CN110882224A - Preparation method of novel metformin composition - Google Patents
Preparation method of novel metformin composition Download PDFInfo
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- CN110882224A CN110882224A CN201911337865.6A CN201911337865A CN110882224A CN 110882224 A CN110882224 A CN 110882224A CN 201911337865 A CN201911337865 A CN 201911337865A CN 110882224 A CN110882224 A CN 110882224A
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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
- A61K31/13—Amines
- A61K31/155—Amidines (), e.g. guanidine (H2N—C(=NH)—NH2), isourea (N=C(OH)—NH2), isothiourea (—N=C(SH)—NH2)
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- 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
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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Abstract
The invention discloses a preparation method of a novel metformin composition, S1, firstly, screening and granulating raw materials and auxiliary materials respectively by using a screening machine with a 100-mesh screen; s2, weighing quantitative metformin hydrochloride, a filling agent and an adhesive according to the prescription amount, and fully and uniformly mixing the components; s3, adding a proper amount of 70% ethanol solution, and sieving and granulating by using a 24-mesh sieve sieving machine. The in-vitro drug release of the metformin hydrochloride sustained release tablet meets the Hihuchi equation within 12h, and the sustained release characteristics of a common hydrogel sustained release preparation, as the main sustained release agent in the prescription is HPMC and the release of the water-soluble drug is mainly carried out by the diffusion of the drug from an HPMC skeleton to a dissolution medium, the gel layer can possibly play a role similar to a diaphragm for controlling the rate when the HPMC hydrogel body is kept intact in the drug release process, so that the drug can be released at a constant speed, the toxic and side effects of the drug can be reduced, the drug taking frequency per day can be reduced, and the compliance of a patient can be increased.
Description
Technical Field
The invention relates to the technical field of metformin hydrochloride, in particular to a preparation method of a novel metformin composition.
Background
Metformin hydrochloride is sugar-coated or film-coated, the color is white after removing the coating, used for type II diabetes patient that is not satisfied with simple diet control, especially obesity and accompanied with hyperinsulinemia, metformin hydrochloride not only has hypoglycemic action, may also reduce the effects of light weight and hyperinsulinemia, can have effects on some patients with poor sulfonylureas, such as with sulfonylureas, small intestine glycosidase inhibitor or thiazolidinedione hypoglycemic drug, the effect that is used separately better than separately, can also be used for the patient of insulin treatment, in order to reduce the insulin dosage.
Metformin hydrochloride is a biguanide hypoglycemic drug, can improve insulin resistance, can also reduce the danger of macrovascular complications (coronary heart disease, apoplexy) and the like, is widely applied to the treatment of type II diabetes due to small adverse reaction, and becomes a typical representative of biguanide drugs.
Disclosure of Invention
The invention aims to solve the defects in the prior art and provides a preparation method of a novel metformin composition.
In order to achieve the purpose, the invention adopts the following technical scheme:
a preparation method of a novel metformin composition comprises the following steps:
s1, firstly, screening and granulating the raw materials and the auxiliary materials respectively by using a screening machine with a 100-mesh screen;
s2, weighing quantitative metformin hydrochloride, a filling agent and an adhesive according to the prescription amount, and fully and uniformly mixing the components;
s3, adding a proper amount of 70% ethanol solution, and sieving and granulating by using a 24-mesh sieve screening machine;
s4, after finishing, placing the prepared material in a blast drying oven at 55-60 ℃ for drying, and then granulating by using a granulator with a 20-mesh screen;
and S5, finally adding a certain amount of magnesium stearate, and tabletting after uniformly mixing to prepare the novel metformin composition tablet.
Preferably, the filler in S2 is microcrystalline cellulose.
Preferably, the binder in S2 is 70% ethanol.
Preferably, the microcrystalline cellulose is used in an amount of 10-30 mg.
Preferably, the dosage of the metformin hydrochloride is 50-150 mg.
The in-vitro drug release of the metformin hydrochloride sustained release tablet meets the Hihuchi equation within 12h, and the sustained release characteristics of a common hydrogel sustained release preparation, as the main sustained release agent in the prescription is HPMC and the release of the water-soluble drug is mainly carried out by the diffusion of the drug from an HPMC skeleton to a dissolution medium, the gel layer can possibly play a role similar to a diaphragm for controlling the rate when the HPMC hydrogel body is kept intact in the drug release process, the drug can be released at a constant speed, the side effect brought to patients is reduced, the toxic and side effect of the drug is favorably reduced, the number of times of taking the drug per day is reduced, and the compliance of patients is increased.
