CN101269007A - Dosage form containing levorotation gossypol as active component - Google Patents
Dosage form containing levorotation gossypol as active component Download PDFInfo
- Publication number
- CN101269007A CN101269007A CNA2008100181552A CN200810018155A CN101269007A CN 101269007 A CN101269007 A CN 101269007A CN A2008100181552 A CNA2008100181552 A CN A2008100181552A CN 200810018155 A CN200810018155 A CN 200810018155A CN 101269007 A CN101269007 A CN 101269007A
- Authority
- CN
- China
- Prior art keywords
- vitamin
- levorotation gossypol
- active component
- gossypol
- capsule
- 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.)
- Pending
Links
- QBKSWRVVCFFDOT-UHFFFAOYSA-N gossypol Chemical compound CC(C)C1=C(O)C(O)=C(C=O)C2=C(O)C(C=3C(O)=C4C(C=O)=C(O)C(O)=C(C4=CC=3C)C(C)C)=C(C)C=C21 QBKSWRVVCFFDOT-UHFFFAOYSA-N 0.000 title claims abstract description 130
- QHOPXUFELLHKAS-UHFFFAOYSA-N Thespesin Natural products CC(C)c1c(O)c(O)c2C(O)Oc3c(c(C)cc1c23)-c1c2OC(O)c3c(O)c(O)c(C(C)C)c(cc1C)c23 QHOPXUFELLHKAS-UHFFFAOYSA-N 0.000 title claims abstract description 65
- 229930000755 gossypol Natural products 0.000 title claims abstract description 65
- 229950005277 gossypol Drugs 0.000 title claims abstract description 65
- 239000002552 dosage form Substances 0.000 title claims description 8
- WCUXLLCKKVVCTQ-UHFFFAOYSA-M Potassium chloride Chemical compound [Cl-].[K+] WCUXLLCKKVVCTQ-UHFFFAOYSA-M 0.000 claims abstract description 46
- 239000001103 potassium chloride Substances 0.000 claims abstract description 23
- 235000011164 potassium chloride Nutrition 0.000 claims abstract description 23
- 239000003814 drug Substances 0.000 claims abstract description 17
- 238000002347 injection Methods 0.000 claims abstract description 9
- 239000007924 injection Substances 0.000 claims abstract description 9
- 229960002816 potassium chloride Drugs 0.000 claims abstract description 4
- 229930003270 Vitamin B Natural products 0.000 claims description 42
- 239000011720 vitamin B Substances 0.000 claims description 42
- 235000019156 vitamin B Nutrition 0.000 claims description 42
- 239000002775 capsule Substances 0.000 claims description 18
- 239000008187 granular material Substances 0.000 claims description 17
- 239000003826 tablet Substances 0.000 claims description 14
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 8
- 239000000843 powder Substances 0.000 claims description 8
- 239000007788 liquid Substances 0.000 claims description 6
- 239000002994 raw material Substances 0.000 claims description 6
- 239000007901 soft capsule Substances 0.000 claims description 6
- 239000007919 dispersible tablet Substances 0.000 claims description 5
- 239000006187 pill Substances 0.000 claims description 4
- JZRWCGZRTZMZEH-UHFFFAOYSA-N thiamine Chemical compound CC1=C(CCO)SC=[N+]1CC1=CN=C(C)N=C1N JZRWCGZRTZMZEH-UHFFFAOYSA-N 0.000 claims description 4
- 239000003795 chemical substances by application Substances 0.000 claims description 3
- 239000007902 hard capsule Substances 0.000 claims description 2
- 238000004519 manufacturing process Methods 0.000 claims description 2
- 230000003213 activating effect Effects 0.000 claims 1
- 230000002421 anti-septic effect Effects 0.000 claims 1
- 150000002500 ions Chemical class 0.000 claims 1
- 238000011287 therapeutic dose Methods 0.000 claims 1
- 238000002360 preparation method Methods 0.000 abstract description 20
- 150000001875 compounds Chemical class 0.000 abstract description 7
