CN101596181A - A kind of pharmaceutical composition that contains dimeticone/simethicone - Google Patents
A kind of pharmaceutical composition that contains dimeticone/simethicone Download PDFInfo
- Publication number
- CN101596181A CN101596181A CNA2009101042439A CN200910104243A CN101596181A CN 101596181 A CN101596181 A CN 101596181A CN A2009101042439 A CNA2009101042439 A CN A2009101042439A CN 200910104243 A CN200910104243 A CN 200910104243A CN 101596181 A CN101596181 A CN 101596181A
- Authority
- CN
- China
- Prior art keywords
- simethicone
- pharmaceutical composition
- dimeticone
- acetylcysteine
- pharmaceutically acceptable
- 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.)
- Pending
Links
- AMTWCFIAVKBGOD-UHFFFAOYSA-N dioxosilane;methoxy-dimethyl-trimethylsilyloxysilane Chemical compound O=[Si]=O.CO[Si](C)(C)O[Si](C)(C)C AMTWCFIAVKBGOD-UHFFFAOYSA-N 0.000 title claims abstract description 88
- 229940083037 simethicone Drugs 0.000 title claims abstract description 85
- 239000008194 pharmaceutical composition Substances 0.000 title claims abstract description 23
- 229960001275 dimeticone Drugs 0.000 title claims abstract description 21
- CXQXSVUQTKDNFP-UHFFFAOYSA-N octamethyltrisiloxane Chemical compound C[Si](C)(C)O[Si](C)(C)O[Si](C)(C)C CXQXSVUQTKDNFP-UHFFFAOYSA-N 0.000 title claims abstract description 21
- 229920000435 poly(dimethylsiloxane) Polymers 0.000 title claims abstract description 21
- PWKSKIMOESPYIA-BYPYZUCNSA-N L-N-acetyl-Cysteine Chemical compound CC(=O)N[C@@H](CS)C(O)=O PWKSKIMOESPYIA-BYPYZUCNSA-N 0.000 claims abstract description 39
- 229960004308 acetylcysteine Drugs 0.000 claims abstract description 33
- 239000003814 drug Substances 0.000 claims abstract description 25
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- -1 hydrobromate Chemical compound 0.000 claims description 4
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 claims description 4
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- 235000010232 propyl p-hydroxybenzoate Nutrition 0.000 description 1
- 239000004405 propyl p-hydroxybenzoate Substances 0.000 description 1
- 235000013772 propylene glycol Nutrition 0.000 description 1
- QELSKZZBTMNZEB-UHFFFAOYSA-N propylparaben Chemical compound CCCOC(=O)C1=CC=C(O)C=C1 QELSKZZBTMNZEB-UHFFFAOYSA-N 0.000 description 1
- 208000008128 pulmonary tuberculosis Diseases 0.000 description 1
- 238000012552 review Methods 0.000 description 1
- 238000010008 shearing Methods 0.000 description 1
- 239000002002 slurry Substances 0.000 description 1
- 239000011734 sodium Substances 0.000 description 1
- 229910052708 sodium Inorganic materials 0.000 description 1
- 235000010413 sodium alginate Nutrition 0.000 description 1
- 239000000661 sodium alginate Substances 0.000 description 1
- 229940005550 sodium alginate Drugs 0.000 description 1
- 239000007779 soft material Substances 0.000 description 1
- 239000007787 solid Substances 0.000 description 1
- 239000000600 sorbitol Substances 0.000 description 1
- 208000024794 sputum Diseases 0.000 description 1
- 210000003802 sputum Anatomy 0.000 description 1
- 238000013112 stability test Methods 0.000 description 1
- 235000019408 sucralose Nutrition 0.000 description 1
- BAQAVOSOZGMPRM-QBMZZYIRSA-N sucralose Chemical compound O[C@@H]1[C@@H](O)[C@@H](Cl)[C@@H](CO)O[C@@H]1O[C@@]1(CCl)[C@@H](O)[C@H](O)[C@@H](CCl)O1 BAQAVOSOZGMPRM-QBMZZYIRSA-N 0.000 description 1
- 230000002195 synergetic effect Effects 0.000 description 1
- 231100000419 toxicity Toxicity 0.000 description 1
- 230000001988 toxicity Effects 0.000 description 1
- 210000003437 trachea Anatomy 0.000 description 1
- 230000000007 visual effect Effects 0.000 description 1
- 239000000080 wetting agent Substances 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
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/19—Carboxylic acids, e.g. valproic acid
- A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
- A61K31/197—Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid
- A61K31/198—Alpha-amino acids, e.g. alanine or edetic acid [EDTA]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K49/00—Preparations for testing in vivo
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Epidemiology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
This discloses a kind of pharmaceutical composition that contains dimeticone/simethicone, has mainly been made by following bulk drugs: 1～500 part of 1～1000 part of acetylcysteine or its pharmaceutically acceptable salt and simethicone or Simethicone.Said composition can be made into various pharmaceutically acceptable dosage forms; The purposes of the adjuvant drug that compositions gives before as digestive endoscopy inspection and treatment or imaging examination art, with singly use relatively with the acetylcysteine of dosage or simethicone, Simethicone, the present composition has stronger froth breaking effect, also has simultaneously the stronger mucus effect of dispeling, therefore can effectively improve and check and treatment degree of getting a clear view, reduce mistaken diagnosis and fail to pinpoint a disease in diagnosis the effectiveness of raising diagnosis and treatment, the early diagnosis that is beneficial to digestive tract disease is found, is with a wide range of applications.
Description
Technical field
The present invention relates to medical technical field, relate to the pharmaceutical composition of a kind of acetylcysteine or its pharmaceutical salts and dimeticone/simethicone particularly.
Background technology
Digestive endoscopy has important status in the diagnosis digestive tract disease, be subjected to doctor's favor because of it is directly perceived, simple, and is commonly used especially in clinical diagnosis and treatment.But owing to have a large amount of foams and mucus in the digestive tract, cause the visual field unclear, the review time prolongs, and the patient suffering increases, and causes mistaken diagnosis easily and fail to pinpoint a disease in diagnosis, and more is unfavorable for the early diagnosis discovery of digestive tract disease.
Simethicone (I) is the most frequently used clinically medical science defoamer, is usually used in the preceding froth breaking of art of digestive endoscopy inspection and treatment or abdominal part imaging examination.Simethicone is a dimethylsiloxane polymer, because its surface tension is little, can change bubble surface tension force, and it is broken, thereby eliminates foam.As far back as twentieth century five, the sixties, simethicone just is applied to medical domain as defoamer.Simethicone (II) is the complex of simethicone and silicon dioxide, has the froth breaking ability identical or stronger with simethicone.Simethicone and Simethicone all belong to pharmacology and physiology's inert substance, and its froth breaking act as physical process, and material itself does not relate to chemical change.
Acetylcysteine (III) for N-acetyl group-L-cysteine, is mucolytic agent; has stronger phlegm dissolving effect; ((S-S-) fracture reduces mucous viscosity to contained sulfydryl in its molecule, and makes it liquefaction SH-) to make the disulfide bond in the mucoprotein polypeptide chain in the mucus.Be usually used at present the dyspnea that sticking in a large number stagnation of phlegm plug causes clinically, as the postoperative difficulty of coughing up phlegm, anxious giving birth to and the thick sputum that chronic bronchitis, an ammonia enlargement of pipe, pulmonary tuberculosis, pneumonia, emphysema etc. cause, the difficulty of coughing up phlegm, stagnation of phlegm trachea etc., still can be used for the detoxifcation of poisoning by paracetamol.
Summary of the invention
The object of the present invention is to provide a kind of pharmaceutical composition that contains dimeticone/simethicone, this pharmaceutical composition can be eliminated the digestive tract inner foam, can remove the interior viscous liquid of digestive tract by Eradicates again; This pharmaceutical composition can be used in digestive endoscopy inspection and treatment or imaging examination as the adjuvant drug before the art.
For achieving the above object, the present invention adopts following technical scheme:
A kind of pharmaceutical composition that contains dimeticone/simethicone is mainly made by following bulk drugs: 1～500 part of 1～1000 part of acetylcysteine or its pharmaceutically acceptable salt and simethicone or Simethicone.
Because simethicone or the effect of Simethicone froth breaking are stronger, but Eradicates removes a little less than the mucous effect of digestive tract.And the mucus dissolution of acetylcysteine just in time can remedy simethicone or Simethicone Eradicates and remove the more weak deficiency of mucus effect, and the pharmacology of dimeticone/simethicone and physiology's inertia make itself and acetylcysteine not have incompatibility.Therefore, simethicone or Simethicone and acetylcysteine applied in any combination have synergistic function, and drug interaction can not take place, and produce incompatibility.
Up to the present, do not see the research and the use report of the compositions that simethicone or Simethicone and acetylcysteine or its pharmaceutical salts are arranged.
Be preferably: 20～200 parts of 50～500 parts of the salt that acetylcysteine or its are pharmaceutically accepted, simethicone or Simethicones;
More preferably: 20～50 parts of 80～200 parts of the salt that acetylcysteine or its are pharmaceutically accepted, simethicone or Simethicones.
