Nicardipine hydrochloride sustained release pellets and preparation method thereof

A technology of nicardipine hydrochloride and nicardipine hydrochloride, which is applied in the direction of microcapsules, bulk delivery, and cardiovascular system diseases, and can solve the problems of packaging, transportation, and storage inconvenience, low drug release stability, and large gastrointestinal irritation and other issues, to achieve the effect of improving bioavailability, small individual differences, and easy absorption

Inactive Publication Date: 2016-02-03
HEILONGJIANG ZHICHENG MEDICAL TECH
View PDF5 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] At present, among the nicardipine hydrochloride drugs for the treatment of essential hypertension on the market, there are low drug release stability effects, great irritation to the gastrointestinal tract, and bioavailability Low density, inconvenient packaging, transportation and storage, and complicated preparation methods

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Nicardipine hydrochloride sustained release pellets and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] A nicardipine hydrochloride sustained-release pellet, comprising drug-containing pellets and a coating layer, characterized in that: the coating layer wraps the drug-containing pellets, and the drug-containing pellets include: 10 mg of nicardipine hydrochloride , 70mg blank ball core, 110-150mg filler, 18-68mg lubricant, 2-10mg binder, the coating layer includes: 29-145mg Eudragit NE30D, 4-44mg talcum powder.

[0030] The optimal mass ratio of raw materials in the drug-containing pellets is: 10 mg nicardipine hydrochloride, 70 mg blank pellet core, 140 mg filler, 35 mg lubricant, and 5 mg binder.

[0031] The optimal mass ratio of raw materials in the coating layer is: 59mg Eudragit NE30D, 13mg talcum powder.

[0032] The filler is microcrystalline cellulose.

[0033] Described lubricant is talcum powder.

[0034] The binder is hypromellose.

[0035] The coating layer also includes traces of sodium lauryl sulfate or polyethylene glycol.

Embodiment 2

[0037] A preparation method of nicardipine hydrochloride sustained-release pellets, comprising the following steps:

[0038] Step 1: material preparation: according to the above mass ratio, nicardipine hydrochloride is pulverized with a pulverizer, and passed through a 100-mesh sieve;

[0039] Step 2: Mixing: Weigh nicardipine hydrochloride and microcrystalline cellulose according to the above mass ratio, put them into a three-dimensional mixer and mix for 30 minutes to make a fine powder of the drug, and take it out for later use;

[0040] Step 3: Preparation of adhesive: Weigh an appropriate amount of hypromellose according to the above mass ratio, add an appropriate amount of hot water to prepare an adhesive with a concentration of 2%, and set aside;

[0041] Step 4: Pill making: put the mixed drug fine powder into the feeding tank of the centrifugal pellet machine, put the adhesive into the liquid supply tank, put the blank pellet core into the pot, turn on the m...

Embodiment 3

[0047] Indications: essential hypertension.

[0048] medicine interactions:

[0049] 1. This product is used together with β-blockers and is well tolerated.

[0050] 2. When this product is used in combination with cimetidine, the plasma concentration of this product will increase.

[0051] 3. When this agent is used in combination with other antihypertensive drugs, there may be an additive effect, and more attention should be paid when using it.

[0052] 4. When this agent is used in combination with digoxin, the blood concentration of digoxin should be measured.

[0053] 5. When this product is used in combination with cyclosporine, the plasma concentration of cyclosporine increases.

[0054] 6. In vitro, therapeutic concentrations of furosemide, propranolol, dipyridamole, warfarin, quinidine, etc. added to human plasma do not change the protein binding rate of this product.

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

PUM

No PUM Login to view more

Abstract

The invention provides nicardipine hydrochloride sustained release pellets. The nicardipine hydrochloride sustained release pellets comprise medicine-containing pellets and coating layers, wherein the medicine-containing pellets are coated with the coating layers; the medicine-containing pellets comprise nicardipine hydrochloride, hollow cores, filling agents, lubricating agents and bonding agents; and the coating layers comprise Eudragit NE30D and talcum powder. A preparation method of the nicardipine hydrochloride sustained release pellets comprises the following procedures: 1. material preparation; 2. mixing; 3. preparation of the bonding agents; 4. preparation of the pellets; 5. preparation of coating agents; 6. coating; 7. filling; and 8. aluminium-plastic packaging and preparation of finished products. The nicardipine hydrochloride sustained release pellets are applicable to primary hypertension, are stable in medicine release, have good effects, have minor irritation to gastrointestinal tracts, have good bioavailability, are convenient to package, transport and store and are suitable for industrial production. The products are well absorbed after being orally administrated. Although the products can be taken on an empty stomach or after the meal, the total absorbed dose of the products can be increased by food.

Description

technical field [0001] The invention belongs to the field of chemical drug sustained-release preparations, and in particular relates to nicardipine hydrochloride sustained-release pellets and a preparation method thereof. Background technique [0002] Based on the current level of medical development and examination methods, the exact cause of blood pressure can be found, which is called secondary hypertension; otherwise, the exact cause of blood pressure can not be found, it is called essential hypertension. Most people with high blood pressure have essential hypertension, but to make a definite diagnosis of essential hypertension, secondary hypertension must first be ruled out. At present, it is believed that secondary hypertension accounts for 5% to 10% of the hypertensive population, but with the continuous progress of medical development and examination methods, the proportion of secondary hypertension will continue to increase, and the proportion of primary hypertensio...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

Application Information

Patent Timeline
no application Login to view more
Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/50A61K9/16A61K31/4422A61P9/12A61P31/04
Inventor 张昕
Owner HEILONGJIANG ZHICHENG MEDICAL TECH
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Try Eureka
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap