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Slow-releasing micro-pills of sophocarpidine and its preparing method

A technology of slow-release pellets and matrine, which is applied in the direction of pill delivery, bulk delivery, digestive system, etc., can solve the problems of difficult to control drug release rate, unsteady drug effect, short maintenance time, etc. To achieve the effect of easy quality control, wide range of drug-containing percentage, and good fluidity

Inactive Publication Date: 2007-10-03
SHANDONG INST OF PHARMA IND
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] The existing dosage forms of matrine include capsules, tablets, injections, etc. Because the biological half-life is less than 1 hour, the effective blood concentration in the body after oral administration is maintained for a short time, and patients need to take it 3 to 4 times a day, so the compliance Poor, especially when the time interval is long after taking the medicine at night and in the morning, the blood drug concentration is very low in the morning, and there is a "peak and valley" phenomenon, the effect of the medicine cannot be exerted smoothly, and the side effects are also large
Therefore, matrine sustained-release tablets are being developed, and there have been three related patent publications, the application numbers are 03106240.7, 03112629.4 and 03112655.3, but because matrine is easily soluble in water and the dosage is relatively large, the skeleton-type sustained-release Formulation is difficult to control drug release rate

Method used

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  • Slow-releasing micro-pills of sophocarpidine and its preparing method
  • Slow-releasing micro-pills of sophocarpidine and its preparing method
  • Slow-releasing micro-pills of sophocarpidine and its preparing method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] Embodiment 1 Preparation of pill core containing drug

[0042] A. Prescription:

[0043] Matrine 500g

[0044] Microcrystalline Cellulose (MCC) 500g

[0045] Total 1000g

[0046] B. Preparation process:

[0047] Take matrine raw material, pulverize and pass through a 120-mesh sieve, add microcrystalline cellulose, pass through an 80-mesh sieve and mix thoroughly; add a certain amount of wetting agent (such as 50% ethanol) to the mixed material to make a soft material , passed through a 16-mesh sieve to obtain wet granules; put the wet granules into the extruder and extrude them into strip-shaped extrudates; quickly add the extrudates to the spheronizer for spheronization, and take them out after a certain period of time to obtain pellets ;Dry the prepared pellets at 45°C for 8 hours to obtain dry pellets; as a result, the appearance of the pellets is smooth and spherical, and the dissolution test results are shown in Figure 1. It can be seen that t...

Embodiment 2

[0049] The core of the pills containing the medicines prepared in Example 1 is coated with ethyl cellulose slow-release film coating, and the matrine sustained-release pellets are obtained.

[0050] A. Prescription of coating solution:

[0051] Ethyl cellulose 60g

[0052] PEG1500 6g

[0053] Diethyl phthalate 5g

[0054] Talc powder 15g

[0055] 95% ethanol to 1000mL

[0056] B. Preparation process:

[0057] Mix ethyl cellulose and porogen PEG1500 at a ratio of 10:1, add ethanol and stir until clear, then add appropriate amount of plasticizer diethyl phthalate and talcum powder, stir at a high speed and homogenize, and then coat and polymerize The weight gain is between 7% and 8%. The release rate of the drug in water was determined by spectrophotometry, and the results are shown in Figure 2.

Embodiment 3

[0059] The drug-containing pellet core prepared in Example 1 was coated according to the following coating liquid prescription to obtain matrine sustained-release pellets.

[0060] A. Prescription of coating solution:

[0061] Surelease 600g

[0062] 5% PEG6000 solution 75g

[0063] Water up to 1000g

[0064] B. Preparation process:

[0065] According to the above prescription, take Surelease and porogen 5% PEG6000 solution, mix it at a ratio of 8:1, dilute it with water to a solid content of about 15%, stir at a high speed to coat evenly, and the weight gain is between 10% and 12%. . The release rate of the drug in water was determined by spectrophotometry, and the results are shown in Figure 3.

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Abstract

A slow-releasing kurarinol micropill is composed of a pill core containing kurarinol (20-90%) and prepared by rounding method, and a coated slow-release film prepared by fluidized-bed coating method.

Description

Technical field: [0001] The invention belongs to the technical field of drug sustained-release preparations, and in particular relates to a sustained-release pellet containing active ingredient matrine and a preparation method thereof. technical background: [0002] Matrine is oxymatrine. Oxymatrine is an aqueous alkaloid preparation extracted from the traditional Chinese medicine Sophora sophora, in which oxymatrine (oxymatrine) accounts for more than 98%, and the molecular formula is C 15 h 24 N 2 o 2 ·H 2 O, the molecular weight is 282, and there are a very small amount of sophocarpine and sophoramine. [0003] In recent years, the main progress of oxymatrine in the treatment of viral hepatitis is as follows: ①Oxymatrine has a direct anti-hepatitis B virus effect; ②Oxymatrine can inhibit collagen activity and prevent liver fibrosis; Matrine can block abnormal apoptosis of liver cells; ④ Oxymatrine has a protective effect on experimental liver failure in mice; 64 ca...

Claims

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Application Information

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IPC IPC(8): A61K31/4375A61K9/16A61K9/20A61K9/48A61P1/16A61P31/20
Inventor 陈修毅
Owner SHANDONG INST OF PHARMA IND
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