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Bupropion hydrochloride sustained-release pellet and preparation method thereof

A technology of bupropion hydrochloride and sustained-release pellets, which is applied in the direction of non-active ingredient medical preparations, pharmaceutical formulas, medical preparations containing active ingredients, etc., can solve the problems of release differences, reduce production costs, High solubility, no pH-dependent effect

Inactive Publication Date: 2009-07-22
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the change of PH in the body is greatly affected by food, individual differences, etc., so the release of the above-mentioned enteric-coated pellets to different individuals also has certain differences

Method used

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  • Bupropion hydrochloride sustained-release pellet and preparation method thereof
  • Bupropion hydrochloride sustained-release pellet and preparation method thereof
  • Bupropion hydrochloride sustained-release pellet and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] Step 1: Preparation of Pill Hearts Containing Pills

[0041] prescription:

[0042] Bupropion Hydrochloride 300g

[0043] Microcrystalline Cellulose 180g

[0044] Lactose 20g

[0045] Distilled water 250g

[0046] Preparation process: Grind bupropion hydrochloride raw material, pass through 80-mesh sieve with microcrystalline cellulose and lactose respectively, then sieve and mix three times, add distilled water to make softener, and extrude the softener into bars at an extrusion speed of 20rpm Then put it into a spheronizer and spheronize at a speed of 20HZ for 8min. Afterwards, the pill core is dried overnight at 50°C, and the 20-40 mesh pellets are taken for later use.

[0047] Step 2: Pack the drug-containing pill core in step 1 with a Surelease coating.

[0048] prescription:

[0049] Surelease (solid content 25%) 240g

[0050] Distilled water 510g

[0051] PEG6000 2.4g

[0052] Preparation process: Dilute Surelease with distilled water, then add PEG6000 t...

Embodiment 2

[0055] Step 1: Preparation of Pill Hearts Containing Pills

[0056] prescription:

[0057] Bupropion Hydrochloride 300g

[0058] Microcrystalline Cellulose 116g

[0059] Lactose 13g

[0060] Distilled water 160g

[0061] Preparation process: Grind bupropion hydrochloride raw material and pass through 80-mesh sieve with microcrystalline cellulose respectively, then sieve and mix three times, add distilled water to make softener, and extrude the softener into strips at an extrusion speed of 20rpm , and then put it into a spheronizer and spheronize at a speed of 20HZ for 8 minutes, then dry the core of the pills loaded at 50°C overnight, and take 20-40 mesh pellets for later use.

[0062] Step 2: Coat the pill core in step 1 with a Surelease coating.

[0063] prescription:

[0064] Surelease (solid content 25%) 172g

[0065] Distilled water 364g

[0066] Lactose 0.514g

[0067] Preparation process: Dilute Surelease with distilled water, then add lactose and magnetically ...

Embodiment 3

[0070] Step 1: Preparation of Pill Hearts Containing Pills

[0071] prescription:

[0072] Bupropion Hydrochloride 300g

[0073] Microcrystalline Cellulose 200g

[0074] Distilled water 250g

[0075] Preparation process: Grind bupropion hydrochloride raw material and pass through 80-mesh sieve with microcrystalline cellulose respectively, then sieve and mix three times, add distilled water to make softener, and extrude the softener into strips at an extrusion speed of 20rpm , and then put it into a spheronizer and spheronize at a speed of 20HZ for 8 minutes, then dry the core of the pills loaded at 50°C overnight, and take 20-40 mesh pellets for later use.

[0076] Step 2 Coat the core of the drug-containing pill in step 1 with HPMC.

[0077] prescription:

[0078] HPMC 15g

[0079] PEG6000 1.5g

[0080] Distilled water 285g

[0081] Preparation process: Dissolve 15gHPMC (viscosity 5cps) and 1.5gPEG6000 in distilled water, place the pill core in the material hopper of ...

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Abstract

The invention relates to the field of a drug preparation, in particular to a hydrochloric acid bupropion slow release micro pill and a method for preparing the same. The micro pill consists of a drug containing pill core and a slow release coating layer which consists of slow release materials and a pore-forming agent, wherein the weight of the slow release materials against the weight of the drug containing pill core is between 8 and 15 percent, and the weight of the pore-forming agent against the weight of the slow release materials is between 1 and 6 percent. The micro pill does not need to be combined by a plurality of micro pills with different release modes, and only adopts a single micro pill to achieve the good release performance, thereby lowering production cost and simplifying production process.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a bupropion hydrochloride sustained-release pellet and a preparation method thereof. Background technique [0002] Bupropion Hydrochloride (Bupropion Hydrochloride) is an aminoketone antidepressant, the chemical name is (±)-1-(3-chlorophenyl)-2-[(1,1-methylethyl)amino ]—1—acetone hydrochloride, molecular formula is C 13 h 18 CINO.HCI is a racemic mixture with a molecular weight of 276.20g / mol. This product is a white or off-white crystalline powder; it tastes bitter and numb; its melting point is 233-234°C; its solubility in water is 312mg / ml, and its solubility in ethanol is 193mg / ml, the solubility in 0.1N HCI is 333mg / ml; pKa is 7.9. The LD50 in mice and rats are 230mg / kg and 210mg / kg respectively. Vd is 19L / Kg, and the distribution in the body is relatively uniform; the plasma protein binding rate is 82% to 88%. It is basically completely metabolized by the li...

Claims

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Application Information

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IPC IPC(8): A61K9/16A61K47/32A61K47/38A61K31/137A61P25/24
Inventor 平其能吕文莉陈玲萍
Owner CHINA PHARM UNIV
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