CN101947222A - Ointment for treating high blood pressure and preparation method thereof - Google Patents
Ointment for treating high blood pressure and preparation method thereof Download PDFInfo
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- CN101947222A CN101947222A CN 201010255704 CN201010255704A CN101947222A CN 101947222 A CN101947222 A CN 101947222A CN 201010255704 CN201010255704 CN 201010255704 CN 201010255704 A CN201010255704 A CN 201010255704A CN 101947222 A CN101947222 A CN 101947222A
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- China
- Prior art keywords
- ointment
- reactive compound
- base material
- phenoxybenzamine
- clonidine
- Prior art date
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- 239000002674 ointment Substances 0.000 title claims abstract description 58
- 206010020772 Hypertension Diseases 0.000 title claims abstract description 25
- 238000002360 preparation method Methods 0.000 title claims abstract description 15
- 150000001875 compounds Chemical class 0.000 claims abstract description 28
- 239000000463 material Substances 0.000 claims abstract description 28
- HMJIYCCIJYRONP-UHFFFAOYSA-N (+-)-Isradipine Chemical compound COC(=O)C1=C(C)NC(C)=C(C(=O)OC(C)C)C1C1=CC=CC2=NON=C12 HMJIYCCIJYRONP-UHFFFAOYSA-N 0.000 claims abstract description 19
- 229960004427 isradipine Drugs 0.000 claims abstract description 19
- 239000000203 mixture Substances 0.000 claims abstract description 13
- 238000003756 stirring Methods 0.000 claims abstract description 10
- 238000010438 heat treatment Methods 0.000 claims abstract description 9
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 claims description 54
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 claims description 33
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 claims description 33
- IAZDPXIOMUYVGZ-UHFFFAOYSA-N Dimethylsulphoxide Chemical compound CS(C)=O IAZDPXIOMUYVGZ-UHFFFAOYSA-N 0.000 claims description 26
- 230000001631 hypertensive effect Effects 0.000 claims description 21
- QZVCTJOXCFMACW-UHFFFAOYSA-N Phenoxybenzamine Chemical compound C=1C=CC=CC=1CN(CCCl)C(C)COC1=CC=CC=C1 QZVCTJOXCFMACW-UHFFFAOYSA-N 0.000 claims description 19
- 229960003418 phenoxybenzamine Drugs 0.000 claims description 19
- GJSURZIOUXUGAL-UHFFFAOYSA-N Clonidine Chemical compound ClC1=CC=CC(Cl)=C1NC1=NCCN1 GJSURZIOUXUGAL-UHFFFAOYSA-N 0.000 claims description 18
- 229960002896 clonidine Drugs 0.000 claims description 18
- 238000011282 treatment Methods 0.000 claims description 16
- -1 crow draw place Chemical compound 0.000 claims description 15
- ZTHYODDOHIVTJV-UHFFFAOYSA-N Propyl gallate Chemical compound CCCOC(=O)C1=CC(O)=C(O)C(O)=C1 ZTHYODDOHIVTJV-UHFFFAOYSA-N 0.000 claims description 14
- LNTHITQWFMADLM-UHFFFAOYSA-N gallic acid Chemical compound OC(=O)C1=CC(O)=C(O)C(O)=C1 LNTHITQWFMADLM-UHFFFAOYSA-N 0.000 claims description 14
- NOOLISFMXDJSKH-UTLUCORTSA-N (+)-Neomenthol Chemical compound CC(C)[C@@H]1CC[C@@H](C)C[C@@H]1O NOOLISFMXDJSKH-UTLUCORTSA-N 0.000 claims description 13
- AXTGDCSMTYGJND-UHFFFAOYSA-N 1-dodecylazepan-2-one Chemical compound CCCCCCCCCCCCN1CCCCCC1=O AXTGDCSMTYGJND-UHFFFAOYSA-N 0.000 claims description 13
- NOOLISFMXDJSKH-UHFFFAOYSA-N DL-menthol Natural products CC(C)C1CCC(C)CC1O NOOLISFMXDJSKH-UHFFFAOYSA-N 0.000 claims description 13
- 229960001760 dimethyl sulfoxide Drugs 0.000 claims description 13
- 229960003639 laurocapram Drugs 0.000 claims description 13
- 229940041616 menthol Drugs 0.000 claims description 13
- 239000000230 xanthan gum Substances 0.000 claims description 13
- 235000010493 xanthan gum Nutrition 0.000 claims description 13
- 229920001285 xanthan gum Polymers 0.000 claims description 13
- 229940082509 xanthan gum Drugs 0.000 claims description 13
- 229920000161 Locust bean gum Polymers 0.000 claims description 11
- 239000002202 Polyethylene glycol Substances 0.000 claims description 11
- 239000004283 Sodium sorbate Substances 0.000 claims description 11
- GVJHHUAWPYXKBD-UHFFFAOYSA-N d-alpha-tocopherol Natural products OC1=C(C)C(C)=C2OC(CCCC(C)CCCC(C)CCCC(C)C)(C)CCC2=C1C GVJHHUAWPYXKBD-UHFFFAOYSA-N 0.000 claims description 11
- 239000000711 locust bean gum Substances 0.000 claims description 11
