CN105902512A - Olaparib effervescent tablet and preparation method thereof - Google Patents
Olaparib effervescent tablet and preparation method thereof Download PDFInfo
- Publication number
- CN105902512A CN105902512A CN201610408577.5A CN201610408577A CN105902512A CN 105902512 A CN105902512 A CN 105902512A CN 201610408577 A CN201610408577 A CN 201610408577A CN 105902512 A CN105902512 A CN 105902512A
- Authority
- CN
- China
- Prior art keywords
- buddhist nun
- handkerchief buddhist
- effervescent tablet
- aura handkerchief
- aura
- 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.)
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Classifications
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- 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
- A61K31/50—Pyridazines; Hydrogenated pyridazines
- A61K31/502—Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with carbocyclic ring systems, e.g. cinnoline, phthalazine
-
- 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
- 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
-
- 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
- A61K9/2095—Tabletting processes; Dosage units made by direct compression of powders or specially processed granules, by eliminating solvents, by melt-extrusion, by injection molding, by 3D printing
Abstract
The invention relates to an olaparib effervescent tablet for maintenance treatment of platinum-sensitive recurrent BRCA mutation ovarian cancer adult patients and a preparation method thereof, and is aimed at providing a novel olaparib effervescent tablet rapid in disintegration, rapid in absorption, high in bioavailability, convenient to take, little in intestine residue and small in size effect for vast patients and medical workers. Olaparib serves as the raw material, some specific type and ratio of auxiliaries are added, the olaparib effervescent tablet is prepared according to the technical means described in the invention, and the product is sweet in taste, fragrant, rapid in effect, high in bioavailability and capable of particularly and easily improving medication compliance of patients.
Description
Technical field
The present invention relates to medicine of a kind of taking convenience and preparation method thereof, particularly to be for platinum sensitivity recurrent
Aura handkerchief Buddhist nun's effervescent tablet of maintaining treatment of BRCA sudden change ovarian cancer adult patient and preparation method thereof.
Background technology
The medicine of biotech company of Olaparib Yuan Shi Britain KuDOS Pharmaceuticals, A Sili in 2005
Health by after KuDOS corporate buyout, continual exploitation.The anticarcinogen Aura handkerchief Buddhist nun of December in 2014 AstraZeneca on the 19th (olaparib,
Trade name: Lynparza) " waking up from death ", EU Committee (EC) approved Lynparza, as one list medication, is used for
The maintaining treatment of platinum sensitivity recurrent BRCA sudden change ovarian cancer adult patient, this medicine also becomes for BRCA sudden change platinum sensitivity recurrence
The first PARP inhibitor of property ovarian cancer.Aura handkerchief Buddhist nun (Olaparib) is that a kind of innovation, pioneering oral poly ADP ribose gather
Synthase (PARP) inhibitor, PARP DNA plerosis can damage, plays an important role in DNA damage reparation with apoptosis.Logical
If often DNA double chain interruption can not get repairing, cell death can be triggered.Healthy cell is owing to there being a plurality of reparation DNA breakage
Signal path, PARP inhibitor is little on its impact, and some specific sudden changes that cancerous cell occurs, to PARP suppression sensitivity.
PARP is relevant to tumor type widely, this binding mode, gives Aura handkerchief Buddhist nun treatment and has the most swollen of DNA reparation defect
The potentiality of tumor type.Especially breast carcinoma and ovarian cancer.2009 " New England Journal of Medicines " and 2010 " lancet " are miscellaneous
It is significant that will all announces medicine Olaparib effect when treating breast carcinoma, ovarian cancer and carcinoma of prostate.Lynparza's is granted, is
Data based on an II phase clinical research (Study 191).This research is carried out in carrying BRCA sudden change ovarian cancer patients, number
According to showing, compared with placebo, Aura handkerchief Buddhist nun significantly extends Progression free survival phase (PFS) (11.2 months vs 4.3 months, p
< 0.00001).Although have 61 sections of breast cancer treatment medicines at present to obtain the approval of U.S. FDA, but in the fierce market competition
In, this medicine is still placed high hopes by AstraZeneca CEO Pascal Soriot, because medicine Olaparib once lists it
Sales volume reaches as high as 2,000,000,000 dollars.Effervescent tablet is a kind of quick-effective preparation grown up, and due to its distinctive advantage, the most more comes
More 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 Aura handkerchief Buddhist nun's 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 medicine that can be effectively improved Aura handkerchief Buddhist nun are dense
Degree, taking convenience, Aura handkerchief Buddhist nun's effervescent tablet and preparation method thereof of few side effects.
