CN105687499A - Betaxolol containing pharmaceutical composition for treating hypertension and preparation method thereof - Google Patents
Betaxolol containing pharmaceutical composition for treating hypertension and preparation method thereof Download PDFInfo
- Publication number
- CN105687499A CN105687499A CN201610175842.XA CN201610175842A CN105687499A CN 105687499 A CN105687499 A CN 105687499A CN 201610175842 A CN201610175842 A CN 201610175842A CN 105687499 A CN105687499 A CN 105687499A
- Authority
- CN
- China
- Prior art keywords
- betaxolol
- pharmaceutical composition
- parts
- injection volume
- hypertension
- 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.)
- Withdrawn
Links
- 229960004324 betaxolol Drugs 0.000 title claims abstract description 69
- NWIUTZDMDHAVTP-UHFFFAOYSA-N betaxolol Chemical compound C1=CC(OCC(O)CNC(C)C)=CC=C1CCOCC1CC1 NWIUTZDMDHAVTP-UHFFFAOYSA-N 0.000 title claims abstract description 69
- 239000008194 pharmaceutical composition Substances 0.000 title claims abstract description 50
- 206010020772 Hypertension Diseases 0.000 title claims abstract description 47
- 238000002360 preparation method Methods 0.000 title claims abstract description 20
- 239000003814 drug Substances 0.000 claims abstract description 21
- 229940079593 drug Drugs 0.000 claims abstract description 13
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims description 37
- 238000002347 injection Methods 0.000 claims description 28
- 239000007924 injection Substances 0.000 claims description 28
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 22
- 241000628997 Flos Species 0.000 claims description 21
- 239000013543 active substance Substances 0.000 claims description 19
- 239000000843 powder Substances 0.000 claims description 19
- 239000008187 granular material Substances 0.000 claims description 18
- 238000009835 boiling Methods 0.000 claims description 9
- 239000000706 filtrate Substances 0.000 claims description 9
- 238000001694 spray drying Methods 0.000 claims description 9
- 239000002671 adjuvant Substances 0.000 claims description 7
- 238000007796 conventional method Methods 0.000 claims description 4
- 239000002552 dosage form Substances 0.000 claims description 4
- 230000008719 thickening Effects 0.000 claims description 2
- 230000000694 effects Effects 0.000 abstract description 9
- 244000269722 Thea sinensis Species 0.000 abstract description 2
- 235000006468 Thea sinensis Nutrition 0.000 abstract description 2
- 239000000463 material Substances 0.000 abstract description 2
- 206010067484 Adverse reaction Diseases 0.000 abstract 1
- 235000009024 Ceanothus sanguineus Nutrition 0.000 abstract 1
- 244000037364 Cinnamomum aromaticum Species 0.000 abstract 1
- 235000014489 Cinnamomum aromaticum Nutrition 0.000 abstract 1
- 240000003553 Leptospermum scoparium Species 0.000 abstract 1
- 235000015459 Lycium barbarum Nutrition 0.000 abstract 1
- 230000006838 adverse reaction Effects 0.000 abstract 1
- 229940126680 traditional chinese medicines Drugs 0.000 abstract 1
- 230000036772 blood pressure Effects 0.000 description 11
- 229920000858 Cyclodextrin Polymers 0.000 description 7
- FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 description 7
- 229930195725 Mannitol Natural products 0.000 description 7
- 239000000594 mannitol Substances 0.000 description 7
- 235000010355 mannitol Nutrition 0.000 description 7
- 239000000203 mixture Substances 0.000 description 7
- HFHDHCJBZVLPGP-UHFFFAOYSA-N schardinger α-dextrin Chemical compound O1C(C(C2O)O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC(C(O)C2O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC2C(O)C(O)C1OC2CO HFHDHCJBZVLPGP-UHFFFAOYSA-N 0.000 description 7
- TVXBFESIOXBWNM-UHFFFAOYSA-N Xylitol Natural products OCCC(O)C(O)C(O)CCO TVXBFESIOXBWNM-UHFFFAOYSA-N 0.000 description 6
- 230000035487 diastolic blood pressure Effects 0.000 description 6
- HEBKCHPVOIAQTA-UHFFFAOYSA-N meso ribitol Natural products OCC(O)C(O)C(O)CO HEBKCHPVOIAQTA-UHFFFAOYSA-N 0.000 description 6
- 239000000811 xylitol Substances 0.000 description 6
- 235000010447 xylitol Nutrition 0.000 description 6
- HEBKCHPVOIAQTA-SCDXWVJYSA-N xylitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)CO HEBKCHPVOIAQTA-SCDXWVJYSA-N 0.000 description 6
- 229960002675 xylitol Drugs 0.000 description 6
- 239000011230 binding agent Substances 0.000 description 5
- 230000036471 bradycardia Effects 0.000 description 5
- 208000006218 bradycardia Diseases 0.000 description 5
- 230000006870 function Effects 0.000 description 5
- QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 description 3
- 208000007530 Essential hypertension Diseases 0.000 description 3
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 3
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 description 3
- 239000002220 antihypertensive agent Substances 0.000 description 3
- 229940127088 antihypertensive drug Drugs 0.000 description 3
- 239000003795 chemical substances by application Substances 0.000 description 3
- 230000036541 health Effects 0.000 description 3
- 210000004185 liver Anatomy 0.000 description 3
- 238000000034 method Methods 0.000 description 3
- 238000012360 testing method Methods 0.000 description 3
- 230000001225 therapeutic effect Effects 0.000 description 3
- CIWBSHSKHKDKBQ-JLAZNSOCSA-N Ascorbic acid Chemical compound OC[C@H](O)[C@H]1OC(=O)C(O)=C1O CIWBSHSKHKDKBQ-JLAZNSOCSA-N 0.000 description 2
- VTYYLEPIZMXCLO-UHFFFAOYSA-L Calcium carbonate Chemical compound [Ca+2].[O-]C([O-])=O VTYYLEPIZMXCLO-UHFFFAOYSA-L 0.000 description 2
- 241000196324 Embryophyta Species 0.000 description 2
- DHMQDGOQFOQNFH-UHFFFAOYSA-N Glycine Chemical compound NCC(O)=O DHMQDGOQFOQNFH-UHFFFAOYSA-N 0.000 description 2
- 206010019280 Heart failures Diseases 0.000 description 2
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 2
- NBIIXXVUZAFLBC-UHFFFAOYSA-N Phosphoric acid Chemical compound OP(O)(O)=O NBIIXXVUZAFLBC-UHFFFAOYSA-N 0.000 description 2
- WCUXLLCKKVVCTQ-UHFFFAOYSA-M Potassium chloride Chemical compound [Cl-].[K+] WCUXLLCKKVVCTQ-UHFFFAOYSA-M 0.000 description 2
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 2
- 241001122767 Theaceae Species 0.000 description 2
- XSQUKJJJFZCRTK-UHFFFAOYSA-N Urea Chemical compound NC(N)=O XSQUKJJJFZCRTK-UHFFFAOYSA-N 0.000 description 2
- POJWUDADGALRAB-UHFFFAOYSA-N allantoin Chemical compound NC(=O)NC1NC(=O)NC1=O POJWUDADGALRAB-UHFFFAOYSA-N 0.000 description 2