More than form to be by weight as proportioning, under the geostationary situation of ratio, can to adjust consumption according to production scale.
The consumption of drug component of the present invention draws through the big quantity research of inventor, all has good froth breaking and Eradicates and remove the mucus effect in above-mentioned weight portion scope.
In the pharmaceutical composition that contains dimeticone/simethicone of the present invention, described acetylcysteine pharmaceutically acceptable salt can be organic nitrogen salt, hydrochlorate, sulfate, acetate, mesylate, tartrate, maleate, fumarate, hydrobromate, aspartate.
The pharmaceutical composition that contains dimeticone/simethicone of the present invention can add one or more pharmaceutically acceptable carriers, uses in the mode of oral administration.
The pharmaceutical composition that contains dimeticone/simethicone of the present invention can be prepared into oral solid formulation with it, as granule, powder, dry suspension etc., or makes oral liquid, as suspension, Emulsion etc.
The pharmaceutical composition that contains dimeticone/simethicone of the present invention can adopt the conventional method production in the existing pharmaceutical field, can add various pharmaceutically acceptable carriers when needing.
Described carrier comprises filler, binding agent, wetting agent, disintegrating agent, lubricant, suspending agent, emulsifying agent, correctives, antiseptic, antioxidant of pharmaceutical field routine etc.
Described alternative filler has: starch, dextrin, sucrose, microcrystalline Cellulose, mannitol, glucose, lactose, pregelatinized Starch etc.;
Alternative binding agent has: sodium carboxymethyl cellulose, polyvidone, hydroxypropyl cellulose, starch slurry etc.;
Alternative disintegrating agent has: starch, polyvinylpolypyrrolidone, cross-linking sodium carboxymethyl cellulose, carboxymethyl starch sodium, low-substituted hydroxypropyl cellulose etc.;
Available lubricant has: magnesium stearate, Pulvis Talci, micropowder silica gel etc.;
Alternative suspending agent or emulsifying agent have: tragakanta, arabic gum, xanthan gum, sodium alginate, sodium carboxymethyl cellulose, hypromellose, ethyl cellulose, hydroxyethyl-cellulose, Tweens, spans, polyglycol distearate, Polyethylene Glycol cetylate, glyceryl monostearate etc.;
Alternative antiseptic has: methyl parahydroxybenzoate or its sodium salt, ethylparaben, propyl p-hydroxybenzoate or its sodium salt, sorbic acid, benzyl alcohol, benzoic acid, glycerol, propylene glycol etc.;
Selectable antioxidant has: disodiumedetate, EDTA calcium complex disodium salt, 2,6 ditertiary butyl p cresol, Butylated hydroxyanisole etc.;
Correctives is then selected sweeting agent and aromatic pharmaceutically commonly used for use, as saccharin sodium, sucrose, aspartame, sucralose, steviosin, sorbitol, mannitol, various fruity flavors etc.
The purposes of the adjuvant drug that the present invention has given before also providing the above-mentioned pharmaceutical composition that contains dimeticone/simethicone as digestive endoscopy inspection and treatment or imaging examination art.Because simethicone or the effect of Simethicone froth breaking are stronger, but Eradicates makes that except that a little less than the mucous effect of digestive tract effect was not good enough when it was used separately in digestive endoscopy inspection and treatment or imaging examination.When the present invention is intended to be applied to eliminate the digestive tract inner foam in digestive endoscopy inspection and treatment or the imaging examination, can remove the interior viscous liquid of digestive tract by Eradicates again, thereby the visibility of improve checking reduces mistaken diagnosis and fails to pinpoint a disease in diagnosis, and is beneficial to the early diagnosis discovery of digestive tract disease.
The pharmaceutical composition that the present invention contains dimeticone/simethicone has the following advantages:
(1) provide a kind of acetylcysteine or its pharmaceutical salts and dimeticone/simethicone compatibility to be used to prepare that froth breaking and Eradicates remove mucous pharmaceutical composition and purposes before digestive endoscopy inspection and treatment or the imaging examination first, said composition is carried out digestive endoscopy inspection and treatment or imaging examination after using again, can effectively improve and check and treatment degree of getting a clear view, improve the digestive tract disease particularly diagnosis of early lesion and the effectiveness of treatment.
(2) first to originally the froth breaking and the Eradicates of bright compositions have carried out in vitro study except that the mucus effect, find to use simethicone, Simethicone or acetylcysteine group relatively with single with the blank group, the present composition has stronger froth breaking simultaneously and Eradicates removes the mucus ability, it is remarkable to show that compositions is removed aspect the mucus effect at froth breaking and Eradicates, and consequently those skilled in the art institute is beyond thought.
