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A pharmaceutical composition containing levocarnitine and its preparation method and application

A composition and drug technology, applied in the field of pharmaceutical preparations, can solve the problems of short ocular residence time, low bioavailability, and poor patient tolerance, and achieve the goal of avoiding blurred vision, high bioavailability, and high drug concentration Effect

Active Publication Date: 2022-02-08
BEIJING UNIV OF CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] Aiming at the problems of short ocular residence time, large loss, low bioavailability, and poor tolerance of patients in existing topical (ophthalmic) pharmaceutical preparations for the prevention and / or treatment of dry eye, the present invention provides A pharmaceutical composition containing levocarnitine and its corresponding preparation method and medical application

Method used

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  • A pharmaceutical composition containing levocarnitine and its preparation method and application
  • A pharmaceutical composition containing levocarnitine and its preparation method and application
  • A pharmaceutical composition containing levocarnitine and its preparation method and application

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preparation example Construction

[0076] Secondly, the present invention provides a preparation method of the above-mentioned pharmaceutical composition containing levocarnitine. The preparation method comprises the following steps:

[0077] 1) Prepare an aqueous tackifier solution: add the tackifier to a part of pharmaceutical water, disperse, swell and dissolve it at room temperature to obtain an aqueous tackifier solution;

[0078] 2) Prepare a blank thermosensitive in-situ gel: add the gel matrix to the thickener aqueous solution obtained in step 1), stir evenly, and place it at 4°C for more than 24 hours to obtain a blank thermosensitive in-situ gel;

[0079] 3) Preparation of the drug-loaded thermosensitive in situ gel: add levocarnitine to the blank thermosensitive in situ gel obtained in step 2), place it at room temperature, add another part of pharmaceutical water to the full amount, and stir evenly to obtain the drug-loaded thermosensitive in situ gel The bit gel is a pharmaceutical composition con...

Embodiment 1

[0086] Example 1: Preparation of a pharmaceutical composition (LC thermosensitive in situ gel formulation) containing levocarnitine.

[0087] Weigh 0.1g HA-Na and 0.3g CMC-Na, add them into 600mL purified water, disperse, swell and dissolve HA-Na and CMC-Na at room temperature to obtain an aqueous solution of tackifier. Add 0.1g of P407 and 0.2g of P188 to the above-mentioned thickener aqueous solution, stir evenly, put it in a refrigerator at 4°C for more than 24 hours, and obtain a clear and uniformly dispersed blank temperature-sensitive in-situ gel. Add 10g of levocarnitine (LC) to the above blank thermosensitive in situ gel, place it at room temperature, add 400mL of purified water to the full amount (1L), stir evenly, and dissolve levocarnitine to obtain LC thermosensitive in situ gel. Gum (ie pharmaceutical composition comprising levocarnitine).

Embodiment 2

[0088] Example 2: Preparation of a pharmaceutical composition (LC thermosensitive in situ gel formulation) containing levocarnitine.

[0089] Weigh 2.6g of HA-Na and 10.4g of CMC-Na, add them into 800mL of purified water, disperse, swell and dissolve HA-Na and CMC-Na at room temperature to obtain an aqueous thickener solution. Add 300g of P407 and 150g of P188 to the above-mentioned thickener aqueous solution, stir evenly, put it in a refrigerator at 4°C for more than 24 hours, and obtain a clear and uniformly dispersed blank temperature-sensitive in-situ gel. Add 10g of levocarnitine (LC) to the above blank thermosensitive in situ gel, place it at room temperature, add 200mL of purified water to the full amount (1L), stir evenly, and dissolve levocarnitine to obtain LC thermosensitive in situ gel. Gum (ie pharmaceutical composition comprising levocarnitine).

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Abstract

The invention belongs to the technical field of pharmaceutical preparations, and relates to a pharmaceutical composition containing levocarnitine, a corresponding preparation method and a medical application thereof. Specifically, the pharmaceutical composition of the present invention comprises levocarnitine, a gel matrix, a thickener and pharmaceutical water, and is a temperature-sensitive in-situ gel preparation. Compared with common ophthalmic preparations, the temperature-sensitive in-situ gel preparation of the present invention has the following characteristics: 1) it has a hydrophilic three-dimensional network structure and good tissue compatibility; 2) it has strong affinity with mucosal tissues, Long residence time, high local drug concentration, high bioavailability, etc.; 3) It can avoid the "blurry phenomenon" produced by ordinary oily eye ointments, and reduce the irritation to the eyes; 4) It is simple to prepare and easy to use, greatly increasing the 5) The dosage of the drug can be accurately controlled, and the slow and controlled release effect of the medicinal active ingredient can be achieved.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and relates to a pharmaceutical composition containing levocarnitine, a corresponding preparation method and a medical application thereof. Background technique [0002] Dry Eye Disease, also known as Keratoconjunctivitis Sicca, refers to abnormal tear quality or quantity or abnormal dynamics caused by any reason, which leads to a decrease in the stability of the tear film, accompanied by ocular Common symptoms include dry eyes, easy fatigue, itchy eyes, foreign body sensation, burning sensation, sticky secretions, fear of wind, photophobia, Sensitivity to external stimuli, etc.; in severe cases, the eyes will be red and swollen, hyperemic, keratinized, corneal epithelium is broken and filaments adhere, and over time it can cause keratoconjunctival lesions and affect vision. In addition, the osmotic pressure of tears in patients with dry eye disease was significantly increase...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/06A61K47/10A61K47/32A61K47/34A61K47/38A61K47/36A61K31/205A61P27/02
CPCA61K47/10A61K47/32A61K47/34A61K47/36A61K47/38A61P27/02A61K9/0048A61K9/06A61K31/205
Inventor 曲昌海倪健黄平情尹兴斌董晓旭赛那吴慧敏
Owner BEIJING UNIV OF CHINESE MEDICINE