CN102727456B - Drug port cavity disintegrating tablet and preparation method thereof - Google Patents
Drug port cavity disintegrating tablet and preparation method thereof Download PDFInfo
- Publication number
- CN102727456B CN102727456B CN201210236262.9A CN201210236262A CN102727456B CN 102727456 B CN102727456 B CN 102727456B CN 201210236262 A CN201210236262 A CN 201210236262A CN 102727456 B CN102727456 B CN 102727456B
- Authority
- CN
- China
- Prior art keywords
- solution
- preparation
- medicine
- spray drying
- effervescent
- 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.)
- Active
Links
Abstract
The present invention relates to and a kind of there is rapid delivery of pharmaceuticals and the good orally disintegrating tablet preparation of taste, the prescription designed for insoluble drug specifically and preparation method。Its preparation method by being sequentially carried out spray drying treatment by medicine, each adjuvant in same container, and obtaining is Powdered or microparticle shape mixture。Owing to adopting the mode of layering spray drying, have while part coating effect and disintegrate is rapid, and exposed drug moiety can take the lead in dissolving, and is followed successively by coating portion, core, is thought of as good Concentraton gradient, so as to medicine can fully be absorbed。Therefore, inapplicable effervescent or use a small amount of effervescent to can be achieved with the fater disintegration dissolution of medicine。
Description
Technical field
The invention belongs to field of pharmaceutical preparations, relate to a kind of there is rapid delivery of pharmaceuticals and the good orally disintegrating tablet preparation of taste, the prescription designed for insoluble drug specifically and preparation method。
Background technology
Oral cavity disintegration tablet is a kind of new oral dosage forms。Such preparation can under anhydrous condition (or only have a small amount of water exist) fater disintegration in oral cavity, enter digestive tract with swallowing act, without mucosa absorption in oral cavity, body absorption, metabolic process are consistent with conventional tablet。According to estimates, there are about the people of 50% to swallowing tablet and capsule is had any problem, have impact on the compliance of Drug therapy。At department of pediatrics and old medicine, the solid preparation that can dissolve in water or suspend, can chew or can dissolve rapidly in mouth there is very big demand。
The ultimate challenge of exploitation rapidly dissolving tablet is exactly that the physical property of tablet and disintegrating property will be good。Eurand company of Italy develops Ziplets technology, is applicable to water-insoluble drug。This technology mainly adopts the appropriate water-insoluble inorganic auxiliary material of addition and effervescent combined, even if when compression force and tablet hardness are all relatively low, rapidly dissolving tablet also can have good physical property and disintegrating property simultaneously。But, the water-insoluble materials of employing larger proportion is, easily producing grittiness, cause and take constant, simultaneously the flavored action of effervescent is limited, this is because effervescent needs just can play a role under water function, and for oral environment, consider disintegrate and the medicine dissolution needs of whole tablet, should not use in a large number, and time less, sufficient bubble cannot be produced again and play the effect covering poor taste。
Summary of the invention
It is an object of the invention to improve the deficiency of existing insoluble drug oral cavity disintegration tablet, it is provided that a kind of taking convenience, absorb rapid-action, good mouthfeel and the high insoluble drug orally disintegrating tablet preparation of bioavailability。
Of the present invention and insoluble drug oral cavity disintegration tablet, according to weight ratio, insoluble drug 5-50%, binding agent 1-10%, filler 20-90%, disintegrating agent 5-45%, effervescent 0-30%, fluidizer 0-5%, lubricant 0-3%。
Described further and insoluble drug oral cavity disintegration tablet, according to weight ratio, insoluble drug 10-20%, binding agent 3-5%, filler 40-90%, disintegrating agent 10-40%, effervescent 0-30%, may also include fluidizer 0-5%, lubricant 0-3%。
