CN105997922A - Ranitidine-hydrochloride effervescent tablet and preparing method thereof - Google Patents
Ranitidine-hydrochloride effervescent tablet and preparing method thereof Download PDFInfo
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- CN105997922A CN105997922A CN201610406284.3A CN201610406284A CN105997922A CN 105997922 A CN105997922 A CN 105997922A CN 201610406284 A CN201610406284 A CN 201610406284A CN 105997922 A CN105997922 A CN 105997922A
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- ranitidine
- effervescent tablet
- ranitidine hydrochloride
- hydrochloride
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- 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
- A61K9/0002—Galenical forms characterised by the drug release technique; Application systems commanded by energy
- A61K9/0007—Effervescent
-
- 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
- A61K31/33—Heterocyclic compounds
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/34—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
- A61K31/341—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide not condensed with another ring, e.g. ranitidine, furosemide, bufetolol, muscarine
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- 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
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2013—Organic compounds, e.g. phospholipids, fats
- A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
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- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
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- Bioinformatics & Cheminformatics (AREA)
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- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
The invention relates to a ranitidine-hydrochloride effervescent tablet for treating stomach and duodenal ulcer and a preparing method thereof, and aims at providing the new-preparation ranitidine-hydrochloride effervescent tablet which is quick in disintegration and absorption, high in bioavailability, convenient to take and small in intestinal residual and side effect for spacious patients and medical workers. The preparing method includes the steps that ranitidine hydrochloride serves as a raw material, some specific kinds of auxiliary materials in specific proportion are added, and the ranitidine-hydrochloride chewable is prepared according to the technical means. The product is sweet in taste, fragrant, quick in effect taking and high in bioavailability, the medication compliance of patients is specially easy to improve.
Description
Technical field
The present invention relates to medicine of a kind of taking convenience and preparation method thereof, particularly to be for treat stomach, 12
Ranitidine hydrochloride effervescent tablet of Duodenalulcer and preparation method thereof.
Background technology
Ranitidine hydrochloride is antacid and the hydrochlorate of Mucosta ranitidine, the same ranitidine of pharmacological action,
Ranitidine is also known as ranitidine, and chemical constitution is similar to cimetidine, is a kind of new of synthesis on the basis of cimetidine
Type bisfentidine, untoward reaction is few compared with cimetidine, and the effect of gastric acid secretion inhibiting is 5～8 times of cimetidine.Right
Taste-blindness rate curative effect is high, and has quick-acting and long-acting feature, after effectively suppressing histamine and pentagastrin to stimulate
The gastric acid secretion caused, reduces gastric acid and gastric activity.Its suppression gastric acid output at night and 24 hours gastric acid amounts are in mass ratio
And molar concentration rate, titer is respectively 4～9 times and 5～12 times of cimetidine.While gastric acid secretion inhibiting, it is possible to press down
Pepsinia processed, and do not affect the secretion of gastrin and gonadal hormone etc..Though can be combined with Cytochrome P450, but affine
Power is the 1/10 of cimetidine.The rat stomach that oral or intragastric administration can suppress digestibility, irritability and indomethacin to cause is burst
The Cavia porcellus taste-blindness rate that infections and histamine cause, its inhibitory action is in direct ratio with drug level.Its chemical name is:
N'-methyl-N-[2 [[5-[(dimethylamino) methyl-2-furyl] methyl] sulfur generation] ethyl]-2-nitro-1,1-ethylene diamine
Hydrochlorate, molecular formula: C13H22N4O3S HCl, molecular weight: 350.87.
Only tablet, the capsule of list marketing at present.
The conventional tablet disintegration time of ranitidine hydrochloride is longer, absorption difference, bioavailability are low, supplementary product consumption ratio
Greatly, child, old man's dysphagia patients take inconvenience, compliance difference etc., have impact on ranitidine hydrochloride therapeutical effect send out
Wave.Effervescent tablet is a kind of quick-effective preparation grown up, and due to its distinctive advantage, is the most increasingly paid close attention to by people.