- 229940024606 amino acid Drugs 0.000 description 2
- 235000001014 amino acid Nutrition 0.000 description 2
- 150000001413 amino acids Chemical class 0.000 description 2
- 230000008901 benefit Effects 0.000 description 2
- 239000002775 capsule Substances 0.000 description 2
- 230000008602 contraction Effects 0.000 description 2
- 238000003745 diagnosis Methods 0.000 description 2
- 201000010099 disease Diseases 0.000 description 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 2
- 238000005516 engineering process Methods 0.000 description 2
- 230000003203 everyday effect Effects 0.000 description 2
- 238000007689 inspection Methods 0.000 description 2
- 239000007788 liquid Substances 0.000 description 2
- 230000007774 longterm Effects 0.000 description 2
- 210000004072 lung Anatomy 0.000 description 2
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 description 2
- 238000010606 normalization Methods 0.000 description 2
- 239000000825 pharmaceutical preparation Substances 0.000 description 2
- 239000006187 pill Substances 0.000 description 2
- 230000002265 prevention Effects 0.000 description 2
- 239000000047 product Substances 0.000 description 2
- 238000011160 research Methods 0.000 description 2
- GEHJYWRUCIMESM-UHFFFAOYSA-L sodium sulfite Chemical compound [Na+].[Na+].[O-]S([O-])=O GEHJYWRUCIMESM-UHFFFAOYSA-L 0.000 description 2
- 238000007619 statistical method Methods 0.000 description 2
- 238000002560 therapeutic procedure Methods 0.000 description 2
- QIJRTFXNRTXDIP-UHFFFAOYSA-N (1-carboxy-2-sulfanylethyl)azanium;chloride;hydrate Chemical compound O.Cl.SCC(N)C(O)=O QIJRTFXNRTXDIP-UHFFFAOYSA-N 0.000 description 1
- AXTGDCSMTYGJND-UHFFFAOYSA-N 1-dodecylazepan-2-one Chemical compound CCCCCCCCCCCCN1CCCCCC1=O AXTGDCSMTYGJND-UHFFFAOYSA-N 0.000 description 1
- FPIPGXGPPPQFEQ-UHFFFAOYSA-N 13-cis retinol Natural products OCC=C(C)C=CC=C(C)C=CC1=C(C)CCCC1(C)C FPIPGXGPPPQFEQ-UHFFFAOYSA-N 0.000 description 1
- CYDQOEWLBCCFJZ-UHFFFAOYSA-N 4-(4-fluorophenyl)oxane-4-carboxylic acid Chemical compound C=1C=C(F)C=CC=1C1(C(=O)O)CCOCC1 CYDQOEWLBCCFJZ-UHFFFAOYSA-N 0.000 description 1
- FHVDTGUDJYJELY-UHFFFAOYSA-N 6-{[2-carboxy-4,5-dihydroxy-6-(phosphanyloxy)oxan-3-yl]oxy}-4,5-dihydroxy-3-phosphanyloxane-2-carboxylic acid Chemical compound O1C(C(O)=O)C(P)C(O)C(O)C1OC1C(C(O)=O)OC(OP)C(O)C1O FHVDTGUDJYJELY-UHFFFAOYSA-N 0.000 description 1
- 108010022579 ATP dependent 26S protease Proteins 0.000 description 1
- QTBSBXVTEAMEQO-UHFFFAOYSA-M Acetate Chemical compound CC([O-])=O QTBSBXVTEAMEQO-UHFFFAOYSA-M 0.000 description 1
- POJWUDADGALRAB-PVQJCKRUSA-N Allantoin Natural products NC(=O)N[C@@H]1NC(=O)NC1=O POJWUDADGALRAB-PVQJCKRUSA-N 0.000 description 1
- GUBGYTABKSRVRQ-XLOQQCSPSA-N Alpha-Lactose Chemical compound O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O GUBGYTABKSRVRQ-XLOQQCSPSA-N 0.000 description 1
- 239000005995 Aluminium silicate Substances 0.000 description 1
- 206010003671 Atrioventricular Block Diseases 0.000 description 1
- 208000024172 Cardiovascular disease Diseases 0.000 description 1
- 206010008190 Cerebrovascular accident Diseases 0.000 description 1
- 206010011224 Cough Diseases 0.000 description 1
- FBPFZTCFMRRESA-FSIIMWSLSA-N D-Glucitol Natural products OC[C@H](O)[C@H](O)[C@@H](O)[C@H](O)CO FBPFZTCFMRRESA-FSIIMWSLSA-N 0.000 description 1
- ZZZCUOFIHGPKAK-UHFFFAOYSA-N D-erythro-ascorbic acid Natural products OCC1OC(=O)C(O)=C1O ZZZCUOFIHGPKAK-UHFFFAOYSA-N 0.000 description 1
- FBPFZTCFMRRESA-JGWLITMVSA-N D-glucitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-JGWLITMVSA-N 0.000 description 1
- 201000004624 Dermatitis Diseases 0.000 description 1
- 229920002307 Dextran Polymers 0.000 description 1
- 241000346136 Dracocephalum heterophyllum Species 0.000 description 1
- 206010059866 Drug resistance Diseases 0.000 description 1
- 208000010228 Erectile Dysfunction Diseases 0.000 description 1
- 206010017553 Furuncle Diseases 0.000 description 1
- 108010010803 Gelatin Proteins 0.000 description 1
- 239000004471 Glycine Substances 0.000 description 1
- 206010019233 Headaches Diseases 0.000 description 1
- FFEARJCKVFRZRR-BYPYZUCNSA-N L-methionine Chemical compound CSCC[C@H](N)C(O)=O FFEARJCKVFRZRR-BYPYZUCNSA-N 0.000 description 1
- 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 1
- 229910019142 PO4 Inorganic materials 0.000 description 1
- 239000002202 Polyethylene glycol Substances 0.000 description 1
- 229920001214 Polysorbate 60 Polymers 0.000 description 1
- 201000004681 Psoriasis Diseases 0.000 description 1
- 229920002472 Starch Polymers 0.000 description 1
- 208000006011 Stroke Diseases 0.000 description 1
- QAOWNCQODCNURD-UHFFFAOYSA-N Sulfuric acid Chemical compound OS(O)(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-N 0.000 description 1
- GSEJCLTVZPLZKY-UHFFFAOYSA-N Triethanolamine Chemical compound OCCN(CCO)CCO GSEJCLTVZPLZKY-UHFFFAOYSA-N 0.000 description 1
- FPIPGXGPPPQFEQ-BOOMUCAASA-N Vitamin A Natural products OC/C=C(/C)\C=C\C=C(\C)/C=C/C1=C(C)CCCC1(C)C FPIPGXGPPPQFEQ-BOOMUCAASA-N 0.000 description 1
- 229930003268 Vitamin C Natural products 0.000 description 1
- 229930003316 Vitamin D Natural products 0.000 description 1
- QYSXJUFSXHHAJI-XFEUOLMDSA-N Vitamin D3 Natural products C1(/[C@@H]2CC[C@@H]([C@]2(CCC1)C)[C@H](C)CCCC(C)C)=C/C=C1\C[C@@H](O)CCC1=C QYSXJUFSXHHAJI-XFEUOLMDSA-N 0.000 description 1
- 208000027418 Wounds and injury Diseases 0.000 description 1
- 230000002159 abnormal effect Effects 0.000 description 1
- 235000011054 acetic acid Nutrition 0.000 description 1
- 230000001154 acute effect Effects 0.000 description 1
- 230000002411 adverse Effects 0.000 description 1
- 229940072056 alginate Drugs 0.000 description 1
- 235000010443 alginic acid Nutrition 0.000 description 1
- 229920000615 alginic acid Polymers 0.000 description 1
- 229910000288 alkali metal carbonate Inorganic materials 0.000 description 1
- 150000008041 alkali metal carbonates Chemical class 0.000 description 1
- FPIPGXGPPPQFEQ-OVSJKPMPSA-N all-trans-retinol Chemical compound OC\C=C(/C)\C=C\C=C(/C)\C=C\C1=C(C)CCCC1(C)C FPIPGXGPPPQFEQ-OVSJKPMPSA-N 0.000 description 1
- 229960000458 allantoin Drugs 0.000 description 1
- 229910000147 aluminium phosphate Inorganic materials 0.000 description 1
- 235000012211 aluminium silicate Nutrition 0.000 description 1
- 208000002399 aphthous stomatitis Diseases 0.000 description 1
- 239000007864 aqueous solution Substances 0.000 description 1
