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Sitagliptin sustained-release pellet and preparation method thereof

A technology for sitagliptin and sustained-release pellets, applied in the field of sitagliptin sustained-release pellets and preparation thereof, can solve the problems of low bioavailability, peak and valley phenomenon of blood drug concentration, frequent medication times and the like

Inactive Publication Date: 2013-04-10
HYBIO PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] A sitagliptin phosphate tablet was approved by the U.S. FDA in 2006, and the trade name is Januvia, but the preparation is a common tablet of sitagliptin phosphate, and patients are prone to peaks and valleys in blood concentration after taking the tablet Phenomenon, drugs have high toxic and side effects on the human body, low bioavailability, frequent medication times, and patients are prone to adverse reactions to drugs

Method used

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  • Sitagliptin sustained-release pellet and preparation method thereof
  • Sitagliptin sustained-release pellet and preparation method thereof
  • Sitagliptin sustained-release pellet and preparation method thereof

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preparation example Construction

[0105] The present invention also provides a preparation method of sitagliptin sustained-release pellets, comprising the steps of:

[0106] Dissolve the active ingredients of the drug and the binder in water to obtain a drug solution;

[0107] Coating the drug solution on the pellet core through the first coating to obtain the drug-loaded pill;

[0108] Dissolving the slow-release material, plasticizer and porogen in aqueous ethanol to obtain a slow-release coating solution;

[0109] The sustained-release coating solution is coated on the drug-loaded pills through the second coating, and dried to obtain;

[0110] The active ingredient of the drug is sitagliptin or a pharmaceutically acceptable salt thereof;

[0111] Pharmaceutically acceptable salts are phosphate, hydrochloride, sulfate, maleate, glutarate, glucuronate, lactate, oxalate, fumarate, citrate.

[0112] When preparing the sustained-release coating solution, the solvent used is ethanol, and in some embodiments pr...

Embodiment 1

[0163] Example 1 Preparation of sitagliptin sustained-release pellets

[0164] Based on the preparation of 1000g drug-loaded vegetarian pills and the preparation of 500mL sustained-release coating solution, the prescription of sitagliptin sustained-release pellets is:

[0165]

[0166] The preparation method of sitagliptin sustained-release pellets is as follows:

[0167] Preparation of drug-loaded pills: weigh the prescribed amount of sitagliptin phosphate and HPMC (5cp), measure the prescribed amount of purified water and heat it to 80°C, dissolve the prescribed amount of HPMC (5cp) in purified water, and then Add the prescribed amount of sitagliptin phosphate to prepare a drug solution, and spray the drug solution on the surface of the microcrystalline cellulose pellet core in a fluidized bed coating machine in the form of a bottom spray. The material temperature control range is 40-70 ° C. After the preparation is completed, it is taken out and dried to obtain drug-loa...

Embodiment 2

[0170] Example 2 Preparation of sitagliptin sustained-release pellets

[0171] Based on the preparation of 1000g drug-loaded vegetarian pills and the preparation of 500mL sustained-release coating solution, the prescription of sitagliptin sustained-release pellets is:

[0172]

[0173]

[0174] The preparation method of sitagliptin sustained-release pellets is as follows:

[0175] Preparation of drug-loaded pills: weigh the prescribed amount of sitagliptin phosphate and HPMC (5cp), measure the prescribed amount of purified water and heat it to 80°C, dissolve the prescribed amount of HPMC (5cp) in purified water, and then Add the prescribed amount of sitagliptin phosphate to prepare a drug solution. In the fluidized bed coating machine, spray the drug solution on the surface of the sucrose core by means of bottom spraying. The material temperature control range is 40-50 ° C. After the preparation is completed , taken out, and dried to obtain drug-loaded pills with a part...

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Abstract

The invention relates to the field of sustained-release pharmaceutical preparations, in particular to a sitagliptin sustained-release pellet and a preparation method thereof. The sitagliptin sustained-release pellet consists of a drug carrying blank pellet and a sustained-release covering at a mass ratio of 1:(0.08-0.12); the drug carrying blank pellet consists of a drug active ingredient, a pellet core and adhesive at a mass ratio of (40-80):(15-55):(1-10); the drug active ingredient is sitagliptin or pharmaceutically acceptable salt; and the sustained-release covering consists of a sustained-release material, a plasticiser and a pore-foaming agent at a mass ratio of (60-80):(5-15):(10-30). The sitagliptin sustained-release pellet has an obvious sustained-release function, the peak and valley drug concentrations are avoided, toxic and side effects of a drug on human bodies are reduced; the bioavailability of the drug is improved, the administration frequency is reduced, and the compliance of patients is improved.

Description

technical field [0001] The invention relates to the field of sustained-release pharmaceutical preparations, in particular to a sitagliptin sustained-release pellet and a preparation method thereof. Background technique [0002] Due to many factors such as the improvement of living standards, changes in dietary structure, increasingly tense pace of life, and a less active and more sedentary lifestyle, the incidence of diabetes worldwide is increasing rapidly. Diabetes has become the third serious threat after tumors and cardiovascular diseases. Chronic diseases of human health. At present, there are more than 120 million people with diabetes in the world, and the number of patients in China ranks second in the world. The incidence of diabetes in China is as high as 9.6%. Diabetes will remain a serious public health problem in China in the next 50 years. Type 2 diabetes is the main type of diabetes population in China, accounting for 93.7%. Therefore, drugs for the prevention...

Claims

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Application Information

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IPC IPC(8): A61K9/16A61K31/4985A61K9/20A61K9/48A61P3/10
Inventor 左灵静陶安进马亚平袁建成
Owner HYBIO PHARMA