- 235000010420 locust bean gum Nutrition 0.000 claims description 11
- 229920001223 polyethylene glycol Polymers 0.000 claims description 11
- LROWVYNUWKVTCU-STWYSWDKSA-M sodium sorbate Chemical compound [Na+].C\C=C\C=C\C([O-])=O LROWVYNUWKVTCU-STWYSWDKSA-M 0.000 claims description 11
- 235000019250 sodium sorbate Nutrition 0.000 claims description 11
- 239000011732 tocopherol Substances 0.000 claims description 11
- 235000010384 tocopherol Nutrition 0.000 claims description 11
- 229960001295 tocopherol Drugs 0.000 claims description 11
- 229930003799 tocopherol Natural products 0.000 claims description 11
- GVJHHUAWPYXKBD-IEOSBIPESA-N α-tocopherol Chemical compound OC1=C(C)C(C)=C2O[C@@](CCC[C@H](C)CCC[C@H](C)CCCC(C)C)(C)CCC2=C1C GVJHHUAWPYXKBD-IEOSBIPESA-N 0.000 claims description 11
- 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 claims description 9
- 229920002907 Guar gum Polymers 0.000 claims description 9
- 239000000665 guar gum Substances 0.000 claims description 9
- 235000010417 guar gum Nutrition 0.000 claims description 9
- 229960002154 guar gum Drugs 0.000 claims description 9
- WXMKPNITSTVMEF-UHFFFAOYSA-M sodium benzoate Chemical compound [Na+].[O-]C(=O)C1=CC=CC=C1 WXMKPNITSTVMEF-UHFFFAOYSA-M 0.000 claims description 9
- 239000004299 sodium benzoate Substances 0.000 claims description 9
- 235000010234 sodium benzoate Nutrition 0.000 claims description 9
- 239000000600 sorbitol Substances 0.000 claims description 9
- 238000001816 cooling Methods 0.000 claims description 8
- 235000004515 gallic acid Nutrition 0.000 claims description 7
- 229940074391 gallic acid Drugs 0.000 claims description 7
- 239000003292 glue Substances 0.000 claims description 7
- LHGVFZTZFXWLCP-UHFFFAOYSA-N guaiacol Chemical compound COC1=CC=CC=C1O LHGVFZTZFXWLCP-UHFFFAOYSA-N 0.000 claims description 7
- 239000000473 propyl gallate Substances 0.000 claims description 7
- 235000010388 propyl gallate Nutrition 0.000 claims description 7
- 229940075579 propyl gallate Drugs 0.000 claims description 7
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims description 7
- 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 claims description 6
- 230000002421 anti-septic effect Effects 0.000 claims description 4
- 239000003963 antioxidant agent Substances 0.000 claims description 4
- 230000003078 antioxidant effect Effects 0.000 claims description 4
- 239000003623 enhancer Substances 0.000 claims description 4
- 239000002562 thickening agent Substances 0.000 claims description 4
- 239000000080 wetting agent Substances 0.000 claims description 4
- 239000003814 drug Substances 0.000 abstract description 19
- 230000000694 effects Effects 0.000 abstract description 7
- 206010019233 Headaches Diseases 0.000 abstract description 5
- 231100000869 headache Toxicity 0.000 abstract description 5
- 208000024891 symptom Diseases 0.000 abstract description 2
- 208000012886 Vertigo Diseases 0.000 abstract 1
- 238000000227 grinding Methods 0.000 abstract 1
- 238000002156 mixing Methods 0.000 abstract 1
- 238000007873 sieving Methods 0.000 abstract 1
- 231100000889 vertigo Toxicity 0.000 abstract 1
- 229940079593 drug Drugs 0.000 description 8
- ICMGLRUYEQNHPF-UHFFFAOYSA-N Uraprene Chemical compound COC1=CC=CC=C1N1CCN(CCCNC=2N(C(=O)N(C)C(=O)C=2)C)CC1 ICMGLRUYEQNHPF-UHFFFAOYSA-N 0.000 description 7
- 229960001130 urapidil Drugs 0.000 description 7
- HEDRZPFGACZZDS-UHFFFAOYSA-N Chloroform Chemical compound ClC(Cl)Cl HEDRZPFGACZZDS-UHFFFAOYSA-N 0.000 description 6
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 6
- 208000002173 dizziness Diseases 0.000 description 5
- RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 description 4
- 239000011230 binding agent Substances 0.000 description 4
- 238000006243 chemical reaction Methods 0.000 description 3
- 239000000843 powder Substances 0.000 description 3
- 230000002792 vascular Effects 0.000 description 3
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 3
- 208000012895 Gastric disease Diseases 0.000 description 2
- 206010031127 Orthostatic hypotension Diseases 0.000 description 2
- 230000017531 blood circulation Effects 0.000 description 2
- 230000003130 cardiopathic effect Effects 0.000 description 2
- 208000017169 kidney disease Diseases 0.000 description 2
- 208000019423 liver disease Diseases 0.000 description 2
- 210000001013 sinoatrial node Anatomy 0.000 description 2
- 230000007480 spreading Effects 0.000 description 2
- 208000018556 stomach disease Diseases 0.000 description 2
- 230000035488 systolic blood pressure Effects 0.000 description 2
- 230000024883 vasodilation Effects 0.000 description 2
- 206010002383 Angina Pectoris Diseases 0.000 description 1
- 229940127291 Calcium channel antagonist Drugs 0.000 description 1
- 206010010774 Constipation Diseases 0.000 description 1
- 208000000059 Dyspnea Diseases 0.000 description 1
- 206010013975 Dyspnoeas Diseases 0.000 description 1
- 208000010228 Erectile Dysfunction Diseases 0.000 description 1
- 206010028748 Nasal obstruction Diseases 0.000 description 1
- 206010041349 Somnolence Diseases 0.000 description 1
- 208000001871 Tachycardia Diseases 0.000 description 1
- 206010000059 abdominal discomfort Diseases 0.000 description 1
- 230000002159 abnormal effect Effects 0.000 description 1
- 238000010521 absorption reaction Methods 0.000 description 1
- 230000009471 action Effects 0.000 description 1
- 206010002906 aortic stenosis Diseases 0.000 description 1
- 230000006793 arrhythmia Effects 0.000 description 1
- 206010003119 arrhythmia Diseases 0.000 description 1
- 210000001367 artery Anatomy 0.000 description 1
- 230000008901 benefit Effects 0.000 description 1
- 230000036772 blood pressure Effects 0.000 description 1
- 210000004204 blood vessel Anatomy 0.000 description 1
- 239000002775 capsule Substances 0.000 description 1
- 230000008859 change Effects 0.000 description 1
- 238000007796 conventional method Methods 0.000 description 1
- 239000003218 coronary vasodilator agent Substances 0.000 description 1
- 210000004351 coronary vessel Anatomy 0.000 description 1
- 230000006378 damage Effects 0.000 description 1
- 230000002950 deficient Effects 0.000 description 1
- 230000035487 diastolic blood pressure Effects 0.000 description 1
- 125000004925 dihydropyridyl group Chemical group N1(CC=CC=C1)* 0.000 description 1
- 201000010099 disease Diseases 0.000 description 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 1
- 206010013781 dry mouth Diseases 0.000 description 1
- 201000001881 impotence Diseases 0.000 description 1
- 230000006872 improvement Effects 0.000 description 1
- 238000002347 injection Methods 0.000 description 1
- 239000007924 injection Substances 0.000 description 1
- 210000003734 kidney Anatomy 0.000 description 1
- 230000003908 liver function Effects 0.000 description 1
- 238000000034 method Methods 0.000 description 1
- 230000004048 modification Effects 0.000 description 1
- 238000012986 modification Methods 0.000 description 1
- 208000010125 myocardial infarction Diseases 0.000 description 1
- 210000005259 peripheral blood Anatomy 0.000 description 1
- 239000011886 peripheral blood Substances 0.000 description 1
- 239000011505 plaster Substances 0.000 description 1
- 230000004044 response Effects 0.000 description 1
- 238000007086 side reaction Methods 0.000 description 1
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- 210000001562 sternum Anatomy 0.000 description 1
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Landscapes
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
The invention relates to a western medicament ointment for treating high blood pressure and preparation method thereof, wherein the ointment contains 10 to 60 weight parts of reactive compounds including isradipine. The preparation method comprises the following steps of: 1) mixing base materials in percentage by weight, heating the mixture at 60 to 90 DEG C and stirring to dissolve the mixture; 2) grinding and sieving the reactive compounds, then adding the reactive compounds into the mixture obtained by the step 1) and stirring for 15 to 25 minutes, and lowering the temperature to 20 to 60 DEG C to obtain finished products. The ointment can be absorbed by human body through skin, and the synergy of active compounds can greatly improve the bioavailability of the ointment; moreover, the ointment has a great degree of security and a few side effects and avoids the symptoms including headache, vertigo, cardiopalmus and face flush basically.
