CN1827110A - Pharmaceutical composition using hydrochlorothiazide and benazepril hydrochloride as active ingredients, its preparation method and use - Google Patents
Pharmaceutical composition using hydrochlorothiazide and benazepril hydrochloride as active ingredients, its preparation method and use Download PDFInfo
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- CN1827110A CN1827110A CN 200610075611 CN200610075611A CN1827110A CN 1827110 A CN1827110 A CN 1827110A CN 200610075611 CN200610075611 CN 200610075611 CN 200610075611 A CN200610075611 A CN 200610075611A CN 1827110 A CN1827110 A CN 1827110A
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- hydrochlorothiazide
- benazepril hydrochloride
- pharmaceutical composition
- active component
- benazepril
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Abstract
This invention is about a medicine composition taking hydrochlorothiazide and hydrochloric acid benapuli as active component and its preparing method and usages. It takes hydrochlorothiazide and hydrochloric acid benapuli as medicine active component, and is formed by mixing acceptable finding. It can be used to cure miscellaneous tapping hypertensions. It uses hydrochlorothiazide and hydrochloric acid benapuli as raw materials and adds some findings those have specified kinds and ratios. Developing troche, capsule, dispersing tablets, soft capsule, chewing tablets, buccal tablets, droplet, and other oral preparations according to the method in this invention.
Description
Technical field
The present invention relates to a kind of is Pharmaceutical composition of active component and preparation method thereof, purposes with hydrochlorothiazide and benazepril hydrochloride, belongs to medical technical field.
Background technology
Along with the change of the raising of people's living standard and diet structure, life style, the incidence rate of hypertension has the trend that progressively increases in recent years.Hypertension can cause organ injuries such as patient's heart, brain, kidney, and with sugar, lipid metabolic disorder and diabetes substantial connection is arranged, and obviously reduces patients ' life quality, when serious even threat to life.Therefore, more and more cause the attention of Chinese scholars about the research of hypertension incidence mechanism and medicine.
Benazepril hydrochloride can suppress the Angiotensin-Converting activity, reduces the Angiotensin II level, diastole small artery blood vessel.Polytype hypertension is all had tangible hypotensive effect, and can improve the cardiac function of patients with congestive heart failure.Its pharmacological action is mainly reflected in two aspects.(1) blood pressure lowering: this product is hydrolyzed to benazeprilat in liver, becomes a kind of emulative angiotensin converting enzyme inhibitor, and the prevention angiotensin i-converting is an Angiotensin II, and vascular resistance is reduced, and the aldosterone secretion reduces, and plasma renin activity increases.Benazeprilat also suppresses the degraded of Kallidin I, and vascular resistance is reduced, and produces hypotensive effect.(2) lower cardiac load: this product expansion artery and vein, reduce peripheral vascular resistance or cardiac afterload, reduce pulmonary capillary embedding pressure or cardiac preload, also reduce pulmonary vascular resistance, thereby improve cardiac output, make exercise tolerance and time lengthening.
Hydrochlorothiazide is diuretic and the antihypertensive drugs of using always, and its effect is mainly reflected in following aspect: 1) can certain influence be arranged to water, electrolyte excretion.Therefore have: (1) diuresis.This product mechanism of action mainly suppresses the heavily absorption to sodium chloride of distal tubule leading portion and proximal tubule (acting on lighter), thereby increases the Na of distal tubule and collecting tubule
+-K
+Exchange, K
+Secretion increasing.Its mechanism of action is not clear fully as yet.And this product can both suppress the carbonic anhydrase activity to some extent, so can explain its effect to proximal tubule.This class medicine can also suppress phosphodiesterase activity, reduces picked-up and the mitochondrion oxygen consumption of renal tubules to fatty acid, thereby suppresses renal tubules to Na
+, Cl
-Active heavily absorb.(2) hypotensive effect.Except that the effect of diuresis row sodium, may also have the outer mechanism of action of kidney to participate in blood pressure lowering, may be to increase gastrointestinal tract to Na
+Drainage.(2) to the influence of renal hemodynamics and glomerular filtration function.Because renal tubules is to water, Na
+Heavily absorb and reduce, the renal tubules internal pressure raises, and the water of the Distal convoluted tubule of flowing through and Na
+Increase, stimulate macula densa by the reflection of pipe-ball, feritin in the kidney, angiotensin secretion are increased, cause the kidney vasoconstriction, renal blood flow descends, and glomerule goal and efferent glomerular arteriole shrink, and glomerular filtration rate also descends.