- 239000000825 pharmaceutical preparation Substances 0.000 abstract description 2
- LXNHXLLTXMVWPM-UHFFFAOYSA-N pyridoxine Chemical compound CC1=NC=C(CO)C(CO)=C1O LXNHXLLTXMVWPM-UHFFFAOYSA-N 0.000 abstract 2
- 229930003451 Vitamin B1 Natural products 0.000 abstract 1
- 239000004480 active ingredient Substances 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- RADKZDMFGJYCBB-UHFFFAOYSA-N pyridoxal hydrochloride Natural products CC1=NC=C(CO)C(C=O)=C1O RADKZDMFGJYCBB-UHFFFAOYSA-N 0.000 abstract 1
- 239000007787 solid Substances 0.000 abstract 1
- 229960003495 thiamine Drugs 0.000 abstract 1
- DPJRMOMPQZCRJU-UHFFFAOYSA-M thiamine hydrochloride Chemical compound Cl.[Cl-].CC1=C(CCO)SC=[N+]1CC1=CN=C(C)N=C1N DPJRMOMPQZCRJU-UHFFFAOYSA-M 0.000 abstract 1
- 235000010374 vitamin B1 Nutrition 0.000 abstract 1
- 239000011691 vitamin B1 Substances 0.000 abstract 1
- 235000019158 vitamin B6 Nutrition 0.000 abstract 1
- 239000011726 vitamin B6 Substances 0.000 abstract 1
- 229940011671 vitamin b6 Drugs 0.000 abstract 1
- 239000000203 mixture Substances 0.000 description 19
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 description 16
- 238000001035 drying Methods 0.000 description 9
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 8
- 235000019359 magnesium stearate Nutrition 0.000 description 8
- 229920000159 gelatin Polymers 0.000 description 7
- 235000019322 gelatine Nutrition 0.000 description 7
- 108010010803 Gelatin Proteins 0.000 description 6
- 239000008273 gelatin Substances 0.000 description 6
- 235000011852 gelatine desserts Nutrition 0.000 description 6
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 6
- 239000004375 Dextrin Substances 0.000 description 5
- 229920001353 Dextrin Polymers 0.000 description 5
- 229920002472 Starch Polymers 0.000 description 5
- 235000019425 dextrin Nutrition 0.000 description 5
- 238000012856 packing Methods 0.000 description 5
- 239000008107 starch Substances 0.000 description 5
- 235000019698 starch Nutrition 0.000 description 5
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 description 4
- 229930006000 Sucrose Natural products 0.000 description 4
- CZMRCDWAGMRECN-UGDNZRGBSA-N Sucrose Chemical compound O[C@H]1[C@H](O)[C@@H](CO)O[C@@]1(CO)O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 CZMRCDWAGMRECN-UGDNZRGBSA-N 0.000 description 4
- 206010046798 Uterine leiomyoma Diseases 0.000 description 4
- 230000000694 effects Effects 0.000 description 4
- 238000005516 engineering process Methods 0.000 description 4
- 238000005469 granulation Methods 0.000 description 4
- 230000003179 granulation Effects 0.000 description 4
- 238000004806 packaging method and process Methods 0.000 description 4
- GEHJYWRUCIMESM-UHFFFAOYSA-L sodium sulfite Chemical compound [Na+].[Na+].[O-]S([O-])=O GEHJYWRUCIMESM-UHFFFAOYSA-L 0.000 description 4
- 239000005720 sucrose Substances 0.000 description 4
- 229920000623 Cellulose acetate phthalate Polymers 0.000 description 3
- 201000009273 Endometriosis Diseases 0.000 description 3
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 3
- -1 and drying Substances 0.000 description 3
- 229940081734 cellulose acetate phthalate Drugs 0.000 description 3
- 229940079593 drug Drugs 0.000 description 3
- 239000003292 glue Substances 0.000 description 3
- 235000011187 glycerol Nutrition 0.000 description 3
- 229940057995 liquid paraffin Drugs 0.000 description 3
- 239000000314 lubricant Substances 0.000 description 3
- 229920000036 polyvinylpyrrolidone Polymers 0.000 description 3
