Huperzine A sustained release microspheres as well as preparation method and application thereof

A technology of huperzine A and slow-release microspheres, which is applied in the direction of block delivery, can solve the problems of unsatisfactory release effect, incomplete drug release, poor patient compliance, etc., and achieve excellent compressibility, fluidity and breathability The effect of good resistance and good powder properties

Inactive Publication Date: 2018-06-22
SUN YAT SEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Huperzine A is a low-dose, high-efficiency drug. The commercially available oral preparations are only ordinary tablets and capsules (50 μg / tablet / grain). Both of these two preparations have to be taken multiple times a day, have difficulty swallowing and poor patient compliance.
There are also some reports on huperzine A sustained-release preparations, but the existing disclosed huperzine A sustained-release preparations still have the unsatisfactory defect of release effect, such as relatively serious drug burst release phenomenon, or 24-hour drug release. completely wait

Method used

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  • Huperzine A sustained release microspheres as well as preparation method and application thereof
  • Huperzine A sustained release microspheres as well as preparation method and application thereof
  • Huperzine A sustained release microspheres as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] The huperzine A sustained-release microspheres provided in this example are prepared by the following method:

[0040] According to the composition of the prescription shown in Table 1, a certain amount of huperzine A (theoretical drug loading accounts for 0.4% of the dry weight of the skeleton material), the skeleton material ethylcellulose (EC45) and poloxamer (F127), were dissolved in In 200ml of 80% v / v ethanol aqueous solution, the drug solution is prepared; wherein the concentration of the skeleton material ethylcellulose is 5% w / v, and the concentration of the skeleton material poloxamer is 0.20% w / v and 0.25% respectively w / v, 0.5% w / v.

[0041] The obtained drug solution was uniformly fed into UPPS to prepare huperzine A sustained-release microspheres, and three kinds of huperzine A sustained-release microspheres with different F127 contents were obtained. The instrument parameters used are: liquid supply rate 8ml / min, rotating disc rotation speed 9000rpm, vor...

Embodiment 2

[0045] The huperzine A sustained-release microspheres provided in this example are prepared by the following method:

[0046] According to the prescription composition shown in table 2, a certain amount of huperzine A (theoretical drug loading accounts for 0.2wt%, 0.3wt%, 0.4wt%, 0.5wt% of the dry weight of the skeleton material respectively), the skeleton material ethyl fiber (EC45) and poloxamer 127 (F127), dissolved in 100ml of 80% v / v ethanol aqueous solution, to prepare a drug solution; wherein the concentration of the skeleton material ethylcellulose is 5% w / v, the skeleton material poloxamer The concentration of Loxamer 127 was 0.25% w / v.

[0047] The obtained drug solution was uniformly fed into UPPS to prepare huperzine A sustained-release microspheres, and four kinds of huperzine A sustained-release microspheres with different drug loadings were obtained. Wherein the instrument parameter used is identical with embodiment 1.

[0048] Table 2 contains the composition o...

Embodiment 3

[0051] The huperzine A sustained-release microspheres provided in this example are prepared by the following method:

[0052] According to the composition of the prescription shown in Table 3, a certain amount of huperzine A (theoretical drug loading accounts for 0.4wt% of the dry weight of the framework material) and the framework material are dissolved in 100ml of 80% v / v ethanol aqueous solution to prepare Drug solution; wherein the concentration of framework material A is 5% w / v, and the concentration of framework material B is 0.25% w / v.

[0053] The obtained drug solution was uniformly fed into UPPS to prepare huperzine A sustained-release microspheres, and four kinds of huperzine A sustained-release microspheres with different compositions were obtained. Wherein the instrument parameter used is identical with embodiment 1.

[0054] The prescription composition of table 3 huperzine A sustained-release microspheres

[0055] prescription

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Abstract

The invention relates to huperzine A sustained release microspheres as well as a preparation method and an application thereof. The huperzine A sustained-release microspheres are prepared from huperzine A and raw materials of a framework material, the mass ratio of the huperzine A to the framework material is (0.1-0.6):100, and the framework material comprises ethyl cellulose and poloxamer in themass ratio being (10-50):1. The huperzine A sustained-release microspheres have more ideal sustained-release effects, lower sudden release rate, can stably release in 24 h, can realize the release effect of basically complete release in 24 h, have the accumulated release quantity in 24 h up to 90% or above, so that toxic and side effects caused by sudden drug release or drug concentration fluctuation can be effectively reduced, and the utilization rate and bioavailability of the drug can be effectively improved.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical preparations, in particular to a huperzine A sustained-release microsphere and a preparation method and application thereof. Background technique [0002] Since the oral sustained and controlled release preparations were launched in the 1870s, the variety and quantity have increased year by year, and now they have occupied an important market share, because the sustained and controlled release preparations have the following advantages: (1) Compared with ordinary preparations, sustained and controlled release preparations It has the advantages of precisely regulating the drug release behavior, reducing the number of administrations, maintaining stable blood drug concentration, reducing side effects, and improving the safety of clinical medication, which is also consistent with the needs of modern drug treatment concepts; (2) Cardiovascular disease and mental disease It has become a major di...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K47/38A61K47/10A61K31/4748
CPCA61K9/1641A61K9/1652A61K9/1682A61K31/4748
Inventor 潘昕彭婷婷朱春娥施铟吴传斌
Owner SUN YAT SEN UNIV
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