CN106963740A - A kind of diabecron sustained-release tablet and preparation method thereof - Google Patents
A kind of diabecron sustained-release tablet and preparation method thereof Download PDFInfo
- Publication number
- CN106963740A CN106963740A CN201710190273.0A CN201710190273A CN106963740A CN 106963740 A CN106963740 A CN 106963740A CN 201710190273 A CN201710190273 A CN 201710190273A CN 106963740 A CN106963740 A CN 106963740A
- Authority
- CN
- China
- Prior art keywords
- release tablet
- cellulose acetate
- preparation
- diabecron sustained
- release
- 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
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
-
- 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
- A61K31/13—Amines
- A61K31/155—Amidines (), e.g. guanidine (H2N—C(=NH)—NH2), isourea (N=C(OH)—NH2), isothiourea (—N=C(SH)—NH2)
-
- 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
- A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
- A61K9/2806—Coating materials
Landscapes
- Health & Medical Sciences (AREA)
- Epidemiology (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Medicinal Preparation (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
The present invention proposes a kind of diabecron sustained-release tablet and preparation method thereof, formed by medicine-containing particle with direct tablet compressing after pharmaceutically acceptable auxiliary materials and mixing, the medicine-containing particle is that the melbine aqueous solution is added in the acetone soln of cellulose acetate to form suspension, heating is sieved and obtained after being evaporated, and wherein the weight consumption ratio of Metformin hydrochloride and cellulose acetate is 1:0.06~0.3.Preparation method：The acetone soln of Metformin hydrochloride solution, cellulose acetate is well mixed, this suspension is heated, after being evaporated, the particle after sieving is well mixed, tabletting by sieving with pharmaceutically acceptable auxiliary material.Sustained release tablets release is steady, improves the security that medicine is used, and improves the compliance of patient.
Description
Technical field
The invention belongs to treat hyperglycemia technical field of medicine, and in particular to a kind of diabecron sustained-release tablet
And preparation method thereof.
Background technology
Metformin hydrochloride is mainly used in type ii diabetes people control blood glucose as one of common drug for the treatment of diabetes
Level.It is mainly by strengthening uptake and utilization of the surrounding tissue to glucose, and making the anaerobic glycolysis of musculature increases, and has
Oxygen metabolism is constant, and its concentration suppresses absorption of the glucose in intestines, suppress gluconeogenesis, suppress the release of glucagons in intestinal wall
Or suppress the effect of insulin antagonist, and increase the sensitiveness of insulin.Metformin hydrochloride to islet function normally or
The diabetes of forfeiture have hypoglycemic effect per capita, to normal person without hypoglycemic effect.This product can both be individually used for diet alone control
Unsatisfied light, the moderate patient of system.It does not stimulate after beta cell excreting insulin, medication in blood insulin concentration without obvious change
Change.Meanwhile, it can also be shared with insulin or sulfonylurea hypoglycemic agent, be heightened the effect of a treatment.Insulin dosage can be reduced.
Because Metformin hydrochloride is a kind of water-soluble very big medicine, and dosage is larger, therefore, the medicine is made into sustained release
Piece has very big difficulty.For example chip technology, such as single gel type sustained release tablets or rigid backbone piece are being sustained using conventional preparation
Deng being all difficult to reach preferable slow release effect, in particular for controlling steadily to discharge with certain speed in 24 hours, remain steady
Therapeutic plasma concentrations make to reach that internal good therapeutic effect is more difficult.
Diabecron sustained-release tablet disclosed in CN1391890A be using hydroxypropyl methyl cellulose, ethyl cellulose,
The common pharmaceutically conventional high polymer material such as sodium carboxymethylcellulose, to form the sustained release agent of gel-type, and using organic
Carboxylic acid or alcohol are pelletized under 50-60 DEG C of molten condition, and technological operation is extremely inconvenient, and said preparation be also difficult to reach control medicine with
The purpose that certain speed steadily discharges.
CN102119931B discloses a kind of diabecron sustained-release tablet and preparation method thereof, the sustained release material of the sustained release tablets
Material selection chitosan, preparation method is using tabletting after dry granulating machine granulation.But dry granulation dust is larger, pellet hardness
It is not of uniform size, easily cause release non-uniform phenomenon.