- 239000001267 polyvinylpyrrolidone Substances 0.000 description 3
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 description 3
- 230000006340 racemization Effects 0.000 description 3
- 239000000243 solution Substances 0.000 description 3
- IXPNQXFRVYWDDI-UHFFFAOYSA-N 1-methyl-2,4-dioxo-1,3-diazinane-5-carboximidamide Chemical compound CN1CC(C(N)=N)C(=O)NC1=O IXPNQXFRVYWDDI-UHFFFAOYSA-N 0.000 description 2
- IIZPXYDJLKNOIY-JXPKJXOSSA-N 1-palmitoyl-2-arachidonoyl-sn-glycero-3-phosphocholine Chemical compound CCCCCCCCCCCCCCCC(=O)OC[C@H](COP([O-])(=O)OCC[N+](C)(C)C)OC(=O)CCC\C=C/C\C=C/C\C=C/C\C=C/CCCCC IIZPXYDJLKNOIY-JXPKJXOSSA-N 0.000 description 2
- CSCPPACGZOOCGX-UHFFFAOYSA-N Acetone Chemical compound CC(C)=O CSCPPACGZOOCGX-UHFFFAOYSA-N 0.000 description 2
- 229920001661 Chitosan Polymers 0.000 description 2
- 206010013786 Dry skin Diseases 0.000 description 2
- 206010013908 Dysfunctional uterine bleeding Diseases 0.000 description 2
- GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 description 2
- 229920001214 Polysorbate 60 Polymers 0.000 description 2
- 239000002671 adjuvant Substances 0.000 description 2
- 238000007664 blowing Methods 0.000 description 2
- MTHSVFCYNBDYFN-UHFFFAOYSA-N diethylene glycol Chemical compound OCCOCCO MTHSVFCYNBDYFN-UHFFFAOYSA-N 0.000 description 2
- 239000003995 emulsifying agent Substances 0.000 description 2
- 238000002474 experimental method Methods 0.000 description 2
- 239000008101 lactose Substances 0.000 description 2
- 235000010445 lecithin Nutrition 0.000 description 2
- 239000000787 lecithin Substances 0.000 description 2
- 229940067606 lecithin Drugs 0.000 description 2
- 229940031703 low substituted hydroxypropyl cellulose Drugs 0.000 description 2
- 210000004914 menses Anatomy 0.000 description 2
- 238000000034 method Methods 0.000 description 2
- 238000002156 mixing Methods 0.000 description 2
- 239000001253 polyvinylpolypyrrolidone Substances 0.000 description 2
- 235000013809 polyvinylpolypyrrolidone Nutrition 0.000 description 2
- 229920000523 polyvinylpolypyrrolidone Polymers 0.000 description 2
- 238000009702 powder compression Methods 0.000 description 2
- 239000000377 silicon dioxide Substances 0.000 description 2
- 235000012239 silicon dioxide Nutrition 0.000 description 2
- 235000010413 sodium alginate Nutrition 0.000 description 2
- 239000000661 sodium alginate Substances 0.000 description 2
- 229940005550 sodium alginate Drugs 0.000 description 2
- 239000001509 sodium citrate Substances 0.000 description 2
- NLJMYIDDQXHKNR-UHFFFAOYSA-K sodium citrate Chemical compound O.O.[Na+].[Na+].[Na+].[O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O NLJMYIDDQXHKNR-UHFFFAOYSA-K 0.000 description 2
- 235000010265 sodium sulphite Nutrition 0.000 description 2
- 239000007779 soft material Substances 0.000 description 2
- 239000002904 solvent Substances 0.000 description 2
- 239000007921 spray Substances 0.000 description 2
- 239000000725 suspension Substances 0.000 description 2
- 239000006188 syrup Substances 0.000 description 2
- 235000020357 syrup Nutrition 0.000 description 2
- 208000005641 Adenomyosis Diseases 0.000 description 1
- 239000001828 Gelatine Substances 0.000 description 1
- 239000008118 PEG 6000 Substances 0.000 description 1
- 229920001030 Polyethylene Glycol 4000 Polymers 0.000 description 1
- 229920002584 Polyethylene Glycol 6000 Polymers 0.000 description 1
- 229920002494 Zein Polymers 0.000 description 1