The Pharmaceutical composition of described benazepril hydrochloride and hydrochlorothiazide is a compound preparation, and clinically, the use in conjunction of this two classes medicine is the most common, and the compound recipe that fixed dosage is formed is more.No matter the height of its plasma renin levels of hyperpietic behind this two classes drug combination, has played synergism to blood pressure drops.
Summary of the invention
Having the purpose of this invention is to provide a kind of is Pharmaceutical composition of active component and uses thereof with hydrochlorothiazide and benazepril hydrochloride.The present invention for a kind of be the Pharmaceutical composition of active component with hydrochlorothiazide and benazepril hydrochloride, it is characterized in that it is a hydrochlorothiazide and the active component of benazepril hydrochloride formation, with the Pharmaceutical composition of mixing acceptable accessories formation.
Above-mentioned a kind of be the Pharmaceutical composition of active component with hydrochlorothiazide and benazepril hydrochloride, wherein the consumption of hydrochlorothiazide is 5.0mg-37.5mg for per unit dosage.Be preferably 6.25mg-25mg.
Above-mentioned a kind of be the Pharmaceutical composition of active component with hydrochlorothiazide and benazepril hydrochloride, it is characterized in that the consumption of described benazepril hydrochloride is 2.5mg-20mg for per unit dosage.Be preferably 5mg-20mg.
Above-mentioned a kind of be the Pharmaceutical composition of active component with hydrochlorothiazide and benazepril hydrochloride, it is characterized in that the weight ratio of described hydrochlorothiazide and benazepril hydrochloride is 2.5: 1-0.5: 1, be preferably 2: 1-1: 1.
Described a kind of be the Pharmaceutical composition of active component with hydrochlorothiazide and benazepril hydrochloride, it is characterized in that the Pharmaceutical composition of described hydrochlorothiazide and benazepril hydrochloride is an oral formulations.
Described a kind of be the Pharmaceutical composition of active component with hydrochlorothiazide and benazepril hydrochloride, it is characterized in that described oral formulations can be made into tablet, capsule, dispersible tablet, soft capsule, chewable tablet, oral cavity disintegration tablet, drop pill etc.
The specific embodiment
Come hydrochlorothiazide of the present invention and benazepril hydrochloride preparation done further specifying by following example, but be not limited in following example.
Embodiment 1 hydrochlorothiazide and Benazepril hydrochloride contents in tablets agent
Prescription:
| Component | Consumption |
| Hydrochioro benazepril hydrochloride microcrystalline cellulose pregelatinized starch lactose CMS-Na superfine silica gel powder dolomol 95% ethanol | 12.5g 10g 60g 25g 30g 4g 4g 2.5g is an amount of |
| Make altogether | 1000 |
Preparation method:
Hydrochlorothiazide, benazepril hydrochloride, microcrystalline Cellulose, pregelatinized Starch, lactose are crossed 80 mesh sieves respectively, behind the mix homogeneously, add 95% ethanol and make soft material in right amount, 20 mesh sieves are granulated, drying, 18 mesh sieve granulate add magnesium stearate, CMS-Na, micropowder silica gel, adopt suitable punch die compressed tablets behind the mix homogeneously, promptly.
Embodiment 2: hydrochlorothiazide and benazepril hydrochloride capsule
Prescription:
| Component | Consumption |
| Hydrochioro benazepril hydrochloride dextrin starch CMS-Na 2%PVP-k30 aqueous solution dolomol | 12.5g an amount of 1.5g of 10g 20g 60g 2.0g |
Preparation method:
Hydrochlorothiazide, benazepril hydrochloride, dextrin, starch are crossed 80 mesh sieves respectively, behind the mix homogeneously, add the 0.5%PVP-k30 aqueous solution and make soft material in right amount, 24 mesh sieves are granulated, dry, 24 mesh sieve granulate add CMS-Na, the magnesium stearate of recipe quantity, in the suitable capsule shells of packing into behind the mix homogeneously promptly.
