Polymer intensifier in controlled release preparation

A technology of controlled-release preparations and polymers, applied in the field of zero-order release controlled-release preparations and their preparation, and in the field of zero-order release controlled-release preparations, which can solve the problem of rupture of the controlled-release coating, small changes, and no change in drug content, etc. question

Active Publication Date: 2011-04-20
江苏保易制药有限公司
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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: 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 drops significantly, while the drug content in the preparation basically does not change or The magnitude of the change is relatively small
[0008] As another example, the drug release performance or drug release rate of the controlled-release preparation prepared by this technology is often significantly lower than that of the film-controlled release preparation using a water-soluble substance with the same particle size as a pore-forming agent. Membrane controlled-release formulations containing hollow (no pore-forming agent) micropores of the same particle size to con

Method used

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  • Polymer intensifier in controlled release preparation
  • Polymer intensifier in controlled release preparation
  • Polymer intensifier in controlled release preparation

Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0154] Each basic step in the preparation method of the controlled-release preparation is described in detail below.

[0155] 1), preparing a core material containing at least one biologically active substance

[0156] The preparation method of the core material used in the present invention is not particularly limited in the present invention. In general, core preparation methods can be used by direct extrusion methods, extrusion methods of dry, wet or sintered granules, extrusion and subsequent rounding methods, wet or dry granulation or direct pelletization (for example on discs) , or by bonding the powder (powder layer) to active substance-free spheres (granules) or active substance-containing granules, or by forming tablets in a certain way, such as by compression, or a combination of the above methods.

[0157] 2) Coating step: use a solution or aqueous dispersion of a polymer that is insoluble or almost insoluble in water and digestive juices containing sublimable subs...

Embodiment 1

[0184] Embodiment 1 and comparative example 1

[0185] 1, preparation embodiment 1 sample

[0186] 1), prepare tablet core according to the following prescription and process:

[0187]

[0188] Mix diltiazem hydrochloride, lactose, hydroxypropyl cellulose and povidone evenly, and granulate with ethanol; force the wet granulated material to pass through an 18-mesh sieve and dry for 24 hours; after sizing, add magnesium stearate and mix Evenly, use a 12mm standard concave circular die to compress the tablet, the used compression force is 1200-2000kg, and the compression time is 2s. The hardness is 6-10kg.

[0189] 2), the tablet core is coated according to the following prescription and process:

[0190] Coating Solution Prescription:

[0191]

[0192] ※, calcium carbonate coated with stearic acid ( FX), produced by Solvay Company, the contact angle θ with the coating polymer was measured to be 21°.

[0193] The tablet cores were coated on a Hicoater / Fruend coater. ...

Embodiment 2

[0201] Embodiment 2 and comparative example 2

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Abstract

The invention discloses application of a polymer intensifier in the production or the storage of a controlled release preparation, in particular to the controlled release preparation with zero order release. The invention also discloses the controlled release preparation with improved performance, in particular to the controlled release preparation with the zero order release. The controlled release preparation comprises a core material containing a bioactivator and a polymer controlled release coating which is coated on the core material, is provided with a plurality of medicine release micropores filled with air and contains the polymer intensifier, wherein the contact angle of a polymer and the polymer intensifier is less than 90 degrees, and the medicine release micropores are obtained by sublimating sublimable substances and/or degrading degradable harmless gases. The preparation has higher storage stability, higher production repeatability and better medicine release performance in the medicine release aspect; moreover, a controlled release membrane of the polymer intensifier has better mechanical behavior, therefore, the polymer intensifier has lower dosage pouring release possibility and higher administration safety.

Description

technical field [0001] The invention relates to the use of a polymer enhancer in the production or storage of a controlled-release preparation, especially a zero-order release controlled-release preparation. It also relates to a controlled-release preparation, especially a zero-order release controlled-release preparation and a preparation method thereof. More specifically, it relates to a controlled-release formulation with improved performance, especially a zero-order release controlled-release formulation, which comprises a core material containing biologically active substances and a plurality of air-filled A polymer controlled-release film with drug-releasing micropores and a polymer enhancer, wherein the contact angle between the above-mentioned polymer and the above-mentioned polymer enhancer is lower than 90°, and the above-mentioned drug-release micropores are sublimable and sublimable Substances and / or degradation obtained from substances that degrade to harmless ga...

Claims

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Application Information

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IPC IPC(8): A61K47/38A61K47/32
Inventor 钟术光
Owner 江苏保易制药有限公司
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