CN101548978B - Pharmaceutical composition containing alendronate sodium - Google Patents
Pharmaceutical composition containing alendronate sodium Download PDFInfo
- Publication number
- CN101548978B CN101548978B CN2008101033242A CN200810103324A CN101548978B CN 101548978 B CN101548978 B CN 101548978B CN 2008101033242 A CN2008101033242 A CN 2008101033242A CN 200810103324 A CN200810103324 A CN 200810103324A CN 101548978 B CN101548978 B CN 101548978B
- Authority
- CN
- China
- Prior art keywords
- alendronate sodium
- pharmaceutical composition
- mixing
- solid dispersion
- following
- 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
Landscapes
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
Abstract
The invention discloses a pharmaceutical composition containing alendronate sodium and a preparation method thereof. By preparing a solid dispersion, the pharmaceutical composition improves the solubility of the medicament, reduces the irritability of the medicament to the mucous membrane, and increases the bioavailability of the principal medicament and is used for curing osteoporosis.
Description
Technical field
The invention discloses a kind of pharmaceutical composition that is used to treat osteoporosis, particularly relate to a kind of pharmaceutical composition that contains the solid dispersion of Alendronate sodium.
Background technology
Alendronate sodium is a third generation diphosphate treatment osteoporosis.Alendronate sodium is new and effective bone resorption inhibitor, can suppress the activity of osteoclast, reduces bone resorption, directly is not suppressed to the active and bone formation process of osteocyte.Oral Alendronate sodium 10mg/ days or 70mg/ can suppress to reduce relevant bone loss with endogenous estrogen during week very effectively, and toleration is good, is a kind of Therapeutic Method of alternative postmenopausal osteoporosis newly.
The holdup time of Alendronate sodium intravenously administrable in blood is very short, and about 60%～70% concentrates in bone very soon, and remainder (30%～40%) is by RE.Behind the oral administration, the Alendronate sodium bioavailability is merely 0.7%.The main cause that produces is that Alendronate sodium can not can only pass through epithelial tight connection through the epithelial cell barrier through cell traffic, absorbs through paracellular shunt pathway and passes through.But its molecular weight is relatively large, has hindered this transhipment; In addition, under the small intestinal physiological pH, the complete ionization of Alendronate sodium, BBM institute is electronegative to have hindered them with the other approach transhipment of cell.Simultaneously Alendronate sodium has also reduced the oral administration biaavailability of Alendronate sodium with calcium ion and other bivalent cation complexations in small intestinal.
Alendronate sodium has certain stimulation to esophagus.Find that in clinical practice erosive esophagitis takes place the minority women, thus these article should not be used for esophagostenosis, relax can not or the patient of other esophagus emptying obstacles, to dyspepsia, the women Yao Shenyong of dysphagia or other gastroenteropathys.
The bioavailability that the Alendronate sodium oral formulations is extremely low makes most medicine fail fully to be absorbed by human body effectively, and excessive Alendronate sodium is the main cause that causes side effect to take place.So the zest of the dissolubility of increase medicine, the bioavailability that improves, minimizing mucosa becomes the subject matter of this medicine.
CN1745753A, two pieces of patents of CN1745754A disclose the preparation that adopts inclusion technique and the preparation of nanoscale principal agent respectively.Because the poorly water-soluble of Alendronate sodium, more than two pieces of patents do not mention the problems such as zest that improve bioavailability, minimizing mucosa through the dissolubility that adopts the method that prepare solid dispersion to improve principal agent.The applicant finds through a large amount of experiment, and the solid dispersion system that adopts Eudragit E100 and PEG6000 and Alendronate sodium to process efficiently solves the poorly soluble problem of principal agent, raising bioavailability of medicament, the toxic and side effects of reduction Alendronate sodium.
Summary of the invention
The present invention provides a kind of pharmaceutical composition that contains Alendronate sodium, contains the solid dispersion and the acceptable accessories of Alendronate sodium.
Pharmaceutical composition provided by the invention, described solid dispersion carrier are the mixture that Eudragit F100 and PEG6000 form.
Solid dispersion provided by the invention, the percentage by weight of said Eudragit E100 are 1%～15%.Solid dispersion according to claim 2 is characterized in that described PEG6000 percentage by weight is 5%～30%.
Pharmaceutical composition provided by the invention, described acceptable auxiliary are starch, microcrystalline Cellulose.
