Metformin hydrochloride floating sustained-release tablet and preparation method thereof

A metformin hydrochloride, gastric flotation technology, applied in pharmaceutical formulations, medical preparations with non-active ingredients, and medical preparations containing active ingredients, etc. problem, to achieve the effect of excellent flotation performance and sustained release performance

Inactive Publication Date: 2018-12-11
奕利制药有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This kind of floating tablet usually has a floating time, that is, the tablet itself cannot float when it just contacts with water (or liquid in the stomach), usually this floating time is several minutes to ten minutes, which causes A potential risk is that the tablet may be excluded from the pylorus and enter the duodenum before floating, thus losing the effect of gastric floating; another disadvantage of this kind of gastric floating tablet is that due to its main The ingredients are matrix controlled-release materials. During the drug release process, with the erosion of the matrix controlled-release materials, the tablets gradually become smaller and the floating ability gradually decreases, so many tablets lose their floating ability after 8-12 hours
[0004] CN101536989A discloses a metformin hydrochloride intragas

Method used

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  • Metformin hydrochloride floating sustained-release tablet and preparation method thereof
  • Metformin hydrochloride floating sustained-release tablet and preparation method thereof
  • Metformin hydrochloride floating sustained-release tablet and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0045] In the present embodiment, the tablet core prescription of metformin hydrochloride gastric floating sustained-release tablet is as shown in Table 1:

[0046] Table 1

[0047] Element

Weight (mg)

Proportion(%)

Metformin Hydrochloride

1000

80.00

Hypromellose E5

50

4.00

Crospovidone

190

15.20

Glyceryl behenate

10

0.80

[0048] The coating prescription outside the tablet core is as shown in Table 2:

[0049] Table 2

[0050] Element

Weight (mg)

Udrake RL100

50

Udrake RS100

50

talcum powder

50

triethyl citrate

10

95% ethanol

950

[0051] The preparation method is as follows: granulate metformin hydrochloride and hypromellose solution, dry, granulate, mix with crospovidone and glyceryl behenate, and compress into tablets so that the tablet core density is less than 1.0g / cm 3 , coating.

[0052] Metformin hydrochloride gastric floati...

Embodiment 2

[0054] In this embodiment, the tablet core prescription of metformin hydrochloride gastric floating sustained-release tablet is as shown in Table 3:

[0055] table 3

[0056]

[0057]

[0058] The coating prescription outside the tablet core is as shown in Table 4:

[0059] Table 4

[0060] Element

Weight (mg)

Eudragit NE 30D

100

Titanium dioxide

0.9

talcum powder

30

Hypromellose E5

9

purified water

170

[0061] The preparation method is as follows: granulate metformin hydrochloride and hydroxypropyl cellulose solution, dry, granulate, mix with crospovidone and glyceryl behenate, and compress into tablets so that the tablet core density is less than 1.0g / cm 3 , coating.

[0062] The dissolution profile of Metformin Hydrochloride Gastric Float Sustained-release Tablet under the same dissolution profile determination condition as described in Example 1 is as follows figure 2 shown.

Embodiment 3

[0064] In the present embodiment, the tablet core prescription of metformin hydrochloride gastric floating sustained-release tablet is as shown in Table 5:

[0065] table 5

[0066]

[0067]

[0068] The coating prescription outside the tablet core is as shown in Table 6:

[0069] Table 6

[0070] Element

Weight (mg)

Ethyl cellulose

70

polyethylene glycol

30

90% ethanol

900

[0071] The preparation method is as follows: granulate metformin hydrochloride and polyvinyl alcohol solution, dry, granulate, mix with crospovidone, silicon dioxide, and glyceryl behenate, and compress into tablets so that the tablet core density is less than 1.0 g / cm 3 , coating.

[0072] The dissolution profile of Metformin Hydrochloride Gastric Float Sustained-release Tablet under the same dissolution profile determination condition as described in Example 1 is as follows image 3 shown.

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Abstract

The invention provides a metformin hydrochloride floating sustained-release tablet and a preparation method thereof. The metformin hydrochloride floating sustained-release tablet comprises a tablet core and a non-gastric-soluble coating film wrapped outside the tablet core, wherein the tablet core comprises metformin hydrochloride, a floating material, an adhesive and other excipients, and non-gastric-soluble coating film comprises a film forming material and other excipients. The tablet core is prepared by matching the above materials, and is matched with the non-gastric-soluble coating filmoutside the tablet core, and the density of the tablet core is less than 1g/cm<3>, so that the metformin hydrochloride floating sustained-release tablet can immediately float in water or gastric juice, thereby reducing the possibility of the tablet being discharged from the stomach into the duodenum, and prolonging the time in which the metformin hydrochloride sustained-release tablet floats in the stomach; the metformin hydrochloride floating sustained release tablet can float until the contents of the stomach are emptied, thereby ensuring that the medicine is released in the stomach; the metformin hydrochloride floating sustained-release tablet provided by the invention does not swell substantially in water or gastric juice, thereby reducing the possibility of abdominal distension feeling of a patient.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to a metformin hydrochloride gastric floating sustained-release tablet and a preparation method thereof. Background technique [0002] Metformin is the drug of choice for the treatment of type 2 diabetes, and it is also recognized as a first-line drug and basic drug worldwide. Its absorption site is mainly at the upper end of the small intestine, so if it is made into an ordinary sustained-release preparation, when the preparation has passed through the main absorption site and the drug contained in it has not been released, part of the drug will not be fully absorbed, resulting in a decrease in bioavailability . The metformin hydrochloride gastric floating sustained-release preparation floats in the stomach for a long time and slowly releases the drug, so that almost all the drug can be absorbed through the main absorption site in the upper small intestine, so it has the a...

Claims

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Application Information

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IPC IPC(8): A61K9/36A61K9/32A61K47/32A61K47/38A61K47/36A61K47/10A61K31/155A61P3/10
CPCA61K9/0065A61K9/2027A61K9/2031A61K9/205A61K9/2054A61K9/284A61K9/2866A61K31/155A61P3/10
Inventor 田武王燕姜建平
Owner 奕利制药有限公司
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