CN1823781A - Etholadin maleate stomach retention tablet - Google Patents
Etholadin maleate stomach retention tablet Download PDFInfo
- Publication number
- CN1823781A CN1823781A CN 200510062041 CN200510062041A CN1823781A CN 1823781 A CN1823781 A CN 1823781A CN 200510062041 CN200510062041 CN 200510062041 CN 200510062041 A CN200510062041 A CN 200510062041A CN 1823781 A CN1823781 A CN 1823781A
- Authority
- CN
- China
- Prior art keywords
- parts
- gastric
- tablet
- hpmc
- 100000cpas
- 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.)
- Granted
Links
Landscapes
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
Abstract
A gastric detention tablet of ethorlatine maleate is proportionally prepared from ethorlatine maleate, HPMC, foaming agent, filler, lubricant and adhesive. Its detention time in stomach is more than 8 hr.
Description
(1) technical field
The present invention relates to a kind of MN-1695 gastric residential tablet.
(2) background technology
Floating in stomach is detained preparation, also cry the floating drug transmission system (Floating Drug DeliverySystem, FDDS).Because the density of preparation is lower than gastric juice, so, can swim on the gastric juice after oral, the emptying of food is less to the influence of Entogastric lingering, contained medicine slowly releases with certain rule in flotation process, enters the body circulation again after absorbing, or plays a role in the gastric part.This type of preparation has caused the great attention of pharmaceutical industry.
Irsogladine maleate is a kind of novel gastric mucosa protectant; compare with numerous gastric mucosa protectants, it has its unique mechanism of action, promptly by increasing the cyclic adenosine monophosphate content in the gastric mucosa; strengthen the connection of gastric epithelial cell, stablize gastric mucosal cell and bring into play the cytophylaxis effect.Simultaneously its blood flow that can also increase normal gastric mucosa and ulcer edge mucosa to be promoting mucosa regeneration, and few with consumption, price is low, untoward reaction is few etc., and characteristics are won victory in similar medicine, as bismuth preparation, prostate class medicine etc.This medicine went on the market in Japan in 1989, China's Ministry of Public Health approval of import in 1993.A large amount of clinical data show that this medicine presents excellent curative to active gastric ulcer both at home and abroad.
Yet because common irsogladine maleate tablet is shorter in the time of staying of stomach, drug treating time is shorter.Thereby need a kind of time of staying of exploitation badly and grow, have the dosage form of slow release effect
(3) summary of the invention
The object of the invention is providing a kind of MN-1695 gastric residential tablet.
Described MN-1695 gastric residential tablet comprises the component of following weight portion:
Principal agent: 4～10 parts of MN-1695,
Adjuvant: 30～45 parts of the HPMC of viscosity 4000～100000cpas,
6～10 parts of foaming agent,
40～50 parts of filleies,
0.5～2 part of lubricant,
0.1～5 part of binding agent.
Described HPMC viscosity is preferably 100000cpas.
Described foaming agent is preferably NaHCO
3Adding foaming agent is in order to reduce the density of tablet, NaHCO
3With the hydrochloric acid generation chemical reaction in the simulated gastric fluid:
, the CO of generation
2Bubble is enclosed in the skin of tablet, has increased the volume of tablet, has reduced density, and the buoyancy of floating tablets is increased.NaHCO
3Content has well to rise when 8% left and right sides and floats and hold the time of floating, and does not reach in 6 hours completely and discharge, and its content is 10% o'clock the time of floating and 8% close of rising, but stripping is very fast, so NaHCO most preferably
3Content is 8%.
Described filler is preferably lactose.
Described lubricant is preferably Pulvis Talci.
Described binding agent is preferably PVP.
MN-1695 gastric residential tablet of the present invention preferably includes the component of following weight portion:
Principal agent: 4～6 parts of MN-1695,
35～45 parts of the HPMC of adjuvant: viscosity 100000cpas,
NaHCO
36～10 parts,
40～45 parts of lactose,
0.5～1.5 part of Pulvis Talci,
2～5 parts of PVP.
Described MN-1695 gastric residential tablet, most preferably form by the component of following weight parts:
4 parts of MN-1695,
40 parts of the HPMC of viscosity 100000cpas,
NaHCO
38 parts,
42 parts of lactose,
1 part of Pulvis Talci,
5 parts of PVP.
MN-1695 gastric residential tablet provided by the invention can continue to discharge medicine at gastric more than 8 hours; prolonged the holdup time of medicine than other oral tablet at gastric; strengthen medicine to the gastric mucosal protection effect, thereby can treat gastric ulcer better.