Description
[technical field]
The present invention relates to treat hypertensive medicine and preparation, relate to a kind of hypertensive ointment and preparation method thereof that is used for the treatment of specifically.
[background technology]
At present, be used for the treatment of hypertensive medicine two kinds in Chinese medicine and Western medicine arranged.Wherein being used for the treatment of the oral form of the most employings of hypertensive Western medicine is absorbed by the body, as everyone knows, Chinese medicine adopts oral mode lighter relatively to the harm of human body, and in a single day Western medicine enters human body, can be to human body generation side reaction in various degree, such as: because the headache due to the vasodilation, dizzy, cardiopalmus, flush etc., severe patient can cause fatal.In addition, the hypertensive medicine of most treatments will consider other diseases of patient, and the hypertension scope of medication to patient has caused great restriction like this, even when patient's symptom complexity, can not medication, to such an extent as to can't treat.
Isradipine is the dihydropyridines calcium antagonists, and oral post-absorption is good, but the side effect of oral generation is: mainly be because the headache due to the vasodilation, dizzy, cardiopalmus, flush etc.; Accidental abnormal liver function, and of short duration when being, gastrointestinal upset etc. appears sometimes; Aortic stenosis, the sick syndrome of sinuatrial node and the low careful usefulness of systolic pressure patient.
Urapidil is white or yellow crystalline powder slightly, easily holds in chloroform, dissolves slightly soluble in water or ether in ethanol; Untoward reaction after it is oral: dizzy, perspire, be on tenterhooks, constriction and dyspnea etc. after the tired cardiopalmus, arrhythmia, breastbone.
Cola is decided to be white crystalline powder, in water or ethanol, dissolves, and soluble,very slightly in chloroform, almost insoluble in ether; Untoward reaction after it is oral: drowsiness, dry mouth and constipation, idol has postural hypotension and sexual impotence.
Application number has been CN200510090104.7, denomination of invention for the patent application patent disclosure of " clonidine, weekly-effect, skin-permeable and control-released plaster " percutaneous dosing, but its time with the compatible stable performance release of skin only be 7 days, wherein the effect of Pi Luing haves much room for improvement.
Phenoxybenzamine is white or off-white color crystalline powder, and is almost tasteless, easily molten in ethanol or chloroform, soluble,very slightly in water.Untoward reaction such as its oral back postural hypotension, nasal obstruction and tachycardia.Idol can cause angina pectoris or myocardial infarction.
[summary of the invention]
The objective of the invention is to overcome the above-mentioned defective that prior art exists, a kind of ointment that is used for the treatment of hypertensive through the skin administration that provides, and it is fast that the synergism between the reactive compound makes that this ointment absorbs, bioavailability improves, safety, side effect is little, seldom has the situation of headache, dizzy, cardiopalmus, flush to take place.
A kind of hypertensive ointment that is used for the treatment of provided by the invention, wherein said ointment comprise that reactive compound isradipine, crow draw place, clonidine, phenoxybenzamine and base material; Percentage meter by weight wherein, reactive compound is 10-60%.
Provided by the inventionly be used for the treatment of hypertensive preferred ointment, described ointment is the percentage meter by weight, reactive compound: isradipine 2-20%, crow are drawn place 5-13%, clonidine 1-10%, phenoxybenzamine 2-17%; Base material 40-90%.
Provided by the inventionly be used for the treatment of a hypertensive preferred ointment again, described ointment is the percentage meter by weight, reactive compound: isradipine 5-16%, crow are drawn place 7-10%, clonidine 3-7%, phenoxybenzamine 5-13%; Base material 55-80%.
The hypertensive the 3rd preferred ointment that is used for the treatment of provided by the invention, it is its hydrochlorate that described crow is drawn place, clonidine, phenoxybenzamine.
