Multilayer pharmaceutically active compound release microparticles in liquid dosage form

A technology for liquid compositions and compounds, applied in the directions of drug combination, drug delivery, organic active ingredients, etc., can solve the problems of time instability, unpleasant taste, unpleasant palatability, etc.

Active Publication Date: 2022-01-04
比利时法贝尔制造股份有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there is a risk that the microparticles are chewed prior to swallowing, leading to potential degradation of the PHA in the acidic gastric environment once ingested (e.g. acid-labile PHA) and thus a lack of control over the administered dose
Other disadvantages of dispersing the microparticles in a liquid carrier prior to ingestion are: handling errors due to repeated handling of the dosage form (e.g. improper dispersion, loss of fractions of the microparticles); Possible unpleasant taste (in the case of chewable microparticles) and unpleasant palatability, which lead to rejection or inappropriate dosage by patients, especially young patients
Furthermore, such coatings will still function as an enteric coating layer and thus should be unstable over time in liquid formulations with a pH above 6

Method used

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  • Multilayer pharmaceutically active compound release microparticles in liquid dosage form
  • Multilayer pharmaceutically active compound release microparticles in liquid dosage form
  • Multilayer pharmaceutically active compound release microparticles in liquid dosage form

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0201] Example 1: Development of 5-layer coated microparticles according to the invention

[0202] 500g of 1000 poured into the fluidized bed unit.

[0203] The first layer contains: Omeprazole (as model drug, pharmaceutically active compound according to the present invention), ascorbyl palmitate (as antioxidant), PVP (as binder), talc (as bulk agent) )). Disperse the material in ethanol. Therefore, the coating has the first layer of Corresponds to a core comprising a pharmaceutically active compound according to the invention.

[0204] The purpose of the second layer is to combine drugs with L-shaped membrane polymer isolation. This layer contains: PVP (as both release and binding polymer), titanium dioxide (as opacifying agent) and talc (as extender). Disperse the material in ethanol. This second layer corresponds to the protective intermediate coating layer according to the invention.

[0205] The third layer is the effective layer that provides the final relea...

Embodiment 2

[0218] Example 2: Composition suitable for preparing the outermost outer layer according to the invention

[0219] To test the barrier properties of the outermost outer layer composition, omeprazole-containing microparticles were prepared on which different compositions comprising gastrosoluble polymers and hydrophobic agents were deposited.

[0220] Microparticles were prepared as follows: In the first step, 500 g 1000 (microcrystalline cellulose pellets) were poured into a fluidized bed coater (Aeromatic, STREA-1 TM ; Laboratory scale), and spray the solution / suspension (in ethanol) containing omeprazole, PVP, ascorbyl palmitate with a flow rate of 8g / min with a peristaltic pump. The outermost outer layer is then deposited by spraying a solution comprising: E (polycationic gastrosoluble polymer (a) according to the present invention), and ethyl cellulose, RS, stearic acid, 888 One of ATO, magnesium stearate or GMS (glyceryl monostearate) (as hydrophobic and / or insolu...

Embodiment 3

[0238] Example 3: with a GMS and Omeprazole-containing multilayer microparticles of the outermost outer layer of E (Formulation 3 and Form 4)

[0239] Two batches of multilayer microparticles (dosage form 3 and dosage form 4) containing omeprazole were prepared, and the multilayer microparticle coatings were coated with the The outermost outer layer of E and GMS. The samples differ in that in sample formulation 4 there is direct deposition on the microcrystalline cellulose pellets An additional layer of ethylcellulose on the surface to further help limit the diffusion of water from the surrounding aqueous medium to the core of the microparticles.

[0240] preparation:

[0241] The preparation of the core and layer 1 of dosage form 3 was the same as the preparation of the core and the first layer according to example 2 and as described in the coating parameters of materials and methods. In fact, the 500g of 1000 into a fluidized bed apparatus (Aeromatic, Switzerland). ...

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Abstract

The present invention relates to controlled release multilayer microparticles comprising a pharmaceutically active compound intended for oral administration in the form of a liquid pharmaceutical composition or directly into the stomach. The present invention also relates to liquid pharmaceutical compositions comprising said microparticles, kits for preparing said liquid pharmaceutical compositions, pharmaceutical solid compositions intended to be reconstituted in the form of said liquid compositions, and said liquid compositions preparation method.

Description

technical field [0001] The invention belongs to the technical field of controlled-release compositions of pharmaceutically active compounds. In particular, the present invention relates to multilayered pharmaceutically active compound releasing microparticles in liquid pharmaceutical compositions. Background technique [0002] Oral administration of pharmaceutically active compounds improves the quality of life of patients, including by improving the convenience of administration and by simultaneously increasing patient compliance and cost-effectiveness. The flexibility to design a multitude of different pharmaceutical compositions further makes oral administration attractive for formulating a wide variety of active ingredients. [0003] When the bulk of the pharmaceutically active compound is released from the pharmaceutical composition in the gut (ie, the proximal or distal intestinal region), the bulk of the pharmaceutically active compound can achieve maximal pharmacolo...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/50A61K31/00
CPCA61K31/18A61K31/196A61K31/4439A61K31/58A61K31/635A61K9/5073A61P1/04A61K9/0053A61K9/5026A61K9/5036A61K45/06A61K9/08A61K9/5015A61K9/5031A61K9/5042
Inventor 费德丽卡·龙基乔纳森·古尔卡里姆·阿米基乔治斯·纪尧姆文森特·斯蒂芬尼
Owner 比利时法贝尔制造股份有限公司
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