Preparation method of immediate release oral preparation containing sitagliptin or sitagliptin pharmaceutical salt

An immediate-release preparation, the technology of sitagliptin, which is applied in the field of preparation of oral immediate-release preparations, can solve problems such as sticky punching, missing and incomplete tablet surfaces, and poor material compressibility, so as to ensure the therapeutic effect and solve sticky punching The effect of the phenomenon

Active Publication Date: 2015-07-15
华益泰康药业股份有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The inventor encountered the following problems when using the prior art to prepare sitagliptin tablets: 1) when using the powder direct compression method to prepare sitagliptin tablets, serious sticking and punching phenomenon easily occurred, resulting in the loss of tablet surface Incomplete; 2) When prepared by dry granulation and tabletting method, the compressibility of the material is poor, and the disintegration time limit of the tablet is greater than 8 minutes, which is not conducive to the release of the drug; 3) When prepared by wet granulation, subject to the preparation process conditions The impact of the drug is likely to lead to changes in the crystal form of the drug

Method used

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  • Preparation method of immediate release oral preparation containing sitagliptin or sitagliptin pharmaceutical salt
  • Preparation method of immediate release oral preparation containing sitagliptin or sitagliptin pharmaceutical salt
  • Preparation method of immediate release oral preparation containing sitagliptin or sitagliptin pharmaceutical salt

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0067] prescription composition

[0068]

[0069] According to the above prescription, coated oral immediate-release tablets were prepared as follows:

[0070] Dissolving povidone K30 in purified water to prepare a binder solution with a weight percent content of 7.5%;

[0071] Sitagliptin phosphate, microcrystalline cellulose and anhydrous calcium hydrogen phosphate were mixed uniformly in a high-shear granulator to obtain a premix, wherein the stirring blade rotating speed was 180rpm, and the cutting knife rotating speed was 1500rpm; the granulation time was 10 minute;

[0072] Add the above binder solution to the above premix for wet granulation, sieve the soft material with a 1.0mm sieve for wet granulation, dry at 50°C for 2 hours, and then use a 1.0mm sieve for dry granulation to obtain particles;

[0073] Mix the croscarmellose sodium with the above-mentioned granules evenly (the rotation speed is 10rpm, mix for 15min), then add magnesium stearate and sodium stear...

Embodiment 2

[0078] prescription composition

[0079]

[0080] A coated oral immediate-release tablet was prepared in a similar manner to Example 1 except that the concentration of the binder solution was 7% by weight.

[0081] The quality of the oral immediate-release tablets prepared above was measured: the disintegration time limit was 26"-46", and there was no sticking phenomenon. Dissolution profile as Figure 8 As shown, the X-ray powder diffraction pattern is as Figure 9 As shown, it shows that the crystal form of sitagliptin phosphate hydrate has not changed.

Embodiment 3

[0083] prescription composition

[0084]

[0085] Except that no binder is used, the wetting agent is ethanol, and the granules are sized through a 1.5mm sieve, a method similar to that of Example 1 is used to prepare coated oral immediate-release tablets.

[0086] The quality of the oral immediate-release tablets prepared above was measured: the disintegration time limit was 27"-30", and there was no sticking phenomenon. Dissolution profile as Figure 10 As shown, the X-ray powder diffraction pattern is as Figure 11 As shown, it shows that the crystal form of sitagliptin phosphate anhydrous crystal form I has not changed. The fluidity of the total mixed powder obtained in this embodiment is worse than that of other embodiments, but still can meet the production requirements.

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Abstract

The invention belongs to the field of pharmaceutical preparations, and particularly relates to a preparation method of an immediate release oral preparation containing sitagliptin or sitagliptin pharmaceutical salt. The immediate release oral preparation is characterized in that in a preparation process of the immediate release oral preparation, when sitagliptin or sitagliptin pharmaceutical salt is in a hydrate crystal form, a wetting agent is water, and when sitagliptin or sitagliptin pharmaceutical salt is in an anhydrous crystal form, the wetting agent is ethanol. According to the preparation method, various technical features in the preparation method supplement each other, influence each other and synergistically act, and the crystal form of an active ingredient is not transformed before and after the preparation is prepared, so that the treatment effect is ensured; in addition, the compressibility of a material is improved significantly; the disintegration time is shortened obviously; and the problem of sticking is solved effectively.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to a preparation method of an oral immediate-release preparation containing sitagliptin or a pharmaceutically acceptable salt thereof. Background technique [0002] Diabetes is a common endocrine and metabolic disease. With the change of lifestyle and the acceleration of the aging process, the prevalence of diabetes in my country is showing a rapid upward trend. It has become another serious hazard to the people after cardiovascular and cerebrovascular diseases and tumors. Health important chronic non-communicable diseases. Its acute and chronic complications, especially chronic complications involving multiple organs, cause disability and high mortality, seriously affect the physical and mental health of patients, and bring heavy burdens to individuals, families and society. [0003] The drugs for treating diabetes mainly include sulfonylurea drugs, biguanide ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K9/36A61K31/4985A61K47/38A61K47/36A61K47/32A61P3/10
Inventor 徐国杰诸弘刚杨霖谭海松黄茵
Owner 华益泰康药业股份有限公司
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