Pharmaceutical composition provided by the invention, the percentage by weight of said starch are 15%～35%.
Pharmaceutical composition provided by the invention, the percentage by weight of said microcrystalline Cellulose are 15%～30%.
Pharmaceutical composition provided by the invention, described pharmaceutical composition is used to treat osteoporosis.
The specific embodiment
Below in conjunction with embodiment the present invention is done further detailed description, but be not limited to following embodiment.Wherein " % " is meant " percentage by weight ".
Embodiment 1
This embodiment is for directly processing tablet
Preparation technology: take by weighing Alendronate sodium, PEG6000, Eudragit E100, microcrystalline Cellulose and starch mixing by recipe quantity, use 8% starch slurry solution to be binding agent, 16 order wet granulations, 60 ℃ of oven dry.24 order granulate are measured moisture, after adding magnesium stearate and Pulvis Talci mix, and 60～80N tabletting.
Embodiment 2
This embodiment processes sheet again after processing solid dispersion earlier
Preparation technology: take by weighing Alendronate sodium, PEG6000 by recipe quantity, Eudragit E100 prepares solid dispersion, behind the crushing screening with microcrystalline Cellulose, starch mixing; 16 order wet granulations; 60 ℃ of oven dry, 24 order granulate are measured moisture; After adding the mixing of magnesium stearate and Pulvis Talci, 60～80N tabletting.
Embodiment 3
This embodiment processes sheet again after processing solid dispersion earlier
Preparation technology: take by weighing Alendronate sodium, PEG6000, Eudragit E100 by recipe quantity and prepare solid dispersion, with microcrystalline Cellulose, starch and mixing, use 8% starch slurry solution to be binding agent behind the crushing screening; 16 order wet granulations; 60 ℃ of oven dry, 24 order granulate are measured moisture; After adding the mixing of magnesium stearate and Pulvis Talci, 60～80N tabletting.
Embodiment 1, embodiment 2 and embodiment 3 are carried out drug release determination.
Assay method: according to the assay method of release degree, promptly " 2005 editions two appendix XD drug release determinations of the Chinese pharmacopoeia method three therapeutic methods of traditional Chinese medicine is a release medium with 250mL water, temperature (37.5 ± 0.5) ℃, 75 rev/mins of rotating speeds.The result sees the following form:
Process solid dispersion through this pharmaceutical composition, increase the dissolution rate of principal agent, bioavailability of medicament improves, and reduces toxic and side effects.
Claims (2)
1. a pharmaceutical composition that contains Alendronate sodium is characterized in that, each component percentage composition is following:
Preparation technology is following: take by weighing Alendronate sodium, PEG6000, Eudragit E100 prepares solid dispersion, behind the crushing screening with microcrystalline Cellulose, starch mixing; 16 order wet granulations; 60 ℃ of oven dry, 24 order granulate are measured moisture; After adding the mixing of magnesium stearate and Pulvis Talci, 60～80N tabletting.
2. a pharmaceutical composition that contains Alendronate sodium is characterized in that, each component percentage composition is following:
Preparation technology is following: take by weighing Alendronate sodium, PEG6000, Eudragit E100 and prepare solid dispersion, with microcrystalline Cellulose, starch and mixing, use 8% starch slurry solution to be binding agent behind the crushing screening; 16 order wet granulations; 60 ℃ of oven dry, 24 order granulate are measured moisture; After adding the mixing of magnesium stearate and Pulvis Talci, 60～80N tabletting.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2008101033242A CN101548978B (en) | 2008-04-03 | 2008-04-03 | Pharmaceutical composition containing alendronate sodium |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2008101033242A CN101548978B (en) | 2008-04-03 | 2008-04-03 | Pharmaceutical composition containing alendronate sodium |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN101548978A CN101548978A (en) | 2009-10-07 |
| CN101548978B true CN101548978B (en) | 2012-11-21 |
Family
ID=41153621
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN2008101033242A Active CN101548978B (en) | 2008-04-03 | 2008-04-03 | Pharmaceutical composition containing alendronate sodium |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN101548978B (en) |
Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105796595A (en) * | 2016-04-06 | 2016-07-27 | 海南师范大学 | Application of rare earth alendronate in preparation of osteoporosis treatment drug |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1443065A (en) * | 2000-07-17 | 2003-09-17 | 山之内制药株式会社 | Pharmaceutical composition improved in peroral absorbability |
-
2008
- 2008-04-03 CN CN2008101033242A patent/CN101548978B/en active Active
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1443065A (en) * | 2000-07-17 | 2003-09-17 | 山之内制药株式会社 | Pharmaceutical composition improved in peroral absorbability |
Non-Patent Citations (1)
| Title |
|---|
| 刘红梅等.阿仑膦酸钠片.《中国新药杂志》.1996,第5卷(第05期), * |
Also Published As
| Publication number | Publication date |
|---|---|
| CN101548978A (en) | 2009-10-07 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| CN102970979B (en) | Solid composite medicament with reinforcing agent and preparation method thereof | |
| CN101099729B (en) | Oral solid preparation containing ambroxol hydrochloride and salbutamol active components | |
| CN101278932B (en) | Sustained release medicinal compositions containing Zaltoprofen, preparation method and application thereof | |
| AU2011227446B2 (en) | Process of manufacturing a lyophilized fast dissolving, multi-phasic dosage form | |
| CN102198110B (en) | Tenofovir disoproxil fumarate dispersible tablets and preparation method thereof | |
| CN102225047A (en) | Enteric solid oral dosage form of bisphosphonate containing a chelating agent | |
| TW201138774A (en) | Coated tablet formulations | |
| WO2007026864A1 (en) | Method for preparation of pharmaceutical composition having improved disintegradability | |
| KR20160112012A (en) | Rapid dissolve tablet compositions for vaginal adminstration | |
| US20230404974A1 (en) | Transmucosal dephosphorylated psychoactive alkaloid composition and preparation thereof | |
| CN103705478B (en) | Oral tablet containing tenofovir disoproxil fumarate | |
| JP2008528575A (en) | Pharmaceutical composition containing bisphosphonate for improving oral absorption rate | |
| US20160030358A1 (en) | Solid Dosage Form of Coated Bisphosphonate Particles | |
| KR101050076B1 (en) | Compositions of Oral Formulations Containing Controlled Release Aceclofenac and Methods for Making the Same | |
| CN102451162A (en) | Olanzapine medicine absorbed through oral mucosa | |
| CN102349915B (en) | Acetaminophen, caffeine, chlorphenamine maleate, and vitamin C preparation and preparation method thereof | |
| WO2009084041A4 (en) | Pharmaceutical compositions of dexibuprofen | |
| CN101548978B (en) | Pharmaceutical composition containing alendronate sodium | |
| KR101708086B1 (en) | Pharmaceutical or neutraceutical formulation | |
| CN106667944A (en) | Sustained release preparation containing prostaglandin drugs | |
| CN101099730A (en) | Oral solid preparation containing ambroxol hydrochloride and guaifenesin active components | |
| WO2014125085A1 (en) | Oral pharmaceutical formulations comprising nimesulide and thiocolchicoside | |
| CN104688747B (en) | Pharmaceutical composition comprising tenofovir disoproxil fumarate | |
| CN1762341A (en) | Salvianolic acid compound for treating cardiovascular and cerebrovascular disease and liver disease, and application thereof | |
| CN101756946A (en) | Oral solid preparation for treating chronic bronchitis |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| ASS | Succession or assignment of patent right |
Owner name: VENTURE PHARMACEUTICAL (HAINAN) CO., LTD. Free format text: FORMER OWNER: DEZHONG WANQUAN PHARMACEUTICALS TECH. DEV. CO., LTD., BEIJING Effective date: 20120530 |
|
| C41 | Transfer of patent application or patent right or utility model | ||
| COR | Change of bibliographic data |
Free format text: CORRECT: ADDRESS; FROM: 100097 HAIDIAN, BEIJING TO: 570314 HAIKOU, HAINAN PROVINCE |
|
| TA01 | Transfer of patent application right |
Effective date of registration: 20120530 Address after: 570314 Nanhai Avenue, Hainan, Haikou, China, No. 279 Applicant after: Beijing D-Venturepharm Technology Development Co., Ltd. Address before: 100097 Beijing city Haidian District Sijiqing Wanquan Zhuang 3 Building Applicant before: Dezhong Wanquan Pharmaceuticals Tech. Dev. Co., Ltd., Beijing |
|
| C14 | Grant of patent or utility model | ||
| GR01 | Patent grant |