Aura handkerchief Buddhist nun's effervescent tablet of the present invention is in addition to principal agent, possibly together with adjuvant, by weight percentage, is 1%～15% Austria
La Pani, the adjuvant of 85%～95%.Adjuvant is the available adjuvant of any one being suitable for making effervescent tablet, and they can include
Filler, organic acid, inorganic base, correctives or odor mask, coloring agent, lubricant etc..In each oral formulations unit, containing Austria
La Pani 25mg～150mg, preferred dose is 30mg～150mg mg, and preferred dosage is 50～100mg. due to effervescent tablet
Require suck in the oral cavity clothes make tablet swallow after dissolving, good mouthfeel, to oral mucosa nonirritant.Therefore to supplementary product kind and
The selection of its performance is the key preparing effervescent tablet.The present invention is through selecting, it is determined that be suitable for the medicinal of Aura handkerchief Buddhist nun's effervescent tablet
Adjuvant, wherein filler selects the weight and volume being used for increasing effervescent tablet, in order to the molding of preparation and divided dose, the present invention
At least one in the preferred lactose of middle filler, sucrose, mannitol, sorbitol, xylitol etc..The kind of correctives and consumption
Select for whether this preparation has the mouthfeel of fragrant and sweet happy people most important.The filler lactose of the present invention, sucrose, mannitol, wood
Sugar alcohols etc. have the important function of taste masking concurrently；The organic acid of the present invention includes that tartaric acid, citric acid etc. have the important work of taste masking concurrently
With；The inorganic base sodium bicarbonate of the present invention, sodium carbonate etc. have the important function of taste masking concurrently；Additionally also add appropriate taste masking effect
Higher correctives, the preferred glycyrrhizin of correctives, disodium glycyrrhizinate, trisodium glycyrrhetinate, Rhizoma et radix valerianae, Fructus Pruni pseudocerasi, Fructus Vitis viniferae, Fructus Citri tangerinae, lemon
Lemon, Herba Menthae, grass Pueraria lobota, Fructus Musae, Fructus Ananadis comosi, peach flavor, maltose alcohol, saccharin sodium, protein sugar, sucrose, aspartame, stevioside
In at least one, mask the bad strange taste of Aura handkerchief Buddhist nun further, improve the mouthfeel of effervescent tablet.Effervescent tablet can add
Enter a certain amount of coloring agent, make tablet have pleasing visual appearance, contribute to eliminating the bored patient taken medicine and resist emotion.This
The preferred chlorophyll of bright coloring agent, caramel, sunset yellow, cocoa pigment, sodium-iron-chlorophyllin, lemon yellow, amaranth, kermes
In scarlet, orange, light blue, fast blue red, 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 Aura handkerchief Buddhist nun's powder and 150 mesh lactose powder, equal increments, mixing
Uniformly；Remaining adjuvant filler, organic acid, inorganic base, correctives, odor mask, coloring agent and lubricant equal increments are mixed
200 mesh sieves are crossed after closing uniformly；Join in Aura handkerchief Buddhist nun and lactose mixed-powder, after equal increments method mix homogeneously, directly
Tabletting.
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
Aura handkerchief Buddhist nun 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
Aura handkerchief Buddhist nun's 150g(percentage by weight 15%)
Sucrose 550g
Tartaric acid 60g
Sodium bicarbonate 60g
Disodium glycyrrhizinate 60g
Flavoring orange essence 33g
Red scarlet 32g
Pulvis Talci 55g
Make 1000 altogether
Preparation method: by 200 mesh Aura handkerchief Buddhist nun's powder and 200 mesh lactose powder, equal increments mix homogeneously；Remaining adjuvant is filled
200 mesh sieves are crossed after agent, organic acid, inorganic base, correctives, odor mask, coloring agent and lubricant equal increments mix homogeneously；Add
In Aura handkerchief Buddhist nun and lactose mixed-powder, after equal increments method mix homogeneously, direct compression.
Embodiment 2
Aura handkerchief Buddhist nun 100g (percentage by weight 10%)
Lactose 510g
Citric acid 75 g
Sodium carbonate 75g
Aspartame 7.5g
Glycyrrhizin 10 g
Peach flavor 72.5g
Orange 75g
Micropowder silica gel 75g
Make 1000 altogether
Preparation method: with embodiment 1.
Embodiment 3
Aura handkerchief Buddhist nun 40g (percentage by weight 4%)
Sucrose 515g
Tartaric acid 85g
Sodium bicarbonate 85g
Disodium glycyrrhizinate 60 g
Flavoring orange essence 75g
Red scarlet 75g
Pulvis Talci 65g
Make 1000 altogether
Preparation method: with embodiment 1.
Embodiment 4
Aura handkerchief Buddhist nun's 50g(percentage by weight 5%)
Lactose 535g
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 (6)
1. Aura handkerchief Buddhist nun's effervescent tablet, it is characterised in that: include the supplementary material of following weight percent proportioning,
Aura handkerchief Buddhist nun 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 Aura handkerchief Buddhist nun, be for platinum sensitivity recurrent BRCA sudden change ovarian cancer adult patient maintaining treatment three
Kind new medicine, currently carries out preclinical study.