Provided by the inventionly be used for the treatment of hypertensive ointment, described base material comprises one or more the mixture that is selected from arbitrarily in wetting agent, antiseptic, antioxidant, thickening agent and the transdermal enhancer:
Wetting agent: propylene glycol, Polyethylene Glycol, glycerol, pyrrolidone sodium carboxylate, sorbitol and glycerol;
Antiseptic: parabens, sodium benzoate and citric acid;
Antioxidant: ditertbutylparacresol, tert-butyl group hydroxyanisol, gallic acid, propyl gallate, sodium sorbate and tocopherol;
Thickening agent: xanthan gum, guar gum, cover its glue, locust bean gum and Radix Acaciae senegalis;
Transdermal enhancer: menthol, dimethyl sulfoxide and laurocapram.
A kind of preparation method that is used for the treatment of hypertensive ointment provided by the invention comprises the steps:
1), the base material of described weight percent meter is mixed, in 60-90 ℃ of heating, stirring and dissolving;
2), with reactive compound grind sieve after, add in the mixture that step 1) obtains and stirred 15-25 minute, greenhouse cooling is got product to 20-60 ℃.
In the technique scheme:
The structural formula of reactive compound isradipine (Isradipine):
The structural formula of reactive compound clonidine (Clonidine):
The structural formula of reactive compound urapidil (Urapidil):
The structural formula of reactive compound phenoxybenzamine (Phenoxybenzamine)
Isradipine is to the selectivity height of blood vessel, can the diastole peripheral blood vessel, coronary vasodilator and cerebrovascular, and less to action of the heart, only suppress the spontaneous activity of sinuatrial node, can make blood pressure drops; Urapidil energy diastole small artery reduces the external resistance, and systolic pressure and diastolic pressure are descended; In addition, urapidil can improve blood circulation, increases the kidney blood flow, reduces renal vascular resistance.
Described base material also can select pharmaceutically acceptable other to can be used for the base material of ointment except that enumerating.Between the described reactive compound synergism can take place, make ointment of the present invention by spreading upon on the human body skin, play the hypertensive effect of treatment, reduced the side effect of Western medicine to human body, in addition, smear the mode that adopts percutaneous dosing, improved the degree of safety of drug utilization.
Compared with prior art, a kind of hypertensive ointment that is used for the treatment of provided by the invention has the following advantages:
1, between the reactive compound synergism can take place, absorb soon, make bioavailability improve greatly.
2, degree of safety is big, and side effect is little.
3, seldom there is the situation of headache, dizzy, cardiopalmus, flush to take place.
4, by spreading upon on the human body skin, play the hypertensive effect of treatment and reduced the side effect of Western medicine human body, improved the degree of safety of drug utilization.
5, be not subjected to the influence of other body illnesses of patient, reduced the limitation that part patient can not medication.
[specifically implementing antimode]
[test 1]
Randomly draw 3200 hyperpietics that meet inclusion criteria (patient only suffers from vascular hypertension, does not have the situation of suffering from nephropathy and hepatopathy) and experimentize, and it is divided into four groups: group 1: adopt ointment of the present invention; Group 2 is to adopt prior art to treat hypertensive tablet separately; Group 3 adopts prior art to treat hypertensive capsule; Group 4: adopt prior art to treat hypertensive injection; Every group of patient's dosage is identical, is 15mg/ days, medication after 3 months concrete test situation see Table 1:
Table 1 respectively to organize 1, group 2, group 3 and organize 4 patients' result of the test
[test 2]
Ointment of the present invention suffered from 1000 hypertensively have cardiopathic patient, 1000 simultaneously concurrently and suffer from and hypertensively have migrainous patient and 1000 simultaneously concurrently to suffer from the hypertensive patients that have gastropathy simultaneously concurrently on probation, every group of patient's dosage is identical, be 15mg/ days, the situation of following up a case by regular visits to after patient's medication sees the following form 2:
Patient's response situation behind table 2 ointment of the present invention on probation