Effervescent tablet (chewable tablets) defines: reacted generation by organic acid in sheet and inorganic base in mouth
Bubble, the tablet swallowed again after promoting the rapid disintegrate of tablet.The organic acid being commonly incorporated into has tartaric acid or citric acid；The nothing added
Machine alkali has sodium bicarbonate or sodium carbonate；Addition sucrose, Herba Menthae, flavorant etc., to adjust taste, are suitable for child administration, for
The medicine of disintegrate difficulty is made effervescent tablet and can beneficially be absorbed.Technology requires: 1. mouthfeel, appearance uniform are good；2. foamed time
Should 3. other should meet tablet general rule requirement in 5 minutes.The feature of effervescent tablet: 1. disintegrate is fast, absorb fast, bioavailability
High；2. taking convenience 3. intestinal residual is few, and side effect is little.
Being mainly the sweet taste filleies such as lactose, sucrose, xylitol in prescription of the present invention, other correctivess increase the mouth of sheet
Sense, covers medicine unhappiness abnormal smells from the patient, and coloring agent makes tablet have pleasing appearance, and these are all more beneficial for increasing patient's medication and comply with
Property.Present invention also offers the preparation method about ranitidine hydrochloride effervescent tablet.
Used by the present invention, adjuvant supply producer is Ka Lekang pharmacy, Degussa pharmacy, Le Jiawen pharmacy, International Specialty Products system
Medicine company limited and the mountains and rivers, Huainan pharmaceutical Co. Ltd.
Summary of the invention
It is an object of the invention to provide a kind of absorption rapidly, bioavailability and the blood of ranitidine hydrochloride can be effectively improved
Concentration, taking convenience, the ranitidine hydrochloride effervescent tablet and preparation method thereof of few side effects.
Ranitidine hydrochloride effervescent tablet of the present invention is in addition to principal agent, possibly together with adjuvant, by weight percentage, be 5%～
15% ranitidine hydrochloride, the adjuvant of 85%～95%.Adjuvant is the available adjuvant of any one being suitable for making effervescent tablet, it
Can include filler, organic acid, inorganic base, correctives or odor mask, coloring agent, lubricant etc..Each oral formulations list
In Wei, containing ranitidine hydrochloride 75mg～225mg, preferred dose is 120mg～180mg mg, and preferred dosage is 130
～160mg. make tablet swallow after dissolving owing to effervescent tablet requires to suck in the oral cavity clothes, good mouthfeel, non-stimulated to oral mucosa
Property.Therefore the selection to supplementary product kind and performance thereof is the key preparing effervescent tablet.The present invention is through selecting, it is determined that be suitable for salt
The pharmaceutic adjuvant of acid ranitidine effervescent tablet, wherein filler selects the weight and volume being used for increasing effervescent tablet, in order to system
The molding of agent and divided dose, in the present invention in the preferred lactose of filler, sucrose, mannitol, sorbitol, xylitol etc. at least one
Kind.The kind of correctives and consumption select for whether this preparation has the mouthfeel of fragrant and sweet happy people most important.The present invention fills out
Fill agent lactose, sucrose, mannitol, xylitol etc. and have the important function of taste masking concurrently；The organic acid of the present invention includes tartaric acid, lemon
Lemon acid etc. has the important function of taste masking concurrently；The inorganic base sodium bicarbonate of the present invention, sodium carbonate etc. have the important function of taste masking concurrently；Separately
Also add outward the correctives that appropriate taste masking effect is higher, the preferred glycyrrhizin of correctives, disodium glycyrrhizinate, trisodium glycyrrhetinate,
Rhizoma et radix valerianae, Fructus Pruni pseudocerasi, Fructus Vitis viniferae, Fructus Citri tangerinae, Fructus Citri Limoniae, Herba Menthae, grass Pueraria lobota, Fructus Musae, Fructus Ananadis comosi, peach flavor, maltose alcohol, saccharin sodium, albumen
In sugar, sucrose, aspartame, stevioside, at least one, mask the bad strange taste of ranitidine hydrochloride further, improve bubble
Rise the mouthfeel of sheet.A certain amount of coloring agent can be added in effervescent tablet, make tablet have pleasing visual appearance, contribute to eliminating
It is sick of the patient taken medicine and resists emotion.The preferred chlorophyll of coloring agent of the present invention, caramel, sunset yellow, cocoa pigment, chlorophyll
In ferrum sodium salt, lemon yellow, amaranth, carmine, scarlet, orange, light blue, fast blue indigo, red at least one.
