Oral formulations containing metformin and a-glycosidase inhibitor, and preparation method thereof

A technology of glycosidase inhibitors and oral preparations, which is applied in the direction of medical preparations containing active ingredients, pharmaceutical formulas, metabolic diseases, etc. It can solve the problems of metformin not being released quickly and the bioavailability of metformin decline, so as to control blood sugar and increase blood sugar. adaptive effect

Inactive Publication Date: 2013-04-10
CJ HEALTHCARE CORP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Therefore, formulations containing metformin do not release metformin rapidly and then migrate to the lower part of the gastrointestinal tract over time, making metformin less bioavailable

Method used

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  • Oral formulations containing metformin and a-glycosidase inhibitor, and preparation method thereof
  • Oral formulations containing metformin and a-glycosidase inhibitor, and preparation method thereof
  • Oral formulations containing metformin and a-glycosidase inhibitor, and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0043] Example 1: Preparation of metformin and voglibose compound preparation (1)

[0044] 300g of metformin hydrochloride and 36g of hydroxypropyl cellulose were uniformly mixed; sieved with a 20-mesh mesh; added to a fluidized bed granulator; and then preheated at 60°C for 10 minutes. 6 g of hydroxypropyl cellulose was dissolved in 120 mL of water to prepare a binding solution; the binding solution was sprayed at a rate of 7 mL per minute, thereby preparing primary granules; and the primary granules were then sieved using a 20-mesh mesh.

[0045] 0.18 g of voglibose and 6 g of hydroxypropyl cellulose were dissolved in 120 mL of water by thorough stirring, and then fully sprayed onto the granules prepared in the above manner to prepare secondary granules. Finish by sieving the secondary granules using a 20 mesh mesh, then drying.

Embodiment 2

[0046] Example 2: Preparation of metformin and voglibose compound preparation (2)

[0047] 300g of metformin hydrochloride and 36g of hydroxypropyl cellulose were uniformly mixed; sieved with a 20-mesh mesh; added to a fluidized bed granulator; and then preheated at 60°C for 10 minutes. 6 g of hydroxypropyl cellulose was dissolved in 120 mL of water to prepare a binding solution; the binding solution was sprayed at a rate of 7 mL per minute, thereby preparing primary granules; and the primary granules were then sieved using a 20-mesh mesh.

[0048] 0.12 g of voglibose and 6 g of hydroxypropyl cellulose were dissolved in 120 mL of water by thorough stirring, and then sprayed onto the granules prepared in the above manner to prepare secondary granules. Finish by sieving the secondary granules using a 20 mesh mesh, then drying.

Embodiment 3

[0049] Example 3: Preparation of metformin and voglibose compound preparation (3)

[0050] 300g of metformin hydrochloride and 36g of hydroxypropyl cellulose were uniformly mixed; sieved with a 20-mesh mesh; added to a fluidized bed granulator; and then preheated at 60°C for 10 minutes. 6 g of hydroxypropyl cellulose was dissolved in 120 mL of water to prepare a binding solution; the binding solution was sprayed at a rate of 7 mL per minute, thereby preparing primary granules; and the primary granules were then sieved using a 20-mesh mesh.

[0051] 0.36 g of voglibose and 6 g of hydroxypropyl cellulose were dissolved in 120 mL of water by thorough stirring, and then sprayed onto the granules prepared in the above manner to prepare secondary granules. Sieve the secondary granules through the use of a 20-mesh mesh, then dry and finish.

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Abstract

The present invention provides an oral preparation comprising secondary wet granules prepared by coating the primary wet granules with a mixed aqueous solution of an α-glucosidase inhibitor and hydroxypropyl cellulose, wherein the primary wet granules are prepared by coating the primary wet granules with A mixed powder comprising metformin and hydroxypropyl cellulose is prepared by combining an aqueous solution of hydroxypropyl cellulose as a binding solution. In addition, the present invention provides a method for preparing an oral preparation, comprising the steps of: injecting mixed powder of metformin and hydroxypropyl cellulose into a fluidized bed granulator, and injecting an aqueous solution of hydroxypropyl cellulose spraying onto the mixed powder to produce primary wet granules; and spraying a mixed aqueous solution of an α-glucosidase inhibitor and hydroxypropyl cellulose onto the primary wet granules in a fluidized bed granulator to produce secondary wet granules.

Description

technical field [0001] The present invention relates to an oral preparation comprising metformin and voglibose, wherein the oral preparation is used for treating type II diabetes, and a preparation method thereof. More specifically, the present invention relates to an oral formulation capable of improving medication compliance of patients because it is easy to take and has an effect equal to or greater than that of metformin and voglibose co-administered as separate formulations. Background technique [0002] Type 2 diabetes, non-insulin-dependent diabetes, is the most common metabolic disease, with a global prevalence of about 5%. In addition, it is estimated that from now to 2010, the prevalence of type II diabetes will rise steadily to 7%, and within 10 years from now, the total number of diabetic patients will increase to about double. [0003] The pathophysiology of type II diabetes is characterized by insulin secretory dysfunction and insulin resistance. Insulin resi...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/16A61P3/10
CPCA61K9/167A61K31/155A61K45/06A61P3/10A61P43/00A61K2300/00A61K9/16
Inventor 赵日焕洪一基安泰军李镕宅郑善五尹明植权五亿李恃氾吴多苑崔洛铉李熙贞卢贤贞
Owner CJ HEALTHCARE CORP
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