(3) preparation technology of the present invention is simple, and drug quality is uniform and stable, can guarantee safety of clinical administration.
(4) the present invention has been prepared into compositions with simethicone or Simethicone and acetylcysteine or its pharmaceutical salts, and its definite effect is for clinician and patient provide medication preferably to select.Even with simethicone or Flatulex and Mucosolvin use in conjunction, it is more easy that the present composition also makes the patient take medicine respectively, saved and once checked the trouble of repeatedly taking medicine.
Below routine by experiment beneficial effect of further setting forth medicine of the present invention.In the following example: the compositions of simethicone or Simethicone, acetylcysteine is called for short second ammonia silicone oil composite.
In the following example: the compositions of simethicone or Simethicone, acetylcysteine is called for short second ammonia silicone oil composite.
Experimental example 1
Second ammonia silicone oil composite drug efficacy study---froth breaking ability determination test
Material: logical X-100 (Triton X-100) in the spy, SIGMA reagent; Simethicone Emulsion, trade name: this health of coffee, Japanese Kissei Pharmaceutical Co., Ltd. produces, specification: 20mg/ml, lot number: AXN2899; Simethicone emulsion, trade name: Bai Xi, Berlin, Germany chemistry joint-stock company produces specification: 40mg/ml, lot number: 74041; The mucolyticum granulates, specification: the 0.1g/ bag, Hainan drugmaker produces; Second ammonia silicone oil composite, self-control (preparation method is seen embodiment 1～4).
Method: get and lead to eight parts of X-100 aqueous solution 100ml in 1% spy, the careful 250ml graduated cylinder that injects eight cleanings, add simethicone Emulsion 5ml, Simethicone emulsion 2.5ml, 1 bag of mucolyticum granulates, 1 bag of second ammonia silicone oil composite granule, 1/2 bag of second ammonia silicone oil composite powder, second ammonia silicone oil composite suspensoid 2ml, second ammonia silicone oil composite Emulsion 1ml respectively in graduated cylinder, the 8th graduated cylinder do not add.Seal eight graduated cylinder ports, place the strong jolting of shaking screen 2 minutes simultaneously, take out, write down the foam height of each graduated cylinder.Foam height with the 8th graduated cylinder of n.s is 100%, reduces foam volume percentage calculation froth breaking ability with each sample.Triplicate is averaged.
The result: the average froth breaking ability of seven duplicate samples is respectively: 98%, 95%, 6%, 98%, 98%, 99%, 99%, show that present composition sample froth breaking ability is all very strong, foam is almost completely eliminated, with single suitable with the froth breaking ability of simethicone or Simethicone, and single froth breaking ability of acetylcysteine of using is very weak.Illustrate also that simultaneously acetylcysteine in the compositions can not influence the froth breaking ability of simethicone wherein or Simethicone.
Experimental example 2
Second ammonia silicone oil composite drug efficacy study---Eradicates removes mucus ability determination test
Test sample: simethicone Emulsion, trade name: this health of coffee, Japanese Kissei Pharmaceutical Co., Ltd. produces, specification: 20mg/ml, lot number: AXN2899; Simethicone emulsion, trade name: Bai Xi, Berlin, Germany chemistry joint-stock company produces specification: 40mg/ml, lot number: 74041; Second ammonia silicone oil composite suspensoid (self-control, preparation method is seen embodiment 3).
Method: laboratory animal is 4 of the male dogs of about 15kg, and body weight and healthy sign no significant difference are tested preceding two days feeding same food.After sernyl anesthesia, tighten the duodenum end of stomach to the duodenum section excision esophagus lower end.Inject respectively from the esophagus end: water A.100ml; B. simethicone Emulsion 10ml+ water 100ml; C. Simethicone 5ml+ water 100ml; D. second ammonia silicone oil composite suspensoid 4ml+ water 100ml.After 20 minutes, arrogant lateral bending cuts, and gathers each one of body of stomach top and pylorus specimen, and painted with the ivens orchid.Microscopically is observed mucus adhesion condition in the specimen.
Body of stomach top and pylorus that result: A organizes the flushing of water only gastric chamber all adhere to a large amount of mucus and bubble, especially the pylorus position; After B group and C group adopted simethicone or Simethicone emulsion flushing gastric chamber, body of stomach top and pylorus bubble obviously reduced, but still the attachment portion mucus; And adopt the B group body of stomach top and the pylorus in second ammonia silicone oil composite suspensoid 4ml+ water 100ml flushing gastric chamber only to adhere to a small amount of mucus and bubble, can clearly observe area gastrica and superficial epithelium cell.
Conclusion: second ammonia silicone oil composite can obviously be eliminated the intravital mucus of gastral cavity.Its effect is significantly better than water and independent simethicone or the Simethicone of using.