- 208000006673 asthma Diseases 0.000 description 1
- 208000010668 atopic eczema Diseases 0.000 description 1
- 230000009286 beneficial effect Effects 0.000 description 1
- 239000002876 beta blocker Substances 0.000 description 1
- 229940097320 beta blocking agent Drugs 0.000 description 1
- 235000019636 bitter flavor Nutrition 0.000 description 1
- 238000009534 blood test Methods 0.000 description 1
- 210000004556 brain Anatomy 0.000 description 1
- NKWPZUCBCARRDP-UHFFFAOYSA-L calcium bicarbonate Chemical compound [Ca+2].OC([O-])=O.OC([O-])=O NKWPZUCBCARRDP-UHFFFAOYSA-L 0.000 description 1
- 229910000020 calcium bicarbonate Inorganic materials 0.000 description 1
- 229910000019 calcium carbonate Inorganic materials 0.000 description 1
- 229960003563 calcium carbonate Drugs 0.000 description 1
- CJZGTCYPCWQAJB-UHFFFAOYSA-L calcium stearate Chemical compound [Ca+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O CJZGTCYPCWQAJB-UHFFFAOYSA-L 0.000 description 1
- 235000013539 calcium stearate Nutrition 0.000 description 1
- 239000008116 calcium stearate Substances 0.000 description 1
- 235000013877 carbamide Nutrition 0.000 description 1
- 239000004202 carbamide Substances 0.000 description 1
- 206010007625 cardiogenic shock Diseases 0.000 description 1
- 239000001913 cellulose Substances 0.000 description 1
- 229920002678 cellulose Polymers 0.000 description 1
- 239000007766 cera flava Substances 0.000 description 1
- 208000026106 cerebrovascular disease Diseases 0.000 description 1
- 230000008859 change Effects 0.000 description 1
- 230000001684 chronic effect Effects 0.000 description 1
- 208000020832 chronic kidney disease Diseases 0.000 description 1
- 235000009508 confectionery Nutrition 0.000 description 1
- 230000001186 cumulative effect Effects 0.000 description 1
- 229960001305 cysteine hydrochloride Drugs 0.000 description 1
- 230000006378 damage Effects 0.000 description 1
- 238000001514 detection method Methods 0.000 description 1
- ACYGYJFTZSAZKR-UHFFFAOYSA-J dicalcium;2-[2-[bis(carboxylatomethyl)amino]ethyl-(carboxylatomethyl)amino]acetate Chemical compound [Ca+2].[Ca+2].[O-]C(=O)CN(CC([O-])=O)CCN(CC([O-])=O)CC([O-])=O ACYGYJFTZSAZKR-UHFFFAOYSA-J 0.000 description 1
- FPAFDBFIGPHWGO-UHFFFAOYSA-N dioxosilane;oxomagnesium;hydrate Chemical compound O.[Mg]=O.[Mg]=O.[Mg]=O.O=[Si]=O.O=[Si]=O.O=[Si]=O.O=[Si]=O FPAFDBFIGPHWGO-UHFFFAOYSA-N 0.000 description 1
- 239000000890 drug combination Substances 0.000 description 1
- 230000000857 drug effect Effects 0.000 description 1
- 238000002651 drug therapy Methods 0.000 description 1
- 230000002526 effect on cardiovascular system Effects 0.000 description 1
- 208000028208 end stage renal disease Diseases 0.000 description 1
- 201000000523 end stage renal failure Diseases 0.000 description 1
- 235000019441 ethanol Nutrition 0.000 description 1
- BEFDCLMNVWHSGT-UHFFFAOYSA-N ethenylcyclopentane Chemical compound C=CC1CCCC1 BEFDCLMNVWHSGT-UHFFFAOYSA-N 0.000 description 1
- -1 gallate ester Chemical class 0.000 description 1
- 229920000159 gelatin Polymers 0.000 description 1
- 239000008273 gelatin Substances 0.000 description 1
- 235000019322 gelatine Nutrition 0.000 description 1
- 235000011852 gelatine desserts Nutrition 0.000 description 1
- 235000011187 glycerol Nutrition 0.000 description 1
- 231100000869 headache Toxicity 0.000 description 1
- 210000002216 heart Anatomy 0.000 description 1
- 208000019622 heart disease Diseases 0.000 description 1
- 241000411851 herbal medicine Species 0.000 description 1
- 235000008216 herbs Nutrition 0.000 description 1
- BXWNKGSJHAJOGX-UHFFFAOYSA-N hexadecan-1-ol Chemical compound CCCCCCCCCCCCCCCCO BXWNKGSJHAJOGX-UHFFFAOYSA-N 0.000 description 1
- 235000011167 hydrochloric acid Nutrition 0.000 description 1
- 201000001881 impotence Diseases 0.000 description 1
- 230000006872 improvement Effects 0.000 description 1
- 208000030603 inherited susceptibility to asthma Diseases 0.000 description 1
- 208000014674 injury Diseases 0.000 description 1
- 238000011835 investigation Methods 0.000 description 1
- FZWBNHMXJMCXLU-BLAUPYHCSA-N isomaltotriose Chemical compound O[C@@H]1[C@@H](O)[C@H](O)[C@@H](CO)O[C@@H]1OC[C@@H]1[C@@H](O)[C@H](O)[C@@H](O)[C@@H](OC[C@@H](O)[C@@H](O)[C@H](O)[C@@H](O)C=O)O1 FZWBNHMXJMCXLU-BLAUPYHCSA-N 0.000 description 1
- NLYAJNPCOHFWQQ-UHFFFAOYSA-N kaolin Chemical compound O.O.O=[Al]O[Si](=O)O[Si](=O)O[Al]=O NLYAJNPCOHFWQQ-UHFFFAOYSA-N 0.000 description 1
- 210000003734 kidney Anatomy 0.000 description 1
- 238000009592 kidney function test Methods 0.000 description 1
- 239000008101 lactose Substances 0.000 description 1
- 238000011031 large-scale manufacturing process Methods 0.000 description 1
- 229940057995 liquid paraffin Drugs 0.000 description 1
- 230000003908 liver function Effects 0.000 description 1
- 201000003265 lymphadenitis Diseases 0.000 description 1
- 235000019359 magnesium stearate Nutrition 0.000 description 1
- 235000012054 meals Nutrition 0.000 description 1
- 238000005259 measurement Methods 0.000 description 1
- 229930182817 methionine Natural products 0.000 description 1
- 229960004452 methionine Drugs 0.000 description 1
- 235000006109 methionine Nutrition 0.000 description 1
- 239000002674 ointment Substances 0.000 description 1
- NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 description 1
- 239000010452 phosphate Substances 0.000 description 1
- 150000003904 phospholipids Chemical class 0.000 description 1
- 235000011007 phosphoric acid Nutrition 0.000 description 1
- 210000002826 placenta Anatomy 0.000 description 1
- 229920001223 polyethylene glycol Polymers 0.000 description 1
- 239000001818 polyoxyethylene sorbitan monostearate Substances 0.000 description 1
- 235000010989 polyoxyethylene sorbitan monostearate Nutrition 0.000 description 1
- 229940113124 polysorbate 60 Drugs 0.000 description 1
- 239000001267 polyvinylpyrrolidone Substances 0.000 description 1
- 229920000036 polyvinylpyrrolidone Polymers 0.000 description 1
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 description 1
- XAEFZNCEHLXOMS-UHFFFAOYSA-M potassium benzoate Chemical compound [K+].[O-]C(=O)C1=CC=CC=C1 XAEFZNCEHLXOMS-UHFFFAOYSA-M 0.000 description 1
- 239000001103 potassium chloride Substances 0.000 description 1
- 235000011164 potassium chloride Nutrition 0.000 description 1
- 230000035935 pregnancy Effects 0.000 description 1
- 235000013772 propylene glycol Nutrition 0.000 description 1
