Pharmaceutical Co., Ltd. Contract record no.: 2011120000159 Denomination of invention: Radix bupleuri dripping pill and its preparing method Granted publication date: 20081105 License type: Exclusive License Open date: 20060104 Record date: 20110824 |
|
| C56 | Change in the name or address of the patentee |
Owner name: TASLY PHARMACEUTICAL GROUP CO., LTD. Free format text: FORMER NAME: TIANJIN TASLY PHARMACEUTICAL CO., LTD. |
|
| CP01 | Change in the name or title of a patent holder |
Address after: 300402, No. 1, Liaohe East Road, Beichen Science Park, Beichen District, Tianjin Patentee after: Tasly Pharmaceutical Group Co., Ltd. Address before: 300402, No. 1, Liaohe East Road, Beichen Science Park, Beichen District, Tianjin Patentee before: Tianjin Tianshili Pharmaceutical Co., Ltd. |
|
| CP01 | Change in the name or title of a patent holder | ||
| CP01 | Change in the name or title of a patent holder |
Address after: 300402, No. 1, Liaohe East Road, Beichen Science Park, Beichen District, Tianjin Patentee after: Tasly Pharmaceutical Group Limited by Share Ltd Address before: 300402, No. 1, Liaohe East Road, Beichen Science Park, Beichen District, Tianjin Patentee before: Tasly Pharmaceutical Group Co., Ltd. |