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Crystallization modifier capable of improving properties of chemical drug raw material powder and preparation method for crystallization modifier

The technology of raw material powder and modified substance is applied in the field of crystalline modification for improving the chemical properties of chemical raw material powder and its preparation, which can solve the problems of high cost, large consumption of organic solvent, hidden dangers in drug use safety, and the like. Outline reduction effect

Active Publication Date: 2015-07-01
广东彼迪药业有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] The above crystallization technology belongs to the category of raw material production technology, restricted by laws and regulations, it is only suitable for the application of raw material production enterprises, and cannot be realized in the process of preparation production
In addition, method 1 may also leave additives that are unnecessary for preparation processing and not related to curative effect remaining in raw materials
Harmful organic solvents such as acetone, dichloromethane, chloroform, and petroleum ether must be used in the preparation process of methods 2 and 3, which will also leave hidden dangers for the safety of drugs due to the residue of solvents
Moreover, the three methods are relatively complicated to operate, the crystallization process takes a long time, and a large amount of organic solvents are consumed. The solvents used are highly specific to the species and the cost is high. They have not been widely promoted and applied at present.

Method used

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  • Crystallization modifier capable of improving properties of chemical drug raw material powder and preparation method for crystallization modifier
  • Crystallization modifier capable of improving properties of chemical drug raw material powder and preparation method for crystallization modifier
  • Crystallization modifier capable of improving properties of chemical drug raw material powder and preparation method for crystallization modifier

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Example 1: Hypromellose-paracetamol crystalline modification tablet compression process (API: 87.30%)

[0035] Paracetamol (100 mesh) 10.10kg

[0036] Modifier A-1 2.10kg

[0037] Preparation Process:

[0038] 1. Modifier preparation

[0039] Take 0.10 kg of hypromellose (3-10 mPa·s) and dissolve it in 2.40 kg of water under stirring to obtain modifier A-1.

[0040] 2. Preparation of modifiers

[0041] (1) Take acetaminophen (needle crystal) and pulverize it, pass through a 100-mesh sieve to obtain I.

[0042] (2) Put I in a high-speed mixing granulator, stir at a low speed, slowly add modifier A-1, cut and granulate at a low speed, mix until the cutting current is 4.0A, and obtain II.

[0043] (3) Put II in the fluidized granulator, control the inlet air temperature to 70°C, the humidity to 45% to 65%, and the moisture to 1.5% to 2.5%. The obtained intermediate product was passed through a 30-mesh sieve to obtain 10.15 kg of hypromellose-paracetamol crystalline mod...

Embodiment 2

[0076] Example 2: Hypromellose-sulpiride crystalline modification tablet compression process (API: 77.93%)

[0077] Sulpiride (100 mesh) 10.20kg

[0078] Modifier A-2 2.40kg

[0079] Preparation Process:

[0080] 1. Modifier preparation

[0081] Take 0.05 kg of hypromellose (3-10 mPa·s) and dissolve it in 2.45 kg of alcohol-containing water (weight percentage: ethanol: water = 50:50) under stirring to obtain modifier A-2.

[0082] 2. Preparation of modifiers

[0083] ⑴ Take the raw material of sulpiride, pulverize it, and pass through a 100-mesh sieve to obtain I.

[0084] (2) Put I in a high-speed mixing granulator, stir at a low speed, slowly add modifier A-2, cut and granulate at a low speed, mix until the cutting current is 3.6A, and obtain II.

[0085] (3) Put II in the fluidized granulator, control the inlet air temperature to 70°C, the humidity to 45%-65%, and the moisture content to be 1.0%-2.0%. The obtained intermediate product was passed through a 30-mesh siev...

Embodiment 3

[0095] Example 3: Hypromellose-amlodipine besylate crystal modification tablet compression process (API: 3.93%)

[0096] Amlodipine besylate (100 mesh) 10.10kg

[0097] Modifier A-3 2.20kg

[0098] Preparation Process:

[0099] 1. Modifier preparation

[0100]Take 0.10 kg of hypromellose (3-10 mPa·s) and dissolve it in 2.40 kg of alcohol-containing water (weight percentage: ethanol: water = 30:70) under stirring to obtain modifier A-3.

[0101] 2. Preparation of modifiers

[0102] (1) Take amlodipine besylate raw material and pulverize it, pass through a 100-mesh sieve to obtain I.

[0103] (2) Put Ⅰ in a high-speed mixing granulator, turn on low-speed stirring, slowly add modifier A-3 into the granulator, turn on low-speed cutting and granulating, mix until the cutting current is 3.8A, and get Ⅱ.

[0104] (3) Put II in the fluidized granulator, control the inlet air temperature at 70°C, humidity at 45% to 65%, dry, and control the moisture at 2.0% to 2.5%. The obtained ...

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Abstract

The invention discloses a crystallization modifier capable of improving properties of chemical drug raw material powder and a preparation method for the crystallization modifier. The crystallization modifier is a drug-containing granule obtained by filling, adhering and polymerizing a modifier among chemical drug raw material crystals. The preparation method comprises the following steps: (1) crushing and screening chemical drug raw material crystals; (2) mixing a modifier solution with the chemical drug raw material crystals, and filling, adhering and polymerizing the modifier among the chemical drug raw material crystals to obtain the drug-containing granule; (3) drying and screening the drug-containing granule. According to the crystallization modifier, a direct tableting technology is further developed in practical application, and the drug stability can be improved.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to the pretreatment technology of chemical drug raw materials before the production of solid preparations, in particular to a crystal modification for improving the powder properties of chemical drug raw materials and a preparation method thereof. Background technique [0002] Chemical drugs are mostly organic synthetic chemicals that exist in crystalline form. In addition to the active pharmaceutical ingredient (API), solid preparations usually contain a variety of excipients, such as fillers, disintegrants, lubricants and other chemical substances. The traditional wet granulation technology is to use water, ethanol, starch slurry, sugar, dextrin, hypromellose, carmellose sodium, povidone K30 and other auxiliary materials as binders to bond raw materials and fillers. Wet granules, followed by drying, aim to obtain granules with better uniformity, fl...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/38A61K9/16A61K31/167A61K31/40A61K31/4422
Inventor 蒋林波刘小兰钟燕珍
Owner 广东彼迪药业有限公司
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