Colon positioned releasing micropills and production thereof

A technology of colon positioning and micropills, which is applied in the direction of pharmaceutical formula, medical preparations of non-active ingredients, block delivery, etc. It can solve the problems of excretion out of the body, achieve high bioavailability, facilitate absorption, and gastric irritation small effect

Inactive Publication Date: 2007-06-20
珠海天翼医药技术开发有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

When we imitated this prescription and made tablets containing barium sulfate, we found that 3 out of 5 cases did not disintegrate in the colon through human X-ray irradiation, and the whole tablet was excreted out of the body with the human body. Therefore, this protection prescription needs to be improved

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Ball core prescription:

[0026] Secnidazole 250.0g

[0027] PVP 7.5g

[0028] MCC 42.5g

[0029] 95% ethanol appropriate amount

[0030] Ball core process: After sieving and mixing the raw materials and auxiliary materials of the prescription amount, add binder to make soft pellets, put them in a spheronizer to make wet pellets, dry at 20-40°C, and sieve to obtain the pellets for coating. pill.

[0031] Coating solution prescription (pellet 100 grams):

[0032] Eudragit S100 30.0g

[0033] 3 g triethyl citrate

[0034] Talc powder 15g

[0035] Proper amount of ethanol

[0036] Coating process: Place the pellets in a high-efficiency coating pan and coat them by continuous spraying. After the weight gain of the coating meets the requirements, dry them with hot air for 20 minutes, then dry them in a drying oven at 40°C for 24 hours, and dry them at room temperature. for 3 days.

Embodiment 2

[0038] Ball core prescription:

[0039] Secnidazole 500.0g

[0040] HPMC 5.0g

[0041] Cross-linked carboxymethyl starch sodium 50.0g

[0042] Starch 15.0g

[0043] Magnesium Stearate 5.0g

[0044] Micro Silica Gel 5.0g

[0045] 95% ethanol appropriate amount

[0046] Ball core process: After sieving and mixing the raw materials and auxiliary materials of the prescription amount, add binder to make soft pellets, put them in a spheronizer to make wet pellets, dry at 20-40°C, and sieve to obtain the pellets for coating. pill.

[0047] Coating solution prescription (pellet 100 grams):

[0048] Eudragit L100 25.0g

[0049]Eudragit S100 75.0g

[0050] Polyethylene glycol 5 grams

[0051] Talc powder 25g

[0052] Proper amount of ethanol

[0053] Coating process: Place the pellets in a high-efficiency coating pan and coat them by continuous spraying. After the weight gain of the coating meets the requirements, dry them with hot air for 20 minutes, then dry them in a dryi...

Embodiment 3

[0055] The release measurement was performed on the coated pellets of the above examples. Method: Rotating basket method (according to Chinese Pharmacopoeia 2000 edition two appendix XC first method), 37 ℃, rotating speed 100rpm. Operation: Sampling in pH 1.2 hydrochloric acid solution for 2 hours, sampling in pH 6.8 phosphate buffer solution for 3 hours, and sampling in 45 minutes after changing pH 7.8 phosphate buffer solution. Determination: After sampling in the dissolution media of pH1.2 and pH6.8, directly measure the absorbance at 277nm and 319nm wavelength according to spectrophotometry (Chinese Pharmacopoeia 2000 edition two appendix IVA), calculate release amount; After sampling in the medium, filter, take 2ml of the filtrate into a 50ml volumetric flask, constant volume, measure the absorbance at 319nm, and calculate the release amount.

[0056] The release amount of coated pellets in pH1.2 hydrochloric acid solution for 2 hours should be less than 1%, the release ...

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PUM

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Abstract

An orally taken micropill released only in colon is prepared from active medicine and pharmacologically acceptable auxiliaries through mixing, granulating, extruding, rounding and drying.

Description

technical field [0001] The invention relates to colon-localized release secnidazole pellets and a preparation method thereof, belonging to the field of pharmaceutical preparations. Background technique [0002] Since the 1990s, a new type of targeted drug delivery system—the colon-targeted drug delivery system has received more and more attention. In just a few years, a variety of drug delivery types have been formed, and many a targeted material. [0003] The antiprotozoal and antibacterial activity of metronidazole, a 5-nitroimidazole drug, was first recognized in the 1950s. This type of drug has activity against a variety of anaerobic Gram-positive and Gram-negative bacteria and protozoa, especially in tissues. Amoeba, Giardia lamblia, and Trichomonas vaginalis. In recent years, a new generation of nitroimidazole drugs, secnidazole (SNZ), has been developed abroad, and various phases of clinical research have been completed in China. Compared with other 5-nitroimidazol...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K47/32
Inventor 张晓明王军曾万溪麦耀权
Owner 珠海天翼医药技术开发有限公司
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