In the prior art, using gelatum skeleton material as slow-release material, the problem of existing is that early stage drug release is fast, and the later stage releases
Put not exclusively；Using insoluble framework material, it is difficult to which good Drug controlled release, medicine is either difficult to discharge or discharge
Rapidly；It is coated with insoluble material, by being coated control release, industrialization is difficult, and differences between batches are big.
The content of the invention
The present invention proposes a kind of diabecron sustained-release tablet, and sustained release tablets release is steady, improves the safety that medicine is used
Property, improve the compliance of patient.
The technical proposal of the invention is realized in this way：
A kind of diabecron sustained-release tablet, by direct tablet compressing after medicine-containing particle and pharmaceutically acceptable auxiliary materials and mixing
Into the medicine-containing particle is that the melbine aqueous solution is added in the acetone soln of cellulose acetate to form suspension, heating
Sieve and obtain after being evaporated, wherein the weight consumption ratio of Metformin hydrochloride and cellulose acetate is 1:0.06~0.3.
Further, pharmaceutically acceptable auxiliary material includes filler and lubricant.
Further, one or more of the filler in microcrystalline cellulose, lactose and pregelatinized starch.
Further, one or more of the lubricant in magnesium stearate, superfine silica gel powder and talcum powder.
It is a further object to provide a kind of preparation method of diabecron sustained-release tablet, including following step
Suddenly：
1) Metformin hydrochloride is dissolved in water, it is standby；
2) cellulose acetate is dissolved in acetone, it is standby；
3) acetone soln of Metformin hydrochloride solution, cellulose acetate is well mixed, this suspension is heated, is evaporated
Afterwards, sieve, the particle after sieving is well mixed with pharmaceutically acceptable auxiliary material, tabletting.
Further, pharmaceutically acceptable auxiliary material includes filler and lubricant.
Further, one or more of the filler in microcrystalline cellulose, lactose and pregelatinized starch.
Further, one or more of the lubricant in magnesium stearate, superfine silica gel powder and talcum powder.
Conventional powders packaging technique is, it is necessary to which special equipment, complex operation, repeatability is poor, it is difficult to industrialization amplification.Invention
People's creativeness proposes following scheme：Metformin hydrochloride is dissolved in water, cellulose acetate dissolves in acetone, stirring condition
Under, the aqueous solution of melbine is added in the acetone soln of cellulose acetate, because of solubility reduction, melbine separates out micro-
Microlite is suspended in the acetone soln of cellulose acetate.This suspension is heated, with the volatilization of acetone, cellulose acetate delays
It is slow to separate out, and the top layer of Metformin hydrochloride is attached to, by one layer of cellulose acetate of Metformin hydrochloride Surface coating.It is evaporated
Afterwards, sieve, the particle after sieving and filler, mix lubricant is uniform, and tabletting is produced.Using medicine in different solvents it is molten
Xie Du difference, prepares super-fine medicament particles, while by the granule coating of preparation, the release of medicine is controlled well.
Embodiment
Embodiment 1
A kind of diabecron sustained-release tablet, according to the number of parts by weight, supplementary material is：
0.5 part of 60 parts of Metformin hydrochloride, 6 parts of cellulose acetate, 10 parts of lactose and magnesium stearate.
Preparation method, comprises the following steps：
1) Metformin hydrochloride is dissolved in water, it is standby；
2) cellulose acetate is dissolved in acetone, it is standby；
3) acetone soln of Metformin hydrochloride solution, cellulose acetate is well mixed, this suspension is heated, is evaporated
Afterwards, sieve, the particle after sieving is well mixed with lactose, the magnesium stearate of recipe quantity, tabletting.
Embodiment 2
A kind of diabecron sustained-release tablet, according to the number of parts by weight, supplementary material is：
0.8 part of 65 parts of Metformin hydrochloride, 4 parts of cellulose acetate, 11 parts of microcrystalline cellulose and magnesium stearate.
Preparation method, comprises the following steps：
1) Metformin hydrochloride is dissolved in water, it is standby；
2) cellulose acetate is dissolved in acetone, it is standby；
3) acetone soln of Metformin hydrochloride solution, cellulose acetate is well mixed, this suspension is heated, is evaporated
Afterwards, sieve, the particle after sieving is well mixed with microcrystalline cellulose, the magnesium stearate of recipe quantity, tabletting.
Embodiment 3
A kind of diabecron sustained-release tablet, according to the number of parts by weight, supplementary material is：
0.2 part of 55 parts of Metformin hydrochloride, 16.5 parts of cellulose acetate, 8 parts of cornstarch and magnesium stearate.
