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Dexmethylphenidate hydrochloride dual-release preparation and preparation method thereof

A double-release technology of dexmethylphenidate hydrochloride, which is applied in the fields of pharmaceutical formulation, drug delivery, and nervous system diseases, can solve the problems of drug addiction and dependence, short half-life, poor compliance, etc., and achieve simple preparation process Easy operation, less loss, stable and uniform release performance

Inactive Publication Date: 2011-01-05
孙卫东
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The common preparation of methylphenidate needs to be taken two to three times a day due to its short half-life, and patients are prone to missed doses, poor compliance, and may lead to drug addiction and dependence in the case of exceeding the therapeutic dose

Method used

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  • Dexmethylphenidate hydrochloride dual-release preparation and preparation method thereof
  • Dexmethylphenidate hydrochloride dual-release preparation and preparation method thereof
  • Dexmethylphenidate hydrochloride dual-release preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0071] prescription

[0072] (1) pellet core

[0073] Microcrystalline Cellulose 49g

[0074] Dexmethylphenidate Hydrochloride 5.0g

[0075] Carboxymethylcellulose 1g

[0076] 2% hydroxypropyl methylcellulose solution 44ml

[0077] (2) Immediate release pellets

[0078] Pellet core 56g

[0079] 6% hydroxypropyl methylcellulose solution 11.2ml

[0080] (3) Delayed release pellets

[0081] Pellet core 100g

[0082] 15% solids aqueous dispersion of ethyl cellulose 33.3ml

[0083] Dibutyl phthalate 0.2g

[0084] Talc powder 1.6g

[0085] Preparation process and process:

[0086] (1) Preparation process and technology of pellet core

[0087] The medicine, the filler and the disintegrant were pulverized to a certain particle size range, and after passing through an 80-mesh sieve, they were mixed in a mixer for 1 hour, and then 44ml of 2% (w / v) hydroxypropylmethylcellulose solution was added to prepare into soft material. Turn on the low-temperature refrigerator and con...

Embodiment 2

[0095] prescription

[0096] (1) pellet core

[0097] Microcrystalline Cellulose 49g

[0098] Dexmethylphenidate Hydrochloride 5.0g

[0099] Crospovidone 0.9g

[0100] 2% hydroxypropyl methylcellulose solution 44ml

[0101] (2) Immediate release pellets

[0102] Pellet core 56g

[0103] 20% Opadry I aqueous solution 11.2ml

[0104] (3) Delayed release pellets

[0105] Pellet core 250g

[0106] Udrake L30D-55 166.7g

[0107] Triethyl citrate 12.5g

[0108] Talc powder 12.5g

[0109] water 216ml

[0110] Preparation process and process:

[0111] (1) Preparation process and technology of pellet core

[0112]The drug, filler and disintegrating agent are crushed to a certain particle size range, passed through an 80-mesh sieve, mixed in a mixer for 1 hour, and then 44ml of hydroxypropylmethylcellulose solution is added to make a soft material. Turn on the low-temperature refrigerator and control the temperature at 4-15°C. After 10 minutes, put the soft material into t...

Embodiment 3

[0120] prescription

[0121] (1) pellet core

[0122] Microcrystalline Cellulose 49g

[0123] Dexmethylphenidate Hydrochloride 5.0g

[0124] Povidone 0.5g

[0125] 2% hydroxypropyl methylcellulose solution 44ml

[0126] (2) Immediate release pellets

[0127] Pellet core 56g

[0128] 20% Opadry MP Solution 11.2ml

[0129] (3) Delayed release pellets

[0130] Pellet core 100g

[0131] 15% solids aqueous dispersion of ethyl cellulose 33.33ml

[0132] Preparation process and process:

[0133] (1) Preparation process and technology of pellet core

[0134] The drug, filler and disintegrating agent are crushed to a certain particle size range, passed through an 80-mesh sieve, mixed in a mixer for 1 hour, and then 44ml of hydroxypropylmethylcellulose solution is added to make a soft material. Turn on the low-temperature refrigerator, and control the temperature at 4-15 degrees Celsius. After 10 minutes, put the soft material into the low-temperature and high-pressure extrud...

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Abstract

The invention belongs to the field of medicine, and in particular relates to a dexmethylphenidate hydrochloride dual-release preparation and a preparation method thereof. The preparation of the invention comprises pellets with different release performance, wherein the pellets comprise 10 to 70 percent of quick-response pellets and 20 to 60 percent of enteric-coated pellets based on the total weight of the pellets. The release mode in the preparation can achieve an ideal treatment effect and ensure that the medicament concentration in blood plasma in vivo is maintained as long as 16 to 24 hours. Compared with a dexmethylphenidate hydrochloride common preparation which is taken twice per day, the dual-release preparation can reduce a peak value of the medicament concentration in the blood plasma in vivo after the medicament is taken for the second time, and simultaneously the bioavailability of the medicament is not influenced. The dexmethylphenidate hydrochloride adopted by the invention can effectively reduce toxic and side effects brought by a racemic compound and improve a treatment effect and the medication compliance of a patient.

Description

technical field [0001] The invention relates to a preparation method of pharmaceutical preparations in the field of pharmacy, in particular to a double-release capsule preparation of dexmethylphenidate hydrochloride and a preparation method thereof. technical background [0002] Dexmethylphenidate hydrochloride, the racemic d-threo enantiomer of methylphenidate hydrochloride, is a central nervous system stimulant. The chemical name is (R,R)-(+)-α-phenyl-2-piperidine acetate methyl ester hydrochloride. It has the molecular formula: C 14 h 19 NO 2 • HCl. The molecular weight is 269.77, and the structural formula is: [0003] [0004] Methylphenidate hydrochloride is a first-line drug for the treatment of attention deficit hyperactivity disorder (ADHD). It is a relatively safe and effective drug with an effective rate of 78-80%. ADHD is the most common childhood mental development disorder. The main symptoms of the disorder are: inattention, impulsive behavior, easily...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/52A61K9/58A61K9/62A61K31/4458A61P25/28A61P25/18
Inventor 孙卫东李学明伍衢
Owner 孙卫东
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