- DPXJVFZANSGRMM-UHFFFAOYSA-N acetic acid;2,3,4,5,6-pentahydroxyhexanal;sodium Chemical compound [Na].CC(O)=O.OCC(O)C(O)C(O)C(O)C=O DPXJVFZANSGRMM-UHFFFAOYSA-N 0.000 description 1
- 230000003509 anti-fertility effect Effects 0.000 description 1
- 230000002513 anti-ovulatory effect Effects 0.000 description 1
- 238000003556 assay Methods 0.000 description 1
- 239000001768 carboxy methyl cellulose Substances 0.000 description 1
- 239000003093 cationic surfactant Substances 0.000 description 1
- 239000011248 coating agent Substances 0.000 description 1
- 238000000576 coating method Methods 0.000 description 1
- 229940000425 combination drug Drugs 0.000 description 1
- 238000013270 controlled release Methods 0.000 description 1
- 238000002651 drug therapy Methods 0.000 description 1
- 239000000839 emulsion Substances 0.000 description 1
- IDGUHHHQCWSQLU-UHFFFAOYSA-N ethanol;hydrate Chemical compound O.CCO IDGUHHHQCWSQLU-UHFFFAOYSA-N 0.000 description 1
- 239000004744 fabric Substances 0.000 description 1
- 239000012530 fluid Substances 0.000 description 1
- 239000006260 foam Substances 0.000 description 1
- 238000009472 formulation Methods 0.000 description 1
- 238000005194 fractionation Methods 0.000 description 1
- 239000002828 fuel tank Substances 0.000 description 1
- 210000001035 gastrointestinal tract Anatomy 0.000 description 1
- 239000007903 gelatin capsule Substances 0.000 description 1
- 238000005213 imbibition Methods 0.000 description 1
- 238000007689 inspection Methods 0.000 description 1
- 238000010255 intramuscular injection Methods 0.000 description 1
- 239000007927 intramuscular injection Substances 0.000 description 1
- 238000010253 intravenous injection Methods 0.000 description 1
- 210000001630 jejunum Anatomy 0.000 description 1
- 239000000463 material Substances 0.000 description 1
- 239000011812 mixed powder Substances 0.000 description 1
- 230000003287 optical effect Effects 0.000 description 1
- 230000000144 pharmacologic effect Effects 0.000 description 1
- 238000005498 polishing Methods 0.000 description 1
- 229920006316 polyvinylpyrrolidine Polymers 0.000 description 1
- 238000007789 sealing Methods 0.000 description 1
- 238000007086 side reaction Methods 0.000 description 1
- 239000002002 slurry Substances 0.000 description 1
- 235000019812 sodium carboxymethyl cellulose Nutrition 0.000 description 1
- 229920001027 sodium carboxymethylcellulose Polymers 0.000 description 1
- 238000005507 spraying Methods 0.000 description 1
- 238000003756 stirring Methods 0.000 description 1
- 230000002459 sustained effect Effects 0.000 description 1
- 238000013268 sustained release Methods 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
- 231100000027 toxicology Toxicity 0.000 description 1
- 235000015112 vegetable and seed oil Nutrition 0.000 description 1
- 239000008158 vegetable oil Substances 0.000 description 1
- 238000005406 washing Methods 0.000 description 1
- 239000000080 wetting agent Substances 0.000 description 1
- 239000005019 zein Substances 0.000 description 1
- 229940093612 zein Drugs 0.000 description 1
Landscapes
- Medicinal Preparation (AREA)
Abstract
The invention relates to a pharmaceutical preparation taking levorotatory gossypol as active ingredient, in particular to a compound preparation which contains the medicine such as levorotatory gossypol, potassium chloride, vitamin B1 and vitamin B6, etc. and is used for curing gynecological disease. The compound preparation comprises an oral solid preparation and an injection.