Experimental example 3
The acute toxicity test of second ammonia silicone oil composite Emulsion
Test sample: second ammonia silicone oil composite Emulsion (self-control, preparation method is seen embodiment 4).
Animal subject: mice, each 5 of every group of male and female, male body weight 24～26g, female body weight 20～22g.
Route of administration: per os is irritated stomach.
Observation item: death toll, general state, body weight, cut open inspection, calculate median lethal dose(LD 50) LD
50
The result: require to carry out prerun according to acute toxicity test, determine that each dosage group dosage is respectively: 1.50ml/10g, 1.12ml/10g, 0.84ml/10g, 0.63ml/10g, 0.47ml/10g, adjacent two dose ratio are 1: 0.75.
| Group | Number of animals (n) | Dosage (ml/10g) | Log10 dose (X) | Mortality rate (P) | P 2 |
| 1 | 10 | 1.5 | 0.1761 | 1.0 | 1.0 |
| 2 | 10 | 1.1 | 0.0414 | 0.6 | 0.36 |
| 3 | 10 | 0.8 | -0.0969 | 0.4 | 0.16 |
| 4 | 10 | 0.6 | -0.2218 | 0.2 | 0.04 |
| 5 | 10 | 0.5 | -0.3010 | 0.1 | 0.01 |
Computing formula: LD
50=Log
-1[Xm-i (∑ P-0.5)], wherein Xm is a maximal dose group logarithm value, and i is the logarithm of height dose ratio between two adjacent groups, and ∑ P is each treated animal mortality rate sum, decimally expression.
Result of calculation: LD
50=0.8939ml/10g=89.39ml/kg.
Conclusion (of pressure testing): second ammonia silicone oil composite Emulsion LD in this test
50Be 89.39ml/kg, be equivalent to about 1000 times of 50kg body weight human body recommended dose.Show that this product toxicity is lower, safe.
Experimental example 4
Second ammonia silicone oil composite accelerated stability test result
Investigate sample: second ammonia silicone oil composite suspensoid (seeing embodiment 3), second ammonia silicone oil composite Emulsion (seeing embodiment 4).
Investigation condition: 30 ± 2 ℃ of temperature, relative humidity 65% ± 5%.
The investigation time: 0 month, January, February, March, June.
Investigate index: (1) second ammonia silicone oil composite suspensoid: character, settling volume ratio, redispersibility, pH value, related substance, content, microbial limit; (2) second ammonia silicone oil composite Emulsion: character, centrifugal stability, pH value, related substance, content, microbial limit.
Result: investigate through quickening test in 6 months, compare with 0 month data, every investigation index of second ammonia silicone oil composite suspensoid and second ammonia silicone oil composite Emulsion has no significant change, and shows that this product suspensoid and emulsion composition are basicly stable, and measurable effect duration is 1.5～2 years.
The specific embodiment
Invention is further described to this reality below in conjunction with the specific embodiment, but this should be interpreted as that the scope of the above-mentioned theme of the present invention only limits to following embodiment.All technology that realizes based on foregoing of the present invention all belong to scope of the present invention.The adjuvant of each dosage form can be replaced with acceptable accessories in following examples, perhaps reduces, increases.
Embodiment 1
The preparation of second ammonia silicone oil composite granule
1, prescription:
Simethicone 100g
Silicon dioxide 5g
Acetylcysteine 500g
Cane sugar powder 200g
Ethanol is an amount of
Make 1000 bags altogether
2, concrete steps:
(1) acetylcysteine and cane sugar powder are crossed 100 mesh sieves respectively, and be standby;
(2) take by weighing supplementary material by recipe quantity;
(3) simethicone is put 150 ℃ and was placed 3 hours with after silicon dioxide mixes, and take out the cooling back;
(4) behind acetylcysteine and cane sugar powder, the starch mix homogeneously, add in the mixture of simethicone and silicon dioxide, repeatedly mix making it even, make the soft material that suits with an amount of ethanol after;
(5) prepare wet granular with 20 mesh sieves;
(6) wet granular is dried under 60～70 ℃ of conditions;
(7) dried granule 18 mesh sieve granulate;
(8) sieve with 10 mesh sieves and 80 mesh sieves, remove bulky grain and fine powder after, semi-finished product;
(9) behind outward appearance and the drug content, fill becomes bag to semi-finished product after testing, finished product;
(10) product inspection qualified after, the warehouse-in.
3, clinical use
In preceding 20 minutes of digestive endoscopy inspection and treatment or imaging examination, get 1 bag of second ammonia silicone oil composite granule, disperse the back oral with about 50 ml waters dissolving, conduct a survey again after 20 minutes.Medication dose can be taken the circumstances into consideration increase and decrease according to actual effect.
