Self-emulsifying drug delivery system for improving bioavailability of insoluble medicine, and application thereof

A technology for drugs and derivatives, applied in the field of self-microemulsifying drug-carrying systems and their preparation, can solve problems such as different solubility

Active Publication Date: 2016-05-04
李素华
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

First, the solu

Method used

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  • Self-emulsifying drug delivery system for improving bioavailability of insoluble medicine, and application thereof
  • Self-emulsifying drug delivery system for improving bioavailability of insoluble medicine, and application thereof
  • Self-emulsifying drug delivery system for improving bioavailability of insoluble medicine, and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0053] Embodiment 1: the preparation of blank SEDDS prescription

[0054] The oil phase was mixed with CapmulMCM and caprylic acid (1:1w / w) on a shaker at the highest speed for 48h. The oil phase, CremophorRH40 or oil phase, CremophorRH40 and PEG400 were accurately weighed into a 20mL vial, vortexed for 2min, and then shaken on a shaker at room temperature at the highest speed for 48h to prepare a blank SEDDS formulation.

Embodiment 2

[0055] Embodiment 2: Preparation of drug-loaded SEDDS prescription

[0056] The excipients of drug-loaded SEDDS prescription and blank SEDDS prescription are the same. The drug loading is calculated based on the dissolution performance of the blank SEDDS after dispersion. The preparation method of the drug-loaded SEDDS dosage form is as follows: Weigh the various excipients and drugs of the blank SEDDS into a 20mL vial, vortex and mix for 2min, and then shake on a shaker at room temperature at the highest speed for 48h to prepare the drug-loaded SEDDS prescription.

[0057] In order to prevent the drug from being precipitated in the gastrointestinal tract, the drug loading of SEDDS was calculated based on the dissolving ability of the drug after the blank SEDDS was dispersed. For example, 1 g of blank SEDDS formulation F5:5 dispersed in phosphoric acid solution exhibited the lowest solubility for danazol (19 μg / mL). Therefore, for danazol-loaded SEDDS formulation, 1 g of F5:5...

Embodiment 3

[0059] Embodiment 3: the research of solubility property

[0060] The study of solubility properties is to measure the equilibrium solubility of danazol, indomethacin and haloperidol in the microemulsion formed after dispersion in the blank SEDDS aqueous medium. Using method II (paddle method) in the United States Pharmacopoeia, disperse 1, 2, 3, 4, 5g blank SEDDS prescriptions in 250mL water (pH7.0), hydrochloric acid buffer (pH1.2), phosphate buffer ( pH6.8) to obtain blank SEDDS microemulsion. During the experiment, the temperature of the aqueous medium was maintained at 37°C, the rotation speed was 50 rpm, and the dispersion time was 60 minutes. The hydrochloric acid buffer and phosphate buffer were prepared according to the method of the United States Pharmacopoeia. Thereafter, take 5 mL of blank SEDDS microemulsion in a 20 mL vial, and add excess danazol, indomethacin or haloperidol, respectively. The vial was shaken at 37° C., 220 rpm in a water-bath shaker for 48 h t...

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Abstract

The invention provides a novel self-emulsifying drug delivery system (SEDDS). An SEDDS carrier material comprises a surfactant and an oil phase containing Capmul MCMs and medium chain fatty acids, is suitable for loading pH-dependent (weakly acidic and weakly alkaline) and a pH-independent (neutral) insoluble medicines, greatly improves the solubility of the medicines to realize optimum bioavailability, and has important application values in the development of preparations of the insoluble medicines.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a self-microemulsifying drug-carrying system for improving the bioavailability of insoluble drugs, a preparation method and application thereof. Background technique [0002] Poorly soluble drugs usually mean low oral bioavailability due to their extremely poor water solubility and extremely low dissolution rate. If they are to be developed into oral preparations such as tablets, capsules and other commonly used dosage forms, these drugs often require preparation or process improvement to increase their water solubility and dissolution rate to achieve the best oral bioavailability. [0003] Emulsions are a dosage form commonly used to improve the absorption of fat-soluble drugs. However, conventional emulsions are not well accepted due to their bulk, short shelf life and poor palatability. Therefore, self-emulsifying drug delivery systems (SEDDS, self-emulsifyingdrugd...

Claims

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Application Information

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IPC IPC(8): A61K47/14A61K47/12A61K47/34A61K47/44A61K31/405A61K31/4515A61K31/58
CPCA61K9/4858A61K9/4866A61K31/405A61K31/4515A61K31/58
Inventor 李素华李继喜
Owner 李素华
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