Description
Technical field
The invention belongs to medical technical field, relating to the levorotation gossypol is the medicine of active component, particularly a kind of levorotation gossypol, potassium chloride, vitamin B of containing
1, vitamin B
6Etc. the combination drug of Drug therapy gynaecopathia, be made into capsule or oral liquid or tablet or powder or pill or granule or injection.
Background technology
Gossypol is confirmed clinically as men's birth control medicine, and is also confirmed by a large amount of pharmacological toxicologies and clinical experiment as treatment gynaecopathia such as hysteromyoma, endometriosis etc.Chinese scholar Huang Liang etc. at first finish the fractionation work of racemization gossypol.Prove that now levo form is effective optical isomer of oral antifertility, and d-isomer is invalid.Show through animal experiment: levorotation gossypol treatment gynaecopathia curative effect is 2 times of racemization gossypol, especially for treatment dysfunctional uterine hemorrhage, hysteromyoma bimonthly menses through too much, endometriosis etc., have good effect, and side effect is few than the racemization gossypol.
Summary of the invention
The object of the present invention is to provide a kind of is the drug agents of active component with the levorotation gossypol, be used for the treatment of gynaecopathia such as anovulatory dysfunctional uterine hemorrhage, hysteromyoma bimonthly menses through too much reaching treating adenomyosis uteri, this preparation had both had better therapeutic effect, can reduce side effect again, and different dosage forms can satisfy different patient's medication requirements.
Characteristics of the present invention: this kind medicament can be used for gynaecopathia, as hysteromyoma, endometriosis etc., mainly be active component with the levorotation gossypol, or levorotation gossypol is equipped with potassium chloride, vitamin B
1, vitamin B
6Wait other composition, adopt excipient or pharmaceutic adjuvant to make a kind of pharmaceutical preparation and use for oral or injection.Add vitamin B
1, vitamin B
6To alleviate the side reaction of gastrointestinal tract etc., improved the compliance that the patient takes simultaneously, make things convenient for patient's medication, increase bioavailability, be equipped with suitable adjuvant to it, make capsule or enteric coated capsule or soft capsule or sustained and controlled release capsule or oral liquid or dispersible tablet or enteric coatel tablets or powder or pill or granule or injection.
The invention process is as follows:
The present invention is the medicament of active component with the levorotation gossypol, is to be that the raw material prescription of weight portion forms by following consumption.
Levorotation gossypol 1-30 potassium chloride 30-350
Vitamin B
1The 1-20 vitamin B
61-20
The present invention is the medicament of active component with the levorotation gossypol, mainly is made up of left-handed (-) gossypol and excipient or pharmaceutic adjuvant.
Wherein be that the dosage form of active component comprises that hard capsule, enteric coated capsule, soft capsule, slow (control) release capsule, powder, pill, oral liquid, dispersible tablet, enteric coatel tablets, delay (control) and release sheet, granule, injection with the levorotation gossypol.It is specific as follows:
With the levorotation gossypol is the capsule of active component, is by levorotation gossypol 1-30, potassium chloride 30-350, vitamin B
11-20, vitamin B
61-20 adds dextrin and starch, mix homogeneously, and granulation, dry, granulate divide the softgel shell of packing into, make capsule or enteric coated capsule; Or add adjuvants such as gelatin, glycerol, and according to preparation soft capsule technology, with emulsifying agent raw materials such as levorotation gossypol are made to drip behind the suspension and make to gelatin solution, make soft capsule; Or add slow releasing agent such as polyvinylpyrrolidone, and raw materials such as levorotation gossypol are made slow-releasing granules, the capsulae vacuus of packing into is then made slow releasing capsule.