- 230000005180 public health Effects 0.000 description 1
- 230000002685 pulmonary effect Effects 0.000 description 1
- 238000012216 screening Methods 0.000 description 1
- 150000003376 silicon Chemical class 0.000 description 1
- 239000011780 sodium chloride Substances 0.000 description 1
- 235000002639 sodium chloride Nutrition 0.000 description 1
- HRZFUMHJMZEROT-UHFFFAOYSA-L sodium disulfite Chemical compound [Na+].[Na+].[O-]S(=O)S([O-])(=O)=O HRZFUMHJMZEROT-UHFFFAOYSA-L 0.000 description 1
- 239000001540 sodium lactate Substances 0.000 description 1
- 229940005581 sodium lactate Drugs 0.000 description 1
- 235000011088 sodium lactate Nutrition 0.000 description 1
- 235000010262 sodium metabisulphite Nutrition 0.000 description 1
- 235000010265 sodium sulphite Nutrition 0.000 description 1
- AKHNMLFCWUSKQB-UHFFFAOYSA-L sodium thiosulfate Chemical compound [Na+].[Na+].[O-]S([O-])(=O)=S AKHNMLFCWUSKQB-UHFFFAOYSA-L 0.000 description 1
- 235000019345 sodium thiosulphate Nutrition 0.000 description 1
- 235000010199 sorbic acid Nutrition 0.000 description 1
- 239000004334 sorbic acid Substances 0.000 description 1
- 229940075582 sorbic acid Drugs 0.000 description 1
- 239000000600 sorbitol Substances 0.000 description 1
- 235000010356 sorbitol Nutrition 0.000 description 1
- 239000008107 starch Substances 0.000 description 1
- 235000019698 starch Nutrition 0.000 description 1
- 239000001117 sulphuric acid Substances 0.000 description 1
- 235000011149 sulphuric acid Nutrition 0.000 description 1
- 239000004094 surface-active agent Substances 0.000 description 1
- 208000024891 symptom Diseases 0.000 description 1
- 230000002195 synergetic effect Effects 0.000 description 1
- 239000003826 tablet Substances 0.000 description 1
- UEUXEKPTXMALOB-UHFFFAOYSA-J tetrasodium;2-[2-[bis(carboxylatomethyl)amino]ethyl-(carboxylatomethyl)amino]acetate Chemical compound [Na+].[Na+].[Na+].[Na+].[O-]C(=O)CN(CC([O-])=O)CCN(CC([O-])=O)CC([O-])=O UEUXEKPTXMALOB-UHFFFAOYSA-J 0.000 description 1
- 210000001685 thyroid gland Anatomy 0.000 description 1
- 229940045136 urea Drugs 0.000 description 1
- 235000019155 vitamin A Nutrition 0.000 description 1
- 239000011719 vitamin A Substances 0.000 description 1
- 235000019154 vitamin C Nutrition 0.000 description 1
- 239000011718 vitamin C Substances 0.000 description 1
- 235000019166 vitamin D Nutrition 0.000 description 1
- 239000011710 vitamin D Substances 0.000 description 1
- 150000003710 vitamin D derivatives Chemical class 0.000 description 1
- 229940045997 vitamin a Drugs 0.000 description 1
- 229940046008 vitamin d Drugs 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/13—Amines
- A61K31/135—Amines having aromatic rings, e.g. ketamine, nortriptyline
- A61K31/138—Aryloxyalkylamines, e.g. propranolol, tamoxifen, phenoxybenzamine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
- A61K36/18—Magnoliophyta (angiosperms)
- A61K36/185—Magnoliopsida (dicotyledons)
- A61K36/53—Lamiaceae or Labiatae (Mint family), e.g. thyme, rosemary or lavender
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
- A61K36/18—Magnoliophyta (angiosperms)
- A61K36/185—Magnoliopsida (dicotyledons)
- A61K36/54—Lauraceae (Laurel family), e.g. cinnamon or sassafras
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
- A61K36/18—Magnoliophyta (angiosperms)
- A61K36/185—Magnoliopsida (dicotyledons)
- A61K36/82—Theaceae (Tea family), e.g. camellia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
- A61K9/1605—Excipients; Inactive ingredients
- A61K9/1629—Organic macromolecular compounds
- A61K9/1652—Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2236/00—Isolation or extraction methods of medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicine
- A61K2236/30—Extraction of the material
- A61K2236/33—Extraction of the material involving extraction with hydrophilic solvents, e.g. lower alcohols, esters or ketones
- A61K2236/331—Extraction of the material involving extraction with hydrophilic solvents, e.g. lower alcohols, esters or ketones using water, e.g. cold water, infusion, tea, steam distillation or decoction
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2236/00—Isolation or extraction methods of medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicine
- A61K2236/30—Extraction of the material
- A61K2236/39—Complex extraction schemes, e.g. fractionation or repeated extraction steps
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2236/00—Isolation or extraction methods of medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicine
- A61K2236/50—Methods involving additional extraction steps
- A61K2236/51—Concentration or drying of the extract, e.g. Lyophilisation, freeze-drying or spray-drying
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2236/00—Isolation or extraction methods of medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicine
- A61K2236/50—Methods involving additional extraction steps
- A61K2236/53—Liquid-solid separation, e.g. centrifugation, sedimentation or crystallization
Landscapes
- Health & Medical Sciences (AREA)
- Natural Medicines & Medicinal Plants (AREA)
- Life Sciences & Earth Sciences (AREA)
- Engineering & Computer Science (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Chemical & Material Sciences (AREA)
- Epidemiology (AREA)
- Biotechnology (AREA)
- Botany (AREA)
- Medical Informatics (AREA)
- Microbiology (AREA)
- Mycology (AREA)
- Alternative & Traditional Medicine (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines Containing Plant Substances (AREA)
Abstract
The invention belongs to the technical field of medicines and particularly relates to a betaxolol containing pharmaceutical composition for treating hypertension and a preparation method thereof. The betaxolol containing pharmaceutical composition for treating the hypertension, provided by the invention, is prepared from the following raw pharmaceutical materials in parts by weight: 5-15 parts of betaxolol, 2,000-4,000 parts of herba dracocephali heterophylli, 2,000-4,000 parts of camellia sinensis, 2,000-4,000 parts of tea tree roots and 2,000-4,000 parts of cassia twigs. According to the betaxolol containing pharmaceutical composition for treating the hypertension and the preparation method thereof, the traditional Chinese medicines and the betaxolol are combined, so that common adverse reactions of the betaxolol can be avoided, and the treatment effect on the hypertension is improved.
