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Venlafaxine hydrochloride sustained release capsule and preparation method thereof

A technology of venlafaxine hydrochloride and sustained-release capsules, which is applied in the field of medicine, can solve the problems that the spray rate affects the drug application rate, unsatisfactory drug release performance, and poor sustained-release effect of pellets, etc., achieving considerable economic and social benefits , The production environment is friendly, and the drug release effect is stable

Active Publication Date: 2014-07-02
CSPC ZHONGQI PHARM TECH (SHIJIAZHUANG) CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0016] 1. Poor production efficiency
Since the drug is sprayed on the surface of the pellets in the form of a solution or suspension, the spray rate affects the drug application rate. Because the pellets are small in size and easy to stick to each other, the spray rate is often small and the production efficiency is low;
[0017] 2. The finished product yield is low
Due to the volatilization of the solvent during the coating process, the drug in the coating solution will dry in advance and cannot be recovered, and cannot be completely bonded to the pellets;
[0018] 3. Unsatisfactory drug release performance
The patent claims that a large amount of sodium chloride or potassium chloride is added to the pellet core to make the pellets with high content of active ingredients easy to prepare, but the inventor found that the yield of pellets prepared by this method is low, only 40%. About, far less than the productive rate of more than 75% claimed by the patent, and the sustained-release effect of the obtained pellets is relatively poor

Method used

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  • Venlafaxine hydrochloride sustained release capsule and preparation method thereof
  • Venlafaxine hydrochloride sustained release capsule and preparation method thereof
  • Venlafaxine hydrochloride sustained release capsule and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1-4

[0064] The inventor prepared pellet cores and coatings respectively by using the following prescriptions, only changing the mass percentage of coating (weight gain) relative to the pellet cores, prepared venlafaxine hydrochloride sustained-release capsules, and obtained products that meet the standards.

[0065]

[0066] The coating weight gains of Examples 1-4 were 13.0%, 14.5%, 16.5%, and 20.5%, respectively.

[0067] Preparation:

[0068] 1. Mix venlafaxine hydrochloride, microcrystalline cellulose, and hypromellose evenly;

[0069] 2. Add water to make soft materials;

[0070] 3. Add to the extruder (Nica E-140) for extrusion, equipment parameters: feeding speed 70rpm; extrusion speed 70rpm; screen diameter 0.8mm;

[0071] 4. The extruded product is spheronized in a spheronizer (CGC-350 multifunctional centrifugal granulation coating machine). Equipment parameters: ball rolling speed 1000rpm; blast frequency 20Hz; blast temperature 25°C; ball rolling time 8-10min;

...

Embodiment 5

[0082] The inventor changed the ratio of the core components to prepare venlafaxine hydrochloride sustained-release capsules, and also obtained products that meet the requirements.

[0083]

[0084] Coating weight gain was 15.2%. The preparation method is the same as in Example 1. The yield rate of the above prescription and method product is 85%.

[0085] Release measurement: with embodiment 1, the results are shown in the following table:

[0086] .

[0087] Conclusion: Changing the dosage ratio of venlafaxine hydrochloride and microcrystalline cellulose in the preparation of pellet cores, the in vitro release results meet the quality standards.

Embodiment 6

[0089] The inventor changed the ratio of the core components to prepare venlafaxine hydrochloride sustained-release capsules, and also obtained products that meet the requirements.

[0090]

[0091] Coating weight gain was 10.5%. The preparation method is the same as in Example 1. The product yield of the above prescription and preparation method is 86%.

[0092] Release measurement: with embodiment 1, the results are shown in the following table:

[0093] .

[0094] Conclusion: Changing the dosage ratio of venlafaxine hydrochloride and microcrystalline cellulose in the preparation of pellet cores, the in vitro release results meet the quality standards.

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Abstract

The invention relates to a venlafaxine hydrochloride sustained release capsule. Sustained release pellets serve as contents of the sustained release capsule prepared by the invention, wherein the pellets comprise medicine-containing pill cores and sustained release coatings; the medicine-containing pill cores contain venlafaxine hydrochloride, hydroxypropyl methyl cellulose and microcrystalline cellulose. The venlafaxine hydrochloride sustained release capsule disclosed by the invention is stable to release medicines, free from a problem of organic solvent residue, safe to take and environment-friendly during producing. Furthermore, the invention provides a preparation method of the venlafaxine hydrochloride sustained release capsule. The method is high in production efficiency, simple in process, convenient to operate, low in cost and easy in industrial production; the method can be used for saving the cost for medicine production enterprises, and can bring about considerable economic and social benefits.

Description

technical field [0001] The invention belongs to the field of medicine and relates to a pharmaceutical preparation, in particular to a venlafaxine hydrochloride sustained-release capsule and a preparation method thereof. Background technique [0002] Venlafaxine HCl, the chemical name is (R / S)-1-[2-(dimethylamine)-1-(4-methoxyphenyl)ethyl]cyclohexanol hydrochloride. Chemical Structure: [0003] . [0004] This product is suitable for various types of depression, including depression accompanied by anxiety, and generalized anxiety disorder, and belongs to serotonin / norepinephrine reuptake inhibitors. At present, the adult dose of venlafaxine hydrochloride immediate-release tablets is 75-350 mg / day, which is divided into 2-3 times a day. After the administration of venlafaxine hydrochloride immediate-release tablets, the drug dissolves and releases rapidly, which leads to a high blood concentration in a short period of time, and then drops rapidly, so the dosage of the dr...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/52A61K31/137A61K47/38A61P25/24
Inventor 刘峰刘翠艳樊俊红王彦卜利超白晓雪耿佳刘磊娜赵曦
Owner CSPC ZHONGQI PHARM TECH (SHIJIAZHUANG) CO LTD
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