Further, above-mentioned insoluble drug oral cavity disintegration tablet, according to weight ratio, effervescent 5-20%, may also include fluidizer 3-5%, lubricant 1-3%。
Wherein, binding agent includes but are not limited to sky hot glue family macromolecule polymer, hydrophilic cellulose base polymer, polyvinyl alcohol, Polyethylene Glycol, polyvinylpyrrolidone (PVP), alginic acid and alginate, xanthan gum, hydroxypropyl cellulose and the hydroxypropyl methyl celluloses (HPMC) such as starch, pregelatinized Starch, dextrin, maltodextrin, sucrose, arabic gum or gelatin, can be used alone, it is possible to combination uses。It is preferably polyvinylpyrrolidone (PVP), arabic gum, gelatin, hypromellose。
Filler is tasteless or sweet cpd, include but are not limited to mannitol, xylitol, sorbitol, maltose, erythrol, microcrystalline Cellulose,SMCC, polymerization sugarCoupling sugar, glucose, lactose, sucrose, dextrin and starch etc., it is possible to be used alone, it is also possible to combination application。It is preferably mannitol, xylitol, sorbitol。
Disintegrating agent includes but are not limited to crospolyvinylpyrrolidone (PVPP), carboxymethyl starch sodium (CMS-Na), low substituted hydroxy-propyl methylcellulose (L-HPC), cross-linking sodium carboxymethyl cellulose (CCNa) and soybean polysaccharideDeng, can be used alone, it is possible to combination uses。It is preferably crospolyvinylpyrrolidone (PVPP)。
Fluidizer includes but are not limited to micropowder silica gel, Pulvis Talci, Cab-O-sil, Arosil, hydrated sodium aluminosilicate。Lubricant includes but are not limited to magnesium stearate, calcium stearate, zinc stearate, glyceryl monostearate, Polyethylene Glycol, hydrogenated vegetable oil, sodium stearyl fumarate, polyoxyethylene monostearate, single Laurel sucrose acid ester, sodium laurylsulfate, lauryl alcohol sulphuric acid younger sister, Stepanol MG and Pulvis Talci etc., can be used alone, it is possible to combination uses。
Effervescent includes but are not limited to the mixture of malic acid, citric acid or citric acid and sodium bicarbonate or sodium carbonate。
Above-mentioned oral cavity disintegration tablet, it is by special preparation method, namely in same container, medicine, each adjuvant is sequentially carried out spray drying treatment, and obtaining is Powdered or microparticle shape mixture。Except fluidizer and lubricant, the adjuvant of all the other kinds, for instance binding agent, filler, disintegrating agent, three's order can arbitrarily change or or one of which be joined in other two kinds with arbitrary proportion。Same process can also be taked when increasing other kind adjuvants。
Concrete preparation method includes:
1., by medicine, filler, disintegrating agent mixed dissolution in solvent, it is called solution 1, solution 2, solution 3。
2. solution 1 first carry out spray drying in fluid bed or spray dryer, and making medicine is after " boiling " state, then sprays into solution 2 and solution 3 successively, dry, and obtaining is Powdered or microparticle shape solids。
3. by the solids mixing that 2. step obtains, mix with other adjuvants, direct compression or granulation。
It should be noted that the order that above-mentioned solution 2 and 3 sprays into is unrestricted, it is only necessary to spray into successively。Preferably, disintegrating agent solution 3 is finally sprayed into。
Preferably, above-mentioned preparation method, it is possible to disintegrating agent equivalent is divided equally or arbitrary proportion is dissolved in each solution, in ie in solution 1 and 2, and no longer prepare solution 3。
Preferably, part adhesive can be dissolved in solvent and be formed after solution 4 by above-mentioned preparation method, in the 2. step, sprays into spraying into after solution 1 makes medicine be " boiling " state。Equivalent or arbitrary proportion can also be dissolved in solution 2,3 and spraying into together。
Similarly, it is spray into after " boiling " state that correctives also can also can be taked said method to carry out being formed after solution 5 until medication medication by above-mentioned preparation method, equivalent or arbitrary proportion can also be dissolved in solution 2,3,4 and spraying into together。