Description
Technical field
The invention belongs to pharmaceutical technology field, be specifically related to a kind of pharmaceutical composition for the treatment of hypertension containing betaxolol and preparation method thereof。
Background technology
Hypertension is Important cause of disease and the risk factor of cardiovascular and cerebrovascular disease, and the people that there is 20%-30% in the whole world suffers from blood pressure。Hypertension can affect the 26S Proteasome Structure and Function of the heart, brain, kidney, can dramatically increase the onset risk of apoplexy, heart failure, end stagerenaldisease。Essential hypertension accounts for the 95% of hypertension incidence, and the investigation of 2002 is shown in more than 18 years old prevalence of China up to 18.8%, and number of patients reaches 1.6 hundred million。Therefore the prevention of hypertension and treatment, becomes China and great public health problem that the whole world is paid close attention to the most。
The Therapeutic Method of current hypertension is except changing living habit, and topmost effective prevention method is exactly that furuncle controlled by medicine, and antihypertensive drugs conventional at present is divided into 5 classes, clinically alone the and drug combination two class scheme of main employing。But antihypertensive drugs still has a lot of bad compliance asking untoward reaction, drug resistance phenomenon and patient that such as Long-term taking medicine causes in clinical application。There are some researches show that the patient accepting Drug therapy only has 53% successfully to control blood pressure, make controlling of blood pressure at≤140/90mmHg。
Betaxolol is the beta-blocker of clinical conventional treatment hypertension。This product is applicable to hypertension therapeutic, and especially alignment degree hypertension and the young hyperpietic's best results without severe complication, can be used in combination with other antihypertensive drugs。But, the side effect of long-term taking betaxolol is also very big to the injury of human body。What allow people has a headache most is may result in bradycardia。This untoward reaction limits betaxolol in clinical use。
Summary of the invention
In order to solve the technical problem of the big restriction use crowd of betaxolol side effect, the invention provides the compositions of a kind of betaxolol and Chinese medicine, by the compatibility with Chinese medicine, alleviate the untoward reaction of betaxolol, thus realizing the purpose of attenuation synergistic。
The present invention is realized by following technical scheme:
The pharmaceutical composition of a kind for the treatment of hypertension containing betaxolol, is made up of the crude drug of following weight proportion: betaxolol 5-15 part, Herba Ajugae 2000-4000 part, Flos Camelliae Japonicae 2000-4000 part, Radix Camelliae sinensis 2000-4000 part, Ramulus Cinnamomi 2000-4000 part。
The pharmaceutical composition of the above-mentioned treatment hypertension containing betaxolol, its weight is preferably: betaxolol 7.5-12.5 part, Herba Ajugae 2500-3500 part, Flos Camelliae Japonicae 2500-3500 part, Radix Camelliae sinensis 2500-3500 part, Ramulus Cinnamomi 2500-3500 part。
The pharmaceutical composition of the above-mentioned treatment hypertension containing betaxolol, its weight the best is: betaxolol 10 parts, Herba Ajugae 3000 parts, Flos Camelliae Japonicae 3000 parts, Radix Camelliae sinensis 3000 parts, Ramulus Cinnamomi 3000 parts。
In the composition described above of the present invention, the weight of each taste Chinese medicine calculates with crude drug, if in grams, as made preparation, then because varying in size of preparation can be made into 100-1000 agent。Described 100-1000 agent refers to the dosage form of unit dose, such as tablet 100-1000 sheet, capsule 100-1000 grain, granule l00-1000g, oral liquid l00-l000ml, unguentum l00-l000g, pill 100-1000 ball etc.。
Composition described above is by weight as proportioning, can increase according to corresponding proportion when producing or reduce, as large-scale production can in units of kg, or with t(ton) for unit；Preparation can also in units of g on a small scale。Weight can increase or reduce, but the constant rate of the raw medicinal herbs weight proportion between each composition。
The ratio of above weight proportion obtains through science screening, for especial patient, such as serious symptom or mild, fat or modest patient, it is possible to the proportioning of the corresponding amount adjusting composition, increases or reduces less than 100%, and drug effect is basically unchanged。
The pharmaceutical composition of the present invention, individually or as required can add some pharmaceutically acceptable adjuvants of injection volume, it is possible to adopt galenic pharmacy routine techniques to prepare this pharmaceutical preparation, as mixed with pharmaceutically acceptable adjuvant by pharmaceutically active substance。Can make any pharmaceutically useful peroral dosage form when making pharmaceutical preparation, these dosage forms are selected from: granule, tablet, capsule, oral liquid, suck agent, pill, powder, it is preferred that granule。
The preparation method of the pharmaceutical composition of the above-mentioned treatment hypertension containing betaxolol, comprises the steps of:
A. by Herba Ajugae, Flos Camelliae Japonicae, Radix Camelliae sinensis, Ramulus Cinnamomi boiling 2 times, adding injection volume 6 ~ 8 times amount water, decocts 1 ~ 2 hour for the 1st time, second time adds injection volume 4 ~ 6 times amount water, decocts 0.5 ~ 1.5 hour, and merging decoction liquor is standby；
B. by decoction liquor 55 ~ 65 DEG C, be condensed into the clear paste that relative density is 1.08 ~ 1.12 under-0.04 ~-0.08Mpa condition, adding ethanol to alcohol content is 75%, places 12 hours, filters, filtrate is concentrated into the clear paste that relative density is 1.15 ~ 1.20, and spray drying must dry medicated powder；
C. by betaxolol and the mixing of dry medicated powder, granulate, obtain the active substance of pharmaceutical composition of the present invention；
D. this active substance individually or mixes with pharmaceutically acceptable adjuvant, prepares according to galenic pharmacy conventional method。
In the preparation method of the pharmaceutical composition of the above-mentioned treatment hypertension containing betaxolol, adding injection volume 7 times amount water the 1st time, decoct 1.5 hours in institute portion step a, second time adds injection volume 5 times amount water, decocts 1 hour；In described step b thickening temperature be 60 DEG C, concentration pressure be-0.06Mpa。
Preferably, the preparation method stating the pharmaceutical composition for the treatment of hypertension containing betaxolol, detailed step is as follows:
A. by Herba Ajugae, Flos Camelliae Japonicae, Radix Camelliae sinensis, Ramulus Cinnamomi boiling 2 times, adding injection volume 7 times amount water, decocts 1.5 hours for the 1st time, second time adds injection volume 5 times amount water, decocts 1 hour, and merging decoction liquor is standby；
B. by decoction liquor 60 DEG C, be condensed into the clear paste that relative density is 1.08 ~ 1.12 under-0.06Mpa condition, adding ethanol to alcohol content is 75%, places 12 hours, filters, and filtrate is concentrated into the clear paste that relative density is 1.15 ~ 1.20, and spray drying must dry medicated powder；
C. by betaxolol and the mixing of dry medicated powder, granulate, obtain the active substance of pharmaceutical composition of the present invention；
D. this active substance individually or mixes with pharmaceutically acceptable adjuvant, prepares according to galenic pharmacy conventional method。
