CN108939045A - A kind of lisinopril oral administration solution and preparation method thereof - Google Patents

A kind of lisinopril oral administration solution and preparation method thereof Download PDF

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Publication number
CN108939045A
CN108939045A CN201710379924.0A CN201710379924A CN108939045A CN 108939045 A CN108939045 A CN 108939045A CN 201710379924 A CN201710379924 A CN 201710379924A CN 108939045 A CN108939045 A CN 108939045A
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China
Prior art keywords
oral administration
administration solution
lisinopril
solution according
solution
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CN201710379924.0A
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Chinese (zh)
Inventor
李之韬
王宇杰
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Beijing Wanquan Dezhong Medical Biological Technology Co Ltd
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Beijing Wanquan Dezhong Medical Biological Technology Co Ltd
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Priority to CN201710379924.0A priority Critical patent/CN108939045A/en
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/05—Dipeptides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/26—Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
    • 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
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
    • 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
    • A61K9/08—Solutions

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Nutrition Science (AREA)
  • Physiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Medicinal Preparation (AREA)

Abstract

The present invention provides a kind of lisinopril oral administration solution and preparation method thereof, said preparation is mainly used for treating essential hypertension.It the advantage is that drug with molecular state dispersion in the medium, dispersion degree is big, it is fast to absorb, drug effect can be played rapidly, be conducive to improve the bioavilability of drug, and the compliance of patient medication can be improved, it is convenient to take, it is easy to divided dose, especially suitable for gerontal patient, preparation method described in the oral administration solution is easy to operate, is not necessarily to special installation.

