CN107441037A - A kind of Risperidone oral administration solution - Google Patents
A kind of Risperidone oral administration solution Download PDFInfo
- Publication number
- CN107441037A CN107441037A CN201710700700.5A CN201710700700A CN107441037A CN 107441037 A CN107441037 A CN 107441037A CN 201710700700 A CN201710700700 A CN 201710700700A CN 107441037 A CN107441037 A CN 107441037A
- Authority
- CN
- China
- Prior art keywords
- risperidone
- oral administration
- solution
- administration solution
- added
- 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
Classifications
-
- 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
- A61K9/0087—Galenical forms not covered by A61K9/02 - A61K9/7023
- A61K9/0095—Drinks; Beverages; Syrups; Compositions for reconstitution thereof, e.g. powders or tablets to be dispersed in a glass of water; Veterinary drenches
-
- 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
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- 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
- A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
- A61K47/12—Carboxylic acids; Salts or anhydrides thereof
-
- 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
- A61K47/22—Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones
-
- 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
- A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
- A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
-
- 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
- A61K47/46—Ingredients of undetermined constitution or reaction products thereof, e.g. skin, bone, milk, cotton fibre, eggshell, oxgall or plant extracts
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- Inorganic Chemistry (AREA)
- Botany (AREA)
- Medicinal Preparation (AREA)
Abstract
The present invention relates to a kind of Risperidone oral administration solution, the invention belongs to pharmaceutical preparation production field.Risperidone raw material has stronger bitter taste, it is prepared into bitter taste after preparation to take a turn for the better, but still it is bad mouthfeel to be present, the characteristics of poor compliance, it is necessary to develop a kind of steady quality, Risperidone oral solution formulation curative for effect and good in taste, in addition, Risperidone oral administration solution dissolubility is good prepared by the present invention, bioavilability is high, and preparation technology is simple, cost is low, is adapted to industrialized production.
Description
Technical field
The present invention relates to a kind of Risperidone oral administration solution, belong to pharmaceutical preparation production technical field.
Background technology
Risperidone is Ben Bing isoxazole derivativeses, and chemical name is：3- [2- [4- (fluoro- 1, the 2- benzos isoxazole -3- of 6-
Base) -1- piperidyls] ethyl] -6,7,8,9- tetrahydrochysene -2- methyl -4H- pyridos [1,2- α] pyrimidin-4-ones.
Risperidone is the atypical antipsychotic agents of a new generation, is developed and listed by Belgian Janssen companies, trade name dimension
Think logical (Risperdal), listed in Canada and Britain within 1993, obtain within 1994 FDA approvals.China started to ratify in 1997
Use.Risperidone oral administration solution was realized local production by Xi'an Yang Sen in 2001.The formulation applied in the market removes mouth
Take outside solution, also oral disintegrating tablet, dispersible tablet, conventional tablet, capsule, microsphere for injection etc..Risperidone is in global antipsychotic city
Field is constantly in leadership, " cookle " level kind is become within 2001, when annual sales amount is up to 18.45 hundred million dollars, 2007
Year has more reached 46.97 hundred million dollars, and turning into influenceed greatly the original new drug of human lives in last 10 years ten of 20th century.And city at home
In, only the Risperidone of Xi'an Janssen Pharmaceutica just occupies the 36.3% of whole market share, it is seen that Risperidone is applied extensive.
It is contemplated that before the higher antipsychotics of better efficacy, security occurs, Risperidone can be still treatment mental disease
First-line drug, there is great social value and meaning.
Marketing enterprises include the list that original grinds import Risperidal and the medicine of domestic Changzhou four for the Risperidone oral administration solution country at present
Gram, about 140 yuan/bottle of being marked the price in the former 30ml specifications, about 50 yuan/bottle of being marked the price in the latter's same size, import price is somewhat expensive.Separately
Outside, the bitter taste of Risperidone bulk drug, although still having patient by diluting and bitter taste decrease during preparation of preparation
It is heavier that bitter taste is reacted after taking, the problem of poor taste.
Through retrieval, do not find that Risperidone oral administration solution adds the Patents documents of flavouring temporarily.It is therefore desirable to develop
A kind of favorable solubility, steady quality, compliance are good, and cheap Risperidone oral solution formulation.
The content of the invention
The bitter taste of Risperidone bulk drug, although by diluting and bitter taste decrease during preparation of preparation, still
There is patient to react bitter taste after taking heavier, the problem of poor taste.Risperidone, compared with indissoluble solution, has certain in acid condition in water
Dissolubility, acidic materials increase the solubility of insoluble drug, may be such that the bioavilability of insoluble drug as cosolvent
Greatly improve.The present invention has used Arabic gum, saccharin sodium and flavoring orange essence to eliminate Risperidone as flavouring composition
The problem of poor tastes such as the bitter taste of oral administration solution, while fruity odours are also added, taken so as to improve children and the elderly
With the compliance of this product；This product also uses DL- tartaric acid as pH adjusting agent, is favorably improved the dissolubility of Risperidone, from
And improve bioavilability.
Present invention aims to overcome that the defects of prior art, there is provided a kind of Risperidone oral administration solution, feature are mouthfeel
And comply with preferably, bioavilability greatly improves, and more former triturate is cheap.
The Risperidone oral administration solution of the present invention includes Risperidone, pH adjusting agent, flavouring composition, preservative, purified water.
Each composition of Risperidone oral administration solution of the present invention presses total formulation weight gauge：
Preferably, each composition of Risperidone oral administration solution of the invention presses total formulation weight gauge：
PH adjusting agent of the present invention is 0.75% DL- tartaric acid and 0.1% sodium hydroxide.
Flavouring composition of the present invention is Arabic gum, saccharin sodium and flavoring orange essence, weight ratio is 1000~
10000:1~8:15~150, preferred weight ratio is 2000~6000:1~5:30~100.
The one kind of preservative of the present invention in benzoic acid, sodium benzoate, sorbic acid, preferably benzoic acid.
Another object of the present invention is to provide a kind of preparation method of Risperidone oral administration solution：
(1) pH adjusting agent is added in purified water, stirring and dissolving, adds Risperidone and stir to being completely dissolved；
(2) flavouring and preservative are added into mixed solution, stirring and dissolving, supplements Purified Water q. s, is mixed, filtering；
(3) above-mentioned solution is filling, sterilizes, dispenses and produce.
The present invention has the advantages that：
Risperidone oral administration solution steady quality of the present invention, it is curative for effect and good in taste, in addition, sharp prepared by the present invention
It is good to train ketone oral administration solution dissolubility, bioavilability is high, and preparation technology is simple, and cost is low, is adapted to industrialized production.
Embodiment
The following examples explanation present invention, but do not limit the invention in any way.
Embodiment 1 (1000 bottles of amounts)
(1) by DL- tartaric acid, sodium hydroxide is added in purified water, and adjusts pH to 3~4, stirring and dissolving, adds profit
Training ketone is stirred to being completely dissolved；(2) Arabic gum, saccharin sodium, flavoring orange essence and benzoic acid are added into mixed solution, stirring is molten
Solution, Purified Water q. s are supplemented, mixed, filtering；(3) above-mentioned solution is filling, sterilizes, dispenses and produce.
Embodiment 2 (1000 bottles of amounts)
(1) by DL- tartaric acid, sodium hydroxide is added in purified water, and adjusts pH to 3~4, stirring and dissolving, adds profit
Training ketone is stirred to being completely dissolved；(2) Arabic gum, saccharin sodium, flavoring orange essence and benzoic acid are added into mixed solution, stirring is molten
Solution, Purified Water q. s are supplemented, mixed, filtering；(3) above-mentioned solution is filling, sterilizes, dispenses and produce.
Embodiment 3 (1000 bottles of amounts)
(1) by DL- tartaric acid, sodium hydroxide is added in purified water, and adjusts pH to 3~4, stirring and dissolving, adds profit
Training ketone is stirred to being completely dissolved；(2) Arabic gum, saccharin sodium, flavoring orange essence and benzoic acid are added into mixed solution, stirring is molten
Solution, Purified Water q. s are supplemented, mixed, filtering；(3) above-mentioned solution is filling, sterilizes, dispenses and produce.
Embodiment 4 (1000 bottles of amounts)
(1) by DL- tartaric acid, sodium hydroxide is added in purified water, and adjusts pH to 3~4, stirring and dissolving, adds profit
Training ketone is stirred to being completely dissolved；(2) Arabic gum, saccharin sodium, flavoring orange essence and benzoic acid are added into mixed solution, stirring is molten
Solution, Purified Water q. s are supplemented, mixed, filtering；(3) above-mentioned solution is filling, sterilizes, dispenses and produce.
Embodiment 5 (1000 bottles of amounts)
(1) by DL- tartaric acid, sodium hydroxide is added in purified water, and adjusts pH to 3~4, stirring and dissolving, adds profit
Training ketone is stirred to being completely dissolved；(2) Arabic gum, saccharin sodium, flavoring orange essence and benzoic acid are added into mixed solution, stirring is molten
Solution, Purified Water q. s are supplemented, mixed, filtering；(3) above-mentioned solution is filling, sterilizes, dispenses and produce.
