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Delayed total release gastrointestinal drug delivery system

A technology for the gastrointestinal tract and drug delivery device, which can be used in the digestive system, muscular system diseases, neuromuscular system diseases, etc., and can solve problems such as potential toxicity of azo compounds

Inactive Publication Date: 2009-10-14
DEXCEL PHARMA TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0052] Currently available pharmaceutical formulations of enterocides designed for colonic release are unlikely to be used in humans in the long term, in part due to the potential toxicity of this azo compound

Method used

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  • Delayed total release gastrointestinal drug delivery system
  • Delayed total release gastrointestinal drug delivery system
  • Delayed total release gastrointestinal drug delivery system

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1-7

[0142] Materials and methods

[0143] Calcium pectate (food grade) containing 4% calcium was supplied by Genu-Copenhager Pectin (Denmark). To prepare the coating suspension, the calcium pectate was fractionated using a sieve shaker (Levy Laboratory Equipment, LTD) and a 149[mu] sieve (ASTM 100, 8" diameter) to obtain a fraction with a particle size of <149[mu]. Emcocel 90M (Microcrystalline Cellulose) (BP Grade), Eudragit E 100 (Eud.E), Ethyl Cellulose EC-N100 NF0100 (EC), Magnesium Stearate (USP Grade), Cross-Linked Polyvinylpyrrolidone (USP Grade) ) (CPVP or Crospovidone), diclofenac sodium (BP grade) and sodium salicylate (USP grade) were purchased from Mendel, Rohm Pharma (Germany), Aqualon (Netherlands), Merk (Germany), Basf, Amoli Organics (India), respectively and Merk (Germany). Pyridostigmine bromide was purchased from Orgasynth Industries (France). Ethanol was USP grade.

[0144] The mixture for compression in a tablet machine is prepared by granulation or dry blen...

Embodiment 1

[0149] Control of burst time by weight (thickness) of coat

[0150] Tablets are prepared by dry blending the ingredients. The recipe for the core is shown in Table 1 (229-76A). The core has a diameter of 8mm and a hardness of 11-12Kp. The uncoated core disintegrates within seconds in the intestinal TS, releasing all the diclofenac sodium. The cores were spray coated with varying amounts of ethylcellulose:calcium pectate (1:1 w / w). The results are shown in figure 1 middle. Each tablet is coated with a 2-hour delay at 8 mg, 4 hours at 11 mg, 9 hours at 17 mg, and 12 hours at 20 mg. In each case, the tablet disintegrated completely after a delay time.

[0151] Reducing the amount of cross-linked polyvinylpyrrolidone to 5% (Formula 229-99A) gave essentially the same results. figure 2 , the 7 mg coating per tablet produced an 8-hour delay before burst release of the drug. The cross-linked polyvinylpyrrolidone-free formulation does not provide burstiness at all.

[0152] T...

Embodiment 2

[0155] The effect of tablet hardness

[0156] The tablet cores were dry blended and compressed at different pressures to obtain tablets of different hardnesses. The formulation was identical to 229-76A (Table 1). Tablet core 229-93B has a hardness of 11-13 Kp, while tablet core 229-93A has a hardness of 5-8 Kp. The core was spray coated as in Example 1 with a 1 : 1 weight ratio of ethyl cellulose: calcium pectate.

[0157] image 3 The dissolution study of the coated tablet shown in shows that the 12 mg coating produced a 5 hour delay before burst release of drug. The coated tablet 229-93A did not exhibit a burst of drug release. For a coating level of approximately 10 mg per tablet, the drug is released as a slow-type after a delay of 7-8 hours ( Figure 4 ).

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Abstract

A gastrointestinal drug delivery system is provided. The system includes a drug combined with a swellable core material surrounded by a water-insoluble or relatively water-insoluble coating material in which the particulate water-insoluble material is embedded. When the drug delivery device enters the gastrointestinal tract, the particulate matter absorbs liquid, thereby forming a channel between the drug-containing core and the exterior of the drug delivery device. Liquid enters the core through these channels and swells the core to the point of breaking the coating. When the integrity of the coating is compromised, the core disintegrates, immediately releasing all or most of the drug at a specific location. By controlling parameters in the device such as core material, carrier material in the coating, and particulate matter, the site of drug release can be carefully controlled. Therefore, the object of the present invention is also a method of using this device to treat diseases by releasing drugs in the gastrointestinal tract in a position- and time-dependent manner.

Description

Field of Invention [0001] The present invention relates to drug delivery systems that deliver enterically administered drugs to specific locations along the gastrointestinal tract by immediately releasing (non-sustained release) all or most of the drug at the specific location. The drug delivery system has the ability to completely lose its integrity in a very short period of time, thereby releasing virtually all of the drug contained therein at the site of disintegration. Features that confer this capability are a channel-forming coating that allows controlled access of liquid to the core and a core that absorbs liquid and swells sufficiently to rupture the coating that encloses the core, where the core is located. The integrity of the coating is destroyed and disintegrates rapidly. Background of the Invention [0002] Specific administration to selected targets in the gastrointestinal tract is a need to treat a wide variety of diseases. It is particularly desirable to be...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/20A61K9/48A61K47/30A61K9/16A61K9/28A61K9/52A61K31/19A61K31/27A61K31/407A61K31/44A61K45/00A61K47/32A61K47/36A61K47/38A61P1/00A61P1/06A61P21/02A61P29/00
CPCA61K9/2866A61K9/5084A61K9/205A61K9/286A61P1/00A61P1/06A61P21/02A61P29/00A61K9/28
Inventor E·I·勒纳M·弗莱施纳A·潘哈斯
Owner DEXCEL PHARMA TECH