Retigabine micro pellet capsule and preparation method thereof

A technology of retigabine and retigabine pellets, applied in capsule delivery, pharmaceutical formulation, drug delivery, etc., can solve the problems of slow dissolution, drug waste, drug side effects, etc., reduce taste, increase stability, and reduce particle size The effect of uniform diameter

Inactive Publication Date: 2014-12-10
WATERSTONE PHARMA WUHAN
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] However, because retigabine is an insoluble drug, the oral bioavailability is only 60%, which not only causes waste of medicine but also causes many side effects when taking medicine in large doses
On the other hand, experimental studies have found that the existing formulations of retigabine have slow dissolution during long-term storage
[0005] Therefore, the current drug formulation of retigabine still needs to be improved

Method used

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  • Retigabine micro pellet capsule and preparation method thereof
  • Retigabine micro pellet capsule and preparation method thereof
  • Retigabine micro pellet capsule and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0072] Embodiment 1 prepares retigabine micropill capsule

[0073] Retigabine 500g

[0074] Microcrystalline Cellulose Core 222g

[0075] Hypromellose E5 52g

[0076] Croscarmellose Sodium 16g

[0077] Opadry 03F 24g

[0078] Crushing of the raw material drug: the retigabine raw material was pulverized with a GTM-50 jet mill until its D90=6 μm; drug-loaded layer suspension preparation: measure 1100ml of water, dissolve hypromellose in it, and then add The crushed retigabine raw material and croscarmellose sodium in the prescribed amount were stirred until uniformly dispersed, and passed through an 80-mesh sieve to obtain a suspension of the drug-loaded layer; The parameters are as follows: air volume 100m 3 / h, liquid supply speed 8g / min, atomization pressure 1.7bar, air inlet temperature 50°C, material temperature 40°C, spacer height 10cm; fluidized bed drying for 20min after the drug application, the parameters are as follows: air volume 90m 3 / h, liquid supply rate 0g...

Embodiment 2

[0085] Embodiment 2 prepares retigabine micropill capsule

[0086] Retigabine 500g

[0087] Sucrose core 100g

[0088] Hydroxypropyl Cellulose EF 100g

[0089] Low-substituted hydroxypropyl cellulose 32g

[0090] Opadry II 40g

[0091] Grinding of raw materials: Grinding the retigabine raw material with a KEQ-2L ball mill until its D90=20 μm; preparation of drug-loaded layer suspension: measure 2000ml of water, dissolve hydroxypropyl cellulose in it, and then add the prescribed amount The pulverized retigabine raw material and croscarmellose sodium were stirred until uniformly dispersed, and passed through an 80-mesh sieve to obtain a drug-loaded layer suspension; LZW-300 centrifugal granulation coating machine was used for drug application, and the parameters As follows: air volume 60m 3 / h, liquid supply rate 10g / min, atomization pressure 1.8bar, air inlet temperature 55°C, material temperature 40°C, turntable speed 20r / min; oven dry at 60°C for 2h after drug applicatio...

Embodiment 3

[0092] Embodiment 3 prepares retigabine micropill capsule

[0093] Retigabine 500g

[0094] Lactose core 400g

[0095] Povidone K30 50g

[0096] Sodium carboxymethyl starch 8g

[0097] Talc powder 9g

[0098] Opadry 03K 48g

[0099] Grinding of the raw material: Grinding the retigabine raw material with a jet mill until its D90=11 μm; preparation of the adhesive: taking 1000ml of water, dissolving povidone K30 in it, stirring until uniformly dispersed, passing through an 80-mesh sieve That is ready; mix: mix the retigabine raw material and carboxymethyl starch sodium after the prescription amount is pulverized evenly; apply the medicine with LZW-300 centrifugal granulation coating machine, the parameters are as follows: air volume 50m 3 / h, liquid supply speed 10g / min, atomization pressure 1.6bar, air inlet temperature 55°C, material temperature 40°C, turntable speed 20r / min, feed hopper speed 6r / min; fluidized bed drying for 20min after drug application; Preparation of ...

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Abstract

The invention relates to a retigabine micro pellet capsule and a preparation method thereof. The pellet capsule is filled with retigabine micro pellets, wherein the retigabine micro pellet comprises 16 to 44 parts by weight of empty core, a medicine layer, and 2 to 8 parts by weight of coating layer, wherein the medicine layer comprises 49 to 74 parts by weight of micronized retigabine, 2 to 16 parts by weight of adhesive, and 0.5 to 8 parts by weight of disintegrating agent. According to the retigabine micro pellet capsule, the retigabine micro pellet, serving as the content of the retigabine micro pellet capsule, has a circular appearance and is uniform in particle size, and therefore, the oral bioavailability of retigabine can be improved; meanwhile, the problem that a solid retigabine preparation becomes slow to dissolve in vitro in long-term storage can be solved, the stability of retigabine can be improved, and the generation of relevant substances can be reduced.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular, the invention relates to a retigabine pellet capsule and a preparation method thereof. Background technique [0002] Retigabine (Retigabine, trade name Potiga) chemical name N-[2-amino-4-(4-fluorobenzylamino) phenyl] ethyl carbamate, is an adjuvant treatment drug for partial seizures in adults , was approved by the US FDA on June 10, 2011, and the listed dosage form is a tablet. [0003] [0004] However, because retigabine is a poorly soluble drug, its oral bioavailability is only 60%, which not only causes waste of drugs but also causes many side effects when taking drugs in large doses. On the other hand, experimental studies have found that the existing formulations of retigabine have a slow dissolution phenomenon during long-term storage. [0005] Therefore, the current drug formulation of retigabine still needs to be improved. Contents of the invention [00...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/48A61K9/52A61K31/27A61P25/08A61J3/07
Inventor 周晓星刘大鹏钱丽娜金晶程稳王珍项斌
Owner WATERSTONE PHARMA WUHAN
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