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Acyclovir sustained release tablet and preparation method thereof

A technology of sustained-release tablets and sustained-release granules, which is applied in the direction of pharmaceutical formulas, medical preparations with non-active ingredients, antiviral agents, etc. short-term problems, to achieve the effect of reducing drug expenditure, reducing the frequency of administration, and reducing costs

Active Publication Date: 2012-10-10
HAYAO GRP SANJING MINGSHUI PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Due to the short half-life of acyclovir (t 1 / 2 =2.5 hours), the bioavailability is low (only 10%~20%), in order to effectively control the disease, take the oral preparation of acyclovir of conventional immediate release, the patient needs to take medicine 5 times every day
Too many times of taking medicine every day, regardless of day and night, it is difficult for the patient to follow the doctor's advice, and many of them miss taking the medicine, which is not conducive to the control of the disease. In clinical treatment, there is an urgent need for a drug with a longer drug action cycle than the common preparation of acyclovir. Controlled-release preparations, thereby greatly reducing the number of daily doses and improving patient compliance
At present, acyclovir sustained-release tablets have been produced in the domestic market, the specification is 200mg / tablet, 3 times a day, 2 tablets each time, as a "sustained-release" preparation, it still needs to be administered multiple times a day, which is not conducive to convenient administration and Effective control of the disease

Method used

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  • Acyclovir sustained release tablet and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment approach 1

[0023] Raw material ratio:

[0024] Aciclovir 600g

[0025] Hypromellose K100M 109g

[0026] Hypromellose E5LV 12.2g

[0027] Microcrystalline Cellulose 150g

[0028] Lactose 50g

[0029] Micronized silica gel 24g

[0030] Magnesium stearate 4.8g

[0031] Preparation:

[0032] Immediate-release part: add 1 / 3 of the prescribed amount of acyclovir, lactose and 1 / 5 of the prescribed amount of microcrystalline cellulose according to the method of equal incremental dilution, mix well, and add an appropriate amount of 5% hypromellose with an airless spray system Soft material made of cellulose E5LV aqueous solution, granulated with 40 mesh sieve, dried at 60°C, granulated with 40 mesh sieve.

[0033] Sustained-release part: add 2 / 3 of the prescribed amount of acyclovir, hypromellose K100M, and 2 / 5 of the prescribed amount of microcrystalline cellulose according to the method of equal incremental dilution, mix well, and add with an airless spray system Appropriate amount of 5...

Embodiment approach 2

[0036] Raw material ratio:

[0037] Aciclovir 600g

[0038] Hypromellose K100M 109g

[0039] Hypromellose E5LV 12.2g

[0040] Microcrystalline Cellulose 175g

[0041] Lactose 50g

[0042] Micronized silica gel 24g

[0043] Magnesium stearate 4.8g

[0044] Preparation:

[0045] Immediate-release part: add 1 / 4 of the prescribed amount of acyclovir, lactose and 1 / 5 of the prescribed amount of microcrystalline cellulose according to the method of equal incremental dilution, mix well, and add an appropriate amount of 5% hypromellose with an airless spray system Soft material made of cellulose E5LV aqueous solution, granulated with 40 mesh sieve, dried at 60°C, granulated with 40 mesh sieve.

[0046] Sustained-release part: Add 3 / 4 of the prescribed amount of acyclovir, hypromellose K100M, and 2 / 5 of the prescribed amount of microcrystalline cellulose according to the method of equal incremental dilution, mix well, and add with an airless spray system Appropriate amount of 5...

Embodiment approach 3

[0049] Raw material ratio:

[0050] Aciclovir 600g

[0051] Hypromellose K100M 109g

[0052] Hypromellose E5LV 12.2g

[0053] Microcrystalline Cellulose 200g

[0054] Lactose 50g

[0055] Micronized silica gel 24g

[0056] Magnesium stearate 4.8g

[0057] Preparation:

[0058] Immediate-release part: add 1 / 5 of the prescribed amount of acyclovir, lactose and 1 / 5 of the prescribed amount of microcrystalline cellulose according to the method of equal incremental dilution, mix well, and add an appropriate amount of 5% hypromellose with an airless spray system Soft material made of cellulose E5LV aqueous solution, granulated with 40 mesh sieve, dried at 60°C, granulated with 40 mesh sieve.

[0059] Sustained-release part: Add 4 / 5 of the prescribed amount of acyclovir, hypromellose K100M, and 2 / 5 of the prescribed amount of microcrystalline cellulose according to the method of equal incremental dilution, mix well, and add with an airless spray system Appropriate amount of 5...

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Abstract

The invention relates to an acyclovir sustained release tablet and a preparation method thereof. The acyclovir sustained release tablet comprises the following components in percentage by weight: 60-64 percent of acyclovir, 10-12 percent of hydroxypropyl methylcellulose K100M, 1.2-1.3 percent of hydroxypropyl methylcellulose E5LV, 15-20 percent of microcrystalline cellulose, 5-6 percent of lactose, 2.4-2.6 percent of aerosol and 0.4-0.6 percent of magnesium stearate. The preparation method comprises the following steps of: preparing 1 / 3-1 / 5 of the acyclovir, the lactose, 1 / 5 of the microcrystalline cellulose and a proper quantity of the hydroxypropyl methylcellulose E5LV into quick release particles; preparing 2 / 3-4 / 5 of the acyclovir, the hydroxypropyl methylcellulose K100M, 2 / 5 of the microcrystalline cellulose and a proper quantity of the hydroxypropyl methylcellulose E5LV into sustained release particles; and mixing and laminating the quick release particles, the sustained releaseparticles, 2 / 5 of the microcrystalline cellulose, the aerosol and magnesium stearate into the sustained release tablet. The release quantities of 1 hour, 4 fours and 10 hours of the sustained releasetablet respectively reach 30-45 percent, 50-65 percent and higher than 75 percent; the sustained release table is convenient to take and has a definite curative effect; and the release period of the sustained release tablet can reach 12 hours, thereby the administration numbers of times are reduced.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to a preparation method of medicine, in particular to a preparation method of acyclovir sustained-release tablets. Background technique [0002] Aciclovir (Aciclovir) is the second-generation broad-spectrum antiviral drug. One of the drugs. The drug is mainly suitable for acute herpes zoster, genital herpes and chickenpox. [0003] Due to the short half-life of acyclovir (t 1 / 2 =2.5 hours), bioavailability is low (only 10%~20%), for effectively controlling the state of an illness, take the oral preparation of acyclovir of conventional immediate release, the patient needs to take medicine 5 times every day. Too many times of taking medicine every day, regardless of day and night, it is difficult for the patient to follow the doctor's advice, and many of them miss taking the medicine, which is not conducive to the control of the disease. In clinical treatment, there is an u...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/22A61K31/522A61K47/38A61P31/12A61P31/22
Inventor 范宁张红梅
Owner HAYAO GRP SANJING MINGSHUI PHARMA CO LTD