Described pharmaceutically acceptable adjuvant is selected from: starch, magnesium stearate, mannitol, sorbitol, sorbic acid or potassium salt, sodium pyrosulfite, sodium sulfite, sodium thiosulfate, cysteine hydrochloride, TGA, methionine, vitamin A, vitamin C, tie up main element E, vitamin D, azone, EDETATE SODIUM, Ethylenediaminetetraacetic Acid Calcium Salt, the alkali-metal carbonate of monovalence, acetate, phosphate or its aqueous solution, hydrochloric acid, acetic acid, sulphuric acid, phosphoric acid, aminoacid, sodium chloride, potassium chloride, sodium lactate, xylitol, dextran, glycine, lactose, mannitol, silicon derivative, cellulose and its derivates, alginate, gelatin, polyvinylpyrrolidone, glycerol, propylene glycol, ethanol, polysorbate60～80, Span～80, Cera Flava, lanoline, liquid paraffin, hexadecanol, gallate ester, triethanolamine, basic amino acid, carbamide, allantoin, calcium carbonate, calcium bicarbonate, surfactant, Polyethylene Glycol, cyclodextrin, β～cyclodextrin, phospholipid material, Kaolin, Pulvis Talci, calcium stearate etc.。
The present invention treat hypertension pharmaceutical composition be applicable to treatment essential hypertension, can individually or with other depressor use in conjunction。
The present invention treats the pharmaceutical composition usage and dosage of hypertension:
Oral: to start cumulative dosage from low dose。Usual initial dose be one time 1 bag, 2 times on the one；Take with meal。
The present invention treats the pharmaceutical composition of hypertension and disables in patient's disabling of: bronchial asthma, severe COPD, II or III degree of atrioventricular block, obvious heart failure or cardiogenic shock。Pulmonary insufficiency, imbalance of thyroid function and diabetics are cautious use of。During gestation, the-permeable Placenta Hominis of this product is not yet determined in the safety of medication。Suckling should be stopped during lacting woman medication。
In the pharmaceutical composition of the present invention,
Radix Camelliae sinensis source is the root of plant of theaceae tea。Bitter in the mouth, property is put down。Function controls heart disease, aphtha, psoriasis。
Herba Ajugae another name is very sweet (" Chinese herbal medicine handbook is commonly used in Qinghai ") in vain。The herb of source labiate dracocephalum heterophyllum。Toil, cold。Function suppressing the hyperactive liver, heat clearing away。Control hypertension, lymphadenitis, cough due to lung-heat。
Flos Camelliae Japonicae is the flower of plant of theaceae tea Camelliasinensis (L.) O.Kuntze ［ TheasinensisL. ］。Mildly bitter flavor；Cool in nature。Return lung；Liver Channel。Function lung heat clearing suppressing the hyperactive liver。Main nasal eczema；Hypertension。
The beneficial effects of the present invention is: Chinese medicine is combined with betaxolol by the present invention, to avoid the common untoward reaction of betaxolol, and improve the therapeutic effect to hypertension。Clinical test results shows: the oral present invention patient containing betaxolol compositions, and preliminary judgement is better than simple application betaxolol person in controlling blood pressure level。It addition, the present invention's applies betaxolol person effect notable (P < 0.05) than simple containing betaxolol pharmaceutical composition in improving betaxolol adverse effect。Illustrate that the pharmaceutical composition containing betaxolol of the present invention truly has curative effect in reducing blood pressure, and there is the advantage that side effect is little。
Detailed description of the invention
Below in conjunction with specific embodiment, the present invention is further described, in order to those skilled in the art knows more about the present invention, but and is not so limited the present invention。
Embodiment 1
A kind of pharmaceutical composition treating hypertension, is made up of the crude drug of following weight:
Betaxolol 10g, Herba Ajugae 3000g, Flos Camelliae Japonicae 3000g, Radix Camelliae sinensis 3000g, Ramulus Cinnamomi 3000g。
The preparation method of the pharmaceutical composition of this treatment hypertension:
A. by Herba Ajugae, Flos Camelliae Japonicae, Radix Camelliae sinensis, Ramulus Cinnamomi boiling 2 times, adding injection volume 7 amount water, decocts 1.5 hours for the 1st time, second time adds injection volume 5 times amount water, decocts 1 hour, and merging decoction liquor is standby；
B. by decoction liquor 60 DEG C, be condensed into the clear paste that relative density is 1.08 ~ 1.12 under-0.06Mpa condition, adding ethanol to alcohol content is 75%, places 12 hours, filters, and filtrate is concentrated into the clear paste that relative density is 1.15 ~ 1.20, and spray drying must dry medicated powder；
C. by betaxolol and the mixing of dry medicated powder, granulate, obtain the active substance of pharmaceutical composition of the present invention；
D. this active substance adds injection volume xylitol, mannitol and β～cyclodextrin, and binding agent makes granule in right amount。
Prepare 1000 bags altogether, every bag of weight 5g。
Embodiment 2
A kind of pharmaceutical composition treating hypertension, is made up of the crude drug of following weight:
Betaxolol 7.5g, Herba Ajugae 3500g, Flos Camelliae Japonicae 2500g, Radix Camelliae sinensis 3500g, Ramulus Cinnamomi 2500g。
The preparation method of the pharmaceutical composition of this treatment hypertension:
A. by Herba Ajugae, Flos Camelliae Japonicae, Radix Camelliae sinensis, Ramulus Cinnamomi boiling 2 times, adding injection volume 8 amount water, decocts 2 hours for the 1st time, second time adds injection volume 6 times amount water, decocts 1.5 hours, and merging decoction liquor is standby；
B. by decoction liquor 55 DEG C, be condensed into the clear paste that relative density is 1.08 ~ 1.12 under-0.08Mpa condition, adding ethanol to alcohol content is 75%, places 12 hours, filters, and filtrate is concentrated into the clear paste that relative density is 1.15 ~ 1.20, and spray drying must dry medicated powder；
C. by betaxolol and the mixing of dry medicated powder, granulate, obtain the active substance of pharmaceutical composition of the present invention；
D. this active substance adds injection volume xylitol, mannitol and β～cyclodextrin, binding agent makes granule in right amount。
Prepare 1000 bags altogether, every bag of weight 5g。
Embodiment 3
A kind of pharmaceutical composition treating hypertension, is made up of the crude drug of following weight:
Betaxolol 12.5g, Herba Ajugae 2500g, Flos Camelliae Japonicae 3500g, Radix Camelliae sinensis 2500g, Ramulus Cinnamomi 3500g。
The preparation method of the pharmaceutical composition of this treatment hypertension:
A. by Herba Ajugae, Flos Camelliae Japonicae, Radix Camelliae sinensis, Ramulus Cinnamomi boiling 2 times, adding injection volume 6 amount water, decocts 1 hour for the 1st time, second time adds injection volume 4 times amount water, decocts 0.5 hour, and merging decoction liquor is standby；
B. by decoction liquor 65 DEG C, be condensed into the clear paste that relative density is 1.08 ~ 1.12 under-0.04Mpa condition, adding ethanol to alcohol content is 75%, places 12 hours, filters, and filtrate is concentrated into the clear paste that relative density is 1.15 ~ 1.20, and spray drying must dry medicated powder；
C. by betaxolol and the mixing of dry medicated powder, granulate, obtain the active substance of pharmaceutical composition of the present invention；
D. this active substance adds injection volume xylitol, mannitol and β～cyclodextrin, and binding agent makes granule in right amount。
Prepare 1000 bags altogether, every bag of weight 5g。
Embodiment 4
A kind of pharmaceutical composition treating hypertension, is made up of the crude drug of following weight:
Betaxolol 5g, Herba Ajugae 4000g, Flos Camelliae Japonicae 4000g, Radix Camelliae sinensis 4000g, Ramulus Cinnamomi 4000g。