Embodiment 3: hydrochlorothiazide and benazepril hydrochloride dispersible tablet
Prescription:
| Component | Consumption |
| Hydrochioro benazepril hydrochloride micro crystal cellulose milk sugar CMS-Na 50% ethanolic solution altogether Zhi becomes | 12.5g an amount of 1000 of 10g 80g 40g 9g |
Preparation method:
Hydrochlorothiazide, benazepril hydrochloride, microcrystalline Cellulose, lactose are crossed 80 mesh sieves respectively, behind the mix homogeneously, add 50% alcoholic solution and make soft material in right amount, 24 mesh sieves are granulated, drying, and 20 mesh sieve granulate add disintegrating agent CMS-Na, tabletting behind the mix homogeneously, promptly.
Embodiment 4: hydrochlorothiazide and benazepril hydrochloride soft capsule
Prescription:
| Component | Consumption |
| Hydrochlorothiazide benazepril hydrochloride PEG400 water propylene glycol is made altogether | 2.5g 1000 of 10g 210g 10g 10g |
Preparation method:
Earlier will about 10%PEG400 and the water of recipe quantity be heated to 40-60 ℃, after the adding hydrochlorothiazide stirs and makes dissolving fully, continue to add about 70%PEG400, benazepril hydrochloride, the same stirring makes dissolving, the propylene glycol that adds recipe quantity again, after stirring, continue and add surplus PEG400, obtain clear and bright solution; Adjust content weight, compacting, promptly.
Embodiment 5: hydrochlorothiazide and benazepril hydrochloride chewable tablet
Prescription
| Component | Consumption |
| Hydrochlorothiazide | 12.5g |
| Benazepril hydrochloride sweet mellow wine microcrystalline cellulose Stevioside lemon powdered flavor 2%PVP-K30 50% ethanolic solution altogether Zhi becomes | An amount of 1000 of 10g 50g 170g 6g 2g |
Preparation method:
To all cross hydrochlorothiazide, benazepril hydrochloride, microcrystalline Cellulose, the mannitol mix homogeneously of 80 mesh sieves, with 0.5%PVP-K30 alcoholic solution system soft material, 16 mesh sieves are granulated, dry, 12 mesh sieve granulate add stevioside, Fructus Citri Limoniae powdered flavor, mix homogeneously, tabletting gets final product.
Embodiment 6: hydrochlorothiazide and benazepril hydrochloride oral cavity disintegration tablet
Prescription
| Component | Consumption |
| Hydrochlorothiazide | 12.5g |
| Benazepril hydrochloride PPVP CMS-Na L-HPC sweet mellow wine xylitol Aspartame lemon extract 50% ethanolic solution talcum powder altogether Zhi becomes | 1000 of an amount of 1.5g of 10g 5g 2.5g 2.5g 150g 60g 3.5g 2.5g |
Preparation method:
With all crossing hydrochlorothiazide, benazepril hydrochloride, mannitol, aspartame, Fructus Citri Limoniae essence, L-HPC, PPVP, the xylitol of 80 mesh sieves,, granulate with 50% alcoholic solution system soft material, dry, granulate add CMS-Na, Pulvis Talci, mix homogeneously, tabletting gets final product.
Embodiment 7: hydrochlorothiazide and benazepril hydrochloride drop pill
Prescription
| Component | Consumption |
| Hydrochlorothiazide benazepril hydrochloride PEG6000 PEG4000 makes altogether | 12.5g 1000 of 10g 150g 127.5g |
Preparation method:
Hydrochlorothiazide and benazepril hydrochloride are crossed 80 mesh sieves, standby; In addition with PEG6000, PEG4000 mixings post-heating extremely about 60 ℃ make fusion; Hydrochlorothiazide and benazepril hydrochloride be heated in the fused solution stir, move in the dropping funnel, be incubated about 60 ℃, regulate the water dropper size, serves as the cooling phase with-25 ℃ liquid paraffin, the system of dripping, and ball is washed, selects in filtration, gets final product.
Claims (7)
- The present invention for a kind of be the Pharmaceutical composition of active component with hydrochlorothiazide and benazepril hydrochloride, it is characterized in that it is a hydrochlorothiazide and the active component of benazepril hydrochloride formation, with the Pharmaceutical composition of mixing acceptable accessories formation.
- 2. as claimed in claim 1 a kind of be the Pharmaceutical composition of active component with hydrochlorothiazide and benazepril hydrochloride, it is characterized in that the consumption of described hydrochlorothiazide is 5.0mg-37.5mg for per unit dosage.Be preferably 6.25mg-25mg.
- 3. as claimed in claim 1 a kind of be the Pharmaceutical composition of active component with hydrochlorothiazide and benazepril hydrochloride, it is characterized in that the consumption of described benazepril hydrochloride is 2.5mg-20mg for per unit dosage.Be preferably 5mg-20mg.
- 4. as claimed in claim 1 a kind of be the Pharmaceutical composition of active component with hydrochlorothiazide and benazepril hydrochloride, it is characterized in that the weight ratio of described hydrochlorothiazide and benazepril hydrochloride is 2.5: 1-0.5: 1, be preferably 2: 1-1: 1.
- 5. as claimed in claim 1 a kind of be the Pharmaceutical composition of active component with hydrochlorothiazide and benazepril hydrochloride, it is characterized in that the Pharmaceutical composition of described hydrochlorothiazide and benazepril hydrochloride is an oral formulations.
- 6. as claimed in claim 5 a kind of be the Pharmaceutical composition of active component with hydrochlorothiazide and benazepril hydrochloride, it is characterized in that described oral formulations can be made into tablet, capsule, dispersible tablet, soft capsule, chewable tablet, oral cavity disintegration tablet, drop pill etc.
- Claim 1-6 described a kind of be the Pharmaceutical composition of active component with hydrochlorothiazide and benazepril hydrochloride, can be used for treating all kinds hypertension.And select the Pharmaceutical composition of different unit dose according to the state of an illness.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200610075611 CN1827110A (en) | 2006-04-14 | 2006-04-14 | Pharmaceutical composition using hydrochlorothiazide and benazepril hydrochloride as active ingredients, its preparation method and use |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200610075611 CN1827110A (en) | 2006-04-14 | 2006-04-14 | Pharmaceutical composition using hydrochlorothiazide and benazepril hydrochloride as active ingredients, its preparation method and use |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN1827110A true CN1827110A (en) | 2006-09-06 |
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ID=36945790
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN 200610075611 Pending CN1827110A (en) | 2006-04-14 | 2006-04-14 | Pharmaceutical composition using hydrochlorothiazide and benazepril hydrochloride as active ingredients, its preparation method and use |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN1827110A (en) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102579346A (en) * | 2012-03-02 | 2012-07-18 | 海南美兰史克制药有限公司 | Liposome solid preparation of benazepril/hydrochlorothiazide medicine combination |
| CN104740636A (en) * | 2015-03-09 | 2015-07-01 | 西安汉丰药业有限责任公司 | Compound antihypertensive preparation and application thereof |
-
2006
- 2006-04-14 CN CN 200610075611 patent/CN1827110A/en active Pending
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102579346A (en) * | 2012-03-02 | 2012-07-18 | 海南美兰史克制药有限公司 | Liposome solid preparation of benazepril/hydrochlorothiazide medicine combination |
| CN102579346B (en) * | 2012-03-02 | 2013-09-25 | 海南美兰史克制药有限公司 | Liposome solid preparation of benazepril/hydrochlorothiazide medicine combination |
| CN104740636A (en) * | 2015-03-09 | 2015-07-01 | 西安汉丰药业有限责任公司 | Compound antihypertensive preparation and application thereof |
| CN104740636B (en) * | 2015-03-09 | 2018-10-26 | 西安汉丰药业有限责任公司 | A kind of composite antihypertensive preparation and its application |
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Open date: 20060906 |