Description

A kind of lisinopril oral administration solution and preparation method thereof
Technical field
The present invention relates to a kind of lisinopril preparations, more specifically, being related to a kind of lisinopril oral administration solution and its system Preparation Method belongs to technical field of medicine.
Background technique
Lisinopril is the lysine derivative of enalaprilat, belongs to third generation angiotensin converting enzyme inhibitor, The activity that can inhibit Angiotensin-Converting, makes angiotensinsIt is reduced with the concentration of aldosterone, it is living to increase plasma renin Property, lead to peripheral blood vessel expansion and vascular resistence decline, to generate pressure reduction effect, is primarily adapted for use in the treatment high blood of primary Pressure.
Entitled N- { N- [(S) -1- carboxyl -3- phenylpropyl]-L- the lysyl }-L-PROLINE of chemistry of lisinopril, point Minor is C21H31N3O5·2H2O, molecular weight 441.52, chemical structural formula is as follows:
。
The current form of medication of lisinopril is mainly oral tablet and capsule.But relative to oral liquid, It not only works slow, bioavilability is low, and higher cost, and preparation process is cumbersome, easily causes the loss of effective component.In addition, certain A little patients, which have any problem, intake and swallows solid oral dosage form, and solid dosage forms is not recommended for children or old because of asphyxia risk increase People.
Oral administration solution has the characteristics that bioavilability is high, quickly releases the drug, is quickly effective, convenient to take, is made into mouth Solution is taken, to reach raising bioavilability, more fully performance curative effect of medication, reduction adverse reaction wait mesh convenient for taking 's.
Summary of the invention
Present invention aim to address above-mentioned deficiencies, provide a kind of preparation method of lisinopril oral administration solution.
Lisinopril oral administration solution of the invention, comprising lisinopril, preservative, corrigent, pH adjusting agent, aromatic, Solvent, it is characterised in that the appearance character of the oral administration solution is faint yellow clear transparent solutions, pH value range 4.5-5.5.
The lisinopril oral administration solution, which is characterized in that by weight, the specific composition of every 1000ml is as follows: rely Promise Puli 2.5g-20g, preservative 0.25g-10g, corrigent 80g-300g, pH adjusting agent 2.5g-100g, aromatic 1.0g- 10g, solvent 40.0-80g, Purified Water q. s.
The preservative in methylparaben, ethylparaben, sorbic acid, benzoic acid, sodium benzoate at least It is a kind of.
The corrigent in sucrose, stevioside, saccharin sodium, Aspartame, xylitol, maltose, fructose extremely Few one kind, preferably sucrose, the corrigent can be added in the form of solid or solution.
The pH adjusting agent is selected from citric acid and sodium citrate, glacial acetic acid and sodium acetate, lactic acid, preferably citric acid and Chinese holly Rafter acid sodium.
The aromatic in orange essence, peach flavor, blackcurrant essence, blueberry flavor, strawberry essence one Kind.
The solvent is selected from least one of glycerol, propylene glycol.
The lisinopril oral administration solution, pH value are preferably 5.08.
Specific embodiment
The following is specific embodiments of the present invention, is described further to technical solution of the present invention, but of the invention Protection scope is not limited to these examples.It is all to be included in the present invention without departing substantially from the change of present inventive concept or equivalent substitute Protection scope within.
Embodiment 1: the preparation of lisinopril oral administration solution
Composition:
。
Preparation process:
1) recipe quantity glycerol and 40% purified water are weighed, be mixed uniformly, sequentially added under 50 DEG C of water bath conditions sodium acetate with Main ingredient stirs to dissolve completely, adds sucrose and stirs to dissolve, and lets cool to room temperature, obtains solution 1；
2) recipe quantity propylene glycol is preheated in 50 DEG C of water-baths, adds ethylparaben, stir to dissolve to obtain solution 2；
3) solution 1 is uniformly mixed with solution 2, is settled to 1000ml after acetic acid on the rocks, orange essence, stirs evenly；
It is 4) through 0.22 μm of membrane filtration, gained filtrate is filling into brown oral medicinal liquor bottle according to the trimmed size of factory, Under the conditions of 105 DEG C moist heat sterilization 20 minutes to get.
Embodiment 2: the preparation of lisinopril oral administration solution
Composition:
。
Preparation process:
1) recipe quantity glycerol and 40% purified water are weighed, sodium citrate and main ingredient are added under 50 DEG C of water bath conditions, stirring keeps its molten Solution, adds sucrose and fructose stirs to dissolve, let cool to room temperature, obtain solution 1；
2) recipe quantity propylene glycol is preheated in 50 DEG C of water-baths, adds methylparaben, stir to dissolve to obtain solution 2；
3) solution 1 is uniformly mixed with solution 2, is settled to 1000ml after adding citric acid, peach flavor, stirs evenly；
It is 4) through 0.22 μm of membrane filtration, gained filtrate is filling into brown oral medicinal liquor bottle according to the trimmed size of factory, Under the conditions of 105 DEG C moist heat sterilization 20 minutes to get.
Embodiment 3: the preparation of lisinopril oral administration solution
Composition:
。
Preparation process:
1) recipe quantity glycerol and 40% purified water are weighed, sodium citrate and main ingredient are added under 50 DEG C of water bath conditions, stirring keeps its molten Solution, adds xylitol, stevioside stirs to dissolve, and lets cool to room temperature, obtains solution 1；
2) 20% purified water is weighed, sodium benzoate is added, stirs to dissolve to obtain solution 2；
3) solution 1 is uniformly mixed with solution 2, is settled to 1000ml after adding citric acid, blackcurrant essence, stirs evenly；
It is 4) through 0.22 μm of membrane filtration, gained filtrate is filling into brown oral medicinal liquor bottle according to the trimmed size of factory, Under the conditions of 105 DEG C moist heat sterilization 20 minutes to get.
Embodiment 4: the preparation of lisinopril oral administration solution
Composition:
。
Preparation process:
1) recipe quantity glycerol and 40% purified water are weighed, sodium acetate and main ingredient are added under 50 DEG C of water bath conditions, stirring keeps its molten Solution, adds maltose, saccharin sodium stirs to dissolve, and lets cool to room temperature, obtains solution 1；
2) recipe quantity propylene glycol is preheated in 50 DEG C of water-baths, adds ethylparaben, stir to dissolve to obtain solution 2；
3) solution 1 is uniformly mixed with solution 2, is settled to 1000ml after acetic acid on the rocks, blueberry flavor, stirs evenly；
It is 4) through 0.22 μm of membrane filtration, gained filtrate is filling into brown oral medicinal liquor bottle according to the trimmed size of factory, Under the conditions of 105 DEG C moist heat sterilization 20 minutes to get.
Embodiment 5: the preparation of lisinopril oral administration solution
Composition:
。
Preparation process:
1) recipe quantity glycerol and 40% purified water are weighed, sodium citrate and main ingredient are added under 50 DEG C of water bath conditions, stirring keeps its molten Solution, adds Aspartame, maltose stirs to dissolve, and lets cool to room temperature, obtains solution 1；
2) 20% purified water is weighed, sodium benzoate is added, stirs to dissolve to obtain solution 2；
3) solution 1 is uniformly mixed with solution 2, is settled to 1000ml after adding citric acid, strawberry essence, stirs evenly；
It is 4) through 0.22 μm of membrane filtration, gained filtrate is filling into brown oral medicinal liquor bottle according to the trimmed size of factory, Under the conditions of 105 DEG C moist heat sterilization 20 minutes to get.
Embodiment 6: the stability experiment testing result of lisinopril oral administration solution
。
Stability experiment testing result shows: each inspection project of embodiment 1-5 meets the requirements, and accelerated test 6 months Clarity of solution is qualified afterwards, does not generate insoluble matter；With sweet taste, mouthfeel is suitable for；PH value is kept constant；Stable content；It is related Substance (total miscellaneous) growth is more slow, illustrates the lisinopril oral administration solution stable the present invention can obtain quality.
Embodiment 7: the mouthfeel evaluation test of lisinopril oral administration solution
For assess lisinopril oral administration solution mouthfeel and bitterness intensity, choose 20-40 age bracket 10 male and female into Row sensory test.Bitter taste assessment is divided into six grades by following standard and is indicated by average value, assessment result table:
。
Lisinopril oral administration solution mouthfeel evaluation test result table:
。
The result shows that: oral administration solution excellent taste of the invention.