With the levorotation gossypol is the powder of active component, and its raw material is by levorotation gossypol 1-30, potassium chloride 30-350, vitamin B
11-20, vitamin B
6The 1-20 weight portion is formed, sub-dose packaging gained behind adding sucrose, the magnesium stearate mix homogeneously.
With the levorotation gossypol is the oral liquid of active component, is by levorotation gossypol 1-30, potassium chloride 30-350, vitamin B
11-20, vitamin B
6The 1-20 weight portion is formed, and adds mix homogeneously such as sodium citrate and syrup again, adds water to 1000ml, and packing forms.
With the levorotation gossypol is the tablet of active component, is by levorotation gossypol 1-30, potassium chloride 30-350, vitamin B
11-20, vitamin B
6The 1-20 weight portion is formed, and adds dextrin and starch or lactose etc., mix homogeneously, granulation, drying, tabletting, coating; Or add low-substituted hydroxypropyl cellulose, the swollen shallow lake P5000 of dimension, polyvinylpolypyrrolidone INF-10, PEG6000, PEG4000, colloidality silicon dioxide, magnesium stearate etc., and cross 100 mesh sieves, mix homogeneously, direct powder compression are made dispersible tablet; Or add cellulose acetate-phthalate (CAP), magnesium stearate and polyvinylpyrrolidone etc., according to tablet manufacturing technology, make enteric coatel tablets; Or with chitosan and sodium alginate mixed, add the mix homogeneously that sieves behind the medicine (mixture is 0.2: 1 with the ratio of medicine) by 2: 3, the system soft material is granulated, dry, granulate, add moderate lubrication agent magnesium stearate mixing after tabletting make slow releasing tablet.
With the levorotation gossypol is the granule of active component, is by levorotation gossypol 1-30, potassium chloride 30-350, vitamin B
11-20, vitamin B
6The 1-20 weight portion is formed, and adds sucrose, dextrin or other excipient, granulate, and drying, granulate, sub-dose packaging is made.
With the levorotation gossypol is the injection of active component, is by levorotation gossypol 1-30, potassium chloride 30-350, vitamin B
11-20, vitamin B
6The 1-20 weight portion is formed, and adds polyoxyethylene sorbitan monoleate, lecithin, sodium sulfite, cationic surfactant etc., makes according to process for preparation of injection.
The preparation of different dosage form among the present invention can provide different preparation formulations at different suitable crowds, satisfying patient's needs, improves patient's compliance of taking medicine.The specific embodiment:
1, with the levorotation gossypol is the preparation method of the capsule of active component
(1) preparation prescription of capsule or enteric coated capsule
Levorotation gossypol 10g potassium chloride 250g vitamin B
110g
Vitamin B
610g starch 54.4g dextrin 37.8g
Make 1000 altogether
Every contains levorotation gossypol 10mg
With compound medicine mix homogeneously such as above-mentioned levorotation gossypols, granulation, dry, granulate after the assay was approved, divide in pack into capsulae vacuus or the jejunum colloidal sol capsule, promptly according to prescription.
