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Microemulsion of total glucosides of paeony and active components

A technology of total glycosides microemulsion and Paeonia lactiflora, applied in the field of total glycosides of Paeonia lactiflora and its effective components microemulsion, can solve the problem that the main action mechanism and action target are difficult to clarify clearly, the bioavailability of paeoniflorin is low, absorption, distribution, metabolism Pharmacokinetic characteristics such as excretion and excretion are not easy to elucidate.

Inactive Publication Date: 2009-12-16
魏伟 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Because TGP contains multiple active ingredients such as paeoniflorin, hydroxypaeoniflorin, paeoniflorin, paeoniflorin, benzoylpaeoniflorin, etc., its main mechanism of action and target are difficult to elucidate clearly. Pharmacokinetic characteristics such as metabolism and excretion are not easy to elucidate
When total glucosides of paeony were used clinically, it was found that the bioavailability of paeoniflorin was low; after increasing the oral dose, some patients had gastrointestinal reactions such as abdominal distension, diarrhea, loss of appetite, or abdominal pain, nausea, dizziness and other manifestations in the early stage of treatment

Method used

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  • Microemulsion of total glucosides of paeony and active components
  • Microemulsion of total glucosides of paeony and active components
  • Microemulsion of total glucosides of paeony and active components

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0084] a. Take paeoniflorin 1.2g, Tween-8036g, polyethylene glycol 40036g, oleic acid 9g and distilled water 190g, set aside;

[0085] b. Mix Tween-80, polyethylene glycol 400, and oleic acid, stir, and add distilled water dropwise until the system forms a clear liquid;

[0086] c. Add paeoniflorin, stir and dissolve at normal temperature and pressure until the system forms a clear liquid, and obtain paeoniflorin microemulsion with a particle size of 10-100 nm;

[0087] d. Filling the paeoniflorin microemulsion and sterilizing it to prepare the paeoniflorin microemulsion oral liquid.

Embodiment 2

[0089] a. Take total glucosides of paeony 1.5g, Tween-8036g, polyethylene glycol 40036g, oleic acid 9g and distilled water 190g, set aside;

[0090] b. Mix Tween-80, polyethylene glycol 400, and oleic acid, stir, and add distilled water dropwise until the system forms a clear liquid;

[0091] c. Add total glucosides of paeony, stir and dissolve at normal temperature and pressure until the system forms a clear liquid, and obtain total glucosides of paeony microemulsion with a particle size of 10-100 nm;

[0092] d. Filling the total glucosides of paeony microemulsion to prepare the total glucosides of paeony microemulsion oral liquid.

Embodiment 3

[0094] a. Take paeoniflorin 0.6g, polyethylene glycol-vitamin E succinate 15.0g, propylene glycol 8.0g, soybean oil for injection 10.0g and water for injection 62g, set aside;

[0095] b. Add soybean oil for injection into the mixture of polyethylene glycol-vitamin E succinate and propylene glycol, mix well, and set aside;

[0096]c. Stir at normal temperature and pressure, and slowly add the amount of water for injection in which paeoniflorin has been dissolved, until the system forms a clear liquid to obtain a transparent paeoniflorin microemulsion with a particle size of 10-100 nm.

[0097] d. Filling and sterilizing the paeoniflorin microemulsion to prepare the paeoniflorin microemulsion injection.

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Abstract

The invention discloses a microemulsion of total glucosides of paeony and active components, which consists of the total glucosides of paeony and the active components, a surfactant, a cosurfactant, an oil phase and a water phase. The microemulsion has transparent appearance, a particle size of between 10 and 100 nanometers and good stability, and can remarkably improve the absorption of paeoniflorin so as to improve the bioavailability of medicaments, reduce the toxic side effects, and improve the curative effect.

Description

1. Technical field [0001] The invention relates to a traditional Chinese medicine preparation, in particular to a preparation processed from effective parts extracted from Chinese herbal medicines and its active ingredients, specifically a microemulsion of total glucosides of paeony and its active ingredients. 2. Background technology [0002] Microemulsion (referred to as microemulsion) is a transparent or translucent, low viscosity, thermodynamically stable and isotropic oil-water mixed system, which is stabilized by surfactants and co-surfactants. Its droplets are generally between 10 and 100nm, transparent in appearance and close to water in viscosity; stable in thermodynamics, not delaminated or demulsified after long-term storage. As a new drug delivery system, it is stable, slow-release, can improve drug bioavailability and exert targeting effects. [0003] Total glucosides of paeony (TGP) is an effective part extracted from the root of the traditional Chinese medici...

Claims

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Application Information

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IPC IPC(8): A61K36/71A61K9/107A61P29/00A61P37/02
Inventor 魏伟杨昭毅
Owner 魏伟
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