Paliperidone sustained-release microspheres, injection thereof and preparation method of the sustained-release microspheres

A technology of paliperidone and slow-release microspheres, which is applied to medical preparations containing non-active ingredients, medical preparations containing active ingredients, and pharmaceutical formulas, etc. Side effects, increased metabolic by-products and other issues, to achieve the effect of improving bioavailability, relieving pain, and high drug loading

Active Publication Date: 2016-10-05
NEW FOUNDER HLDG DEV LLC +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This method is mainly through the use of special auxiliary materials so that the drug can release the drug at a constant speed in the body. It is administered orally, and the dosage of the drug is relatively lower than that of the injection drug, and the duration is short.
[0004] Chinese Patent Application Publication No.CN102274164A mentions that a compound composed of paliperidone or paliperidone derivatives and polylactide-glycolide / dimethyl sulfoxide is used to make a sustained-release injection, but the After the method is metabolized in the body, the metabolic by-products will be increased, which will increase the toxic and side effects of the drug
[0006] However, there is no paliperidone sustained-release microspheres in the prior art, especially long-acting paliperidone sustained-release microspheres. is a difficulty, if the prepared microspheres are too low in drug loading, the effect of prolonging the administration time will not be achieved

Method used

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  • Paliperidone sustained-release microspheres, injection thereof and preparation method of the sustained-release microspheres
  • Paliperidone sustained-release microspheres, injection thereof and preparation method of the sustained-release microspheres
  • Paliperidone sustained-release microspheres, injection thereof and preparation method of the sustained-release microspheres

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preparation example Construction

[0046] The third aspect of the present invention provides a method for preparing paliperidone sustained-release microspheres, the method comprising the following steps:

[0047] 1) Provide an organic solution of paliperidone and polylactic-co-glycolic acid; and provide an aqueous solution of an emulsifier;

[0048] 2) adding the organic solution to the aqueous solution for emulsification; and

[0049] 3) Separation to obtain the organic phase containing the microspheres, and remove the organic solvent therein to prepare paliperidone sustained-release microspheres;

[0050] Wherein, the volume ratio of the organic solution to the aqueous solution is (7-9):(100-120), preferably 7:100.

[0051] Preferably, the organic solvent in the organic solution is selected from dichloromethane, ethyl acetate or a mixture thereof.

[0052] Preferably, in the organic solution, the polylactic acid-glycolic acid copolymer has a concentration of 0.0085-0.0100 g / ml, and the paliperidone has a co...

Embodiment 1

[0075] Experimental steps:

[0076] 1. Weigh an appropriate amount of PVA, add water to dissolve at 90°C, allow to cool to room temperature, constant volume, and prepare a 0.03g / ml PVA solution to obtain an aqueous phase solution.

[0077] 2. Take 1000ml of the aqueous phase solution obtained in step 1 and place it in a Fluko reaction vessel for later use.

[0078] 3. Weigh 0.175g of Paliperidone bulk drug and 0.7g of PLGA, add 70ml of dichloromethane to dissolve it completely, and obtain an organic phase solution, that is, in this organic phase solution, the concentration of Paliperidone bulk drug is 0.0025 g / ml, the concentration of PLGA is 0.01g / ml.

[0079] 4. Add the organic phase solution dropwise to the aqueous phase solution in the Fluko reaction vessel with a separatory funnel, and perform mechanical stirring while adding dropwise at a stirring speed of 60rmp; centrifuge after stirring for 6 hours, discard the upper layer solution, and collect the lower layer of micr...

Embodiment 2

[0083] Experimental steps:

[0084] 1. Weigh an appropriate amount of PVA, add water to dissolve at 95°C, let it cool to room temperature, constant volume, and prepare a 0.03g / ml PVA solution to obtain an aqueous phase solution.

[0085] 2. Take 1000ml of the aqueous phase solution obtained in step 1 and place it in a Fluko reaction vessel for later use.

[0086] 3. Weigh 0.185 g of paliperidone bulk drug and 0.8 g of PLGA, add 80 ml of dichloromethane to dissolve them completely, and obtain an organic phase solution.

[0087] 4. Add the organic phase solution dropwise to the aqueous phase solution in the Fluko reaction vessel with a separatory funnel, mechanically stir while adding dropwise, the stirring speed is 60rmp, centrifuge after stirring for 7 hours, discard the upper layer solution, collect the lower layer of microspheres, The obtained microspheres were washed three times with water, collected, subpackaged and freeze-dried. The freeze-drying method was freezing at -...

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Abstract

The invention provides a paliperidone sustained release microsphere and an injection thereof, and a preparation method of the sustained release microsphere. The paliperidone sustained release microsphere disclosed by the invention comprises paliperidone and a polylactic acid-glycolic acid copolymer, wherein the weight ratio of the paliperidone to the polylactic acid-glycolic acid copolymer is (0.160-0.190):(0.5-0.9); the grain size of the paliperidone sustained release microsphere is 20-50mum. The paliperidone sustained release microsphere is prepared for the first time, and is high in medicament loading capacity, long in slow release period and good in biocompatibility.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to long-acting sustained-release microspheres containing paliperidone, a preparation method of the sustained-release microspheres and an injection prepared from the sustained-release microspheres. Background technique [0002] Paliperidone is the active metabolite of risperidone, its English name is Paliperidone, and its chemical name is 6,7,8,9-tetrahydro-3-(2-(4-(6-fluoro-1,2-benzene different Azol-3-yl)-1-piperidinyl)ethyl)-9-hydroxy-2-methyl-4H-pyrido[2,1-a]pyrimidin-4-one, developed by Johnson & Johnson, USA, 2006 In December 2009, it was approved for marketing by the US FDA. Studies have shown that it can effectively delay the relapse rate of schizophrenia, and can be used for acute short-term and long-term maintenance treatment of schizophrenia to relieve symptoms and stabilize patients' condition effectively in long-term use. Clinical experiments have proved th...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/16A61K9/19A61K31/519A61K47/34A61P25/18
Inventor 罗敏张洪兰
Owner NEW FOUNDER HLDG DEV LLC
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