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Compound preparation including DPP-4 inhibitor and metformin hydrochloride and preparation method thereof

A technology of metformin hydrochloride and DPP-4, which is applied in the direction of medical preparations containing active ingredients, pharmaceutical formulas, organic active ingredients, etc., and can solve the problems that blood drug concentration is not as stable as controlled-release tablets, poor patient compliance, and short half-life.

Active Publication Date: 2014-07-23
广西中恒创新医药研究有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] However, common metformin hydrochloride preparations have short half-life, low bioavailability, large oral doses, and are prone to adverse reactions. gastrointestinal irritation
Therefore, we usually make metformin hydrochloride into sustained and controlled-release preparations, such as the metformin hydrochloride sustained-release tablets of Bristol-Myers Squibb, which is currently on the market, with the trade name "Glucophage". The blood concentration is not as stable as that of the controlled-release tablets. In addition, the tablet weight of the sustained-release tablets is often large, and the patient compliance is poor, while the tablet weight of the controlled-release tablets is small, and the patient compliance is better.
[0007] The patent (CN102133204) of Shandong Xinhua Pharmaceutical Co., Ltd. and the patent (CN1158999) of Andex Pharmaceutical Co., Ltd. all provide a kind of osmotic pump controlled release tablet of metformin hydrochloride, but the patent of Andex Company has added active agent 12 Alkyl sodium sulfate, Shandong Xinhua patent added active agents polyoxyethylene castor oil and poloxamer, long-term use will produce more adverse effects

Method used

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  • Compound preparation including DPP-4 inhibitor and metformin hydrochloride and preparation method thereof
  • Compound preparation including DPP-4 inhibitor and metformin hydrochloride and preparation method thereof
  • Compound preparation including DPP-4 inhibitor and metformin hydrochloride and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0046] Embodiment 1 (metformin hydrochloride / saxagliptin, 500 / 5mg)

[0047] Metformin Hydrochloride Osmotic Pump Controlled Release Tablet Core Prescription (1000 Tablets)

[0048]

[0049] Prescription of controlled release film coating solution (1000 tablets)

[0050]

[0051] Prescription of saxagliptin immediate release layer coating solution (1000 tablets)

[0052]

[0053] Preparation Process:

[0054] ①Preparation of Metformin Hydrochloride Osmotic Pump Controlled-release Tablet Core: Weigh the prescribed amount of Metformin Hydrochloride and HPMC E5, add equal amounts and mix evenly; add appropriate amount of distilled water to moisten and prepare soft material and granulate; add other remaining excipients after drying and granulating , mix evenly; tablet, hardness 10-12kg.

[0055] ② Coating of controlled-release film: Weigh the prescribed amount of cellulose acetate and glycerol triacetate, dissolve them in acetone, dissolve the prescribed amount of PEG40...

Embodiment 2

[0061] Embodiment 2 (metformin hydrochloride / saxagliptin, 500 / 5mg)

[0062] Metformin Hydrochloride Osmotic Pump Controlled Release Tablet Core Prescription (1000 Tablets)

[0063]

[0064] Prescription of controlled release film coating solution (1000 tablets)

[0065]

[0066] Prescription of saxagliptin immediate release layer coating solution (1000 tablets)

[0067]

[0068] Preparation Process:

[0069] ①Preparation of Metformin Hydrochloride Osmotic Pump Controlled-release Tablet Core: Weigh the prescribed amount of Metformin Hydrochloride and HPMC E5, add equal amounts and mix evenly; add appropriate amount of distilled water to moisten and prepare soft material and granulate; add other remaining excipients after drying and granulating , mix evenly; tablet, hardness 10-12kg.

[0070] ② Coating of controlled-release film: Weigh the prescribed amount of cellulose acetate and glycerol triacetate, dissolve them in acetone, dissolve the prescribed amount of PEG40...

Embodiment 3

[0074] Embodiment 3 (metformin hydrochloride / saxagliptin, 500 / 5mg)

[0075] Metformin Hydrochloride Osmotic Pump Controlled Release Tablet Core Prescription (1000 Tablets)

[0076]

[0077] Prescription of controlled release film coating solution (1000 tablets)

[0078]

[0079] Prescription of saxagliptin immediate release layer coating solution (1000 tablets)

[0080]

[0081]

[0082] Preparation Process:

[0083] ①Preparation of Metformin Hydrochloride Osmotic Pump Controlled-release Tablet Core: Weigh the prescribed amount of Metformin Hydrochloride and HPMC E5, add equal amounts and mix evenly; add appropriate amount of distilled water to moisten and prepare soft material and granulate; add other remaining excipients after drying and granulating , mix evenly; tablet, hardness 10-12kg.

[0084] ② Coating of controlled-release film: Weigh the prescribed amount of cellulose acetate and glycerol triacetate, dissolve them in acetone, dissolve the prescribed amo...

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PUM

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Abstract

The invention relates to a compound preparation including a DPP-4 (Dipepitidyl Peptidase-4) inhibitor and metformin hydrochloride and a preparation method of the compound preparation. According to the compound preparation, the metformin hydrochloride is a controlled release part, and made into a controlled release tablet by using an osmotic pump technology; the DDP-4 inhibitor is a quick release part, and made into a quick release coating layer by adopting a medicine coating method. The compound preparation structurally and sequentially comprises a metformin hydrochloride core, a controlled release film with small medicine release holes and a DPP-4 inhibitor quick release coating layer from inside to outside.

Description

technical field [0001] The invention relates to a compound preparation containing DPP-4 inhibitor and metformin hydrochloride and a preparation method thereof. Background technique [0002] Diabetes is a relative or absolute lack of insulin secretion in the blood, which leads to hyperglycemia, which in turn causes metabolic disorders such as fat and protein. At present, there are mainly two types in clinical practice: type 1 (insulin-dependent) and type 2 (non-insulin-dependent). With the improvement of people's living standards, the incidence of diabetes is also increasing year by year, and it has become the third chronic disease that seriously endangers human health after tumors and cardiovascular and cerebrovascular diseases. According to the statistics of the International Diabetes Federation in 2011, the number of people with diabetes in the world is 366 million, and it is expected to reach 552 million in 2030. [0003] In 2010, the prevalence of adult diabetes in my ...

Claims

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Application Information

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IPC IPC(8): A61K31/403A61K9/30A61K9/36A61K9/32A61K9/44A61P3/10A61K31/155
Inventor 尹莉芳朱春莉赵中原王广基孙宏斌武占楠周芳周春燕王微曹林
Owner 广西中恒创新医药研究有限公司
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