Preparation method, comprises the following steps：
1) Metformin hydrochloride is dissolved in water, it is standby；
2) cellulose acetate is dissolved in acetone, it is standby；
3) acetone soln of Metformin hydrochloride solution, cellulose acetate is well mixed, this suspension is heated, is evaporated
Afterwards, sieve, the particle after sieving is well mixed with cornstarch, the magnesium stearate of recipe quantity, tabletting.
Test example
The release of diabecron sustained-release tablet is investigated
Drug release determination method：Chinese Pharmacopoeia version annex in 2010,75 turns/min of blue laws, to remove the fresh water of air
1000ml is this product release solvent.Ultraviolet spectrophotometry is selected to determine hydrochloride using absorption coefficient method at 233nm double
The release of guanidine sustained release tablets, the results are shown in Table 1.
Metformin Extended-release Tablets release testing result made from the embodiment 1~3 of table 1
| Sample source | 1h (%) | 3h (%) | 6h (%) | 9h (%) | 12h (%) | 24h (%) |
| Embodiment 1 | 22.5 | 39.1 | 63.5 | 83.2 | 90.2 | 99.8 |
| Embodiment 2 | 23.5 | 42.6 | 68.1 | 84.7 | 91.6 | 100.1 |
| Embodiment 3 | 21.8 | 40.5 | 64.2 | 82.4 | 89.4 | 98.2 |
It is flat according to diabecron sustained-release tablet release prepared by the results showed that embodiment of the present invention 1-3 of table 1
Surely.
The foregoing is merely illustrative of the preferred embodiments of the present invention, is not intended to limit the invention, all essences in the present invention
God is with principle, and any modification, equivalent substitution and improvements made etc. should be included in the scope of the protection.
Claims (8)
1. a kind of diabecron sustained-release tablet, it is characterised in that after medicine-containing particle and pharmaceutically acceptable auxiliary materials and mixing
Direct tablet compressing is formed, and the medicine-containing particle is that the melbine aqueous solution is added in the acetone soln of cellulose acetate to form mixed
Suspension, heating is sieved and obtained after being evaporated, and wherein the weight consumption ratio of Metformin hydrochloride and cellulose acetate is 1:0.06~
0.3。
2. diabecron sustained-release tablet according to claim 1, it is characterised in that pharmaceutically acceptable auxiliary material includes
Filler and lubricant.
3. diabecron sustained-release tablet according to claim 2, it is characterised in that filler be selected from microcrystalline cellulose,
One or more in lactose and pregelatinized starch.
4. diabecron sustained-release tablet according to claim 2, it is characterised in that lubricant is selected from magnesium stearate, micro-
One or more in powder silica gel and talcum powder.
5. the preparation method of diabecron sustained-release tablet as claimed in claim 1, it is characterised in that comprise the following steps：
1) Metformin hydrochloride is dissolved in water, it is standby；
2) cellulose acetate is dissolved in acetone, it is standby；
3) acetone soln of Metformin hydrochloride solution, cellulose acetate is well mixed, this suspension is heated, after being evaporated,
Sieving, the particle after sieving is well mixed with pharmaceutically acceptable auxiliary material, tabletting.
6. the preparation method of diabecron sustained-release tablet according to claim 5, it is characterised in that pharmaceutically acceptable
Auxiliary material include filler and lubricant.
7. the preparation method of diabecron sustained-release tablet according to claim 6, it is characterised in that filler is selected from micro-
One or more in crystalline cellulose, lactose and pregelatinized starch.
