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Herpetetrone nanosuspension and dry powder thereof, and preparation methods and applications of herpetetrone nanosuspension and dry powder

A nano-suspension, dry powder technology, applied in powder delivery, pharmaceutical formulations, medical preparations with non-active ingredients, etc., can solve the problems of affecting drug efficacy, low solubility, slow dissolution rate, etc.

Active Publication Date: 2020-07-07
AIR FORCE MEDICAL CENT PLA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, Herpetetrone is a poorly soluble drug. Due to its low solubility and slow dissolution rate, the absorption of the drug is limited, which in turn affects its efficacy.

Method used

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  • Herpetetrone nanosuspension and dry powder thereof, and preparation methods and applications of herpetetrone nanosuspension and dry powder
  • Herpetetrone nanosuspension and dry powder thereof, and preparation methods and applications of herpetetrone nanosuspension and dry powder
  • Herpetetrone nanosuspension and dry powder thereof, and preparation methods and applications of herpetetrone nanosuspension and dry powder

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] Example 1: Preparation of Herpetetrone Nanosuspension:

[0040] (1) Accurately weigh 50 mg of the HPT bulk drug, place it in 10 mL of absolute ethanol and dissolve it completely to obtain solution A;

[0041] (2), accurately weigh povidone K30 10mg into 40mL distilled water and dissolve completely to obtain solution B;

[0042] (3), put solution B under the probe for ultrasonication, quickly inject solution A into solution B, and continue ultrasonication for 15 minutes to obtain Herpetetrone nanosuspension; the mode of ultrasonication is working for 3s and intermittent for 3s; The power is 400W.

Embodiment 2

[0043] Example 2: Preparation of Herpetetrone nanosuspension dry powder:

[0044] (1), preparation of Herpetetrone nano-suspension: accurately weigh 50 mg of HPT bulk drug, place in 20 mL of absolute ethanol and dissolve completely to obtain solution A;

[0045] Accurately weigh 3010 mg of PVPK into 40 mL of distilled water and dissolve completely to obtain solution B;

[0046]Put solution B under the probe and sonicate (work for 3s, intermittent for 3s, power 400W); quickly inject solution A into solution B, and continue to sonicate for 15min with the same ultrasonic mode and frequency to obtain Herpetetrone nanosuspension;

[0047] (2) Preparation of Herpetetrone nanosuspension dry powder: put the HPT-NS prepared in step (1) in a refrigerator at -20°C for 24 hours, and then put it in a freeze dryer with a pressure of 0.10mbar and a temperature of -50°C Freeze-dried for 72 h and then taken out to obtain Herpetetrone nanosuspension dry powder.

Embodiment 3

[0048] Example 3: Preparation of Herpetetrone nanosuspension dry powder:

[0049] In this embodiment, the preparation process of Herpetetrone nanosuspension is the same as that of Example 2, the difference being the preparation of Herpetetrone nanosuspension dry powder, which is obtained by spray drying in this embodiment, and the specific steps are: The HPT-NS prepared in step (1) was spray-dried according to the following conditions: inlet air temperature 100°C, exhaust air temperature 60°C, compressed gas flow rate 465L / h, pumping rate 41m 3 / h, and the spray speed of the feed liquid is 3ml / min to obtain the dry powder of Herpetetrone nanosuspension.

[0050] The determination of a kind of Herpetetrone nanosuspension of the present invention and its dry powder preparation method and its particle size, dispersion index, in vitro dissolution rate, investigation of its inhibitory effect on HSC-T6 liver fibroblasts of the present invention and its comparison with ordinary sus...

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Abstract

The invention provides a Herpetetrone nanosuspension and dry powder thereof, and preparation methods and applications of the herpetetrone nanosuspension and the dry powder and belongs to the technicalfield of traditional Chinese medicinal oral drugs. The Herpetetrone nanosuspension is prepared through an ultrasonic precipitation method. The preparation method of the dry powder of the suspension comprises preparation of the Herpetetrone nanosuspension, and preparation of the dry powder of the Herpetetrone nanosuspension. The dissolvability of the Herpetetrone nanosuspension or the dry powder of the Herpetetrone nanosuspension within 2 h is up to above 90%, and the Herpetetrone nanosuspension or the dry powder of the Herpetetrone nanosuspension has a significant inhibition effect on HSC-T6hepatocyte proliferation. The application is an application in preparation of drugs for treating liver diseases. The Herpetetrone nanosuspension has the advantages that the in-vitro dissolubility is obviously improved, the oral bioavailability in vivo is obviously improved, and meanwhile, the inhibition effect on HSC-T6 cells is enhanced.

Description

technical field [0001] The invention belongs to the technical field of traditional Chinese medicine oral medicine, and relates to a Herpetetrone nanosuspension and its dry powder, preparation method and application; in particular to the preparation and physical and chemical characterization of a Herpetetrone nanosuspension for treating liver diseases; Inhibition and oral bioavailability investigation. Background technique [0002] Hepatic fibrosis is the wound healing response of the liver to liver injury caused by various reasons, and is a common pathological process in various chronic liver diseases. The occurrence of liver fibrosis is characterized by excessive deposition of ECM after the synthesis and degradation of extracellular matrix (ECM) are out of balance. ECM is mainly derived from hepatic stellate cells (HSC), and through the activation and differentiation regulation mechanism of HSC, the excessive deposition of ECM is finally formed, leading to the occurrence o...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/10A61K9/14A61K31/34A61K36/42A61K47/32A61P1/16A61K131/00
CPCA61K9/10A61K9/146A61K31/34A61K47/32A61K36/42A61P1/16Y02A50/30
Inventor 袁海龙申宝德钟雨佶沈成英刘肖
Owner AIR FORCE MEDICAL CENT PLA
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