CN1981756A - Fosinopril sodium dropping balls and their making method - Google Patents
Fosinopril sodium dropping balls and their making method Download PDFInfo
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- CN1981756A CN1981756A CN 200510061982 CN200510061982A CN1981756A CN 1981756 A CN1981756 A CN 1981756A CN 200510061982 CN200510061982 CN 200510061982 CN 200510061982 A CN200510061982 A CN 200510061982A CN 1981756 A CN1981756 A CN 1981756A
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- fosinopril sodium
- sodium
- fosinopril
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- dropping balls
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Abstract
A dripping pill of fosinopril sodium for treating hypertension and heart failure is prepared from fosinopril sodium and matrix. Its preparing process is also disclosed.
Description
Technical field
The invention belongs to the pharmaceutical technology field, particularly a kind of fosinopril sodium (Fosinoprilsodium) and the formulated fosinopril sodium dropping balls of drop pill substrate.
Background technology
Hypertension is one of modal cardiovascular disease in the world today, is the dead and wounded or disabled primary cause of disease of adult.Because the raising of people's living standard, growing tension is striven in work unexpectedly, and the hypertension number of patients increases greatly.China's hypertension prevalence obviously rises, show according to the China's Statistical data, among Chinese 35 to the 74 years old crowd, hypertensive sickness rate is up to about 27 percent, patient's number is near 100,013,000, and annual with the speed increment more than 300 million peoples, China has become the most serious country of hypertension harm in the world.Hypertension can cause the damage of organs such as the heart, brain, kidney, serious threat human beings'health and life.
Fosinopril belongs to phosphinylidyne base class ACE inhibitor, at first sold at English market in 1991, and in succession in the listing of states such as the U.S. and Italy, 1998 in China's listing, at present in many countries conduct treatment hypertension clinical applications such as America and Europes.Fosinopril sodium, chemistry 4-cyclohexyl-1-(1-hydroxy-2-methyl propoxyl group) (4-phenyl butyl) phosphinyl fourth acetyl group by name)-L-proline propionic ester.Fosinopril is Angiotensin-Converting (ACE) inhibitor that a new generation contains phosphonate group, is a prodrug, absorbs the back and is hydrolyzed into activated diacid complex fosinoprilat and has an effect at gastrointestinal tract and liver.All ACE inhibitor of fosinopril and other are the same, can combine with the active aglucon zinc ion of ACE competitively, and the blocking-up angiotensin I is transformed into Angiotensin II, thereby distend the blood vessels, the aldosterone secretion reduces, and makes blood pressure drops, and hypotensive effect slowly and steadily.Fosinopril also can suppress kininase, and Kallidin I is decomposed reduce, thereby distend the blood vessels, and the performance hypotensive effect.Fosinopril can make systemic vascular resistance reduce, and makes the full increase of cardiac output, left ventricular ejection fraction and left ventricle, thereby improves cardiac function.Also can make kidney blood flow, glomerular filtration and plasma volume be kept or improve, renal vascular resistance is reduced.In effective blood pressure lowering, do not cause that cerebral blood flow changes, the onset time of its blood pressure lowering is 1h, the maximum effect time is 3～6h.Fosinopril has unique liver, the excretory advantage of kidney dual pathways compensatory, and body accumulation seldom is applicable to the hyperpietic of liver or renal failure.Than the easier patient's tolerance of other ACEI, and can improve hypertensive patient's left ventricular function, and then improve patient's prognosis, be more suitable for particularly old people's life-time service of patient Yu.Fu Xinpu improves glomerular permeability, improves insulin sensitivity, reduces proteic nonenzymatic glycosylation, stops glomerular basement membrane to thicken, and the treatment diabetic nephropathy is had good efficacy.The cough incidence rate that fosinopril causes is lower, and degree is lighter.Be used for the treatment of hypertension clinically, can use separately as initial therapy or with other antihypertensive drug and unite use.With diuretic combined treatment heart failure, can improve symptom, improve exercise tolerance, alleviate severity of CHF, reduce the frequency of being in hospital because of heart failure.
The fosinopril sodium oral formulations of using clinically is mainly tablet at present.Because shortcomings such as these conventional formulation fabricating technologies have, and make this class oral formulations exist disintegration time long, and onset is slow, and bioavailability is lower, thereby influence giving full play to of drug effect.Fosinopril sodium dropping balls bioavailability height of the present invention, disintegrate is molten loose fast, the dissolution height, steady quality, release fast, produce effects fast can sublingual administration, also can swallow, and is easy to carry and use, for the patient of dysphagia provides a kind of new medication to select.The fosinopril sodium dropping balls can be made into the preparation of 2-10mg different size, can adjust taking dose according to the patient age and the state of an illness easily, and divided dose is accurate.Preparation process of the present invention is simple, and workshop does not have dust, uses supplementary product kind few, and production process is short, and cost is low.
Summary of the invention
The object of the invention provides a kind of medicine fosinopril sodium dropping balls and preparation technology thereof who is used for hypertension and heart failure patient.
The invention is characterized in by fosinopril sodium and drop pill substrate formulated.
The weight ratio of each composition is:
Fosinopril sodium: drop pill substrate=1: 1～1: 20
The present invention can be achieved through the following technical solutions:
Get fosinopril sodium, pulverize, sieve.Fosinopril sodium mixes by weight 1: 1～1: 20 with drop pill substrate, and heating and melting stirs, and splashes in dimethicone or other drop pill coolant, separates drop pill, absorbs coolant, drying, promptly.
