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Preparation method for controlled release preparation, especial for zero-order release controlled release preparation

A technology for controlled release preparations and drug release, which is applied in the direction of pharmaceutical formulations, medical preparations containing no active ingredients, medical preparations containing active ingredients, etc. Drug rate drop and other issues

Active Publication Date: 2011-03-23
OVERSEAS PHARMA +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] For example, there is a big problem with the stability of the preparation, that is, the problem that the dissolution and release characteristics change with aging: after the controlled-release preparation prepared by this technology is stored for a period of time, its drug release performance or drug release rate often has a large drop. Decrease, while the drug content in the preparation has basically no change or the change range is relatively small
However, there are some major gaps in these technologies. For example, when the controlled-release coating contains porogen ingredients, especially those with high water solubility, curing under high humidity conditions may cause these ingredients to be removed from the controlled-release coating. Precipitate, and change the dissolution characteristics

Method used

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  • Preparation method for controlled release preparation, especial for zero-order release controlled release preparation

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preparation example Construction

[0029] Each basic step in the preparation method of the controlled-release preparation is described in detail below.

[0030] Firstly, the most important step 3) of the present invention, the healing (curing) treatment coating film is described.

[0031] In order to improve the stability of the drug release of the preparation, it is necessary to heal the above-mentioned coating film to eliminate the numerous extremely small micropores produced in the coating process in the coating film and form a dense coating film to ensure the relative stability of drug release.

[0032] After the coating is finished, the solvent or dispersant of the polymer in the coating film has basically volatilized, leaving many extremely small micropores in the coating film, and the polymer particles in the coating film are often not completely fused. It is believed that under the action of the micropore additional pressure (ΔP) generated by the interfacial tension between the polymer and the air, thes...

Embodiment 1

[0091] Prepare samples and control samples according to the following prescriptions and processes

[0092] 1), preparation of tablet core:

[0093]

[0094]

[0095] Mix simvastatin, carbopol, ground and 200-mesh sieved sodium citrate, lactose and polyvinylpyrrolidone, and use 10% (by weight) ethanol solution containing water (containing the required BHA) to prepare grain. Pass the wet material through a 18 mesh sieve and dry overnight, granulate, lubricate with magnesium stearate, mix well, and compress the homogeneous mixture with a 1 / 4 inch standard concave round tool, using a compression force of 1000 lbs. . The thickness of the compressed tablet is 3.89 mm, and the hardness is 8-10 kg.

[0096] 2), the tablet core is covered with a water-soluble film coat

[0097] Wrap a water-soluble film coat on the above tablet core. The coating material for water-soluble film coating was an aqueous solution containing 4.5% hydroxypropylmethylcellulose (Pharmacoat, 603 / ShinE...

Embodiment 2

[0119] Prepare samples and control samples according to the following prescriptions and processes

[0120] 1), preparation of tablet core:

[0121]

[0122] Glipizide, polyethylene oxide and sodium chloride are mixed, then mixed with magnesium stearate and then molded into a 502mg tablet core. A 12mm standard concave circular die is used to compress the tablet. The compression force used 1200~1800kg, pressing time 1~2s, 6~8kg.

[0123] 2), preparation of coating solution:

[0124] Add cellulose acetate to ethyl acetate-ethanol (95:5) to obtain a 5% solution as the oil phase, and use a 3 mg / ml sodium lauryl sulfate aqueous solution as the water phase; Slowly add the water phase to the oil phase at a speed of not less than 3000 rpm to form a W / O emulsion, and continue to add until O / W colostrum is formed. Pass the colostrum through a high-pressure homogenizer for 6 times. The organic solvent was removed from the resulting emulsion using a rotary evaporator at 40°C under red...

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Abstract

The invention discloses a preparation method for a controlled release preparation which has improved drug releasing property and mechanical property and increased production repeatability and is externally coated with a controlled release coat film comprising drug released pores filled with air, especial for a zero-order release controlled release preparation. The preparation method comprises thefollowing steps of firstly preparing core material; secondly, coating a controlled release coat film for the core material with solution of polymer containing sublimable matters and / or matter particles capable of being degraded into harmless gases or a dispersion liquid; thirdly, subjecting the polymer coat film to healing processing until the coating core material has a stable dissolution characteristic endpoint; and fourthly, volatilizing and / or degrading the sublimable matters and / or the matters capable of being degraded into harmless gases, wherein the fourth step is finished after the third step.

Description

technical field [0001] The invention relates to a method for preparing a controlled-release preparation, especially a zero-order release controlled-release preparation. More specifically, the present invention relates to a controlled-release film with improved overall performance, especially improved production reproducibility and drug release stability, coated with a controlled-release coating containing numerous air-filled drug release micropores The preparation method of the preparation, especially the controlled release preparation of zero order release. Background technique [0002] Some water-insoluble polymers control drug release by coating in controlled-release formulations, especially zero-order release controlled-release formulations. Due to the water insolubility of the polymer, the micropores of the coating film are often required to improve the permeability of the coating film to facilitate the penetration of water and the release of the drug, especially when ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K9/30A61K9/32A61K9/36A61K9/16A61K47/30A61K45/00
Inventor 钟术光
Owner OVERSEAS PHARMA
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