Drawings
FIG. 1 is a state diagram of the effect of different fillers on the release rate of a process for the preparation of a novel metformin composition according to the present invention;
FIG. 2 is a state diagram of the effect of different binders on the release rate for a process for the preparation of a novel metformin composition according to the present invention;
FIG. 3 is a graph comparing the release rate of the novel metformin hydrochloride sustained release tablet of the present invention with that of a conventional tablet.
Detailed Description
The technical solutions in the embodiments of the present invention will be clearly and completely described below, and it is obvious that the described embodiments are only a part of the embodiments of the present invention, and not all embodiments.
Example 1
A preparation method of a novel metformin composition comprises the following preparation steps:
s1, firstly, screening and granulating the raw materials and the auxiliary materials respectively by using a screening machine with a 100-mesh screen;
s2, weighing 50mg of metformin hydrochloride, 10mg of filler and 70% of ethanol according to the prescription amount, and fully and uniformly mixing;
s3, adding a proper amount of 70% ethanol solution, and sieving and granulating by using a 24-mesh sieve screening machine;
s4, after finishing, placing the prepared material in a blast drying oven at 55-60 ℃ for drying, and then granulating by using a granulator with a 20-mesh screen;
and S5, finally adding a certain amount of magnesium stearate, and tabletting after uniformly mixing to prepare the novel metformin composition tablet.
Example 2
A preparation method of a novel metformin composition comprises the following preparation steps:
s1, firstly, screening and granulating the raw materials and the auxiliary materials respectively by using a screening machine with a 100-mesh screen;
s2, weighing a certain amount of metformin hydrochloride 80mg, a filler 20mg and 70% ethanol according to the prescription amount, and fully and uniformly mixing;
s3, adding a proper amount of 70% ethanol solution, and sieving and granulating by using a 24-mesh sieve screening machine;
s4, after finishing, placing the prepared material in a blast drying oven at 55-60 ℃ for drying, and then granulating by using a granulator with a 20-mesh screen;
and S5, finally adding a certain amount of magnesium stearate, and tabletting after uniformly mixing to prepare the novel metformin composition tablet.
Example 3
A preparation method of a novel metformin composition comprises the following preparation steps:
s1, firstly, screening and granulating the raw materials and the auxiliary materials respectively by using a screening machine with a 100-mesh screen;
s2, weighing 100mg of metformin hydrochloride, 30mg of filler and 70% ethanol according to the prescription amount, and fully and uniformly mixing;
s3, adding a proper amount of 70% ethanol solution, and sieving and granulating by using a 24-mesh sieve screening machine;
s4, after finishing, placing the prepared material in a blast drying oven at 55-60 ℃ for drying, and then granulating by using a granulator with a 20-mesh screen;
and S5, finally adding a certain amount of magnesium stearate, and tabletting after uniformly mixing to prepare the novel metformin composition tablet.
By practicing examples 1-3, the optimum combination of factors should be example 3, i.e., metformin hydrochloride 100mg, sodium carboxymethylcellulose 60mg, and microcrystalline cellulose 30 mg.
As can be seen from fig. 1, the drug release rate is higher when lactose is used as the filler, and the release rate is lower when microcrystalline cellulose is used as the filler, but the difference between the release rates is smaller, indicating that the type of filler has a smaller influence on the release rate. Microcrystalline cellulose was chosen as a filler because its release profile more closely conforms to the Higuchi equation (r-0.9924).
As can be seen from FIG. 2, the sustained release tablets prepared by using two different binders have a small difference in release rate, because the binder is used in a small amount and can only perform a "fine tuning" function. Therefore, 70% ethanol is selected as the adhesive.
As can be seen from fig. 3, the cumulative release rate of the common tablet for 1 hour reaches 96 percent, while the cumulative release rates of the sustained release tablets for 2 hours, 8 hours and 12 hours are respectively 37.07 percent, 76.69 percent and 94.49 percent, and the drug release rate of the sustained release tablet is obviously slowed down, thereby achieving the purpose of sustained release.
