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Ginkgolide B quick release pellet and preparation method thereof

A ginkgolide, quick-release technology, applied in the direction of pharmaceutical formulations, medical preparations containing active ingredients, allergic diseases, etc., can solve the problems of weak improvement of absorption effect, increase of drug particle size, low efficiency, etc. Achieve the effect of improving solubility and dissolution speed, improving absorption efficiency, and ensuring active structure

Active Publication Date: 2016-03-23
JIANGSU KANION PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Chinese patent literature (publication number CN1857255A) discloses a GB injection emulsion, the invention mainly achieves the effect of improving the curative effect by targeting the emulsion particles at the inflammatory tissue and concentrating on the tissue, the efficiency is low, and the absorption effect is improved weak
The advantage of this technology is that there are fewer other carrier materials added, which can achieve higher drug loading; the main disadvantage is that the particle size of the drug increases after long-term storage, and precipitation
[0010] After searching patents and literature, there is no relevant report on using ginkgolide B monomer as an active ingredient to make immediate-release preparations through the combined application of anti-solvent method, wet grinding, and liquid-phase layering drug application technology.

Method used

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  • Ginkgolide B quick release pellet and preparation method thereof
  • Ginkgolide B quick release pellet and preparation method thereof
  • Ginkgolide B quick release pellet and preparation method thereof

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Experimental program
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Effect test

Embodiment 1

[0047] The preparation of embodiment 1 nanosuspension

[0048] According to each prescription of Table 1, the stabilizer of prescription quantity is taken and dissolved in prescription quantity purified water to obtain stabilizer solution, and the ginkgolide B ethanol solution of prescription quantity is added in this solution, and ginkgolide B is mixed with stable The agent solution is fully mixed to obtain a coarse suspension, and then the coarse suspension is added to the nano grinder, and 380-450 g of zirconia beads with a diameter of 0.4 μm are added, and the grinding frequency is set to 3500 rpm, and the grinding is performed for a certain period of time. The time is shown in Table 2, and the ginkgolide B nanosuspension was prepared.

[0049] Table 1: Composition of different prescriptions

[0050]

[0051]

[0052] Table 2: Grinding time of different formulations and average particle size of the suspension after grinding

[0053] prescription number

...

Embodiment 2

[0064] The preparation of embodiment 2 ginkgolide B quick-release pellets

[0065] Curing process prescription:

[0066]

[0067]

[0068] Get recipe quantity mannitol, sodium lauryl sulfate and be dissolved in appropriate amount of water and prepare curing stabilizer solution, get the nano-suspension 200g of ginkgolide B prepared by prescription 1 (the average particle diameter of ginkgolide B in the suspension is between 100 ~500nm range), the two are mixed evenly under the action of magnetic stirring, take the prescribed amount of microcrystalline cellulose pellets and place them in the fluidized bed, open the fluidized bed and set the process parameters (inlet air temperature 36°C; outlet air temperature 33°C ; Air volume 90m 3 / h; liquid supply pump speed 8-15rpm; atomization pressure 0.05-0.1mpa); secondly, turn on the liquid supply pump, and spray the drug nano-suspension onto the surface of the blank pellet core continuously. The latter stage can be accelerated...

Embodiment 3

[0070] The preparation of embodiment 3 ginkgolide B quick-release pellets

[0071] Curing process prescription:

[0072]

[0073] Get prescription quantity mannitol, sodium lauryl sulfate and be dissolved in appropriate amount of water and prepare solidification stabilizer solution, get the nano-suspension 200g of ginkgolide B prepared by prescription 2 (the average particle diameter of ginkgolide B in the suspension is between 100 ~500nm range), the two are mixed evenly under the action of magnetic stirring, take the prescribed amount of microcrystalline cellulose pellets and place them in the fluidized bed, open the fluidized bed and set the process parameters (inlet air temperature 36°C; outlet air temperature 33°C ; Air volume 110m 3 / h; liquid supply pump speed 8-15rpm; atomization pressure 0.05-0.1mpa); secondly, turn on the liquid supply pump, and spray the drug nano-suspension onto the surface of the blank pellet core continuously. The latter stage can be accelera...

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Abstract

The invention relates to a ginkgolide B quick release pellet and a preparation method thereof, and belongs to the field of medicinal preparations. The ginkgolide B quick release pellet comprises a blank pellet core and a medicated layer, wherein the weight ratio of the blank pellet core to the medicated layer is 1:(1.1-10.0); the medicated layer is prepared from ginkgolide B, a crystal stabilizer and a curing stabilizer, wherein the weight ratio of the ginkgolide B to the curing stabilizer is 1:(1.0-2.5). The ginkgolide B quick release pellet disclosed by the invention is rapid in effect, good in absorption, safe and stable, the bioavailability in vivo can be remarkably improved, and the individual difference of oral administration is reduced. The drug loading capacity of the quick release pellet is improved, at the same time, the situations that the grain diameter is increased and precipitation is generated caused by long-term standing of medicament are avoided, and the quick release pellet has high clinical use value, and is simple in preparation technique and suitable for industrial production.

Description

Technical field: [0001] The invention provides ginkgolide B quick-release pellets and a preparation method thereof, belonging to the field of pharmaceutical preparations. Background technique: [0002] In the 1980s, it was found that ginkgolide is a strong antagonist of platelet activating factor (PAF), which has significant curative effect on cardiovascular and cerebrovascular diseases, which caused an upsurge of ginkgo research in the world, most of which are aimed at the overall effect of ginkgo. lactones. In 1984, Braquet et al. proved that ginkgolides have strong specific inhibitory activity on platelet activating factor (PAF) receptors, and have unique pharmacological effects on cardiovascular and cerebrovascular diseases. At present, they are considered to be the most promising natural PAF receptors for clinical application. Antibody antagonists, among which ginkgolide B (GinkgolideB, GB) has the strongest activity. Therefore, ginkgolide B, as a highly active platel...

Claims

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Application Information

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IPC IPC(8): A61K9/16A61K31/365A61P7/02A61P37/06A61P25/28A61P29/00A61P9/00A61P37/08
Inventor 萧伟唐星王振中何海冰张宇郭庆明
Owner JIANGSU KANION PHARMA CO LTD
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