| The number that the former state of an illness increases the weight of | The state of an illness does not have influence | Hypertension is cured responding time | |
| 1000 have cardiopathic patient | 5 | 995 | 1 year |
| 1000 have migrainous patient | 2 | 998 | Half a year |
| 1000 have gastropathy | 1 | 999 | 2 years |
[test 3]
Randomly draw and meet 2000 hyperpietics of inclusion criteria (patient only suffers from vascular hypertension, does not have the situation of suffering from nephropathy and hepatopathy) and experimentize, and it is divided into four groups: group 1: adopt ointment of the present invention; Group 2: adopt the isradipine ointment separately; Group 3: adopt the urapidil ointment separately; Group 4: independent clonidine ointment; Group 5: adopt the phenoxybenzamine ointment separately; Wherein adopt conventional method respectively above-mentioned four kinds of materials to be made ointment; To patient's medication, the dosage of at every turn smearing is identical by the mode of smearing, and smears the concrete test situation of back patient and sees Table 3:
| The time that discharges with the compatible stable performance of skin | Bioavailability | |
| Group 1 (adopting ointment of the present invention); | 10 days | 21％ |
| Group 2 (adopting the isradipine ointment separately) | 5 days | 16.7％ |
| Group 3 (adopting the urapidil ointment separately) | 4 days | 12.1％ |
| Group 4 (clonidine ointment separately) | 7 days | 13.7％ |
| Group 5 (adopting the phenoxybenzamine ointment separately) | 3 days | 12.6％ |
[embodiment 1]
The ointment of present embodiment is by being prepared from by the following component of percentage by weight:
Isradipine 2%, crow are drawn place 5%, clonidine 1%, phenoxybenzamine 2%; With the base material 90% that comprises sorbitol, glycerol, parabens, ditertbutylparacresol, tert-butyl group hydroxyanisol, gallic acid, xanthan gum, locust bean gum, Radix Acaciae senegalis, menthol, dimethyl sulfoxide and laurocapram.
Wherein the binder volume ratio is:
Sorbitol 0.2%, glycerol 0.03%, parabens 0.75%, ditertbutylparacresol 0.036%, tert-butyl group hydroxyanisol 0.05%, gallic acid 0.01%, xanthan gum 0.5%, locust bean gum 0.19%, Radix Acaciae senegalis 0.027%, menthol 0.005%, dimethyl sulfoxide 0.32% and laurocapram 0.15%.
The preparation method of ointment comprises the steps:
1), the base material of described weight percent meter is mixed, in 60 ℃ of heating, stirring and dissolving;
2), with reactive compound grind sieve after, add in the mixture that step 1) obtains and stirred 15 minutes, greenhouse cooling to 20 ℃ is got product.
[embodiment 2]
The ointment of present embodiment is by being prepared from by the following component of percentage by weight:
Isradipine 20%, crow draw place 13%, clonidine 10%, phenoxybenzamine 17% and comprise propylene glycol, Polyethylene Glycol, glycerol, pyrrolidone sodium carboxylate, sorbitol, glycerol, parabens, sodium benzoate, citric acid, ditertbutylparacresol, tert-butyl group hydroxyanisol, gallic acid, propyl gallate, sodium sorbate, tocopherol, xanthan gum, guar gum, cover its glue, base material 40% that locust bean gum, Radix Acaciae senegalis, menthol, dimethyl sulfoxide and laurocapram are formed.
Wherein said binder volume ratio is:
Propylene glycol 0.005%, Polyethylene Glycol 0.03%, glycerol 0.07%, pyrrolidone sodium carboxylate 0.0065%, sorbitol 0.35%, glycerol 0.57%, parabens 0.15%, sodium benzoate 0.85%, citric acid 0.054%, ditertbutylparacresol 0.025%, tert-butyl group hydroxyanisol 0.035%, gallic acid 0.05%, propyl gallate 0.055%, sodium sorbate 0.15%, tocopherol 0.45%, xanthan gum 0.5%, guar gum 0.4%, cover its glue 0.15%, locust bean gum 0.02%, Radix Acaciae senegalis 0.052%, menthol 0.051%, dimethyl sulfoxide 0.053% and laurocapram 0.09%.
The preparation method of ointment is as follows:
1), the base material with described weight percent meter mixes heating, stirring and dissolving under 90 ℃;
2), with reactive compound grind sieve after, add in the mixture that step 1) obtains and stirred 25 minutes, greenhouse cooling to 60 ℃ is got product.
[embodiment 3]
The ointment of present embodiment is by being prepared from by the following component of percentage by weight:
Isradipine 5%, crow are drawn place 7%, clonidine 3%, phenoxybenzamine 5%; With comprise the base material of forming by propylene glycol, Polyethylene Glycol, sorbitol, glycerol, parabens, citric acid, ditertbutylparacresol, propyl gallate, sodium sorbate, tocopherol, xanthan gum, locust bean gum, Radix Acaciae senegalis, menthol, dimethyl sulfoxide and laurocapram 70%.