Embodiment 2
The preparation of second ammonia silicone oil composite powder
1, prescription:
Simethicone 50g
Acetylcysteine 400g
Glucose 850g
Micropowder silica gel 50g
Make 1000 bags altogether
2, concrete steps:
(1) acetylcysteine and glucose are crossed 100 mesh sieves respectively, and be standby;
(2) take by weighing supplementary material by recipe quantity;
(3) adsorb Simethicone with glucose, after fully mixing makes it evenly,, get semi-finished product again with acetylcysteine, micropowder silica gel mix homogeneously;
(4) behind outward appearance and the drug content, fill becomes bag to semi-finished product after testing, finished product;
(5) product inspection qualified after, the warehouse-in.
3, clinical use
In preceding 20 minutes of digestive endoscopy inspection and treatment or imaging examination, get 1 bag of second ammonia silicone oil composite powder, disperse the back oral with about 50 ml waters dissolving, conduct a survey again after 20 minutes.Medication dose can be taken the circumstances into consideration increase and decrease according to actual effect.
Embodiment 3
The preparation of second ammonia silicone oil composite suspensoid
1, prescription:
Simethicone 50g
Silicon dioxide 2.5g
Acetylcysteine 100g
Microcrystalline Cellulose 30g
Xanthan gum 5g
Aspartame 5g
Ethylparaben 2g
Disodiumedetate 1g
Ethanol 20g
The 1M sodium hydroxide solution is an amount of
Purified water is to 1000ml
2, concrete steps:
(1) acetylcysteine, microcrystalline Cellulose, xanthan gum are crossed 100 mesh sieves respectively, and be standby; Purified water is after boiling deoxidation treatment, and is standby; Sodium hydroxide is mixed with the sodium hydroxide solution that concentration is 1M, and is standby;
(2) take by weighing supplementary material by recipe quantity;
(3) simethicone is put 150 ℃ and was placed 3 hours with after silicon dioxide mixes, and take out the cooling back, mixture I; Ethylparaben is dissolved in the ethanol, gets solution I, and is standby; Disodiumedetate and aspartame get solution II with an amount of purified water dissolving fully, and be standby;
(4) behind acetylcysteine and microcrystalline Cellulose, the xanthan gum mix homogeneously, add among the mixture I, repeatedly mixing makes it even, slowly be distributed under the stirring then in glycerol and an amount of after treatment the purified water, add solution I, solution II, when adding purified water to nearly full dose, regulate pH value to 6～7.5 with the 1M sodium hydroxide solution, the reuse purified water is settled to full dose, cross colloid mill after stirring, making its mean diameter is below the 50 μ m, behind the collection colloid mill effluent, mix homogeneously gets semi-finished product once more;
(5) behind outward appearance and the drug content, fill becomes the 30ml/ bottle to semi-finished product after testing, finished product;
(6) product inspection qualified after, the warehouse-in.
3, clinical use
In preceding 20 minutes of digestive endoscopy inspection and treatment or imaging examination, measure 2～4 milliliters of second ammonia silicone oil composite suspensions, adding 100 ml waters, to shake up the back oral, conducts a survey after 20 minutes again.Medication dose can be taken the circumstances into consideration increase and decrease according to actual effect.
Embodiment 4
The preparation of second ammonia silicone oil composite Emulsion
1, prescription:
Simethicone 20g
Tween 80 10g
Sorbester p17 10g
Acetylcysteine 80g
Sodium carboxymethyl cellulose 6g
Saccharin sodium 0.1g
Sorbic acid 1g
2,6 ditertiary butyl p cresol 0.05g
Disodiumedetate 1g
Ethanol 10g
Purified water is to 1000ml
2, concrete steps:
(1) acetylcysteine is crossed 100 mesh sieves, and is standby; Purified water is after boiling deoxidation treatment, and is standby;
(2) take by weighing supplementary material by recipe quantity;
(3) 2,6 ditertiary butyl p cresol is dissolved in the ethanol, gets solution I, and is standby; Disodiumedetate, acetylcysteine and saccharin sodium get solution II with an amount of purified water dissolving fully, and be standby; Sodium carboxymethyl cellulose is scattered in an amount of purified water, gets uniform dispersion soln III, and is standby;
(4) Simethicone and Tween 80, sorbester p17 mix, after adding the equal proportion purified water again, complete with high-shearing dispersion emulsifying machine emulsifying, get the uniform colostrum of milky, stir and slowly add solution III, solution II, solution I and sorbic acid down in first Ruzhong, be settled to full dose with purified water, mix, get semi-finished product;
(5) behind outward appearance, emulsion stability, the drug content, fill becomes the 30ml/ bottle to semi-finished product after testing, finished product;
(6) product inspection qualified after, the warehouse-in.
3, clinical use
In preceding 20 minutes of digestive endoscopy inspection and treatment or imaging examination, measure 4～6 milliliters of second ammonia silicone oil composite Emulsions, adding 100 ml waters, to shake up the back oral, conducts a survey after 20 minutes again.Medication dose can be taken the circumstances into consideration increase and decrease according to actual effect.
Claims (7)
1, a kind of pharmaceutical composition that contains dimeticone/simethicone is characterized in that mainly being made by following bulk drugs: 1～500 part of 1～1000 part of acetylcysteine or its pharmaceutically acceptable salt and simethicone or Simethicone.
2, the pharmaceutical composition that contains dimeticone/simethicone as claimed in claim 1, it is characterized in that: the parts by weight of described crude drug are: 20～200 parts of 50～500 parts of acetylcysteine or its pharmaceutically acceptable salts and simethicone or Simethicones.
3, the pharmaceutical composition that contains dimeticone/simethicone as claimed in claim 2, it is characterized in that: the parts by weight of described crude drug are: 20～50 parts of 80～200 parts of acetylcysteine or its pharmaceutically acceptable salts and simethicone or Simethicones.
4, as the described pharmaceutical composition that contains dimeticone/simethicone of the arbitrary claim of claim 1～3, it is characterized in that: described acetylcysteine pharmaceutically acceptable salt is: organic nitrogen salt, hydrochlorate, sulfate, acetate, mesylate, tartrate, maleate, fumarate, hydrobromate, aspartate.
5, as the described pharmaceutical composition that contains dimeticone/simethicone of the arbitrary claim of claim 1～3, it is characterized in that: described pharmaceutical composition and mixing acceptable accessories are made clinically any or pharmaceutically acceptable dosage form.
6, the pharmaceutical composition that contains dimeticone/simethicone as claimed in claim 5 is characterized in that: clinically described or pharmaceutically acceptable dosage form is a kind of in granule, powder, suspensoid, the Emulsion.
7, the described pharmaceutical composition that contains dimeticone/simethicone of the arbitrary claim of claim 1～3 as digestive endoscopy inspection and treatment or imaging examination art before the purposes of adjuvant drug.
Priority Applications (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA2009101042439A CN101596181A (en) | 2009-07-03 | 2009-07-03 | A kind of pharmaceutical composition that contains dimeticone/simethicone |
| CN2010800298928A CN102470183B (en) | 2009-07-03 | 2010-06-13 | Pharmaceutical composition containing dimethicone/ simethicone |
| PCT/CN2010/000857 WO2011000208A1 (en) | 2009-07-03 | 2010-06-13 | Pharmaceutical composition containing dimethicone/ simethicone |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA2009101042439A CN101596181A (en) | 2009-07-03 | 2009-07-03 | A kind of pharmaceutical composition that contains dimeticone/simethicone |
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| Publication Number | Publication Date |
|---|---|
| CN101596181A true CN101596181A (en) | 2009-12-09 |
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| CNA2009101042439A Pending CN101596181A (en) | 2009-07-03 | 2009-07-03 | A kind of pharmaceutical composition that contains dimeticone/simethicone |
| CN2010800298928A Active CN102470183B (en) | 2009-07-03 | 2010-06-13 | Pharmaceutical composition containing dimethicone/ simethicone |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN2010800298928A Active CN102470183B (en) | 2009-07-03 | 2010-06-13 | Pharmaceutical composition containing dimethicone/ simethicone |
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| Country | Link |
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| CN (2) | CN101596181A (en) |
| WO (1) | WO2011000208A1 (en) |
Cited By (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2011000208A1 (en) * | 2009-07-03 | 2011-01-06 | Wang Guohua | Pharmaceutical composition containing dimethicone/ simethicone |
| CN102048690A (en) * | 2011-01-14 | 2011-05-11 | 四川健能制药有限公司 | Dimeticone emulsion and preparation method thereof |
