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Sustained release gel for injection for paliperidone and paliperidone derivative

A slow-release gel, paliperidone technology, applied in the field of medicine and pharmacy, can solve the problems of large sudden release of drug delivery system, side reactions at the injection site, reducing injection fluidity, etc., so as to reduce toxic side effects and relieve pain , the effect of improving the quality of life

Inactive Publication Date: 2014-07-02
长春斯菲尔生物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, the problem restricting the drug sustained-release system is: on the one hand, the application of organic solvents may cause potential side effects at the injection site, and it is necessary to reduce the amount of solvents as much as possible under the premise of ensuring the injectable fluidity of the preparation; on the other hand , the drug delivery system has a large burst release. In order to suppress the drug burst release, it is usually necessary to reduce the drug load or increase the ratio of polymer / organic solvent, thereby reducing the injection fluidity and increasing the elimination of the polymer in the patient's body. burden

Method used

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  • Sustained release gel for injection for paliperidone and paliperidone derivative
  • Sustained release gel for injection for paliperidone and paliperidone derivative
  • Sustained release gel for injection for paliperidone and paliperidone derivative

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0049] Dissolve 0.4 g of polylactide-glycolide (lactide:glycolide=75:25, molecular weight 105,000) in 2.0 ml of dimethyl sulfoxide, and dissolve under the condition of vortex shaking. 0.1 g of paliperidone was added to disperse evenly, and a slow-release gel with a drug loading of 20% was prepared.

[0050] The sustained-release gel was subjected to in vivo release test in beagle dogs. Administer paliperidone at 0.37 mg / kg, inject subcutaneously with a 1ml disposable syringe, collect blood within 1 to 30 days, and detect by HPLC-MS-MS. See the attached drug-time curve figure 1 , the result proves that the sustained-release gel of the present invention can be continuously released in vivo for at least 1 week.

Embodiment 2

[0052] Dissolve 0.4 g of polylactide-glycolide (lactide:glycolide=50:50, molecular weight 44,000) in 1.6 ml of dimethyl sulfoxide, and dissolve under the condition of vortex shaking. Add 0.17 g of paliperidone to disperse evenly, and prepare a sustained-release gel with a drug loading of about 30%.

[0053] The sustained-release gel was subjected to in vivo release test in beagle dogs. Administer paliperidone at 0.37 mg / kg, inject subcutaneously with a 1ml disposable syringe, collect blood within 1 to 30 days, and detect by HPLC-MS-MS. See the attached drug-time curve figure 2 , the result proves that the sustained-release gel of the present invention can be continuously released in vivo for at least 2 weeks.

Embodiment 3

[0055] Dissolve 0.4 g of polylactide-glycolide (lactide:glycolide=50:50, molecular weight 113,000) in 1.6 ml of dimethyl sulfoxide, and dissolve under vortex shaking conditions. Add 0.4 g of paliperidone to disperse evenly, and prepare a slow-release gel with a drug loading of about 30%.

[0056] The sustained-release gel was subjected to in vivo release test in beagle dogs. Administer paliperidone at 0.37 mg / kg, inject subcutaneously with a 1ml disposable syringe, collect blood within 1 to 30 days, and detect by HPLC-MS-MS. See the attached drug-time curve image 3 , the result proves that the sustained-release gel of the present invention can be continuously released in vivo for at least 1 month.

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Abstract

The invention is an injection slow-release gel for paliperidone and paliperidone derivatives, which consists of paliperidone or paliperidone derivatives and polylactide-glycolide, dimethylmethylene Composed of sulfone, the sustained-release gel of the present invention has small burst release and high drug loading capacity, which greatly reduces the amount of polymers and organic solvents in the drug delivery system, not only reduces production costs, but more importantly, can effectively improve the discomfort at the injection site , the long-acting sustained-release dosage form is more conducive to improving patient compliance, and provides a valuable option for the clinical treatment of psychosis.

Description

technical field [0001] The invention provides a sustained-release gel for injection of paliperidone and paliperidone derivatives, which has the characteristics of long-acting sustained release, high drug loading and low drug burst release, and also provides a preparation method thereof . It belongs to the technical field of medicine and pharmacy. Background technique [0002] Paliperidone is a new drug approved by the U.S. Food and Drug Administration for the treatment of schizophrenia in 2006. Its marketed sustained-release tablet is administered once a day through a drug osmotic pump system. However, its absolute bioavailability is only 28%, which greatly increases its daily dosage, leading to an increase in systemic side effects. In addition, complex dosage forms also lead to high product cost and price, which increases the cost of treatment. The development of long-term sustained-release preparations of paliperidone will greatly improve the bioavailability and avoid t...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/00A61K31/519A61K47/34A61P25/18
Inventor 李又欣王乐希赵晓雷刘喜明王丹孙凤英
Owner 长春斯菲尔生物科技有限公司