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Cnidium lactone foaming microemulsion with optimal mixed materials and preparation method thereof

A technology of osthole and microemulsion, which can be used in emulsion delivery, active ingredients of heterocyclic compounds, sexual diseases, etc., and can solve problems such as mucosal irritation.

Inactive Publication Date: 2018-11-02
SOUTHWEST UNIV +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, microemulsions need to use surfactants and co-surfactants, which are generally irritating to the mucous membranes. Therefore, it is necessary to look for low-toxicity and high-efficiency surfactants and co-surfactants, and even to find low-content surfactants through process optimization. Current key issues in microemulsion research

Method used

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  • Cnidium lactone foaming microemulsion with optimal mixed materials and preparation method thereof
  • Cnidium lactone foaming microemulsion with optimal mixed materials and preparation method thereof
  • Cnidium lactone foaming microemulsion with optimal mixed materials and preparation method thereof

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] 1. Determination of the solubility of osthole in various excipients

[0024] Take about 2mL of different oil phases, surfactants, and co-surfactants into a stoppered graduated test tube, add excess osthole raw material, vortex to disperse, shake in a constant temperature shaking box at 37°C for 48h, and centrifuge at 10,000r / min After 10 minutes, take the supernatant and dilute it with an appropriate amount of absolute ethanol, then measure the solubility of osthole in various auxiliary materials, and the results are shown in Table 1.

[0025] The solubility of table 1 osthole in excipients

[0026]

[0027] As shown in Table 1, osthole has high solubility in ethyl oleate, PGPR, OP, ODO, Labrasol, EL-40, PEG-200, and Transcutol HP, so these excipients are selected for further screening.

[0028] 2. Drawing of ternary phase diagram

[0029] Select the mass ratio (Km value) of surfactant and co-surfactant to be 1:1, 2:1, 3:1, 4:1 respectively, and the mass ratio of o...

Embodiment 2

[0049] Validation of the optimized prescription According to the optimal prescription, the foaming microemulsion was prepared and repeated 3 times. The ratio of the excipients and the test results are shown in Table 4. The results verify that the actual values ​​of each index of the prescription are close to the predicted values, indicating that the D-optimal mixture design has accurate predictability for the ratio of microemulsions.

[0050] Table 4 Comparison of measured value and predicted value of optimized and verified prescription

[0051]

[0052] 1. Characterization of physical and chemical properties of foaming microemulsion

[0053] The microemulsion prepared according to Table 4 was used to characterize its physical and chemical properties such as potential, particle size, polydispersity coefficient, solubility and drug loading.

[0054] Appearance: The Cnidium Fructus Foaming Microemulsion is a clear and transparent liquid with light blue opalescence. Particle...

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Abstract

The invention discloses a cnidium lactone foaming microemulsion with optimal mixed materials and a preparation method thereof, belonging to the technical fields of drugs and drug manufacturing. The cnidium lactone foaming microemulsion contains cnidium lactone and auxiliary materials, wherein the auxiliary materials include ethyl oleate, a mixed surfactant and deionized water; the mixed surfactantcontains polyoxyethylated castor oil 40 and diethylene glycol monoethyl ether; and the ratio of ethyl oleate to polyoxyethylene 40 hydrogenated castor oil to diethylene glycol monoethyl ether to deionized water is 8.13 to 14.81 to 6.58 to 71.44. The cnidium lactone foaming microemulsion has the beneficial effects that the solubility of cnidium lactone in an emulsifying prescription of the cnidiumlactone foaming microemulsion is increased by at least 201 times, so that a solubilizing purpose is achieved, and a certain guiding significance is provided for the later-period one-step preparationformation of the cnidium lactone foaming microemulsion.

Description

technical field [0001] The invention belongs to the technical field of medicine and medicine manufacture, and in particular relates to an optimized osthole foaming microemulsion and a preparation method thereof. Background technique [0002] Vaginitis is a common and frequently-occurring disease in gynecology, and it is a general term for various vaginal mucosal diseases caused by pathogenic microorganism infection. Trichomonal, bacterial, and candidal vaginitis [3] The most common clinical. Osthole is a coumarin compound with anti-inflammatory, anti-pruritic, anti-bacterial, anti-viral, immune-enhancing and anti-allergic effects. It is mainly used for clinical external use. It has a unique effect in the treatment of trichomonal vaginitis and vulvar eczema. curative effect. However, due to the poor water solubility of osthole, there are problems such as low solubility in vivo and poor bioavailability, which limit the clinical application. [0003] The solubilization of p...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K31/37A61K47/14A61K47/44A61K47/10A61P15/02A61P33/02A61P17/00
CPCA61K9/1075A61K31/37A61K47/10A61K47/14A61K47/44
Inventor 杨荣平
Owner SOUTHWEST UNIV
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