| CN103110961A (en) * | 2012-11-30 | 2013-05-22 | 江苏唯德康医疗科技有限公司 | Preparation method of high-definition endoscope mucus-removal defoaming composite preparation |
| WO2013159699A1 (en) * | 2012-04-25 | 2013-10-31 | Wang Guohua | Vision definition enhancement system and method for gastrointestinal endoscope diagnosis and treatment |
| CN107441508A (en) * | 2017-08-13 | 2017-12-08 | 重庆天如生物科技有限公司 | Simethicone composition |
| CN111991373A (en) * | 2020-09-21 | 2020-11-27 | 力品药业（厦门）有限公司 | Aripiprazole orally-dissolving film and preparation method thereof |
| CN112870382A (en) * | 2021-01-28 | 2021-06-01 | 复旦大学附属中山医院 | Arabinose and silicone oil type antifoaming agent combination for bowel preparation |
| CN114099434A (en) * | 2021-11-19 | 2022-03-01 | 海南鑫开源医药科技有限公司 | Preparation process of dimeticone emulsion |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| CN114609079A (en) * | 2022-03-22 | 2022-06-10 | 山东达因海洋生物制药股份有限公司 | Method for detecting content of simethicone in simethicone emulsion |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1240384C (en) * | 1999-11-04 | 2006-02-08 | 美国爱科赛尔制药有限公司 | Transdermal administration of huperzine |
| CN101596181A (en) * | 2009-07-03 | 2009-12-09 | 重庆健能医药开发有限公司 | A kind of pharmaceutical composition that contains dimeticone/simethicone |
-
2009
- 2009-07-03 CN CNA2009101042439A patent/CN101596181A/en active Pending
-
2010
- 2010-06-13 CN CN2010800298928A patent/CN102470183B/en active Active
- 2010-06-13 WO PCT/CN2010/000857 patent/WO2011000208A1/en active Application Filing
Cited By (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2011000208A1 (en) * | 2009-07-03 | 2011-01-06 | Wang Guohua | Pharmaceutical composition containing dimethicone/ simethicone |
| CN102048690A (en) * | 2011-01-14 | 2011-05-11 | 四川健能制药有限公司 | Dimeticone emulsion and preparation method thereof |
| US10046288B2 (en) * | 2012-04-25 | 2018-08-14 | Chongqing Skyforbio Co., Ltd. | View definition enhancement system and method for gastrointestinal endoscope diagnosis and treatment |
| WO2013159699A1 (en) * | 2012-04-25 | 2013-10-31 | Wang Guohua | Vision definition enhancement system and method for gastrointestinal endoscope diagnosis and treatment |
| CN104379051A (en) * | 2012-04-25 | 2015-02-25 | 重庆天如生物科技有限公司 | Vision definition enhancement system and method for gastrointestinal endoscope diagnosis and treatment |
| US20150122294A1 (en) * | 2012-04-25 | 2015-05-07 | Guohua Wang | View definition enhancement system and method for gastrointestinal endoscope diagnosis and treatment |
| JP2015514522A (en) * | 2012-04-25 | 2015-05-21 | 重慶天如生物科技有限公司 | System and method for enhancing clarity of visual field for gastrointestinal endoscopy |
| CN104379051B (en) * | 2012-04-25 | 2017-02-15 | 重庆天如生物科技有限公司 | Vision definition enhancement system and method for gastrointestinal endoscope diagnosis and treatment |
| CN103110961A (en) * | 2012-11-30 | 2013-05-22 | 江苏唯德康医疗科技有限公司 | Preparation method of high-definition endoscope mucus-removal defoaming composite preparation |
| CN107441508A (en) * | 2017-08-13 | 2017-12-08 | 重庆天如生物科技有限公司 | Simethicone composition |
| CN107441508B (en) * | 2017-08-13 | 2020-11-20 | 重庆天如生物科技有限公司 | Simethicone composition |
| CN111991373A (en) * | 2020-09-21 | 2020-11-27 | 力品药业（厦门）有限公司 | Aripiprazole orally-dissolving film and preparation method thereof |
| CN111991373B (en) * | 2020-09-21 | 2022-04-08 | 力品药业(厦门)股份有限公司 | Aripiprazole orally-dissolving film and preparation method thereof |
| CN112870382A (en) * | 2021-01-28 | 2021-06-01 | 复旦大学附属中山医院 | Arabinose and silicone oil type antifoaming agent combination for bowel preparation |
| CN112870382B (en) * | 2021-01-28 | 2023-05-26 | 复旦大学附属中山医院 | Combination of arabinose and silicone oil defoamer for intestinal tract preparation |
| CN114099434A (en) * | 2021-11-19 | 2022-03-01 | 海南鑫开源医药科技有限公司 | Preparation process of dimeticone emulsion |
| CN114099434B (en) * | 2021-11-19 | 2022-12-16 | 海南鑫开源医药科技有限公司 | Preparation process of simethicone emulsion |
Also Published As
| Publication number | Publication date |
|---|---|
| WO2011000208A1 (en) | 2011-01-06 |
| CN102470183B (en) | 2013-12-11 |
| CN102470183A (en) | 2012-05-23 |
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