With common spray drying the difference is that, the present invention is by medicine and major auxiliary burden, and including disintegrating agent, binding agent, after filler etc. sequentially enters spray drying, it is possible to covering the bad of medicine better and ask, meanwhile, disintegrate is rapid。Also can fater disintegration when not needing effervescent。
Preferably, when there being effervescent, above-mentioned steps 3. in add, or step 2. in by acid moieties/alkali part, one of them adds in solution with equivalent or arbitrary proportion, remaining alkali part/acid moieties mix with other adjuvants after tabletting after direct compression or granulation。Owing to adopting the mode of layering spray drying, have while part coating effect and disintegrate is rapid, and exposed drug moiety can take the lead in dissolving, and is followed successively by coating portion, core, is thought of as good Concentraton gradient, so as to medicine can fully be absorbed。Therefore, inapplicable effervescent or use a small amount of effervescent to can be achieved with the fater disintegration dissolution of medicine。
It should be noted that, when taking pelletizing press sheet technique, when selecting have fluidizer, lubricant, add after granulation。Preferably, prescription forms, and according to weight ratio is:
Wherein, above-mentioned adjuvant can use other adjuvants preferred to replace。
Above-mentioned oral cavity disintegration tablet, its preparation method includes:
1. insoluble drug, filler, disintegrating agent, binding agent are dissolved separately in solvent, are called solution A 1, solution A 2, solution A 3。
2. solution A 1 first carries out spray drying, and making medicine is after " boiling " state, then sprays into solution A 2 and solution A 3 successively, dry, and obtaining is Powdered or microparticle shape solids。
3. by the solids mixing that 2. step obtains, mix with other adjuvants, direct compression。Further, prescription forms, and according to weight ratio is:
Wherein, above-mentioned adjuvant can use other adjuvants preferred to replace。
Above-mentioned oral cavity disintegration tablet, its preparation method includes:
1. insoluble drug, filler, disintegrating agent, binding agent are dissolved separately in solvent, are called solution A 1, solution A 2, solution A 3。Meanwhile, by citric acid/sodium bicarbonate, one of them is dissolved in solution A 2 or A3, or is dissolved in solution A 2 and A3 after decile。
2. solution A 1 first carries out spray drying, and making medicine is after " boiling " state, then sprays into solution A 2 and solution A 3 successively, dry, and obtaining is Powdered or microparticle shape solids。
3. by the solids mixing that 2. step obtains, mix with other adjuvants, direct compression。
In the present invention, involved solvent, the solvent namely making medicine, adjuvant etc. dissolve, it is not limited to particular types, as long as making the compound can good solvent, it is possible to select organic solvent, for instance acetone, ethanol etc., it is also possible to select water。
Insoluble drug of the present invention is not limited to specifically treat field, is not limited to certain compounds structure, only the dissolution properties of medicine is required。
Detailed description of the invention
Further explain and describe present invention by the following examples。Described embodiment, only for helping to understand present invention, is understood not to the restriction to present subject matter and protection domain。
The drug release determination method of the present invention is referring to Chinese Pharmacopoeia two annex of version in 2010, with water for release medium。
Embodiment 1
Prescription forms, and according to weight ratio is:
Preparation method includes:
1. insoluble drug, binder/disintegrant, filler are dissolved in 95% ethanol, are called solution B 1, solution B 2, solution B 3。
2. solution B 1 first carries out spray drying, and making medicine is after " boiling " state, then sprays into solution B 2 and solution B 3 successively, dry, and obtaining is Powdered or microparticle shape solids。
3. by the solids mixing that 2. step obtains, mix with magnesium stearate after intermediates content detection, direct compression。
Embodiment 2
Prescription forms, and according to weight ratio is:
Preparation method includes:
1. insoluble drug, binding agent, disintegrating agent/filler are dissolved in acetone solvent, are called solution C 1, solution C 2, solution C 3。
2. solution C 1 first carries out spray drying, and making medicine is after " boiling " state, then sprays into solution C 2 and solution C 3 successively, dry, and obtaining is Powdered or microparticle shape solids。
3. by the solids mixing that 2. step obtains, after intermediates content detection, mix with magnesium stearate, direct compression。
Embodiment 3
Prescription forms, and according to weight ratio is:
Preparation method includes:
1. insoluble drug, binding agent, filler are dissolved in acetone, are called solution D 1, solution D 2, solution D 3, disintegrating agent decile is separately added into solution D 2, solution D 3。
2. solution D 1 first carries out spray drying, and making medicine is after " boiling " state, then sprays into solution D 2 and solution D 3 successively, dry, and obtaining is Powdered or microparticle shape solids。
3. by the solids mixing that 2. step obtains, granulating, 50 DEG C dry, and cross 20 mesh sieves, after intermediates content detection, mix with magnesium stearate, tabletting。
Embodiment 4
Prescription forms, and according to weight ratio is:
Preparation method includes:
1. insoluble drug, binding agent, filler are dissolved in acetone, are called solution E 1, solution E 2, solution E 3, disintegrating agent and one of them decile of citric acid/sodium bicarbonate are separately added into solution E 2, solution E 3。
2. solution E 1 first carries out spray drying, and making medicine is after " boiling " state, then sprays into solution E 2 and solution E 3 successively, dry, and obtaining is Powdered or microparticle shape solids。
3., after the solids that 2. step obtains being detected with residue adjuvant mixing intermediates content, mix with magnesium stearate, tabletting。
Above-described embodiment sample is detected: be placed in 2ml water, measure complete disintegration time and mouthfeel。Refer to following table。
The disintegration time of each embodiment insoluble drug of table 1
It should be noted that, above embodiments is just to illustrating the present invention。Under the premise of the spirit and essence that not necessarily depart from the present invention, those skilled in the art can be designed that multiple alternative and the improvement project of the present invention, and it all should be understood to be within protection scope of the present invention。
Claims (2)
1. an ascorbic oral cavity disintegration tablet, prescription composition according to weight ratio is
2. the preparation method of oral cavity disintegration tablet as claimed in claim 1, including:
1) vitamin C, binding agent, disintegrating agent and filler are dissolved separately in acetone solvent, are called solution C 1, solution C 2, solution C 3；
2) solution C 1 first carrying out spray drying, making medicine is after " boiling " state, then sprays into solution C 2 and solution C 3 successively, dry, and obtaining is Powdered or microparticle shape solids；
3) solids mixing second step obtained, after intermediates content detection, mixes with magnesium stearate, direct compression。
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201210236262.9A CN102727456B (en) | 2012-07-03 | 2012-07-03 | Drug port cavity disintegrating tablet and preparation method thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201210236262.9A CN102727456B (en) | 2012-07-03 | 2012-07-03 | Drug port cavity disintegrating tablet and preparation method thereof |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN102727456A CN102727456A (en) | 2012-10-17 |
| CN102727456B true CN102727456B (en) | 2016-06-22 |
Family
ID=46984230
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201210236262.9A Active CN102727456B (en) | 2012-07-03 | 2012-07-03 | Drug port cavity disintegrating tablet and preparation method thereof |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN102727456B (en) |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103271885A (en) * | 2013-05-23 | 2013-09-04 | 浙江华海药业股份有限公司 | Tadalafil orally disintegrating tablet and preparation method thereof |
| CN105213333A (en) * | 2014-06-30 | 2016-01-06 | 深圳海王药业有限公司 | A kind of tadanafil pharmaceutical composition and preparation method thereof |
