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Huperzine A slow-release orally disintegrating tablets and preparation method thereof

A technology of huperzine A and orally disintegrating tablets, which is applied in the fields of pharmaceutical formulation, pill delivery, drug delivery, etc., can solve problems such as difficulty in swallowing and poor patient compliance, and achieve the goal of solving inconvenience in swallowing, simple preparation method, and avoiding toxic and side effects Effect

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

[0007] 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.

Method used

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  • Huperzine A slow-release orally disintegrating tablets and preparation method thereof
  • Huperzine A slow-release orally disintegrating tablets and preparation method thereof
  • Huperzine A slow-release orally disintegrating tablets and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] The huperzine A sustained-release microspheres provided in this example are prepared by the following method:

[0043] 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 was prepared; wherein the concentration of the skeleton material ethyl cellulose was 5% w / v, and the concentrations of the skeleton material poloxamer 127 were 0.20% w / v, 0.25% w / v, respectively. %w / v, 0.5%w / v.

[0044] 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 9...

Embodiment 2

[0048] The huperzine A sustained-release microspheres provided in this example are prepared by the following method:

[0049] 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.

[0050] 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.

[0051] Table 2 contains the composition...

Embodiment 3

[0054] The huperzine A sustained-release microspheres provided in this example are prepared by the following method:

[0055] 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.

[0056] 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.

[0057] The prescription composition of table 3 huperzine A sustained-release microspheres

[0058] prescription

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Abstract

The invention relates to huperzine A slow-release orally disintegrating tablets and a preparation method thereof. The huperzine A slow-release orally disintegrating tablets are prepared from huperzineA slow-release microspheres and acceptable auxiliary materials in orally disintegrating tablets. The huperzine A slow-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 the mass ratio being (10-50):1. The huperzine A slow-release orally disintegrating tablets have more ideal slow-release effect, 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 and are expected to be prepared into an oral slow-release preparation taken once a day, the medicine taking times of patients are reduced, and the compliance of patients is improved.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a sustained-release orally disintegrating tablet of huperzine A and a preparation method 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 disease ...

Claims

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Application Information

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IPC IPC(8): A61K9/26A61K47/34A61K47/10A61K31/4748
CPCA61K9/2054A61K9/0056A61K9/2031A61K9/2095A61K31/4748
Inventor 潘昕彭婷婷朱春娥施铟吴传斌
Owner SUN YAT SEN UNIV
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