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Controlled release preparation and preparation method thereof

A technology for controlled release preparations and preparations, which is applied in the field of pharmacy and can solve the problems of incomplete release and delay of active ingredients.

Inactive Publication Date: 2010-11-10
GUANGZHOU PUIS PHARMA FACTORY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

To solve the defect that the active ingredients in osmotic pump double-layer tablets cannot be fully released, the method of using 10% more actual content than the labeled amount is currently used, such as Bayer’s osmotic pump nifedipine controlled release tablet Adalat LA 20 (20mg / tablet) , Adalat LA 30 (30mg / tablet) and Adalat LA 60 (60mg / tablet) contain 10% more nifedipine than the labeled amount, that is, the labeled content of each tablet is 20mg / tablet, 30mg / tablet and 60mg / tablet The nifedipine controlled-release tablets actually contain 22mg, 33mg and 66mg of nifedipine ( http: / / emc.medicines.org.uk / medicine / 20531 / SPC / Adalat+LA+20 / #COMPOSITION)
However, it cannot solve the problem that the release of this type of tablet both in vitro and in vivo shows a delay of 1 to 3 hours.

Method used

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  • Controlled release preparation and preparation method thereof
  • Controlled release preparation and preparation method thereof
  • Controlled release preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] Prepare tablet cores according to the following prescription

[0034]

[0035] (1) According to the above drug layer prescription, under a dry environment, pass felodipine through a 100-mesh sieve and fully mix it with lactose, sodium chloride, and polyoxyethylene, and use a dry granulator to make granules with a 20-mesh sieve . Add magnesium stearate and mix well to form drug layer granules.

[0036] (2) According to the above-mentioned propulsion layer prescription (excluding magnesium stearate), after mixing uniformly by conventional methods in a dry environment, use a dry granulator to make granules with an 18-mesh screen. Add magnesium stearate and mix evenly to become push layer granules.

[0037] (3) Place the drug layer granules and the push layer granules respectively in the hopper of a double-layer tablet press, adopt a circular shallow arc die with a diameter of 8mm, and adjust the weights of the drug layer and the push layer to be close to the above-men...

Embodiment 2

[0054] Prepare tablet cores according to the following prescription

[0055]

[0056] (1) Prepared with (1)~(5) of Example 1, the difference is that the amount of felodipine contained in the drug layer in the double-layer tablet core prepared this time is about 4 mg.

[0057] (2) Opadry is placed in 70% ethanol solution, so that the content of Opadry in the solution is about 8%, fully stir with a stirrer to dissolve the hypromellose in it, then add felodipine to make the package The content of felodipine in the coating solution is about 0.3%, and the felodipine is fully stirred with a stirrer or a shear emulsifier to dissolve or fully suspend and maintain stirring. The double-layer tablet prepared above is placed in a coating machine, the air inlet temperature is adjusted to about 45° C., and the coating solution is sprayed on the double-layer tablet until the coating layer contains about 1 mg of felodipine. The drug layer of the double-layer tablet of this product made in t...

Embodiment 3

[0069] Prepare tablet cores according to the following prescription

[0070]

[0071] (1) Same as steps (1) to (3) in Example 1, to make a tablet core with a diameter of 9 mm.

[0072] (2) cellulose acetate and polyethylene glycol 400 (consumption=18% cellulose acetate weight) are dissolved in dichloromethane, make the total solid content containing cellulose acetate and PEG 400 in the dichloromethane be about 5% , stir to dissolve it completely and become a semi-permeable membrane solution. The tablet core is placed in a coating machine, the air inlet temperature is adjusted to 35-45° C., the semipermeable membrane solution is sprayed on the tablet core until the weight gain of the tablet core is about 14%, and a double-layer tablet is obtained.

[0073] (3) Use a laser puncher to punch a hole with a diameter of about 0.4-0.7 mm in the center of the side film of the drug layer of each sheet. The received piece is called piece D.

[0074] (4) The stomach-soluble film coa...

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Abstract

The invention provides a controlled release preparation and a preparation method thereof. The controller release preparation is characterized in that dual-layer osmotic pump tablet semi-permeable membrane is covered by a drug-containing coating layer which can rapidly release partial drug active constituent of marked dosage; and a dual-layer osmotic pump tablet core is formed by two layers, one layer contains most drug active constituent of the marked dosage and permeation enhancing substances, the other layer contains permeable substances, the tablet core is covered by the semi-permeable membrane containing polymers, and a small hole is arranged on the semi-permeable membrane on the side of a drug-containing active constituent layer. The controlled release preparation solves the problem that the release of the dual-layer osmotic pump tablet in vitro and in vivo is lagged behind for 1-3 hour, and can reduce the incomplete release of the active constituent. The preparation method of the controlled release preparation comprises the following steps that the drug active constituent accounting for large part of the marked content is prepared in the dual-layer tablet and then the rest drug active constituent is covered in the coating layer of the dual-layer tablet. Preferably, felodipine is selected as the drug active constituent.

Description

technical field [0001] The invention belongs to the field of pharmacy and provides a controlled-release preparation and a preparation method of the preparation. Background technique [0002] US4765989 discloses a patent on the principle of a push-pull osmotic pump bilayer tablet, which is suitable for active pharmaceutical ingredients nifedipine, doxazosin and prazosin that are poorly water-soluble or insoluble in water. The release of this osmotic tablet is hardly affected by the release medium. Its structure is a double-layer sheet wrapped by a semi-permeable membrane, one of which contains active pharmaceutical ingredients and polymers, and the other layer contains polymers that can generate high osmotic pressure and swelling capabilities, and there is a membrane on the side of the drug-containing layer. The small pores are used to release the pharmaceutical active ingredient. A semi-permeable membrane can only pass water, but not drugs. After encountering water, the w...

Claims

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Application Information

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IPC IPC(8): A61K9/24A61K9/32A61K9/34A61K9/36A61K31/4422A61K47/38A61P9/12
Inventor 贝庆生
Owner GUANGZHOU PUIS PHARMA FACTORY
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