At least one in the preferred micropowder silica gel of lubricant, magnesium stearate, Pulvis Talci.
The effervescent tablet of the present invention can be prepared with direct powder compression.
Direct powder compression preparation process is: by 200 mesh ranitidine hydrochloride powder and 150 mesh lactose powder, equal increments,
Mix homogeneously；Remaining adjuvant filler, organic acid, inorganic base, correctives, odor mask, coloring agent and lubricant equivalent are passed
200 mesh sieves are crossed after increasing mix homogeneously；Join in ranitidine hydrochloride and lactose mixed-powder, by equal increments method mix homogeneously
After, direct compression.
The effervescent tablet of the present invention, its basic prescription composition includes following supplementary material, can be adjusted according to actual needs
With delete.
Composition percentage by weight
Ranitidine hydrochloride 5%～15%
Filler 60%～95%
Organic acid 0.1%～15%
Inorganic base 0.1%～15%
Correctives 0.01%～15%
Coloring agent 0.01%～0.5%
Lubricant 0.6%～5%.
Detailed description of the invention
Embodiment l
Ranitidine hydrochloride 75g(percentage by weight 5%)
Sucrose 1050g
Tartaric acid 75g
Sodium bicarbonate 75g
Disodium glycyrrhizinate 75g
Flavoring orange essence 37.5g
Red scarlet 37.5g
Pulvis Talci 75g
Make 1000 altogether
Preparation method: by 200 mesh ranitidine hydrochloride powder and 150 mesh lactose powder, equal increments mix homogeneously；By remaining adjuvant
200 mesh sieves are crossed after filler, organic acid, inorganic base, correctives, odor mask, coloring agent and lubricant equal increments mix homogeneously；
Join in ranitidine hydrochloride and lactose mixed-powder, after equal increments method mix homogeneously, direct compression.
Embodiment 2
Ranitidine hydrochloride 120g (percentage by weight 8%)
Lactose 980g
Citric acid 75 g
Sodium carbonate 75g
Aspartame 7.5g
Glycyrrhizin 10 g
Peach flavor 82.5g
Orange 75g
Micropowder silica gel 75g
Make 1000 altogether
Preparation method: with embodiment 1.
Embodiment 3
Ranitidine hydrochloride 150g (percentage by weight 10%)
Sucrose 895g
Tartaric acid 85g
Sodium bicarbonate 85g
Disodium glycyrrhizinate 60 g
Flavoring orange essence 75g
Red scarlet 75g
Pulvis Talci 75.0g
Make 1000 altogether
Preparation method: with embodiment 1.
Embodiment 4
Ranitidine hydrochloride 225g (percentage by weight 15%)
Lactose 860g
Citric acid 75 g
Sodium carbonate 75g
Aspartame 25g
Glycyrrhizin 15g
Peach flavor 80g
Orange 70g
Micropowder silica gel 75g
Make 1000 altogether
Preparation method: with embodiment 1.
Claims (5)
1. a ranitidine hydrochloride effervescent tablet, it is characterised in that: include the supplementary material of following weight percent proportioning,
Ranitidine hydrochloride 5%～15%
Filler 60%～95.0%
Organic acid 0.1%～5%
Inorganic base 0.1%～5%
Correctives 0.01%～5%
Coloring agent 0.01%～0.5%
Lubricant 0.6%～5%
Wherein said ranitidine hydrochloride, chemical name is: N'-methyl-N-[2 [[5-[(dimethylamino) methyl-2-furan
Base] methyl] sulfur generation] ethyl]-2-nitro-1,1-ethylene diamine hydrochlorate, molecular formula: C13H22N4O3S HCl, molecular weight:
350.87；
At least one in wherein said filler preferably sucrose, lactose, mannitol, sorbitol, xylitol etc.；Organic acid is excellent
Select at least one in citric acid, tartaric acid, citric acid；At least one in the preferred sodium bicarbonate of inorganic base or sodium carbonate；Institute
The preferred glycyrrhizin of correctives stated, disodium glycyrrhizinate, trisodium glycyrrhetinate, Rhizoma et radix valerianae, Fructus Pruni pseudocerasi, Fructus Vitis viniferae, Fructus Citri tangerinae, Fructus Citri Limoniae, Herba Menthae, grass
In Pueraria lobota, Fructus Musae, Fructus Ananadis comosi, peach flavor, maltose alcohol, saccharin sodium, protein sugar, sucrose, aspartame, stevioside at least one
Kind；The preferred chlorophyll of described coloring agent, caramel, sunset yellow, cocoa pigment, sodium-iron-chlorophyllin, lemon yellow, amaranth,
In carmine, scarlet, orange, light blue, fast blue indigo, red at least one；Described lubricant is selected from micropowder silica gel, stearic acid
In magnesium, Pulvis Talci at least one.
