Process for making multiparticulate gastroretentive dosage forms

A technology of multi-particles and granules, which is applied in the direction of medical preparations containing active ingredients, pill delivery, pharmaceutical formulations, etc., and can solve problems such as inability to mix or obtain super-granular pastes

Inactive Publication Date: 2013-09-18
MELIATYS
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, this method requires constrained manufacturing conditions and ultragranulated pastes remain difficult to mold into suitable dosage forms prior to the drying step
In fact, it may not be possible to incorporate the amount of water necessary to obtain a suitably low density, resulting in a supergranulated paste
Therefore, prior art methods have flaws in their implementation

Method used

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  • Process for making multiparticulate gastroretentive dosage forms
  • Process for making multiparticulate gastroretentive dosage forms
  • Process for making multiparticulate gastroretentive dosage forms

Examples

Experimental program
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Effect test

Embodiment 1

[0110] Embodiment 1: the preparation of multiparticulate oral gastric retention dosage form of the present invention

[0111] The multiparticulate oral gastroretentive dosage form of the present invention can be prepared according to the following method, but not limited to the following examples.

[0112] In one aspect, a powder made of 55g of acetaminophen (active ingredient) together with 40g of HPMC and about 5g of PVPK30 was loaded into a planetary mixer and blended at 150rpm during 2min30sec. On the other hand, a granulation suspension was prepared by dissolving about 10 g of PVP K30 in 200 ml of an aqueous solution containing 15 g of Aerosil R972. The suspension was prepared by using an Ultra turax mixer.

[0113]Granulation was started at 100 rpm by adding the suspension to the powder at a rate of 10 ml / min. Granules were obtained after adding about 130 ml of the solution to the powder. The resulting granules are then dried in a ventilated oven at about 50°C until t...

Embodiment 2

[0115] Embodiment 2: buoyancy

[0116] Five different types of granules of the following composition (based on the weight of the total composition) were tested for buoyancy. Types 1, 4 and 5 were prepared using a hydrophobic excipient (Aerosil R972), while types 2 and 4 were prepared using a hydrophilic excipient (Aerosil 200). The results are shown in the table below.

[0117]

[0118] The results thus show that the buoyant properties of the particles cannot be attributed to the mere presence of the swelling agent (ie HPMC or MCC), as the dosage forms comprising hydrophilic materials do not buoyant. Thus, the use of hydrophobic materials results in an inherently low density of particles.

[0119] Furthermore, it appears that the use of HPMC produces dosage forms with lower densities than those prepared using MCC.

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Abstract

The instant: invention relates to a process for making inherent Sow density particles., comprising the steps of (i) providing a powder mixture comprising a swelling agent; (ii) granulating the powder of step (i) with a granulating solution comprising a lipophilie agent into granules and (iii) drying the granules of step (ii). The instant invention further relates to multiparticulate oral gastro-retentive dosage forms comprising the inherent low density particles: obtainable by the process.

Description

field of invention [0001] The present invention relates to novel pharmaceutical compositions which are retained in the stomach or upper gastrointestinal tract for controlled delivery of drugs. The invention also provides methods for the preparation of these dosage forms and their use in therapy. Background of the invention [0002] Judging the efficacy of a therapeutic agent is closely related to its method of administration. When ingested orally, drugs interact with specific absorption sites located throughout different parts of the gastrointestinal tract (GI), resulting in some active agents being absorbed only in the stomach, upper or lower gut. Therefore, because the drug is not absorbed uniformly throughout the length of the GI tract, the rate of absorption may not be constant and the treatment may not be most effective. These problems can be significantly ameliorated when the method of administration provides controlled delivery of the active ingredient only to the s...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K9/16A61K9/20
CPCA61K9/0065A61K9/1611A61K9/1635A61K9/1652A61K9/2009A61K9/2027A61K9/2054A61K9/16A61K9/1694A61K31/167
Inventor J·S·M·基尔科里安
Owner MELIATYS
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