| CN112022827B (en) * | 2020-09-30 | 2023-03-31 | 上海信谊天平药业有限公司 | Cyproheptadine hydrochloride quick-release pharmaceutical preparation and preparation method thereof |
| CN114392240B (en) * | 2022-01-20 | 2023-12-19 | 北京微智瑞医药科技有限公司 | Vitamin C orally disintegrating micro-tablet and preparation method thereof |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101193638A (en) * | 2005-04-13 | 2008-06-04 | 拜耳医药保健股份公司 | Therapeutic combination in case of benign prostate hyperplasia |
Family Cites Families (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2011030351A2 (en) * | 2009-09-03 | 2011-03-17 | Rubicon Research Private Limited | Taste - masked pharmaceutical compositions |
-
2012
- 2012-07-03 CN CN201210236262.9A patent/CN102727456B/en active Active
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101193638A (en) * | 2005-04-13 | 2008-06-04 | 拜耳医药保健股份公司 | Therapeutic combination in case of benign prostate hyperplasia |
Also Published As
| Publication number | Publication date |
|---|---|
| CN102727456A (en) | 2012-10-17 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP3404648B2 (en) | Fast disintegrating solid preparation | |
| JP5604304B2 (en) | Orally disintegrating solid preparation | |
| JP5053865B2 (en) | Method for producing orally disintegrating solid preparation | |
| CN101888834A (en) | Oral dispersable tablet | |
| JP4524502B2 (en) | Imadafenacin-containing intraoral rapidly disintegrating tablets | |
| RU2616516C2 (en) | Pharmaceutical composition containing olmesartan medoxomil and rosuvastatin or its salt | |
| CN104244930A (en) | Orally disintegrating tablet and method for producing same | |
| JP2010519201A (en) | Controlled release formulation containing cilostazol and method for producing the same | |
| JPWO2011019043A1 (en) | Intraoral quick disintegrating tablet containing two or more kinds of particles | |
| CN102716097A (en) | Method for controlling medicament release rate of orally disintegrating tablet | |
| MX2014004811A (en) | Taste-masked pharmaceutical composition for oral administration and a process for the preparation thereof. | |
| CN102512393A (en) | Oral disintegrated tablet containing tolvaptan | |
| CN109996542A (en) | Oral disnitegration tablet comprising diamine derivative | |
| CN102727456B (en) | Drug port cavity disintegrating tablet and preparation method thereof | |
| CN102631329A (en) | Oral paroxetine disintegrating tablet and preparation process thereof | |
| WO2012029838A1 (en) | Orally disintegrating tablet | |
| JP6479658B2 (en) | Super-fast disintegrating tablet and method for producing the same | |
| EP2848242A1 (en) | Orally disintegrating formulations of Linagliptin | |
| CN102727455B (en) | A kind of tadalafil oral cavity disintegration tablet and preparation method thereof | |
| JP7336388B2 (en) | Tablet and its manufacturing method | |
| JP5614445B2 (en) | Particulate pharmaceutical composition for oral administration | |
| JP2019131597A (en) | Super quick decomposition tablet and production method thereof | |
| JP6469234B2 (en) | Super-fast disintegrating tablet and method for producing the same | |
| JP2008517909A (en) | Tablet containing active substance with poor compressibility and tocopherol polyethylene glycol succinate (TPGS) | |
| CN103720674B (en) | Famotidine floating-adhesive micro-tablet capsule and preparation method thereof |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| C53 | Correction of patent of invention or patent application | ||
| CB02 | Change of applicant information |
Address after: 100083 Haidian District, Xueyuan Road, No. 30, A building, room No. 15, room, room 15 Applicant after: COSCI MED-TECH Co.,Ltd. Address before: 100190, room 1410, satellite building, No. 63, Zhichun Road, Beijing, Haidian District Applicant before: COSCI MED-TECH Co.,Ltd. |
|
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| C14 | Grant of patent or utility model | ||
| GR01 | Patent grant | ||
| TR01 | Transfer of patent right | ||
| TR01 | Transfer of patent right |
Effective date of registration: 20230323 Address after: 8639, Floor 6, Building 3, No. 3, Yongchang North Road, Daxing District, Beijing, 100176 Patentee after: Beijing Kexin Jurun Pharmaceutical Technology Co.,Ltd. Address before: 100083 room 15, 15 / F, block a, Tiangong building, 30 Xueyuan Road, Haidian District, Beijing Patentee before: COSCI MED-TECH Co.,Ltd. |