A kind of ranitidine hydrochloride effervescent tablet the most according to claim 1, it is characterised in that: by weight percentage, contain
Having ranitidine hydrochloride 5%～15%, the percentage by weight of adjuvant is 85%～95.%；
Described ranitidine hydrochloride effervescent tablet every is about 100mg～250mg containing ranitidine.
A kind of ranitidine hydrochloride effervescent tablet the most according to claim 1, it is characterised in that: ranitidine content is preferably
5%～15%, described ranitidine hydrochloride effervescent tablet, per unit weight be 1.5g a piece of in containing ranitidine be 75mg～
225mg。
A kind of ranitidine hydrochloride effervescent tablet the most according to claim 1, it is characterised in that: ranitidine content is preferably
8%～12%, described ranitidine hydrochloride effervescent tablet, per unit weight be 1.5g a piece of in containing ranitidine be 120mg～
180mg。
5. the preparation method of a ranitidine hydrochloride effervescent tablet, it is characterised in that: this by 200 mesh ranitidine hydrochloride powder with
150 mesh lactose powder, equal increments mix homogeneously；By remaining adjuvant filler, organic acid, inorganic base, correctives, odor mask,
200 mesh sieves are crossed after coloring agent and lubricant equal increments mix homogeneously；Join in ranitidine hydrochloride and lactose mixed-powder,
After equal increments method mix homogeneously, direct compression.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610406284.3A CN105997922A (en) | 2016-06-12 | 2016-06-12 | Ranitidine-hydrochloride effervescent tablet and preparing method thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610406284.3A CN105997922A (en) | 2016-06-12 | 2016-06-12 | Ranitidine-hydrochloride effervescent tablet and preparing method thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN105997922A true CN105997922A (en) | 2016-10-12 |
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ID=57091012
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201610406284.3A Pending CN105997922A (en) | 2016-06-12 | 2016-06-12 | Ranitidine-hydrochloride effervescent tablet and preparing method thereof |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN105997922A (en) |
Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5102665A (en) * | 1988-06-24 | 1992-04-07 | Glaxo Group Limited | Pharmaceutical compositions |
| US5728401A (en) * | 1997-04-16 | 1998-03-17 | Ranbaxy Laboratories, Ltd. | Effervescent ranitidine formulations |
| CN1276716A (en) * | 1997-10-21 | 2000-12-13 | 杰哈德·盖尔盖伊 | Effervescent base |
| CN1407885A (en) * | 1999-12-06 | 2003-04-02 | 布里斯托尔-迈尔斯斯奎布公司 | Histamine H2 antagonist effervescent composition |
-
2016
- 2016-06-12 CN CN201610406284.3A patent/CN105997922A/en active Pending
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5102665A (en) * | 1988-06-24 | 1992-04-07 | Glaxo Group Limited | Pharmaceutical compositions |
| US5728401A (en) * | 1997-04-16 | 1998-03-17 | Ranbaxy Laboratories, Ltd. | Effervescent ranitidine formulations |
| CN1276716A (en) * | 1997-10-21 | 2000-12-13 | 杰哈德·盖尔盖伊 | Effervescent base |
| CN1407885A (en) * | 1999-12-06 | 2003-04-02 | 布里斯托尔-迈尔斯斯奎布公司 | Histamine H2 antagonist effervescent composition |
Non-Patent Citations (2)
| Title |
|---|
| 王淑华、林永强: "泡腾片的常用辅料及制备方法", 《食品与药品》 * |
| 陆彬主编: "《药剂学》", 31 January 2003, 中国医药科技出版社 * |
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| PB01 | Publication | ||
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Application publication date: 20161012 |