The preparation method of the pharmaceutical composition of this treatment hypertension:
A. by Herba Ajugae, Flos Camelliae Japonicae, Radix Camelliae sinensis, Ramulus Cinnamomi boiling 2 times, adding injection volume 7 amount water, decocts 1.5 hours for the 1st time, second time adds injection volume 5 times amount water, decocts 1 hour, and merging decoction liquor is standby；
B. by decoction liquor 60 DEG C, be condensed into the clear paste that relative density is 1.08 ~ 1.12 under-0.06Mpa condition, adding ethanol to alcohol content is 75%, places 12 hours, filters, and filtrate is concentrated into the clear paste that relative density is 1.15 ~ 1.20, and spray drying must dry medicated powder；
C. by betaxolol and the mixing of dry medicated powder, granulate, obtain the active substance of pharmaceutical composition of the present invention；
D. this active substance adds injection volume xylitol, mannitol and β～cyclodextrin, and binding agent makes granule in right amount。
Prepare 1000 bags altogether, every bag of weight 5g。
Embodiment 5
A kind of pharmaceutical composition treating hypertension, is made up of the crude drug of following weight:
Betaxolol 15g, Herba Ajugae 2000g, Flos Camelliae Japonicae 2000g, Radix Camelliae sinensis 2000g, Ramulus Cinnamomi 2000g。
The preparation method of the pharmaceutical composition of this treatment hypertension:
A. by Herba Ajugae, Flos Camelliae Japonicae, Radix Camelliae sinensis, Ramulus Cinnamomi boiling 2 times, adding injection volume 7 amount water, decocts 1.5 hours for the 1st time, second time adds injection volume 5 times amount water, decocts 1 hour, and merging decoction liquor is standby；
B. by decoction liquor 60 DEG C, be condensed into the clear paste that relative density is 1.08 ~ 1.12 under-0.06Mpa condition, adding ethanol to alcohol content is 75%, places 12 hours, filters, and filtrate is concentrated into the clear paste that relative density is 1.15 ~ 1.20, and spray drying must dry medicated powder；
C. by betaxolol and the mixing of dry medicated powder, granulate, obtain the active substance of pharmaceutical composition of the present invention；
D. this active substance adds injection volume xylitol, mannitol and β～cyclodextrin, and binding agent makes granule in right amount。
Prepare 1000 bags altogether, every bag of weight 5g。
The pharmaceutical composition containing betaxolol of embodiment 1 preparation has been carried out clinical trial, and result is as follows:
1. data and method
1.1 object of study
80 example primary hypertension patients have been selected in present study, all meet WHO diagnostic criteria in 1999, and meet following condition: 1. make a definite diagnosis for the first time or make a definite diagnosis and do not treat and shrink pressure >=140mmHg, diastolic pressure >=90mmHg less than half a year；2. without serious acute and chronic complication。Qualified 80 example patients are randomly divided into observation group and matched group, often organize 40 examples。Two groups of patient's comparing difference not statistically significants (P > 0.05) in sex, age, Body Mass Index, the course of disease, blood pressure level etc. very physical data, have comparability。
1.2 Therapeutic Method
1. matched group: patient is being carried out the treatment of application betaxolol, each 10mg of betaxolol, every day 2 times on the basis of hypertension health knowledge education。2. observation group: patient is being carried out the pharmaceutical composition that on the basis of hypertension health knowledge education, use in conjunction contains betaxolol, each 1 bag, every day 2 times。Two groups all with 1 Zhou Weiyi treatment stage。
1.3 observation index
1. safety indexes: such as routine blood test, stool routine examination, liver function, kidney function test, electrocardiogram etc.；2. health giving quality index: blood pressure level before and after treatment, blood pressure normalization rate (shrinks pressure≤120mmHg, diastolic pressure≤90mmHg)。3. a situation arises in sexual impotence untoward reaction。
1.4 statistical methods
SPSS17.0 is adopted to carry out the statistical analysis of data。Measurement data adopts t inspection (representing by mean ± standard deviation)；Group data adopts χ2Inspection, using P≤0.05 as statistically significant, using P≤0.01 as there being height statistical significance。
2. result
2.1 clinical efficacy results
Treat contraction pressure and the diastolic pressure level comparing difference not statistically significant (P > 0.05) of first two groups;After treatment, the contraction pressure of two groups and diastolic pressure level substantially reduce before all relatively treating, and difference has statistical significance (P < 0.05);Observation group patient is substantially better than matched group in shrinking pressure and diastolic pressure improvement degree, and difference has statistical significance (P < 0.05)；Blood pressure normalization rate 95.0%(38/40 after observation group's treatment) apparently higher than the 72.5%(29/40 of matched group), difference has statistical significance (P < 0.05);In Table 1。
1 liang of table group patient clinical comparitive study
| Group | Number of cases | Time | Shrink pressure (mmHg) | Diastolic pressure (mmHg) |
| Observation group | 40 | Before treatment | 168.84±13.56 | 116.62±12.29 |
| After treatment | 103.21±9.55*# | 70.69±4.41*# | ||
| Matched group | 40 | Before treatment | 168.81±13.52 | 116.65±12.27 |
| After treatment | 122.74±11.39* | 98.61±5.92* |
Note: * represent with treatment before compare P < 0.05;# represents and compares P < 0.05 after treatment of control group
2.2 safety observations results
In this test, whole experimenters carry out safety indexes detection respectively before and after treatment, and result does not find obvious abnormal change, illustrate that the pharmaceutical composition containing betaxolol of the present invention uses safety。
A situation arises in 2.3 bradycardia untoward reaction
In this research, the bradycardia incidence rate of observation group is 2.5%(1/40) significantly lower than the 30%(12/40 of matched group), difference has statistical significance (P < 0.05)。
3. conclusion
Chinese medicine is combined by the present invention with betaxolol, to avoid the common bradycardia of betaxolol, and improves the therapeutic effect to hypertension。Clinical test results shows: the oral present invention patient containing betaxolol compositions, and preliminary judgement is better than simple application betaxolol person in controlling blood pressure level。It addition, the present invention's applies betaxolol person effect notable (P < 0.05) than simple containing betaxolol pharmaceutical composition in improving betaxolol medicine bradycardia untoward reaction。Illustrate that the pharmaceutical composition containing betaxolol of the present invention is safe and effective in reducing blood pressure, and there is the advantage that side effect is little。
Claims (7)
1. a pharmaceutical composition for the treatment hypertension containing betaxolol, is made up of the crude drug of following weight: betaxolol 5-15 part, Herba Ajugae 2000-4000 part, Flos Camelliae Japonicae 2000-4000 part, Radix Camelliae sinensis 2000-4000 part, Ramulus Cinnamomi 2000-4000 part。
2. the pharmaceutical composition of the treatment hypertension containing betaxolol as claimed in claim 1, it is characterized in that, be made up of the crude drug of following weight: betaxolol 7.5-12.5 part, Herba Ajugae 2500-3500 part, Flos Camelliae Japonicae 2500-3500 part, Radix Camelliae sinensis 2500-3500 part, Ramulus Cinnamomi 2500-3500 part。
3. the pharmaceutical composition of the treatment hypertension containing betaxolol as claimed in claim 2, it is characterized in that, be made up of the crude drug of following weight: betaxolol 10 parts, Herba Ajugae 3000 parts, Flos Camelliae Japonicae 3000 parts, Radix Camelliae sinensis 3000 parts, Ramulus Cinnamomi 3000 parts。