Claims (8)

  1. It include lisinopril, preservative, corrigent, pH adjusting agent, aromatic, solvent 1. a kind of lisinopril oral administration solution, The appearance character for being characterized in that the oral administration solution is faint yellow clear transparent solutions, pH value range 4.5-5.5.
  2. 2. lisinopril oral administration solution according to claim 1, which is characterized in that by weight, every 1000ml's is specific Composition is as follows: lisinopril 2.5g-20g, preservative 0.25g-10g, corrigent 0.1g-100g, pH adjusting agent 2.5g-100g, Aromatic 1.0g-10g, solvent 40.0-80.0g, Purified Water q. s.
  3. 3. oral administration solution according to claim 2, it is characterised in that the preservative is selected from methylparaben, nipalgin At least one of ethyl ester, sorbic acid, benzoic acid, sodium benzoate.
  4. 4. oral administration solution according to claim 2, it is characterised in that the corrigent is selected from sucrose, stevioside, saccharin At least one of sodium, Aspartame, xylitol, maltose, fructose, preferably sucrose, the corrigent can with solid or The form of solution is added.
  5. 5. oral administration solution according to claim 2, it is characterised in that the pH adjusting agent is selected from citric acid and citric acid Sodium, glacial acetic acid and sodium acetate, lactic acid, preferably citric acid and sodium citrate.
  6. 6. oral administration solution according to claim 2, it is characterised in that it is fragrant that the aromatic is selected from orange essence, honey peach One of essence, blackcurrant essence, blueberry flavor, strawberry essence.
  7. 7. oral administration solution according to claim 2, it is characterised in that the solvent in glycerol, propylene glycol at least It is a kind of.
  8. 8. lisinopril oral administration solution according to claim 1, it is characterised in that pH value is preferably 5.08.
CN201710379924.0A 2017-05-25 2017-05-25 A kind of lisinopril oral administration solution and preparation method thereof Pending CN108939045A (en)

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Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20030171301A1 (en) * 2001-06-25 2003-09-11 Roberts Ronald John Amorphous compound
CN104523629A (en) * 2014-12-25 2015-04-22 海南卫康制药(潜山)有限公司 Lisinopril composition freeze-dried tablets and preparation method thereof
US9463183B1 (en) * 2015-10-30 2016-10-11 Silvergate Pharmaceuticals, Inc. Lisinopril formulations
CN106496245A (en) * 2016-09-12 2017-03-15 南通市科通科技信息咨询有限公司 The pharmaceutical composition of lisinopril and its application in biological medicine

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20030171301A1 (en) * 2001-06-25 2003-09-11 Roberts Ronald John Amorphous compound
CN104523629A (en) * 2014-12-25 2015-04-22 海南卫康制药(潜山)有限公司 Lisinopril composition freeze-dried tablets and preparation method thereof
US9463183B1 (en) * 2015-10-30 2016-10-11 Silvergate Pharmaceuticals, Inc. Lisinopril formulations
CN106496245A (en) * 2016-09-12 2017-03-15 南通市科通科技信息咨询有限公司 The pharmaceutical composition of lisinopril and its application in biological medicine

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Application publication date: 20181207