Lurasidone hydrochloride nano mixed suspension solution for durable intramuscular injection and preparation method of mixed suspension solution

A technology of lurasidone hydrochloride and nanosuspension is applied in the directions of non-active ingredient medical preparations, active ingredients-containing medical preparations, pharmaceutical formulas and the like, can solve problems such as low solubility, and achieves simple preparation process, Ease of industrialization, effect of increasing solubility and dissolution rate

Inactive Publication Date: 2019-07-12
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The solubility of lurasidone hydrochloride in water is low, and the preparation of long-acting preparations with a dosage of 3 to 7 days brings challenges to the preparation workers

Method used

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  • Lurasidone hydrochloride nano mixed suspension solution for durable intramuscular injection and preparation method of mixed suspension solution
  • Lurasidone hydrochloride nano mixed suspension solution for durable intramuscular injection and preparation method of mixed suspension solution
  • Lurasidone hydrochloride nano mixed suspension solution for durable intramuscular injection and preparation method of mixed suspension solution

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Experimental program
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Effect test

Embodiment 1

[0040] Weigh 0.1% (w / v) Tween 20 and place it in isotonic water for injection with pH 7.0, dissolve it ultrasonically to obtain a stabilizer solution, then weigh 0.1% (w / v) lurasidone hydrochloride and disperse it in the above stabilizer In the solution, disperse at a high speed of 9000 rpm for 5 minutes to obtain a coarse suspension of lurasidone hydrochloride. Then, the lurasidone hydrochloride nanosuspension can be prepared by stirring for 6 hours under the condition of rotating speed of 1200 r / min by wet media grinding method. Detected with a laser particle size analyzer, the average particle diameter is 460.6nm, and the polydispersity index is 0.365.

Embodiment 2

[0042] Weigh 0.1% (w / v) polyethylene glycol 4000 and place it in isotonic water for injection with pH 7.0, dissolve it ultrasonically to obtain a stabilizer solution, then weigh 0.15% (w / v) lurasidone hydrochloride and disperse it in the above In the stabilizer solution, disperse at a high speed of 9000 rpm for 5 minutes to obtain a coarse suspension of lurasidone hydrochloride. Then, the lurasidone hydrochloride nanosuspension can be prepared by stirring for 8 hours under the condition of rotating speed of 900 r / min by wet media grinding method. Detected with a laser particle size analyzer, the average particle diameter is 384.9nm, and the polydispersity index is 0.274.

Embodiment 3

[0044] Weigh 0.07% (w / v) polyethylene glycol 4000 and 0.04% poloxamer 188 in the isotonic water for injection of pH 7.0, ultrasonically dissolve to obtain a stabilizer solution, and then weigh 0.15% (w / v ) Lurasidone hydrochloride is dispersed in the above stabilizer solution, and dispersed at a high speed of 9000rpm for 5 minutes to obtain a coarse suspension of lurasidone hydrochloride. Then adopt the wet media grinding method and stir at 900r / min for 6h to prepare the lurasidone hydrochloride nanosuspension. Detected with a laser particle size analyzer, the average particle diameter is 351.5nm, and the polydispersity index is 0.237.

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Abstract

The invention discloses a lurasidone hydrochloride nano mixed suspension solution for durable intramuscular injection and a preparation method of the nano mixed suspension solution. The raw materialsof the nano mixed suspension solution comprise 0.1-0.5 wt.% of lurasidone hydrochloride and 0.1-0.3 wt.% of a stabilizer, and a solvent is water for injection. Through high-speed dispersion, in combination with a wet-method medium grinding method, the lurasidone hydrochloride is prepared into the nano mixed suspension solution for intramuscular injection, the first-pass effect is avoided, and thesolubility and dissolution rate of the medicine after muscle injection are improved. After muscle injection, the effect can be achieved continuously for 3-7 days, the drug administration frequency isreduced, fluctuation of the plasma drug concentration is reduced, and the compliance and safety of a patient during medicine taking are improved.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to a lurasidone hydrochloride long-acting intramuscular injection nano suspension and a preparation method thereof. Background technique [0002] Lurasidone hydrochloride is a new type of atypical antischizophrenia drug, the chemical name is (3aR,4S,7R,7aS)-2-{(1R,2R)–2-[4-(1,2 -benzisothiazol-3-yl)piperazin-1-ylmethyl]cyclohexylmethyl}hexahydro-1H-4,7-methylisoindole-1,3-dione hydrochloride. Lurasidone hydrochloride can act on multiple targets, including dopamine D 2 receptor, 5-HT 7 , 5-HT 1A , 5-HT 2A receptor and alpha 2 It has a strong therapeutic effect on improving the positive symptoms, negative symptoms and cognitive function of schizophrenia, and the incidence of metabolic adverse reactions (such as weight gain, dyslipidemia and hyperglycemia) is low. It has obvious advantages in the treatment of schizophrenia and is widely used in the...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/10A61K47/10A61K47/26A61K47/38A61K31/496A61P25/18
CPCA61K9/0019A61K9/10A61K31/496A61K47/10A61K47/26A61K47/38A61P25/18
Inventor 刘建平王丹青亓梓桐
Owner CHINA PHARM UNIV
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