4. the pharmaceutical composition of the treatment hypertension containing betaxolol as described in claim 1 or 2 or 3, it is characterised in that its dosage form is granule。
5. the preparation method of the pharmaceutical composition of the treatment hypertension containing betaxolol described in claim 1 or 2 or 3, comprises the steps of:
A. by Herba Ajugae, Flos Camelliae Japonicae, Radix Camelliae sinensis, Ramulus Cinnamomi boiling 2 times, adding injection volume 6 ~ 8 times amount water, decocts 1 ~ 2 hour for the 1st time, second time adds injection volume 4 ~ 6 times amount water, decocts 0.5 ~ 1.5 hour, and merging decoction liquor is standby；
B. by decoction liquor 55 ~ 65 DEG C, be condensed into the clear paste that relative density is 1.08 ~ 1.12 under-0.04 ~-0.08Mpa condition, adding ethanol to alcohol content is 75%, places 12 hours, filter, filtrate is concentrated into the clear paste that relative density is 1.15 ~ 1.20, spray drying, obtains dry medicated powder；
C. by betaxolol and the mixing of dry medicated powder, granulate, obtain the active substance of pharmaceutical composition of the present invention；
D. this active substance individually or mixes with pharmaceutically acceptable adjuvant, prepares according to galenic pharmacy conventional method。
6. the preparation method of the pharmaceutical composition of the treatment hypertension containing betaxolol as claimed in claim 5, it is characterised in that
Adding injection volume 7 times amount water 1st time in institute portion step a, decoct 1.5 hours, second time adds injection volume 5 times amount water, decocts 1 hour；In described step b thickening temperature be 60 DEG C, concentration pressure be-0.06Mpa。
7. the preparation method of the pharmaceutical composition of the treatment hypertension containing betaxolol as claimed in claim 5, detailed step is as follows:
A. by Herba Ajugae, Flos Camelliae Japonicae, Radix Camelliae sinensis, Ramulus Cinnamomi boiling 2 times, adding injection volume 7 times amount water, decocts 1.5 hours for the 1st time, second time adds injection volume 5 times amount water, decocts 1 hour, and merging decoction liquor is standby；
B. by decoction liquor 60 DEG C, be condensed into the clear paste that relative density is 1.08 ~ 1.12 under-0.06Mpa condition, adding ethanol to alcohol content is 75%, places 12 hours, filters, and filtrate is concentrated into the clear paste that relative density is 1.15 ~ 1.20, spray drying, obtains dry medicated powder；
C. by betaxolol and the mixing of dry medicated powder, granulate, obtain the active substance of pharmaceutical composition of the present invention；
D. this active substance individually or mixes with pharmaceutically acceptable adjuvant, prepares according to galenic pharmacy conventional method。
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610175842.XA CN105687499A (en) | 2016-03-27 | 2016-03-27 | Betaxolol containing pharmaceutical composition for treating hypertension and preparation method thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610175842.XA CN105687499A (en) | 2016-03-27 | 2016-03-27 | Betaxolol containing pharmaceutical composition for treating hypertension and preparation method thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN105687499A true CN105687499A (en) | 2016-06-22 |
Family
ID=56232788
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201610175842.XA Withdrawn CN105687499A (en) | 2016-03-27 | 2016-03-27 | Betaxolol containing pharmaceutical composition for treating hypertension and preparation method thereof |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN105687499A (en) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN113842379A (en) * | 2021-09-12 | 2021-12-28 | 东北农业大学 | New application of betaxolol as NDM-1 inhibitor or antibiotic protective agent |
-
2016
- 2016-03-27 CN CN201610175842.XA patent/CN105687499A/en not_active Withdrawn
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN113842379A (en) * | 2021-09-12 | 2021-12-28 | 东北农业大学 | New application of betaxolol as NDM-1 inhibitor or antibiotic protective agent |
| CN113842379B (en) * | 2021-09-12 | 2024-04-23 | 东北农业大学 | New application of betaxolol as NDM-1 inhibitor or antibiotic protectant |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| CN107260963A (en) | The method that treatment hypertension drug is prepared as main material using dendrobium candidum and radish seed | |
| CN1558768A (en) | A pharmaceutical composition made from Chinese traditional medicine and preparation method thereof | |
| CN102258742A (en) | Chinese medicinal medicine composition for treating depression and preparation method thereof | |
| CN105434738A (en) | Traditional Chinese medicine composition for treating ADHD (Attention Deficit Hyperactivity Disorder) and preparation method thereof | |
| CN106334171B (en) | A kind of Chinese medicine preparation and preparation method for being used to repair hepatic injury | |
| CN105687499A (en) | Betaxolol containing pharmaceutical composition for treating hypertension and preparation method thereof | |
| CN105727089A (en) | Application of medicine composition containing folium artemisiae argyi to preparing medicine for treating irritable bowel syndrome | |
| CN105687765A (en) | Lacidipine containing pharmaceutical composition for treating hypertension and preparation method thereof | |
| CN104491483A (en) | Traditional Chinese medicine composition for improving allergic diseases, preparation method and application thereof | |
| CN108785559A (en) | A kind of drug and preparation method thereof for treating respiratory tract infection | |
| CN102552724A (en) | Chinese medicine composite for curing hypertension | |
| CN102274428A (en) | Pharmaceutical composition with effect on treating irritable bowel syndrome and preparation method and application thereof | |
| CN107095977A (en) | A kind of medicament and its pharmaceutical formulation and preparation method with the malicious effect of fire row of dispelling | |
| CN105687571A (en) | Metoprolol containing pharmaceutical composition for treating hypertension and preparation method thereof | |
| CN105796952A (en) | Gliquidone-containing medicine combination for treating diabetes and preparation method thereof | |
| CN106177347A (en) | A kind of pharmaceutical composition treating constipation | |
| CN105687451A (en) | Lercanidipine containing pharmaceutical composition for treating hypertension and preparation method thereof | |
| CN105770205A (en) | Pharmaceutical composition containing felodipine and capable of treating hypertension and preparation method thereof | |
| CN105853582A (en) | Folium artemisiae argyi containing medicine preparation for treating cholelithiasis and preparation method thereof | |
| CN105708983A (en) | Medicine composition for treating hypertension containing propranolol and preparation method of medicine composition | |
| CN105687400A (en) | Nifedipine containing pharmaceutical composition for treating hypertension and preparation method thereof | |
| CN105535056A (en) | Traditional Chinese medicine preparation for treating viral meningitis and preparation method and application thereof | |
| CN105687874A (en) | Dihydrochlorothiazide (DCT) containing pharmaceutical composition for treating hypertension and preparation method thereof | |
| CN102091260B (en) | Chinese medicinal composition for treating bronchitis | |
| CN111888425A (en) | Traditional Chinese medicine preparation for treating hypotension and preparation method and application thereof |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| WW01 | Invention patent application withdrawn after publication | ||
| WW01 | Invention patent application withdrawn after publication |
Application publication date: 20160622 |