(4) specific embodiment
The invention will be further described below in conjunction with embodiment, but protection scope of the present invention is not limited to this.
Embodiment one
1, the preparation of floating tablets:
Take by weighing the following material of crossing 80 mesh sieves in advance respectively: MN-1695 1.6g, HPMC (K100, viscosity 100000cpas) 16g, NaHCO
33.2g, lactose 18.8g, on blank sheet of paper, mix earlier with the equivalent method of progressively increasing, mix after sieve, put into big mortar then, the PVP of Dropwise 5 % makes soft material while grinding, and crosses the sieve series wet granular with 18 purpose standard screens, puts into electric heating constant temperature air dry oven homoiothermic to 60 ℃ drying 1 hour.Take out the back and carry out granulate with 16 purpose standard screens, add lubricant Pulvis Talci 0.4g again, carry out mixing with the equivalent method of progressively increasing, carry out tabletting with single punch tablet machine at last, control hardness is at 3Kg-4Kg.Suppress 200, every heavy 200mg.
The MN-1695 gastric residential tablet constituent content that finally makes is as follows:
4 parts of MN-1695,
40 parts of the HPMC of viscosity 100000cpas,
NaHCO
38 parts,
42 parts of lactose,
1 part of Pulvis Talci,
5 parts of PVP.
2, the mensuration of flotation time
The above-mentioned tablet that makes is put into the beaker that simulated gastric fluid is housed, observe its floating time and investigate its flotation property.Found that it is 2 minutes that this tablet works the time of floating, continue the flotation time, meet the prescription of gastric residential tablet greater than 8 hours.
The MN-1695 gastric residential tablet that the present invention makes has prolonged the holdup time of medicine at gastric effectively, and is very helpful to chronic gastric ulcer disease patient's treatment.
3, the drug release determination of gastric residential tablet:
Arbitrary extracting is 6 from the tablet that tabletting makes, after precision is weighed, place medicament dissolution instrument (little agar diffusion method), with 200ml, 37 ℃ of simulated gastric fluids is medium, 50 rev/mins of mensuration of carrying out the release in vitro degree of rotating speed, extract dissolution fluid respectively at stipulated time 2,4,6,8,10,12h with the 10ml syringe, pass through filtering with microporous membrane rapidly, collect subsequent filtrate, measuring 5ml with the pipet precision is diluted in the volumetric flask of 25ml, shake up, and record the peak area of medicine with HPLC, the simulated gastric fluid of additional respective amount in the cup simultaneously.Go out release according to the survey calculated by peak area, the result is as shown in table 1 below:
Table 1
| Time/h | 2 | 4 | 6 | 8 | 10 | 12 |
| Release/% | 46 | 70 | 82 | 92 | 96 | 98 |
As can be seen from Table 1, MN-1695 gastric residential tablet of the present invention can continue to discharge medicine at gastric more than 8 hours, has reached the slow release purpose.
Claims (8)
1, a kind of MN-1695 gastric residential tablet comprises the component of following weight portion:
Principal agent: 4～10 parts of MN-1695,
Adjuvant: 30～45 parts of the HPMC of viscosity 4000～100000cpas,
6～10 parts of foaming agent,
40～50 parts of filleies,
0.5～2 part of lubricant,
0.1～5 part of binding agent.
2, MN-1695 gastric residential tablet as claimed in claim 1 is characterized in that described HPMC viscosity is 100000cpas.
3, MN-1695 gastric residential tablet as claimed in claim 1 is characterized in that described foaming agent is NaHCO
3
4, MN-1695 gastric residential tablet as claimed in claim 1 is characterized in that described filler is a lactose.
5, MN-1695 gastric residential tablet as claimed in claim 1 is characterized in that described lubricant is a Pulvis Talci.
6, MN-1695 gastric residential tablet as claimed in claim 1 is characterized in that described binding agent is PVP.
7, MN-1695 gastric residential tablet as claimed in claim 1 is characterized in that comprising the component of following weight portion:
Principal agent: 4～6 parts of MN-1695,
35～45 parts of the HPMC of adjuvant: viscosity 100000cpas,
NaHCO
36～10 parts,
40～45 parts of lactose,
0.5～1.5 part of Pulvis Talci,
2～5 parts of PVP.