Embodiment 6 (1000 bottles of amounts)
(1) by DL- tartaric acid, sodium hydroxide is added in purified water, and adjusts pH to 3~4, stirring and dissolving, adds profit
Training ketone is stirred to being completely dissolved；(2) Arabic gum, saccharin sodium, flavoring orange essence and benzoic acid are added into mixed solution, stirring is molten
Solution, Purified Water q. s are supplemented, mixed, filtering；(3) above-mentioned solution is filling, sterilizes, dispenses and produce.
Embodiment 7：It is not added with flavouring composition comparative examples 1 (1000 bottles of amounts)
(1) by DL- tartaric acid, sodium hydroxide is added in purified water, and adjusts pH to 3~4, stirring and dissolving, adds profit
Training ketone is stirred to being completely dissolved；(2) Arabic gum, saccharin sodium, flavoring orange essence and benzoic acid are added into mixed solution, stirring is molten
Solution, Purified Water q. s are supplemented, mixed, filtering；(3) above-mentioned solution is filling, sterilizes, dispenses and produce.
Embodiment 8：Sensory test
10 subjects are selected, taste tests are carried out to 6 embodiments and 1 comparative example at random, entered according to mouthfeel quality
Row scoring, scoring rank are divided into 10 points (very good), 8 points (fine), 6 points (preferable), 4 points (general), 3 points (poor), 1 point (compared with
Difference).It the results are shown in Table 1：
The embodiment 1-7 sensory tests of table 1
| Embodiment 1 | Embodiment 2 | Embodiment 3 | Embodiment 4 | Embodiment 5 | Embodiment 6 | Comparative example 1 | |
| Subject 1 | 6 | 8 | 10 | 8 | 8 | 4 | 4 |
| Subject 2 | 8 | 10 | 6 | 10 | 6 | 6 | 6 |
| Subject 3 | 8 | 10 | 10 | 8 | 8 | 6 | 3 |
| Subject 4 | 6 | 8 | 10 | 8 | 6 | 4 | 4 |
| Subject 5 | 6 | 8 | 6 | 10 | 8 | 3 | 1 |
| Subject 6 | 10 | 6 | 10 | 10 | 8 | 4 | 3 |
| Subject 7 | 6 | 8 | 6 | 8 | 6 | 6 | 3 |
| Subject 8 | 4 | 6 | 8 | 8 | 6 | 6 | 6 |
| Subject 9 | 4 | 6 | 8 | 10 | 4 | 6 | 4 |
| Subject 10 | 6 | 6 | 10 | 8 | 4 | 6 | 4 |
| Total score | 64 | 76 | 84 | 88 | 64 | 51 | 38 |
Embodiment 9：Medicine stability is investigated
Accelerated test：Every embodiment 1-6 samples and the comparative example 1 for being not added with flavouring composition are placed in (40 ± 2
DEG C), in the insulating box of relative humidity 75%, place six months.One-time detection Risperidone is respectively sampled respectively at the 1st, 2,3, June to contain
Measure, about material and microbial limit, result of the test is shown in Table 2, and observation embodiment 1-7 color samples, transparency results are shown in
Table 3.
The embodiment 1-6 accelerated test results of table 2
The embodiment 1-7 character pair ratios of table 3
Embodiment 1-6 sample is placed 6 months under acceleration conditions, and microbial limit and content have no significant change, miscellaneous
Matter content slightly has rise trend, but compound standard regulation.In accelerated test, the comparative example 1 for being not added with flavouring composition goes out
White opacity is showed, and there are a large amount of insoluble solids, embodiment 1-6 is in colourless transparent liquid, and sample stability is good.
Claims (3)
- A kind of 1. Risperidone oral administration solution, it is characterised in that：Oral administration solution is by Risperidone, pH adjusting agent, flavouring composition, anti- Rotten agent, purified water composition, each composition press total formulation weight gauge：The flavouring composition is made up of Arabic gum, saccharin sodium and flavoring orange essence, and weight ratio is 1000~10000:1~8: 15~150, preferred weight ratio is 2000~6000:1~5:30~90.
- 2. Risperidone oral administration solution according to claim 1, it is characterised in that the pH adjusting agent is 0.75%DL- wine Stone acid and 0.1% sodium hydroxide, the preservative are selected from benzoic acid, sodium benzoate or sorbic acid one of which.
