Guanfacine implant and preparing method thereof

An implant, guanfacine technology, applied in the field of guanfacine implant and preparation, can solve liver toxicity, leg cramps, sudden high blood pressure, high peak blood drug concentration of common dosage form release rate, plasma protein The problem of high binding rate can achieve the effect of small batch difference, good stability and smooth appearance.

Inactive Publication Date: 2016-12-21
BEIJING COLLAB PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Since guanfacine hydrochloride has a strong central action, and the drug has a high plasma protein binding rate, the release rate of the common dosage form is too fast, which may easily lead to a high peak blood concentration and induce its side effects, such as drowsiness, dizziness, and difficulty falling asleep. Nausea, dry mouth, constipation, headache, dry eyes, vomiting, rash or itching, fatigue, indigestion, diarrhea, slow heartbeat, decreased sexual function, unusual tiredness or weakness, confusion, mental depression, forgetfulness, liver toxicity, legs Spasms, sudden hypertension, etc.
[0006] At present, guanfacine hydrochloride preparations are mainly oral preparations, which have large batch-to-batch variability and unstable drug release, which can easily lead to high blood drug concentration and further induce its side effects

Method used

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  • Guanfacine implant and preparing method thereof
  • Guanfacine implant and preparing method thereof
  • Guanfacine implant and preparing method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0043] Prescription (specification: 10mg / bottle, calculated as free base):

[0044]

[0045] preparation:

[0046] Weighing the prescription amount of guanfacine hydrochloride and dissolving it in an appropriate amount of methanol; weighing the prescription amount of polylactic acid-glycolic acid and dissolving it in an appropriate amount of acetone; mixing the above two solutions and spray drying to obtain solid particles; The solid particles were added into a twin-screw hot-melt extruder, and the extrusion temperature was set at 75° C. to obtain a long cylindrical preparation; the prepared preparation was sterilized by radiation, and then packaged in a clean area.

Embodiment 2

[0048] Prescription (specification: 10mg / bottle, calculated as free base):

[0049]

[0050] preparation:

[0051] Weigh the prescribed amount of guanfacine hydrochloride, polylactic acid-glycolic acid copolymer and sodium lauryl sulfate, and mix them uniformly in a mixer to obtain a mixed material; add the mixed material into a twin-screw hot-melt extruder, The extrusion temperature was set at 70° C. to prepare long cylindrical preparations; the prepared preparations were sterilized by radiation and then packaged in a clean area.

Embodiment 3

[0053] Prescription (specification: 10mg / bottle, calculated as free base):

[0054]

[0055] preparation:

[0056]Weigh the prescribed amount of guanfacine hydrochloride and polyethylene glycol-poly(lactic-co-glycolic acid) block copolymer, and mix them uniformly in a mixer to obtain a mixed material; put the mixed material into a twin-screw hot-melt extruder, extrude The outlet temperature was set at 80° C. to prepare long cylindrical preparations; the prepared preparations were sterilized by radiation, and then packaged in a clean area.

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PUM

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Abstract

The invention belongs to the field of pharmaceutical preparations, and particularly relates to a guanfacine implant and a preparing method thereof. The subcutaneous implant comprises guanfacine or salt and carrier thereof, and the mass ratio of guanfacine to the carrier is 10:(1-100). The carrier is a biodegradable material such as polylactic acid-glycollic acid copolymer, polyethylene glycol-poly lactic acid-glycolic acid segmented copolymer, polylactide, polyglycollide and polycaprolactone, and the average molecular weight of the carrier is 8000-100000. The invention further provides the preparing method of the implant. The blank of the prior art is filled, and the preparation is stable in dissolution, long-acting and safe, and has broad application prospects.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to a guanfacine implant and a preparation method. Background technique [0002] Guanfacine is usually administered in the form of its salt, guanfacine hydrochloride, the chemical name is N-amidino-2-(2,6-dichlorophenyl)acetamide hydrochloride, and its molecular formula is: C 9 h 9 Cl 2 N 3 O HCl, the molecular weight is 282.55, the structural formula is as follows: [0003] [0004] Guanfacine hydrochloride is a white to off-white crystalline powder, insoluble in water and ethanol, and has a relatively high solubility in methanol. Guanfacine hydrochloride is the first selective alpha for ADHD 2a -Adrenergic receptor agonists, according to current clinical research, guanfacine hydrochloride can directly bind to receptors in the prefrontal cortex, making postsynaptic α 2a -Receptor stimulation produces effects such as enhancing attention, improving behav...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K47/34A61K47/20A61K47/12A61K31/165A61P25/14
CPCA61K9/0024A61K31/165A61K47/12A61K47/20A61K47/34
Inventor 申超鲍勇胜邱敦有方胜邹德超陈先红王珂
Owner BEIJING COLLAB PHARMA
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