Lurasidone self-microemulsion composition and preparation method thereof
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A technology of lurasidone and its composition, which is applied in the field of lurasidone self-microemulsion composition and its preparation, can solve the problems of poor water solubility, low solubility, and low oral bioavailability, and achieve high solubility and drug loading The effect of increasing the amount and improving bioavailability
Active Publication Date: 2022-04-19
HUNAN HUIZE BIO PHARMA CO LTD
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[0007] In order to solve the problems of poor water solubility and low solubility of lurasidone hydrochloride in the prior art, resulting in low oral bioavailability, the present invention uses lurasidone free base as the raw material drug to prepare lurasidone self-microemulsion combination Improve the solubility of fat-soluble excipients, increase the drug loading capacity of self-microemulsion carriers, reduce gastrointestinal irritation and other side effects
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Embodiment 1
[0038] Lurasidone 20mg
[0039] Caprylic Capric Mono-Diglyceride 400mg
[0040] Tween 80400mg
[0041] Propylene glycol 200mg
[0042] Preparation Process:
[0043] Add lurasidone into caprylic capric acid mono-diglyceride, then add Tween 80 and propylene glycol in turn, stir to mix evenly and then dissolve.
[0044] Particle size: about 500nm.
Embodiment 2
[0046] Lurasidone 20mg
[0047] Glyceryl monocaprylate 200mg
[0048] Polyoxyl 35 castor oil 600mg
[0049] Diethylene glycol monoethyl ether 200mg
[0050] Preparation Process:
[0051] Add lurasidone into glyceryl monocaprylate, then add polyoxyethylene 35 castor oil and diethylene glycol monoethyl ether in turn, stir to mix evenly and then dissolve.
[0052] Particle size: about 15nm.
Embodiment 3
[0054] Lurasidone 20mg
[0055] Glyceryl monocaprylate 165mg
[0056] Oleic acid 165mg
[0057] Polyoxyl 35 castor oil 440mg
[0058] Propylene glycol 230mg
[0059] Preparation Process:
[0060] Add lurasidone into the mixed oil phase of glyceryl monocaprylate and oleic acid, then add polyoxyethylene 35 castor oil and propylene glycol in sequence, stir to mix evenly, and then dissolve.
[0061] Particle size: about 250nm.
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Abstract
The invention belongs to the technical field of medicine, and specifically discloses a lurasidone self-microemulsion composition and a preparation method thereof. In parts by weight, 0.1 to 20 parts of lurasidone, 5 to 70 parts of an oil phase, and an emulsifier 10-70 parts, and 0-50 parts of co-emulsifier; when the self-microemulsion composition of lurasidone contacts with an aqueous medium, it forms and releases a microemulsion. The present invention adopts lurasidone free base as raw material drug, prepares lurasidone self-microemulsion composition, improves the solubility of fat-soluble excipients, improves the drug loading capacity of self-microemulsion carrier, and reduces gastrointestinal irritation and other side effects .
Description
technical field [0001] The invention relates to the technical field of medicine, in particular to a lurasidone self-microemulsion composition and a preparation method thereof. Background technique [0002] Lurasidone hydrochloride (Lurasidone hydrochloride, LH) belongs to atypical antipsychotic drugs. In October 2010, the U.S. FDA approved the listing of lurasidone hydrochloride tablets from Sumitomo Pharmaceutical Co., Ltd., Japan. The trade name is Latuda, and the recommended starting dose is 40mg / d, the maximum recommended dose is 80mg / d; lurasidone should be taken with food at the same time, it is suitable for the first-line treatment of patients with schizophrenia. In clinical preparations, lurasidone mainly exists in the form of its hydrochloride, lurasidone hydrochloride is a BCSII drug with poor solubility, and its oral bioavailability after meal administration in adults is only 9-19%. And the solubility of LH is also pH-dependent, with a maximum solubility at pH 3....
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