- 3. Risperidone oral administration solution according to claim 1, its feature are being that preparation method comprises the following steps：Will PH adjusting agent is added in purified water, stirring and dissolving, is added Risperidone and is stirred to being completely dissolved；Flavoring is added into mixed solution Agent and preservative, stirring and dissolving, Purified Water q. s are supplemented, mixed, filtering；Above-mentioned solution is filling, sterilizes, dispenses and produce.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201710700700.5A CN107441037A (en) | 2017-08-16 | 2017-08-16 | A kind of Risperidone oral administration solution |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201710700700.5A CN107441037A (en) | 2017-08-16 | 2017-08-16 | A kind of Risperidone oral administration solution |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN107441037A true CN107441037A (en) | 2017-12-08 |
Family
ID=60492531
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201710700700.5A Pending CN107441037A (en) | 2017-08-16 | 2017-08-16 | A kind of Risperidone oral administration solution |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN107441037A (en) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN115381773A (en) * | 2022-09-23 | 2022-11-25 | 南京正科医药股份有限公司 | Risperidone oral liquid |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1148226C (en) * | 1994-07-11 | 2004-05-05 | 詹森药业有限公司 | Aqueous risperidone formulations |
| CN101269014A (en) * | 2007-03-21 | 2008-09-24 | 北京德众万全药物技术开发有限公司 | Orally disintegrating tablet of risperidone and preparation method thereof |
| CN101584652A (en) * | 2009-06-19 | 2009-11-25 | 上海医药(集团)有限公司 | Risperidone sustained-release gel injection and preparation method thereof |
-
2017
- 2017-08-16 CN CN201710700700.5A patent/CN107441037A/en active Pending
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1148226C (en) * | 1994-07-11 | 2004-05-05 | 詹森药业有限公司 | Aqueous risperidone formulations |
| CN101269014A (en) * | 2007-03-21 | 2008-09-24 | 北京德众万全药物技术开发有限公司 | Orally disintegrating tablet of risperidone and preparation method thereof |
| CN101584652A (en) * | 2009-06-19 | 2009-11-25 | 上海医药(集团)有限公司 | Risperidone sustained-release gel injection and preparation method thereof |
Non-Patent Citations (1)
| Title |
|---|
| 姚静编: "《药用辅料应用指南》", 31 August 2011, 中国医药科技出版社 * |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN115381773A (en) * | 2022-09-23 | 2022-11-25 | 南京正科医药股份有限公司 | Risperidone oral liquid |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| EP1845805B1 (en) | Non-alcoholic beverage enriched with 1h2 16o | |
| CN109528649B (en) | Self-emulsifying oral preparation of terpene pharmaceutical composition, preparation method and application | |
| Kluk et al. | Application properties of oral gels as media for administration of minitablets and pellets to paediatric patients | |
| CN111346052A (en) | Desloratadine citrate disodium oral liquid preparation and preparation method and application thereof | |
| EP3137056B1 (en) | Bismuth-containing liquid pharmaceutical suspensions | |
| CN107441037A (en) | A kind of Risperidone oral administration solution | |
| CN106309363A (en) | Paroxetine hydrochloride oral suspension and preparation method thereof | |
| Janakiraman et al. | Fabrication and characterization of cocoa butter-based caffeine fast-melting tablets | |
| AU2016351301B2 (en) | Method and product for testing response to oral glucose load | |
| TW200413027A (en) | Oral liquid tolterodine composition | |
| CN107582576A (en) | A kind of composition with biological inflammation-diminishing function and preparation method thereof | |
| CN106265724A (en) | Smectite turbid liquor | |
| CN104383552A (en) | Drug taste-masking agent and preparation method thereof | |
| US11864570B2 (en) | Therapeutic composition including carbonated solution | |
| CN117883379A (en) | Oral alkaline solvent composition and preparation method and application thereof | |
| US9358216B2 (en) | Tincture for infusing resveratrol and methods of use | |
| KR100903690B1 (en) | Composition containing ornithine for relieving hang-over and alcohol liquor containing ornithine | |
| CN111437250A (en) | Stable mefenanamine ammonium oral solution and preparation method thereof | |
| Shoosanglertwijit et al. | Physical, chemical, and microbiological stability of extemporaneous furosemide suspensions | |
| CN113143863A (en) | Oral solvent composition and preparation method and application thereof | |
| CN116531478B (en) | Paclitaxel-traditional Chinese medicine grease composite emulsion and preparation method and application thereof | |
| CN106261215A (en) | Fructus Jujubae fruit drink and preparation method thereof | |
| CN108283664A (en) | Alleviation containing curcumin, which is still drank after a night, uses preparation | |
| CN112715816A (en) | Leisure beverage containing water-soluble nano cannabidiol and preparation method thereof | |
| JP2023143782A (en) | Mango leaf extract-blended beverage |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| PB01 | Publication | ||
| PB01 | Publication | ||
| SE01 | Entry into force of request for substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| WD01 | Invention patent application deemed withdrawn after publication | ||
| WD01 | Invention patent application deemed withdrawn after publication |
Application publication date: 20171208 |