(2) with the levorotation gossypol be the preparation of soft capsule prescription of active component
Levorotation gossypol 10g potassium chloride 250g
Vitamin B
1The 10g vitamin B
610g
Gelatin solution prescription gelatin 100g water 130g
Get an amount of water of gelatin adding and make its imbibition.In addition the water of glycerol and remainder is put and be heated to 70～80 ℃ in the glue pot, mix homogeneously adds expansible gelatin and stirs, and makes it to be melt into uniform glue, is incubated 1～2 hour and leaves standstill, and removes the foam of come-up, filters with cloth bag.Make viscosity and be 2.8～3.2 glue.With levorotation gossypol, potassium chloride, vitamin B
1, vitamin B
6With water or vegetable oil is solvent, and the adding emulsifying agent is made suspension type Emulsion and put into fuel tank, with the glycerin gelatine that has made, puts in the appropriate vessel and is incubated about 60 ℃, and the temperature of liquid paraffin is advisable with 13～17 ℃.20 ℃ of room temperatures are dripped (spray) head place and be should be about 50 ℃.The soft gelatin capsule that oozes is evenly spread out on gauze,, insert and remove surface liquid paraffin more than 4 hours in the blowing of low temperature below 10 ℃, took out in 20 hours 10 ℃ of low temperature blowings again, use ethanol: the mixed liquor flush away surface liquid paraffin of acetone (5: 1), again about 24 hours of 40～50 ℃ of dryings.Drying, lamp inspection are used 95% washing with alcohol, dry up under 40～50 ℃, promptly again.
(3) be that capsular preparation method is released in slow (control) of active component with the levorotation gossypol
Get levorotation gossypol 10g, potassium chloride 250g, vitamin B
110g, vitamin B
610g compound recipe raw material and sucrose fine are even with 1: 9 mixed, use 2% (g/ml) polyvinylpyrrolidine (K-30) pelletize then, (rotating speed is 23r/min by extruder, sieve aperture is 0.8～1.2mm) to extrude, material (rotating speed is 950r/min) in spheronizator grinds and rolled 5 minutes, the wet ball of balling-up is in 50 ℃ of dryings 4 hours, the capsulae vacuus of packing into, promptly.
2, with the levorotation gossypol be the preparation method of active component
With levorotation gossypol 10g, potassium chloride 250g, vitamin B
110g, vitamin B
610g, sub-dose packaging gets compound recipe levorotation gossypol powder behind adding sucrose, the magnesium stearate mix homogeneously.
3, with the levorotation gossypol be the preparation method of the oral liquid of active component
With levorotation gossypol 10g, potassium chloride 250g, vitamin B
110g, vitamin B
610g and sodium citrate 0.07g, sodium carboxymethyl cellulose 0.15g and syrup 20g mix homogeneously add water to 1000ml, and packing forms.
4, with the levorotation gossypol be the preparation of the tablet of active component
(1) with the levorotation gossypol is the preparation method of the dispersible tablet of active component
Low-substituted hydroxypropyl cellulose is crossed 100 mesh sieves, with levorotation gossypol 10g, potassium chloride 250g, vitamin B
110g, vitamin B
610g, the swollen shallow lake P5000 780g of dimension, polyvinylpolypyrrolidone INF-10 600g mix homogeneously are colloidality silicon dioxide, magnesium stearate and above-mentioned mixed powder mix homogeneously, direct powder compression then.
(2) with the levorotation gossypol be the preparation method of the enteric coatel tablets of active component
With levorotation gossypol 10g, potassium chloride 250g, vitamin B
110g, vitamin B
6The lactose mix homogeneously of 10g and 100g, the starch slurry of adding 100g 10% adopts spray granulation technology of fluid bed to granulate, and adds magnesium stearate lubricant 8g and polyvinylpyrrolidone 8g mix homogeneously again, tabletting.Earlier label is screened out fine powder and broken mashed sheet, hang one deck sub-coat, wrap the zein sealing coat again 1-2 time, hang sub-coat number layer again, accomplish thin layer repeatedly, drying is evened up layer by layer.Hang cellulose acetate-phthalate solution, behind the intermittent spraying drying and forming-film, detect, qualified after, continue to hang sub-coat again to stipulating that sheet is heavy, the icing layer, polishing, drying, finished product.