At least one in the most wherein said filler preferably sucrose, lactose, mannitol, sorbitol, xylitol etc.；Organic acid
At least one in preferably citric acid, tartaric acid, citric acid；At least one in the preferred sodium bicarbonate of inorganic base or sodium carbonate；
The preferred glycyrrhizin of described correctives, disodium glycyrrhizinate, trisodium glycyrrhetinate, Rhizoma et radix valerianae, Fructus Pruni pseudocerasi, Fructus Vitis viniferae, Fructus Citri tangerinae, Fructus Citri Limoniae, Herba Menthae,
In grass Pueraria lobota, Fructus Musae, Fructus Ananadis comosi, peach flavor, maltose alcohol, saccharin sodium, protein sugar, sucrose, aspartame, stevioside at least
A kind of；The preferred chlorophyll of described coloring agent, caramel, sunset yellow, cocoa pigment, sodium-iron-chlorophyllin, lemon yellow, Amaranthus mangostanus L.
In red, carmine, scarlet, orange, light blue, fast blue indigo, red at least one；Described lubricant is selected from micropowder silica gel, hard
In fatty acid magnesium, Pulvis Talci at least one.
A kind of Aura handkerchief Buddhist nun's effervescent tablet the most according to claim 1, it is characterised in that: by weight percentage, containing Austria
La Pani 5%～15%, the percentage by weight of adjuvant is 70%～95%, and described Aura handkerchief Buddhist nun's effervescent tablet every contains Aura handkerchief Buddhist nun
Fourth is about 25mg～150mg.
A kind of Aura handkerchief Buddhist nun's effervescent tablet the most according to claim 1, it is characterised in that: ranitidine content be preferably 1%～
15%, described Aura handkerchief Buddhist nun's effervescent tablet, per unit weight be 1g a piece of in containing Aura handkerchief Buddhist nun be 25mg～150mg.
A kind of Aura handkerchief Buddhist nun's effervescent tablet the most according to claim 1, it is characterised in that: Aura handkerchief Buddhist nun's content be preferably 1%～
12%, described Aura handkerchief Buddhist nun's effervescent tablet, per unit weight be 1g a piece of in containing Aura handkerchief Buddhist nun be 25mg～150mg.
6. the preparation method of Aura handkerchief Buddhist nun's effervescent tablet, it is characterised in that: this is by 200 mesh Aura handkerchief Buddhist nun's powder and 200 mesh lactose
Powder, equal increments mix homogeneously；By remaining adjuvant filler, organic acid, inorganic base, correctives, odor mask, coloring agent and profit
200 mesh sieves are crossed after lubrication prescription equal increments mix homogeneously；Join in Aura handkerchief Buddhist nun and lactose mixed-powder, mix by equal increments method
After closing uniformly, direct compression.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610408577.5A CN105902512A (en) | 2016-06-13 | 2016-06-13 | Olaparib effervescent tablet and preparation method thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610408577.5A CN105902512A (en) | 2016-06-13 | 2016-06-13 | Olaparib effervescent tablet and preparation method thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN105902512A true CN105902512A (en) | 2016-08-31 |
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ID=56750771
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201610408577.5A Pending CN105902512A (en) | 2016-06-13 | 2016-06-13 | Olaparib effervescent tablet and preparation method thereof |
Country Status (1)
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| CN (1) | CN105902512A (en) |
Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN107929248A (en) * | 2017-12-06 | 2018-04-20 | 佛山市腾瑞医药科技有限公司 | A kind of Zaltoprofen effervescent tablet and preparation method thereof |
| CN107929249A (en) * | 2017-12-06 | 2018-04-20 | 佛山市腾瑞医药科技有限公司 | A kind of tolvaptan effervescent tablet and preparation method thereof |
| CN107982238A (en) * | 2017-12-07 | 2018-05-04 | 佛山市腾瑞医药科技有限公司 | A kind of ranolazine effervescent tablet and preparation method thereof |
| CN107998098A (en) * | 2017-12-07 | 2018-05-08 | 佛山市腾瑞医药科技有限公司 | A kind of nebivolol hydrochloric acid effervescent tablet and preparation method thereof |
| CN108078947A (en) * | 2017-12-08 | 2018-05-29 | 佛山市腾瑞医药科技有限公司 | A kind of Febustat effervescent tablet and preparation method thereof |
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| CN105254572A (en) * | 2015-11-09 | 2016-01-20 | 北京科莱博医药开发有限责任公司 | Crystal form, preparing method and application of Olaparib |
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Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN107929248A (en) * | 2017-12-06 | 2018-04-20 | 佛山市腾瑞医药科技有限公司 | A kind of Zaltoprofen effervescent tablet and preparation method thereof |
| CN107929249A (en) * | 2017-12-06 | 2018-04-20 | 佛山市腾瑞医药科技有限公司 | A kind of tolvaptan effervescent tablet and preparation method thereof |
| CN107982238A (en) * | 2017-12-07 | 2018-05-04 | 佛山市腾瑞医药科技有限公司 | A kind of ranolazine effervescent tablet and preparation method thereof |
| CN107998098A (en) * | 2017-12-07 | 2018-05-08 | 佛山市腾瑞医药科技有限公司 | A kind of nebivolol hydrochloric acid effervescent tablet and preparation method thereof |
| CN108078947A (en) * | 2017-12-08 | 2018-05-29 | 佛山市腾瑞医药科技有限公司 | A kind of Febustat effervescent tablet and preparation method thereof |
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Application publication date: 20160831 |