8, MN-1695 gastric residential tablet as claimed in claim 7 is characterized in that being made up of the component of following weight parts:
4 parts of MN-1695,
40 parts of the HPMC of viscosity 100000cpas,
NaHCO
38 parts,
42 parts of lactose,
1 part of Pulvis Talci,
5 parts of PVP.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNB2005100620414A CN100438874C (en) | 2005-12-16 | 2005-12-16 | Etholadin maleate stomach retention tablet |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNB2005100620414A CN100438874C (en) | 2005-12-16 | 2005-12-16 | Etholadin maleate stomach retention tablet |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN1823781A true CN1823781A (en) | 2006-08-30 |
| CN100438874C CN100438874C (en) | 2008-12-03 |
Family
ID=36934723
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CNB2005100620414A Expired - Fee Related CN100438874C (en) | 2005-12-16 | 2005-12-16 | Etholadin maleate stomach retention tablet |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN100438874C (en) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN112285040A (en) * | 2020-09-16 | 2021-01-29 | 北京鑫开元医药科技有限公司 | Method for determining free bismuth in bismuth-containing preparation |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2813792B2 (en) * | 1994-12-22 | 1998-10-22 | 大洋薬品工業株式会社 | Preparation for oral administration of irsogladine maleate and its production method |
| JPH09124485A (en) * | 1995-11-06 | 1997-05-13 | Taisho Yakuhin Kogyo Kk | Composition containing irsogladine maleate and its production |
| JPWO2005026132A1 (en) * | 2003-09-17 | 2007-11-08 | 日本新薬株式会社 | CAMP substrate-specific inhibitors of phosphodiesterase |
-
2005
- 2005-12-16 CN CNB2005100620414A patent/CN100438874C/en not_active Expired - Fee Related
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN112285040A (en) * | 2020-09-16 | 2021-01-29 | 北京鑫开元医药科技有限公司 | Method for determining free bismuth in bismuth-containing preparation |
Also Published As
| Publication number | Publication date |
|---|---|
| CN100438874C (en) | 2008-12-03 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| CN100337549C (en) | Prebiotic and probiotic compositions and method for use in gut-based therapies | |
| CN118005727A (en) | Small molecule peptide AGGINLAR and application thereof in preparation of xanthine oxidase inhibitor | |
| CN113061194B (en) | Preparation method and application of Lyophyllum decastes fruiting body polysaccharide | |
| CN1823781A (en) | Etholadin maleate stomach retention tablet | |
| CN103919815A (en) | Use of probiotic bacteria for the preparation of a composition for the elimination of uremic toxins | |
| CN102258494B (en) | Intra-gastric floating sustained-release tablets containing floating konjac glucomannan and preparation method thereof | |
| CN1813684A (en) | Method for preparing 5-fluorouracil/chitosan nano drug-carrying microsphere | |
| CN101036631A (en) | Ginkgo leaves purified lyophiled powder preparing technique | |
| WO2023036203A1 (en) | Cs-4 fermented mycelium heteropolysaccharide, preparation method therefor and use thereof | |
| CN1141101C (en) | Chinese medicine for treating hepatitis B and its preparing process | |
| CN1990494A (en) | Dried rehmannia root oligosaccharide and its preparation method and uses | |
| CN1915324A (en) | Preparation of reenforcing spleen for wean, and preparation method | |
| CN111019010B (en) | Nigella sativa seed polysaccharide, extraction method and application in preparation of medicament for treating type 2 diabetes | |
| CN1611215A (en) | Pharmaceutical use of dihydro myricetin | |
| CN1094762C (en) | Fresh rehmannia root extract for proliferation of bifidobactor and extraction method thereof | |
| CN1631403A (en) | Pharmaceutical composition for treating constipation, its formulation and preparation process thereof | |
| CN113040278A (en) | Montmorillonite modified material and preparation method and application thereof | |
| CN1616655A (en) | Method for preparing superoxide dismutase | |
| CN101084921A (en) | Active carbon intestinal bioadhesive preparation and preparation method thereof | |
| CN1275645C (en) | Changsanye-factor oral liquor and clinical use | |
| CN1686091A (en) | Composition of aiphenyl hepatanone compound and its use | |
| CN1689579A (en) | Application of burdock glycoside or its aglycon in preparation of medicine for treating diabetes or its complications | |
| CN1733055A (en) | Fenugreek seed extract and its preparing process and application | |
| CN1449753A (en) | Chlorogenic acid and isochlorogenic acid composition and medical use thereof | |
| CN1476836A (en) | Anti-SARS action of zizhuisongguo chrysanthemum extract and its medicine composition |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| C14 | Grant of patent or utility model | ||
| GR01 | Patent grant | ||
| C17 | Cessation of patent right | ||
| CF01 | Termination of patent right due to non-payment of annual fee |
Granted publication date: 20081203 Termination date: 20111216 |