Bicyclol double-layer osmotic pump control-released tablet and preparation method thereof

An osmotic pump controlled release and bicyclol technology, which is applied in osmotic transportation, coating, antiviral agents, etc., can solve the problems affecting clinical treatment effects, short half-life of bicyclol, large individual differences, etc., to reduce blood drug concentration difference, improve clinical efficacy, enhance the effect of absorption

Active Publication Date: 2012-11-07
BEIJING UNION PHARMA FACTORY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Bicyclol has a short half-life and needs to be taken 3 times a day during clinical treatment, which is extremely inconvenient for chronic hepatitis B patients who need long-term medication
In addition, the oral release of bicyclol is faster, and the individual differences are large, which affects the clinical therapeutic effect.

Method used

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  • Bicyclol double-layer osmotic pump control-released tablet and preparation method thereof
  • Bicyclol double-layer osmotic pump control-released tablet and preparation method thereof
  • Bicyclol double-layer osmotic pump control-released tablet and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] Drug-containing layer

[0033] Bicyclol 75mg

[0034] Polyoxyethylene 134mg

[0035] PVP K30 24mg

[0036] Sodium chloride 5mg

[0037] Magnesium Stearate 2mg

[0038] The total weight of the drug-containing layer is 240mg

[0039] booster layer

[0040] Polyoxyethylene 64mg

[0041] PVP K30 10mg

[0042] Sodium chloride 35mg

[0043] Iron Oxide Red 0.6mg

[0044] Magnesium stearate 0.4mg

[0045] Booster layer total weight 110mg

[0046] semipermeable membrane coating

[0047] Cellulose acetate 3.9g

[0048] PEG 4000 0.2g

[0049] 95% acetone / water 1000ml

[0050] Preparation:

[0051]1) Preparation of the drug-containing layer: uniformly mix the prescribed amount of bicyclol and other auxiliary materials except magnesium stearate, and add an appropriate amount of ethanol to granulate. Dry at room temperature or in drying equipment.

[0052] 2) The dried main drug layer is sieved, then fully mixed with the magnesium stearate of the prescribed amount. ...

Embodiment 2

[0062] Drug-containing layer

[0063] Bicyclol 75mg

[0064] Polyoxyethylene 139mg

[0065] Hypromellose 24mg

[0066] Magnesium Stearate 2mg

[0067] The total weight of the drug-containing layer is 240mg

[0068] booster layer

[0069] Polyoxyethylene 64mg

[0070] Hypromellose 10mg

[0071] Sodium chloride 35mg

[0072] Iron Oxide Red 0.6mg

[0073] Magnesium stearate 0.4mg

[0074] Booster layer total weight 110mg

[0075] semipermeable membrane coating

[0076] Cellulose acetate 95g

[0077] PEG 3350 5g

[0078] Dichloromethane / methanol (2:10) 2000ml

[0079] Preparation:

[0080] 1) Preparation of the drug-containing layer: uniformly mix the prescribed amount of bicyclol and other auxiliary materials except magnesium stearate, and add an appropriate amount of ethanol to granulate. Dry at room temperature or in drying equipment.

[0081] 2) The dried main drug layer is sieved, then fully mixed with the magnesium stearate of the prescribed amount.

[0082]...

Embodiment 3

[0091] Drug-containing layer

[0092] Bicyclol 165mg

[0093] Polyoxyethylene 393mg

[0094] HPMC 70mg

[0095] Magnesium Stearate 7mg

[0096] The total weight of drug-containing layer is 635mg

[0097] booster layer

[0098] Polyoxyethylene 140mg

[0099] Hypromellose 20mg

[0100] Sodium chloride 71mg

[0101] Iron Oxide Red 1.5mg

[0102] Magnesium Stearate 2.5mg

[0103] Booster layer total weight 235mg

[0104] semipermeable membrane coating

[0105] Cellulose acetate 95g

[0106] PEG 5g

[0107] Dichloromethane / methanol (2:10) 2000ml

[0108] Preparation:

[0109] Same as Example 2, first prepare the drug-containing layer and the booster layer, then compress the double-layer tablet, and finally coat the semi-permeable membrane, laser perforate and moisture-proof isolation layer.

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PUM

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Abstract

The invention discloses a bicyclol double-layer osmotic pump control-released tablet and a preparation method thereof. The preparation, namely the tablet, contains bicyclol and pharmaceutically acceptable auxiliary materials. The structure of the tablet contains two layers of tablet cores, wherein one layer of tablet core is a medicament-containing layer; the other layer of tablet core is a boosting layer; an insoluble semipermeable membrane is wrapped outside the tablet cores; and one or more small medicament-releasing holes are formed on the membrane. The medicament-releasing mechanism of the preparation is novel; the bicyclol medicament is slowly and stably released through an osmotic pressure difference inside and outside the wrapping membrane; the medicament-releasing behavior has good zero-level control-released characteristic and is slightly affected by factors, such as medium environment pH value, gastrointestinal motility, foods and the like; therefore, compared with the ordinary preparation, the preparation provided by the invention can obviously improve the stability of bicyclol blood concentration, reduce the appearance of toxic and side effects and reduce the individual difference of clinical effect.

Description

technical field [0001] The invention relates to a controlled-release dosage form of bicyclol for treating hepatitis, in particular to a double-layer osmotic pump controlled-release preparation and a preparation method thereof. Background technique [0002] Osmotic pump tablet is a new type of controlled-release tablet. It compresses drugs, penetration enhancers or other auxiliary materials with high osmotic pressure into a solid tablet core, and wraps a layer of rate-controlling semi-permeable membrane, and then uses a laser on the tablet core. One or more drug release holes are opened on the coating film. After oral administration, the water in the gastrointestinal tract enters the tablet core through the semipermeable membrane, so that the drug is dissolved into a saturated solution or suspension, and the dissolution of the excipient with high osmotic pressure makes the solution in the tablet membrane a hypertonic solution. There is a large osmotic pressure difference bet...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/24A61K31/36A61K47/32A61K47/34A61K47/38A61P1/16A61P31/14A61P31/20
CPCA61K9/2072A61K9/2866A61K9/0004A61K9/2086A61K31/357A61P1/16A61P31/12A61P31/14A61P31/20A61K9/20
Inventor 郭旻彤吕昭云李燕潘显道杨超莲李强王晓梅兰培赵立敏刘玉娟刘艳
Owner BEIJING UNION PHARMA FACTORY
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