Utilize the drop pill of method preparation of the present invention, its main feature is:
1. the quick stripping of medicine, the dissolution height, rapid-action, the bioavailability height, side effect is little.The fosinopril sodium dropping balls is to utilize solid dispersion technology, to after medicine and the fusion of drop pill substrate medicine be dispersed in the substrate, solidify by system of dripping and quenching, medicine is scattered in the substrate with molecularity or superfine crystal state, help absorption of human body, bring into play curative effect rapidly, improve bioavailability, reduce side effect, safety is reliable.
2. increased administering mode, can swallow, but also sublingual administration.Sublingual administration has made things convenient for the patient of dysphagia for the patient of dysphagia provides a kind of new medication to select.
3. medicine stability is good.Dropping pill formulation by medicine and substrate heating and melting after, splash in the immiscible liquid coolant and make, reduce with the air contact area, be difficult for oxidation, substrate is non-water thing, is difficult for causing drug hydrolysis, stability of drug is increased, thereby guaranteed drug quality.
4. the fosinopril sodium dropping balls can be made into the preparation of 2-10mg different size, can adjust taking dose according to the patient age and the state of an illness easily, and divided dose is accurate.
5. drop pill production technology, production equipment are simple, with short production cycle, the production efficiency height, and cost is low.
6. in the main production process of drop pill, used material all is to carry out under liquid state, has reduced dust pollution, helps labor protection and environmental protection, helps the GMP management.
Fosinopril sodium dropping balls crude drug is a fosinopril sodium.Chemistry 4-cyclohexyl-1-(1-hydroxy-2-methyl propoxyl group) (4-phenyl butyl) phosphinyl fourth acetyl group by name)-L-proline propionic ester
Molecular formula: C
30H
46NO
7P
Molecular weight: 563.66
The detection method of drop pill and result:
One. detection method:
1. dissolve scattered time limit: check according to inspection technique disintegration (" Chinese Pharmacopoeia 2005 version two ones " appendix XA).
2. dissolution: according to dissolution inspection algoscopy (" Chinese Pharmacopoeia 2005 version two ones " the appendix XC three therapeutic methods of traditional Chinese medicine), be dissolution medium with water 100ml, rotating speed is that per minute 75 changes, and operation in accordance with the law in the time of 45 minutes, is got solution and filtered, and gets subsequent filtrate as need testing solution; It is an amount of that precision takes by weighing fosinopril in addition, be dissolved in water and quantitatively be diluted to reference substance solution with the need testing solution same concentrations, according to high performance liquid chromatography (" Chinese Pharmacopoeia 2005 version two ones " appendix vD) test, with μ-BondapakC18 (300 * 4.6mm, 10 μ m) be analytical column, 0.8 triethylamine solution (regulating pH3.0 with phosphoric acid)-acetonitrile (35: 65) is a mobile phase, and detecting wavelength is 215nm, measure in accordance with the law, calculate every dissolution.
Two. testing result
| Sample number | The molten diffusing time (branch) | Dissolution (being labelled amount %) |
| Embodiment 1 | ＜10 | 95.6 |
| Embodiment 2 | ＜10 | 96.1 |
| Embodiment 3 | ＜10 | 95.3 |
| Embodiment 4 | ＜10 | 95.8 |
| Embodiment 5 | ＜10 | 95.1 |
| Embodiment 6 | ＜10 | 95.5 |
The specific embodiment
Further the present invention can be described by the following examples, but not limited by embodiment.
Embodiment: per 1000 fosinopril sodium dropping balls supplementary material proportionings
| The embodiment sequence number | Fosinopril sodium | Polyethylene glycol 6000 | Macrogol 4000 | Carboxymethyl starch sodium | Poloxamer |
| 1 | 5g | 15g | 5g | 1g | |
| 2 | 5g | 50g | |||
| 3 | 5g | 20g | 5g | ||
| 4 | 10g | 25g | 5g | ||
| 5 | 10g | 20g | 5g | 2g | |
| 6 | 10g | 25g | 5g |
Claims (3)
1. fosinopril sodium dropping balls and preparation technology thereof is characterized in that by fosinopril sodium (Fosinopril sodium) and drop pill substrate formulated.The weight ratio of each composition is:
Fosinopril sodium: drop pill substrate=1: 1～1: 20
2. fosinopril sodium dropping balls according to claim 1, it is characterized in that described drop pill substrate is a kind of or several compatibilities in polyethylene glycols, carboxymethyl starch sodium, poloxamer, sodium carboxymethyl cellulose, stearic acid, sodium stearate, the polyoxyethylene monostearate, the content of each compatibility composition all is not equal to zero.
3. according to claim 1 described fosinopril sodium dropping balls, it is characterized in that preparation method is as follows: get fosinopril sodium, pulverize, sieve.Fosinopril sodium mixes by weight 1: 1～1: 20 with drop pill substrate, and heating and melting stirs, and splashes in dimethicone or other drop pill coolant, separates drop pill, absorbs coolant, drying, promptly.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200510061982 CN1981756A (en) | 2005-12-14 | 2005-12-14 | Fosinopril sodium dropping balls and their making method |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200510061982 CN1981756A (en) | 2005-12-14 | 2005-12-14 | Fosinopril sodium dropping balls and their making method |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN1981756A true CN1981756A (en) | 2007-06-20 |
Family
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN 200510061982 Pending CN1981756A (en) | 2005-12-14 | 2005-12-14 | Fosinopril sodium dropping balls and their making method |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN1981756A (en) |
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2005
- 2005-12-14 CN CN 200510061982 patent/CN1981756A/en active Pending
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| PB01 | Publication | ||
| C02 | Deemed withdrawal of patent application after publication (patent law 2001) | ||
| WD01 | Invention patent application deemed withdrawn after publication |