In the invention, metformin hydrochloride is a biguanide hypoglycemic medicament widely used clinically, the current clinical application is still a common tablet, and the long-acting preparation is beneficial to reducing the toxic and side effects of the medicament, reducing the daily administration frequency and increasing the compliance of patients.
The in-vitro drug release of the metformin hydrochloride sustained release tablet meets the Hihuchi equation within 12h, and the sustained release characteristics of a common hydrogel sustained release preparation, as the main sustained release agent in the prescription is HPMC and the release of the water-soluble drug is mainly carried out by the diffusion of the drug from an HPMC skeleton to a dissolution medium, the gel layer can possibly play a role similar to a diaphragm for controlling the rate when the HPMC hydrogel body is kept intact in the drug release process, the drug can be released at a constant speed, and the side effect brought to a patient is reduced.
The above description is only for the preferred embodiment of the present invention, but the scope of the present invention is not limited thereto, and any person skilled in the art should be considered to be within the technical scope of the present invention, and the technical solutions and the inventive concepts thereof according to the present invention should be equivalent or changed within the scope of the present invention.
Claims (5)
1. A preparation method of a novel metformin composition is characterized by comprising the following steps:
s1, firstly, screening and granulating the raw materials and the auxiliary materials respectively by using a screening machine with a 100-mesh screen;
s2, weighing quantitative metformin hydrochloride, a filling agent and an adhesive according to the prescription amount, and fully and uniformly mixing the components;
s3, adding a proper amount of 70% ethanol solution, and sieving and granulating by using a 24-mesh sieve screening machine;
s4, after finishing, placing the prepared material in a blast drying oven at 55-60 ℃ for drying, and then granulating by using a granulator with a 20-mesh screen;
and S5, finally adding a certain amount of magnesium stearate, and tabletting after uniformly mixing to prepare the novel metformin composition tablet.
2. The method for preparing a novel metformin composition according to claim 1, wherein said filler in S2 is microcrystalline cellulose.
3. The method for preparing a novel metformin composition according to claim 1, wherein said binder in S2 is 70% ethanol.
4. The method for preparing a novel metformin composition according to claim 2, wherein said microcrystalline cellulose is used in an amount of 10-30 mg.
5. The method for preparing a novel metformin composition according to claim 1, wherein said metformin hydrochloride is used in an amount of 50 to 150 mg.
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| Application Number | Priority Date | Filing Date | Title |
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| CN201911337865.6A CN110882224A (en) | 2019-12-23 | 2019-12-23 | Preparation method of novel metformin composition |
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| CN201911337865.6A CN110882224A (en) | 2019-12-23 | 2019-12-23 | Preparation method of novel metformin composition |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN111759815A (en) * | 2020-08-05 | 2020-10-13 | 重庆康刻尔制药有限公司 | Metformin hydrochloride controlled-release tablet core and preparation method thereof |
Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102440975A (en) * | 2011-11-22 | 2012-05-09 | 浙江万马药业有限公司 | Metformin hydrochloride sustained-release tablets and preparation method thereof |
| CN103432081A (en) * | 2013-08-26 | 2013-12-11 | 中国人民解放军第150中心医院 | Method for compounding drug-containing pellet core of metformin hydrochloride controlled-release pellet preparation |
| 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 |
| CN106727404A (en) * | 2017-03-27 | 2017-05-31 | 华益药业科技(安徽)有限公司 | Diabecron sustained-release tablet and preparation method thereof |
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- 2019-12-23 CN CN201911337865.6A patent/CN110882224A/en active Pending
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102440975A (en) * | 2011-11-22 | 2012-05-09 | 浙江万马药业有限公司 | Metformin hydrochloride sustained-release tablets and preparation method thereof |
| CN103432081A (en) * | 2013-08-26 | 2013-12-11 | 中国人民解放军第150中心医院 | Method for compounding drug-containing pellet core of metformin hydrochloride controlled-release pellet preparation |
| 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 |
| CN106727404A (en) * | 2017-03-27 | 2017-05-31 | 华益药业科技(安徽)有限公司 | Diabecron sustained-release tablet and preparation method thereof |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN111759815A (en) * | 2020-08-05 | 2020-10-13 | 重庆康刻尔制药有限公司 | Metformin hydrochloride controlled-release tablet core and preparation method thereof |
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