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Verapamil hydrochloride delayed-release capsule and preparation method thereof

A technology of verapamil hydrochloride and capsules, which can be applied to cardiovascular system diseases, active ingredients of nitrile/isonitrile, active ingredients of heterocyclic compounds, etc., can solve the problem of short maintenance time of effective blood concentration, unfavorable industrialized large-scale production, and short biological half-life and other problems, to achieve the effect of good reproducibility of absorption kinetics, improved bioavailability, and small inter-individual differences

Active Publication Date: 2009-05-06
LEPU PHARMACEUTICAL CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

As a calcium ion antagonist, verapamil hydrochloride has good antihypertensive effect, and has few toxic and side effects, so it is popular in clinic, but its main disadvantages are short biological half-life, short maintenance time of effective blood concentration, and frequent administration
If it is prepared into common sustained and controlled release preparations, it can be slowly released in the gastrointestinal tract, so that the drug can be slowly absorbed into the blood circulation, thereby exerting a mild and long-lasting pharmacological effect, but ordinary slow and controlled release preparations can only maintain relatively long-term Low and gentle blood drug concentration is not targeted to the chronorhythm of blood pressure fluctuations; although the pulse drug release system can release the drug regularly, the stable release time cannot be maintained for a long time
[0006] Patent ZL200410014300.1 reports a pellet preparation of verapamil hydrochloride for timed release. This preparation needs to prepare two kinds of pellets, and each pellet consists of a blank core, a drug-containing layer, a swelling layer and a controlled-release pellet. layer composition, the patented process is complex, two types of pellets need to be sprayed with three layers of coating, the drug application process is not easy to implement, and the preparation needs to prepare two types of pellets, the overall process is very complicated, the preparation process is long, and the cost is high. Not conducive to large-scale industrial production

Method used

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  • Verapamil hydrochloride delayed-release capsule and preparation method thereof
  • Verapamil hydrochloride delayed-release capsule and preparation method thereof
  • Verapamil hydrochloride delayed-release capsule and preparation method thereof

Examples

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preparation example Construction

[0029] The preparation of verapamil hydrochloride containing pill core:

[0030] (1) Pass 120g of verapamil hydrochloride, 52g of microcrystalline cellulose and 2g of magnesium stearate through a 100-mesh sieve respectively, mix well, add 4g of purified water to make a suitable soft material, put the prepared soft material into the extruder Out of the extruded material tank of the spheronizer, the soft material is extruded and spheronized to obtain a wet pill core, which is put into a fluidized bed for fluidization drying to obtain a dry pill core for use;

[0031] Preparation of pellets:

[0032] (2) Take 42g hypromellose E5 and add it into purified water while stirring, ultrasonically dissolve and make the solution uniform, and make a solution with a concentration of 3% by weight as the swelling layer coating solution; another step ( 1) The prepared drug-containing pellet core is placed in a fluidized bed, preheated for 15 minutes at an inlet air temperature of 40° C., and ...

Embodiment 2

[0041]

[0042] Preparation method: preparation of verapamil hydrochloride containing pill core:

[0043](1) Pass 120g of verapamil hydrochloride, 40g of pregelatinized starch, 30g of dextrin and 4g of talcum powder through a 100-mesh sieve, mix evenly, add 6g of starch slurry to make a suitable soft material, put the prepared soft material Put it into the extrusion material tank of the extrusion spheronizer, extrude the soft material, and spheronize to obtain a wet pill core, which is put into a fluidized bed for fluidization and drying to obtain a dry pill core for use;

[0044] Preparation of pellets:

[0045] (2) take by weighing 24g hypromellose sodium, add purified water under the situation of stirring, ultrasonically dissolve and make solution uniform, be made into the solution that weight percent concentration is 1%, as swelling layer coating solution; Take another step ( 1) The prepared drug-containing pellet core is placed in a fluidized bed, preheated for 15 min...

Embodiment 3

[0054]

[0055] Preparation:

[0056] The preparation of verapamil hydrochloride containing pill core:

[0057] (1) Pass 120g of verapamil hydrochloride, 52g of starch and 3g of micropowder silica gel through a 100-mesh sieve respectively, mix well, add 10g of polyvinylpyrrolidone to make a suitable soft material, put the prepared soft material into the extrusion spheronizer Extrude into the material tank, extrude the soft material, and roll it into a ball to obtain a wet pellet core, which is put into a fluidized bed for fluidization drying, and then the dry pellet core is obtained for use;

[0058] Preparation of pellets:

[0059] (2) Take 53g hypromellose E5 and add it into purified water while stirring, ultrasonically dissolve and make the solution uniform, and make a solution with a weight percent concentration of 3% as the swelling layer coating solution; another step ( 1) The prepared drug-containing pellet core is placed in a fluidized bed, preheated for 15 minute...

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Abstract

The invention provides a Verapamil Hydrochloride sustained release capsule; the weighting materials in the capsule are micropills; the micropill comprises a pill-containing core, an expansion layer and a controlled release layer from the interior to the exterior in turn; the weight of the pill-containing core accounts for 58 to 68 percent of the weight of the micropills; the expansion layer accounts for the 8 to 18 percent of the weight of the micropills; the controlled release layer accounts for 18 to 28 percent of the weight of the micropills; the Verapamil Hydrochloride sustained release capsule is a sustained release medicament-release system; the system can provide 4 to 6 hours of time lag and then slowly releases the medicament; more constant blood medicine concentration is maintained in a period of time; moreover, the preparation process of the capsule is simple and short; the production cost is lower; moreover, the Verapamil Hydrochloride sustained release capsule is beneficial to large industrial production.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, relates to a delayed-release verapamil hydrochloride capsule, and also relates to a preparation method of the capsule. Background technique [0002] Verapamil Hydrochloride, English name: Verapamil Hydrochloride for delay-onset and sustained release capsules, chemical name: α-[3-[[2-(3,4-dimethoxyphenyl)ethyl]methylamino]propyl ]-3,4-dimethoxy-α-isopropylphenylacetonitrile hydrochloride, the chemical structure is as follows: [0003] [0004] Molecular formula: C 27 h 38 N 2 o 4 • HCl, molecular weight: 491.07. [0005] This product is white or off-white crystal or crystalline powder, odorless, bitter, soluble in water, methanol or chloroform, insoluble in ether or benzene. The indications of verapamil hydrochloride are mainly used for the treatment of essential hypertension, and can also be used for the treatment of variant angina and unstable angina. As a calcium i...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/275A61K31/48A61P9/12
Inventor 张克军王庆鹏杨永芳陈志鹏
Owner LEPU PHARMACEUTICAL CO LTD
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