Wherein said binder volume ratio is:
Propylene glycol 0.11%, Polyethylene Glycol 0.17%, sorbitol 0.21%, glycerol 0.061%, parabens 0.05%, citric acid 0.03%; Ditertbutylparacresol 0.02%, propyl gallate 0.12%, sodium sorbate 0.19%, tocopherol 0.21%, xanthan gum 0.1%, locust bean gum and Radix Acaciae senegalis 0.06%, menthol 0.071%, dimethyl sulfoxide 0.06% and laurocapram 0.28%.
The preparation method of ointment comprises the steps:
1), the base material of described weight percent meter is mixed, in 50 ℃ of heating, stirring and dissolving;
2), with reactive compound grind sieve after, add in the mixture that step 1) obtains and stirred 17 minutes, greenhouse cooling to 40 ℃ is got product.
[embodiment 4]
The ointment of present embodiment is by being prepared from by the following component of percentage by weight:
Isradipine 16%, crow are drawn place 10%, clonidine 7%, phenoxybenzamine 13%; With comprise propylene glycol, Polyethylene Glycol, glycerol, pyrrolidone sodium carboxylate, parabens, sodium benzoate, citric acid, ditertbutylparacresol, sodium sorbate, tocopherol; Xanthan gum, guar gum, cover its glue, locust bean gum and Radix Acaciae senegalis, menthol, dimethyl sulfoxide and laurocapram are at interior base material 54%.
Wherein said binder volume ratio is:
Propylene glycol 0.26%, Polyethylene Glycol 0.2%, glycerol 0.03%, pyrrolidone sodium carboxylate 0.17%, parabens 0.003%, sodium benzoate 0.023%, citric acid 0.005%, ditertbutylparacresol 0.22%, sodium sorbate 0.035%, tocopherol 0.071%, xanthan gum 0.003%, guar gum 0.046%, cover its glue 0.001%, locust bean gum and Radix Acaciae senegalis 0.1%, menthol 0.041%, dimethyl sulfoxide 0.037% and laurocapram 0.04%.
The preparation method of ointment comprises the steps:
The preparation method of ointment comprises the steps:
1), the base material with described weight percent meter mixes heating, stirring and dissolving under 50 ℃;
2), with reactive compound grind sieve after, add in the mixture that step 1) obtains and stirred 17 minutes, greenhouse cooling to 40 ℃ is got product.
[embodiment 5]
The ointment of present embodiment is by being prepared from by the following component of percentage by weight:
13 parts of isradipine, crow are drawn 10 parts at place, 7 parts of clonidines, 5 parts of phenoxybenzamine; With comprise propylene glycol, Polyethylene Glycol, glycerol, sodium benzoate, citric acid, ditertbutylparacresol, sodium sorbate, tocopherol; Xanthan gum, guar gum, Radix Acaciae senegalis, menthol, dimethyl sulfoxide and laurocapram are 55 parts of interior base materials.
Wherein the volume ratio of said base material is:
Propylene glycol 0.025%, Polyethylene Glycol 0.031%, glycerol 0.07%, sodium benzoate 0.2%, citric acid 0.013%, ditertbutylparacresol 0.06%, sodium sorbate 0.08%, tocopherol 0.023%; Xanthan gum 0.035%, guar gum 0.073%, Radix Acaciae senegalis 0.062%, menthol 0.026%, dimethyl sulfoxide 0.013% and laurocapram 0.05%.
The preparation method of ointment comprises the steps:
1), the base material of described weight percent meter is mixed, in 70 ℃ of heating, stirring and dissolving;
2), with reactive compound grind sieve after, add in the mixture that step 1) obtains and stirred 20 minutes, greenhouse cooling to 30 ℃ is got product.
[embodiment 6]
The ointment of present embodiment is by being prepared from by the following component of percentage by weight:
Isradipine 2%, crow is drawn place 5%, clonidine 1%, phenoxybenzamine 2%, with comprise by the formulated base material 80% of following material that is 0.23% ratio by volume: propylene glycol, Polyethylene Glycol, glycerol, pyrrolidone sodium carboxylate, sorbitol, glycerol, parabens, sodium benzoate, citric acid, ditertbutylparacresol, tert-butyl group hydroxyanisol, gallic acid, propyl gallate, sodium sorbate, tocopherol, xanthan gum, guar gum, cover its glue, locust bean gum, Radix Acaciae senegalis, menthol, dimethyl sulfoxide and laurocapram.
The preparation method of ointment comprises the steps:
1), the base material of described weight percent meter is mixed, in 80 ℃ of heating, stirring and dissolving;
2), with reactive compound grind sieve after, add in the mixture that step 1) obtains and stirred 20 minutes, greenhouse cooling to 50 ℃ is got product.
Should be noted that at last: above embodiment is only in order to illustrate that technical scheme of the present invention is not intended to limit; although the present invention is had been described in detail with reference to the foregoing description; those of ordinary skill in the field are to be understood that: the technical staff reads after the present specification still and can make amendment or be equal to replacement the specific embodiment of the present invention, but these modifications or change all do not break away within the claim protection domain that the present patent application awaits the reply.
Claims (6)
1. one kind is used for the treatment of hypertensive ointment, it is characterized in that described ointment comprises that reactive compound isradipine, crow draw place, clonidine, phenoxybenzamine and base material; Percentage meter by weight wherein, reactive compound is 10-60%.
2. according to the described ointment of claim 1, it is characterized in that described ointment percentage meter by weight, said reactive compound isradipine 2-20%, crow are drawn place 5-13%, clonidine 1-10% and phenoxybenzamine 2-17%; Base material 40-90%.
3. according to the described ointment of claim 1, it is characterized in that described ointment percentage meter by weight, said reactive compound isradipine 5-16%, crow are drawn place 7-10%, clonidine 3-7% and phenoxybenzamine 5-13%; Base material 55-80%.
4. according to claim 1 or 2 or 3 described ointments, it is characterized in that it is its hydrochlorate that described reactive compound crow is drawn place, clonidine and phenoxybenzamine.
5. according to the described ointment of claim 1, it is characterized in that described base material comprises one or more the mixture that is selected from arbitrarily in wetting agent, antiseptic, antioxidant, thickening agent and the transdermal enhancer:
Wetting agent: propylene glycol, Polyethylene Glycol, glycerol, pyrrolidone sodium carboxylate, sorbitol and glycerol;
Antiseptic: parabens, sodium benzoate and citric acid;
Antioxidant: ditertbutylparacresol, tert-butyl group hydroxyanisol, gallic acid, propyl gallate, sodium sorbate and tocopherol;
Thickening agent: xanthan gum, guar gum, cover its glue, locust bean gum and Radix Acaciae senegalis;
Transdermal enhancer: menthol, dimethyl sulfoxide and laurocapram.
6. the preparation method according to the described ointment of claim 1 comprises the steps:
1), the base material of described weight percent meter is mixed, in 60-90 ℃ of heating, stirring and dissolving;
2), with reactive compound grind sieve after, add in the mixture that step 1) obtains and stirred 15-25 minute, greenhouse cooling is got product to 20-60 ℃.
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| CN 201010255704 CN101947222A (en) | 2010-08-18 | 2010-08-18 | Ointment for treating high blood pressure and preparation method thereof |
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| CN 201010255704 CN101947222A (en) | 2010-08-18 | 2010-08-18 | Ointment for treating high blood pressure and preparation method thereof |
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103142467A (en) * | 2013-03-21 | 2013-06-12 | 青岛正大海尔制药有限公司 | Calcitriol ointment and preparation method thereof |
| CN108686214A (en) * | 2017-04-05 | 2018-10-23 | 四川科瑞德制药股份有限公司 | Compound antihypertensive drug composition and application thereof |
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| CN1457787A (en) * | 2003-06-25 | 2003-11-26 | 袁重华 | Coating agent for reducing high blood pressure and its use |
| CN101365445A (en) * | 2005-11-08 | 2009-02-11 | 弧离子治疗公司 | Treatment of length dependent neuropathy |
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Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1457787A (en) * | 2003-06-25 | 2003-11-26 | 袁重华 | Coating agent for reducing high blood pressure and its use |
| CN101365445A (en) * | 2005-11-08 | 2009-02-11 | 弧离子治疗公司 | Treatment of length dependent neuropathy |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103142467A (en) * | 2013-03-21 | 2013-06-12 | 青岛正大海尔制药有限公司 | Calcitriol ointment and preparation method thereof |
| CN103142467B (en) * | 2013-03-21 | 2014-07-02 | 青岛正大海尔制药有限公司 | Calcitriol ointment and preparation method thereof |
| CN108686214A (en) * | 2017-04-05 | 2018-10-23 | 四川科瑞德制药股份有限公司 | Compound antihypertensive drug composition and application thereof |
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