8. the preparation method of diabecron sustained-release tablet according to claim 6, it is characterised in that lubricant is selected from hard
One or more in fatty acid magnesium, superfine silica gel powder and talcum powder.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201710190273.0A CN106963740A (en) | 2017-03-27 | 2017-03-27 | A kind of diabecron sustained-release tablet and preparation method thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201710190273.0A CN106963740A (en) | 2017-03-27 | 2017-03-27 | A kind of diabecron sustained-release tablet and preparation method thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN106963740A true CN106963740A (en) | 2017-07-21 |
Family
ID=59336733
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201710190273.0A Pending CN106963740A (en) | 2017-03-27 | 2017-03-27 | A kind of diabecron sustained-release tablet and preparation method thereof |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN106963740A (en) |
Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1391890A (en) * | 2002-08-05 | 2003-01-22 | 成都恒瑞制药有限公司 | Oral melbine hydrocloride slow-releasing prepn and its preparing method |
| CN102119931A (en) * | 2011-02-21 | 2011-07-13 | 寿光富康制药有限公司 | Novel metformin hydrochloride slow-releasing tablet and preparation method thereof |
| CN103417495A (en) * | 2013-08-26 | 2013-12-04 | 中国人民解放军第150中心医院 | Method for preparing pioglitazone hydrochloride controlled-release pellet preparation slow-release layer |
| CN103479592A (en) * | 2013-09-06 | 2014-01-01 | 南京正宽医药科技有限公司 | Metformin hydrochloride sustained release tablets and preparation method thereof |
-
2017
- 2017-03-27 CN CN201710190273.0A patent/CN106963740A/en active Pending
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1391890A (en) * | 2002-08-05 | 2003-01-22 | 成都恒瑞制药有限公司 | Oral melbine hydrocloride slow-releasing prepn and its preparing method |
| CN102119931A (en) * | 2011-02-21 | 2011-07-13 | 寿光富康制药有限公司 | Novel metformin hydrochloride slow-releasing tablet and preparation method thereof |
| CN103417495A (en) * | 2013-08-26 | 2013-12-04 | 中国人民解放军第150中心医院 | Method for preparing pioglitazone hydrochloride controlled-release pellet preparation slow-release layer |
| CN103479592A (en) * | 2013-09-06 | 2014-01-01 | 南京正宽医药科技有限公司 | Metformin hydrochloride sustained release tablets and preparation method thereof |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| CN105213346B (en) | A kind of pharmaceutical composition and preparation method thereof containing cinacalcet hydrochloride | |
| CN103479592B (en) | Metformin hydrochloride sustained release tablets and preparation method thereof | |
| CN107669683B (en) | Pharmaceutical composition containing sitagliptin and metformin | |
| CN107595795A (en) | A kind of Metoprolol succinate sustained-release tablets and preparation method thereof | |
| WO2022012172A1 (en) | Oral sustained-release composition for insoluble drug, and preparation method thereof | |
| CN101579325A (en) | Metformin hydrochloride controlled-release tablet and preparation method thereof | |
| CN114404436B (en) | Metformin-enggliflozin composition and preparation method thereof | |
| CN117815195B (en) | JAK inhibitor composition and preparation process thereof | |
| CN105456270A (en) | Dipeptidyl peptidase IV inhibitor pharmaceutical composition, use and preparation method thereof | |
| CN112220775A (en) | Preparation intermediate granule containing calcium carbonate and vitamin D3 and preparation method thereof | |
| CN106606490A (en) | Dapagliflozin tablet and preparation method thereof | |
| CN104586795B (en) | A kind of canagliflozin piece and preparation method thereof | |
| CN106667936B (en) | Sofosbuvir tablet and preparation method thereof | |
| CN106924237B (en) | It is a kind of containing En Gelie is net and the pharmaceutical composition of Metformin hydrochloride | |
| CN107375247B (en) | Tilmicosin film-controlled enteric-coated sustained-release preparation and preparation method thereof | |
| CN103239449A (en) | Ezetimibe, simvastatin and nicotinic acid compound preparation and preparation method of ezetimibe, simvastatin and nicotinic acid compound preparation | |
| CN105343028A (en) | Medicine composition with norfloxacin and method for preparing medicine composition | |
| CN103127108B (en) | Telmisartan amlodipine tablet, and preparation method and use thereof | |
| CN104415034B (en) | A kind of imidafenacin pharmaceutical composition and preparation method thereof | |
| CN110585155A (en) | Gliclazide tablet (II) and preparation method thereof | |
| CN106963740A (en) | A kind of diabecron sustained-release tablet and preparation method thereof | |
| CN111529500B (en) | Pharmaceutical composition for improving solubility of oryzanol and preparation method thereof | |
| CN103181886A (en) | Artemisinin or its derivative sustained release preparation, and preparation method thereof | |
| CN115715768B (en) | Small sitagliptin-metformin sustained-release tablet and preparation method thereof | |
| CN111617048A (en) | Erlotinib sustained-release preparation for treating non-small cell lung cancer |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| PB01 | Publication | ||
| SE01 | Entry into force of request for substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| RJ01 | Rejection of invention patent application after publication | ||
| RJ01 | Rejection of invention patent application after publication |
Application publication date: 20170721 |