Preparation method of isoniazid slow release microspheres

A technology of sustained-release microspheres and isoniazid, which is applied in the field of medicine, can solve the problem of not establishing a sustained-release system, and achieve the effects of reducing lung burden, small burst release and high encapsulation rate

Inactive Publication Date: 2015-02-25
INST OF MEDICINAL PLANT DEV CHINESE ACADEMY OF MEDICAL SCI
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0006] The purpose of the present invention is to establish a slow-release drug delivery system for pulmonary interventional therapy via bronchoscopy, to solve the problem that the slow-release system has not been established in local interventional therapy, and to provide targeted interventional therapy for refractory, retreatment and multidrug-resistant pulmonary tuberculosis , shorten the closure time of the cavity, promote the absorption of distal lesions, reduce recurrence and dissemination, and strive to significantly improve the cure rate of pulmonary tuberculosis

Method used

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  • Preparation method of isoniazid slow release microspheres
  • Preparation method of isoniazid slow release microspheres
  • Preparation method of isoniazid slow release microspheres

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0120] The preparation of embodiment 1 isoniazid micropowder particles

[0121] Take 0.5g of isoniazid bulk drug and place it in a ball mill, mix it with 20g of grinding balls, then add 3ml of dichloromethane, and grind for 2h with a rotating speed of 650rpm; 161±0.106nm).

Embodiment 2

[0122] The preparation of embodiment 2 isoniazid polylactic acid microspheres (IN-PLA-MS)

[0123] Get 40 mg of isoniazid micropowder particles prepared in Example 1, ultrasonically disperse in 40 ml of methylene chloride, add 800 mg of PLA [viscosity 0.49 dl / g (CHCl 3 / 25°C)], ultrasonically dissolved to obtain S / O suspension; the suspension was spray-dried (spray conditions: inlet temperature 60°C, nozzle cap aperture 5.5 μm), and isoniazid-polylactic acid microspheres were obtained.

[0124] According to the method of "1.2" of Experimental Example 1, the encapsulation efficiency of the isoniazid polylactic acid microspheres was 87.24%, and the drug loading was 4.99%.

[0125] Scanning electron microscopy (SEM) was used to observe the morphology of the microspheres, and the results are shown in figure 2 . From figure 2 In A (overall picture), it can be seen that IN-PLA-MS has a round shape, smooth surface, good dispersion and no adhesion. From figure 2 In B (enlarged...

Embodiment 3

[0128] The preparation of embodiment 3 isoniazid-chitosan composition (IN-CTS)

[0129] Prepare a 1% acetic acid solution, weigh an appropriate amount of chitosan CTS (Mw50000-19000) and add it, stir and swell until completely dissolved, prepare a CTS solution with a concentration of 0.25% for use; press IN:CTS=1:1, take IN and add to In the prepared CTS solution, stir until IN is completely dissolved. While stirring, add TPP aqueous solution according to sodium tripolyphosphate TPP:CTS=3:5 for cross-linking. After low-speed stirring, use B90 spray dryer for spray drying (inlet temperature 90 ℃, outlet temperature ℃, pump speed 2.4mL·min-1) to obtain the isoniazid-chitosan composition.

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Abstract

The invention provides a preparation method of isoniazid slow release microspheres. The method comprises the following steps: 1, uniformly mixing an isoniazid solid component (S) with an oil phase (O) and an organic solvent to form a solid-in-oil (S / O) suspension; and 2, carrying out spray drying on the suspension prepared in step 1 to prepare the slow release microspheres. The method adopting a solid-in-oil spray drying technology to prepare the isoniazid slow release microspheres overcomes the disadvantages of large particle size, burst release of drugs, low entrapment rate, complex preparation method and long preparation time of microspheres in the prior art. The method has the advantages of simple and controllable operation, suitable particle size, high entrapment rate, good slow release effect and no obvious burst release.

Description

technical field [0001] The invention relates to a preparation method of isoniazid sustained-release microspheres, in particular to a method for preparing isoniazid sustained-release microspheres by a solid-in-oil-spray drying method, and belongs to the field of medicine. Background technique [0002] The focus and difficulty of tuberculosis treatment lies in retreatment, refractory and multidrug-resistant tuberculosis. The conventional route of drug administration is poor in chemotherapy effect, and the patient has not healed for many years, and the sputum bacteria are continuously positive or become lifelong bacteria excretion. At present, the interventional therapy for pulmonary tuberculosis usually uses injection or suspension as the dosage form of drug administration. The drug release rate of this type of preparation is fast, and patients need to undergo frequent interventional operations, resulting in poor compliance. [0003] Isoniazid (IN) is a water-soluble small-mo...

Claims

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Application Information

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IPC IPC(8): A61K9/16A61K31/4409B01J13/04A61P31/06
Inventor 朱春燕张丽梅张运
Owner INST OF MEDICINAL PLANT DEV CHINESE ACADEMY OF MEDICAL SCI
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