(3) with the levorotation gossypol be the preparation method that (control) releases sheet of delaying of active component
With chitosan and sodium alginate mixed, add levorotation gossypol 10g, potassium chloride 250g, vitamin B by 2: 3
110g, vitamin B
6The mix homogeneously that sieves behind the compound medicine of 10g (mixture is 0.2: 1 with the ratio of compound medicine) is a wetting agent system soft material with 30% ethanol water, crosses 16 mesh sieve system wet granulars, and 50-55 ℃ of dry back granulate adds tabletting behind the moderate lubrication agent magnesium stearate mixing.
5, with the levorotation gossypol be the preparation of the granule of active component
Get levorotation gossypol 10g, potassium chloride 250g, vitamin B
110g, vitamin B
610g adds starch, dextrin, granulates, and drying, granulate, sub-dose packaging is made granule.
6, the preparation of levorotation gossypol compound injection
Get levorotation gossypol 10g, potassium chloride 250g, vitamin B
110g, vitamin B
610g makes injectable sterile powder, faces with preceding and uses with appropriate solvent dissolving or suspendible; Or add polyoxyethylene sorbitan monoleate, lecithin, sodium sulfite etc., make intramuscular injection or intravenous injection.
Claims (6)
1, a kind of is the pharmaceutical dosage form of active component with the levorotation gossypol, it is characterized in that: it is with levorotation gossypol or levorotation gossypol, potassium chloride, vitamin B
1, vitamin B
6Be the dosage form of primary raw material, comprise levorotation gossypol and the pharmaceutically acceptable excipient and the pharmaceutic adjuvant of effective therapeutic dose.
2, as claimed in claim 1 is the medicament of active component with the levorotation gossypol, it is characterized in that by following consumption being that the feedstock production of weight portion forms:
Levorotation gossypol 1-30 potassium chloride 30-350
Vitamin B
1The 1-20 vitamin B
61-20
3, as claimed in claim 1 is the medicament of active component with the levorotation gossypol, and its dosage form comprises capsule, powder, pill, oral liquid, tablet, granule, injection.
4. pharmaceutic adjuvant as claimed in claim 1 comprises that correctives, antiseptic, ion and nonionic show activating agent etc.
As claim 1 and 3 described be the capsule of active component with the levorotation gossypol, comprise hard capsule, soft capsule, enteric coated capsule, slow releasing capsule.
As claim 1 and 3 described be the tablet of active component with the levorotation gossypol, comprise conventional tablet, slow releasing tablet, enteric coatel tablets, dispersible tablet.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA2008100181552A CN101269007A (en) | 2008-05-09 | 2008-05-09 | Dosage form containing levorotation gossypol as active component |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA2008100181552A CN101269007A (en) | 2008-05-09 | 2008-05-09 | Dosage form containing levorotation gossypol as active component |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN101269007A true CN101269007A (en) | 2008-09-24 |
Family
ID=40003396
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CNA2008100181552A Pending CN101269007A (en) | 2008-05-09 | 2008-05-09 | Dosage form containing levorotation gossypol as active component |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN101269007A (en) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103655526A (en) * | 2013-09-27 | 2014-03-26 | 中国人民解放军第三军医大学第三附属医院 | Novel application of gossypol |
| CN111821288A (en) * | 2020-05-26 | 2020-10-27 | 新疆医科大学 | Active ingredient for preparing medicine for treating uterine fibroids and application thereof |
-
2008
- 2008-05-09 CN CNA2008100181552A patent/CN101269007A/en active Pending
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103655526A (en) * | 2013-09-27 | 2014-03-26 | 中国人民解放军第三军医大学第三附属医院 | Novel application of gossypol |
| CN111821288A (en) * | 2020-05-26 | 2020-10-27 | 新疆医科大学 | Active ingredient for preparing medicine for treating uterine fibroids and application thereof |
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Open date: 20080924 |