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A kind of huperzine A osmotic pump sustained-release pellet capsule and preparation method

A technology of slow-release pellets and huperzine A, which is applied in the direction of microcapsules, capsule delivery, and pharmaceutical formulations, can solve the problems of inconvenient medication, pain, and unfavorable mass production for patients, so as to avoid excessive drug concentration and reduce occurrence rate and degree, and the effect of reducing peak and valley fluctuations

Active Publication Date: 2021-01-08
ZHEJIANG ACAD OF MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Existing huperzine A preparation has following defects: (1) injection has avoided gastrointestinal adverse reaction, but needs regular injection administration, and patient's medication inconvenience, pain; (3) The patch preparation process is complex and the quality stability is difficult to control, which is not conducive to large-scale production
[0004] After searching, there is currently no patent application or literature report on huperzine A osmotic pump sustained-release pellets

Method used

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  • A kind of huperzine A osmotic pump sustained-release pellet capsule and preparation method
  • A kind of huperzine A osmotic pump sustained-release pellet capsule and preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] Embodiment 1: Preparation of huperzine A osmotic pump core

[0023] Huperzine A 350mg

[0024] Sucrose 140g

[0025] Lactose 700g

[0026] Sodium chloride 70g

[0027] The drug pellets of the above prescription were prepared by extrusion spheronization, and the specific operations were as follows: Weighed the prescription amount of huperzine A, added 1.6ml 1mol / L hydrochloric acid and stirred to dissolve, then added water to 175ml, and mixed well to obtain 2mg / ml huperzine A solution, add sucrose and stir evenly to obtain a sucrose solution. Weigh the prescription amount of lactose and sodium chloride respectively, mix well, add sucrose solution to make soft material, extrude with 16-mesh extruder, spheronize on the spheronizer at 40r / min for 30min (55°C), granulate (the screen is 24-30 mesh), the yield of the core of the osmotic pump pellets must not be less than 85%.

Embodiment 2

[0028] Embodiment 2: the influence of sucrose dosage on the quality of ball core

[0029] Weigh 100 g of lactose and 10 g of sodium chloride, mix them evenly with an 80-mesh sieve, and add 20 ml, 25 ml, and 30 ml of sucrose aqueous solution with a concentration of 0.8 mg / ml in triplicate to make soft materials, and extrude them with a 16-mesh extruder. The spheronizer was spheronized at 40r / min for 30min (55°C), sieved and sized, and the particle size, particle size distribution, bulk density, angle of repose and friability were measured respectively.

[0030] The results are shown in table 1. When the amount of sucrose was 20ml (16g), the extrudate was relatively dry, and the particle size of the ball core was mainly distributed in the area of ​​smaller particle size; when the amount of binder was 30ml (24g) , the particle size of the ball core is mainly distributed in the area of ​​larger particle size, and the angle of repose of the ball core increases, and the roundness de...

Embodiment 3

[0033] Example 3: Optimization of preparation process of huperzine A osmotic pump core

[0034] (1) Inspection of rolling speed

[0035] Weigh lactose 100 and sodium chloride 10g respectively, 80 mesh sieve and mix evenly, in triplicate, add the sucrose aqueous solution 25ml that concentration is 0.8mg / ml to make soft material, extrude with 16 mesh extruder, granulate (screen mesh is 24-30 mesh), were spheronized at 30r / min, 40r / min, 50r / min for 30min (55°C), and the particle size, particle size distribution, bulk density, angle of repose and friability were measured respectively.

[0036] The results are shown in Table 2. When the spheronization speed is controlled at 40r / min, the yield of pellets with a particle size of 24-30 mesh is significantly higher than that of 30r / min and 50r / min, and there is no significant difference in other parameters.

[0037] Table 2: The effect of spheronization speed on the quality of pellet core

[0038] Rolling speed (r.min -1 )...

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Abstract

The invention discloses a huperzine a osmotic pump sustained release pellet capsule and a preparation method. The huperzine a osmotic pump sustained release pellet capsule comprises a capsule shell and osmotic pump sustained release pellets in the shell, wherein the osmotic pump sustained release pellets are prepared from osmotic pump pellet cores and sustained release coating layers; each osmoticpump pellet core is prepared from 50mu g huperzine a, 100mg of lactose, 20mg of cane sugar and 10mg of sodium chloride; in a coating layer, ethyl cellulose accounts for 50 to 70 percent by weight ofeach osmotic pump pellet core; the PEG (Polyethylene Glycol)-400 accounts for 5 to 15 percent by weight of the ethyl cellulose, dibutyl phthalate accounts for 20 percent by weight of the ethyl cellulose. Through adoption of the preparation method, the huperzine a osmotic pump sustained release pellet capsule preparation is prepared by combining extrusion-spheronization and a fluidized bed technology, can release medicament continuously within 12 hours, peak valley fluctuation of medicament concentration in blood is lowered; incidence rate and degree of side effects are lowered; the aim of administrating medicament one time every day is fulfilled, and the compliance of patients is enhanced.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical preparations, in particular to a huperzine A osmotic pump sustained-release pellet capsule and a preparation method thereof. Background technique [0002] Huperize A (Hup-A) is a class of lycopodium alkaloids extracted and isolated from the perennial fern Huperzia serrata. It is one of the few drugs first discovered by Chinese scientists and is considered It is a promising new-generation reversible acetylcholinesterase inhibitor for the clinical treatment of Alzheimer's disease (AD), which has aroused strong interest of international and domestic pharmaceutical scientists. Studies have shown that compared with other drugs currently developed for the treatment of AD, Hup-A has a unique chemical structure, high oral bioavailability, easy passage through the blood-brain barrier, multi-target effects, long acting time, and multiple administrations. The drug has the characteristics of no tolera...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/50A61K9/52A61K47/38A61K47/10A61K47/14A61K47/26A61K31/4748A61P25/28
Inventor 尹丽娜张雅雯赵鹏飞王胜浩
Owner ZHEJIANG ACAD OF MEDICAL SCI