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Pharmaceutical formulation with high stability and dissolution and manufacturing process

A technology of pharmaceutical dosage form and high stability, applied in the field of preparing the pharmaceutical dosage form, can solve problems such as poor solubility

Active Publication Date: 2008-08-06
基因制药公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0017] Therefore, the present invention has been made in consideration of the above-mentioned problems, and an object of the present invention is to provide a pharmaceutical dosage form having a crystalline form to solve the problems caused by its low melting point and possible degradation under storage conditions, And conversely, the problem of poor solubility caused by its crystallinity can be solved

Method used

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  • Pharmaceutical formulation with high stability and dissolution and manufacturing process

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0043] Heat 10 grams of polyethylene glycol 400, 10 grams of polyoxyethylene castor oil (Cremophor (Kremophor)), 10 grams of polysorbate and 5 grams of tocopherol acetate (tocopherolacetate) to 40-60 ° C, and then To this was added 120 grams of orlistat. The mixture was uniformly stirred to prepare a pale yellow transparent liquid dosage form. This liquid state transforms into an opaque solidified state at room temperature.

[0044] A portion is used for liquid stability testing. Other fractions are adsorbed to an adsorbent, to which excipients are then added. The obtained mixture was compressed to prepare tablets, followed by film coating (wrapping) to obtain 800 tablet samples.

[0045] 1) Cool a liquid sample to form a solidified mass. The solidified mass has a uniform shape and composition, and exhibits no phase separation and reagglomeration. A series of storage at low temperature (4°C) and high temperature (40°C) was repeated several times, after which a dissolution...

Embodiment 2

[0052] 10 grams of polyoxyethylene castor oil (Cremophor) was heated to 40-60° C. to obtain a clear liquid, and then 10 grams of polysorbate was added thereto while stirring gently. 120 grams of orlistat was added to the mixture and stirred evenly to form a pale yellow transparent liquid dosage form. This liquid state transforms into an opaque solidified state at room temperature.

[0053] A part was used to observe the state of the liquid, while the other part was absorbed to prepare tablets, followed by coating to obtain 800 tablet samples.

[0054] 1) Phase separation and re-agglomeration were not observed in liquid samples. Following the procedure of Example 1, a series of storage at low temperature and high temperature was repeated several times, after which a dissolution test was carried out. As a result, a dissolution rate of about 59% was obtained. These observations indirectly suggest that the solvent chosen in the present invention is suitable and necessarily maxi...

Embodiment 3

[0057] When mixing 10 grams of polyethylene glycol, 10 grams of polysorbate and 5 grams of tocopheryl acetate while heating to obtain a clear liquid, 120 grams of orlistat were added to the mixture. The obtained mixture was uniformly stirred to prepare a pale yellow transparent liquid dosage form. This liquid state transforms into an opaque semi-solidified state at room temperature.

[0058] Following the procedure of Example 1, certain fractions were isolated, rapidly absorbed, and then compressed to prepare tablets.

[0059] 1) During solidification, phase separation, reagglomeration and recrystallization of separated liquid samples were observed. Following the procedure of Example 1, a series of storage at low and high temperatures was repeated several times, after which a dissolution test was performed. As a result, a dissolution rate of about 23% was obtained. These observations suggest that solubilizers are an indispensable component for stable dissolution of dosage f...

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Abstract

Disclosed herein is a pharmaceutical dosage form with high stability and dissolution rate, and a method for preparing the pharmaceutical dosage form. The pharmaceutical dosage form comprises pharmacologically active substances, solvents, solubilizers, surfactants, antioxidants, and adsorbents. According to the pharmaceutical dosage form and the method, the pharmacologically active substance is mixed with solvents, solubilizers and surfactants for improving the solubility of the pharmacologically active substance to obtain an amorphous liquid or semi-solid state, together with the mixture Antioxidants are melted to address the poor chemical stability of pharmacologically active substances in amorphous or liquid states, and the adsorbent is strongly adsorbed to the molten mixture to be converted into a powder form, so that the obtained molecules are reconstituted within the adsorbent very small crystal form to ensure chemical stability.

Description

technical field [0001] The present invention relates to a pharmaceutical formulation (pharmaceutical formulation) having high stability and dissolution, and a method for preparing the pharmaceutical formulation. More specifically, the present invention relates to a pharmaceutical dosage form comprising a pharmacological (science) active substance, a solvent, a solubilizer, a surfactant, an antioxidant and an adsorbent (absorbent, adsorbent), wherein the pharmacologically active substance Mix with solvents, solubilizers and surfactants to improve the solubility (solubility) of pharmacologically active substances to obtain an amorphous liquid or semi-solid state, and melt the antioxidant with the mixture to solve the pharmacologically active substances in the absence of Poor chemical stability of the fixed or liquid state, and the strong adsorption of the adsorbent to the molten mixture (molten mixture) to be converted into a powder form, so that the obtained molecules are recon...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/44
CPCA61K9/2095A61K9/143A61K9/145A61P43/00A61K31/337A61K47/44
Inventor 文柱明李儇娥
Owner 基因制药公司
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