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Agomelatine and agomelatine derivative oral patch preparation and preparation method thereof

An oral patch and derivative technology, which is applied in the directions of pill delivery, pharmaceutical formulations, and drug combinations, can solve problems such as unacceptable adverse reactions, and achieve the effects of avoiding liver first-pass effect, reducing tingling, and increasing convenience.

Pending Publication Date: 2022-01-11
SHENZHEN FONCOO PHARMACEUTICAL CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] Among them, the solid sustained-release capsule disclosed in the Chinese patent CN105194514A is still administered orally and absorbed through the gastrointestinal tract, which cannot avoid the high first-pass effect
Transdermal patches are slowly released and absorbed through the skin, which can avoid the first-pass effect. However, gomelatine is a melatonin receptor agonist. If it exists in the body for a long time during the day, it may cause drowsiness and cause adverse reactions. Accept, similarly, long-acting liposomes and long-acting microsphere injections also have the above-mentioned problems
[0009] In summary, there is no agomelatine oral patch yet, but this dosage form has obvious clinical advantages and needs

Method used

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  • Agomelatine and agomelatine derivative oral patch preparation and preparation method thereof
  • Agomelatine and agomelatine derivative oral patch preparation and preparation method thereof
  • Agomelatine and agomelatine derivative oral patch preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0056] See Table 1, prescription for 10,000 tablets:

[0057] Table 1 Prescription 1 Raw Material Ratio

[0058] Prescription amount percentage agomelatine 19.8g 2.2％ Mannitol 372.6g 41.4％ Purulan 190.8g 21.2％ Hydroxypropylmethylcellulose 228.6g 25.4％ Guar Gum 7.2g 0.8％ Oleic acid 16.2g 1.8％ stevioside 19.8g 2.2％ Ethyl cellulose 45g 5％ sunset yellow 0.27g 0.03％

[0059] Preparation steps:

[0060] a. Grinding the agomelatine raw material, the D90 is about 15 μm;

[0061] b. Put hydroxypropyl methylcellulose and guar gum in an emulsification tank, fully swell in advance, and then add agomelatine, mannitol, pullulan, polysorbate and stevioside to the above solution, Start the stirring and shearing device to make a homogeneous suspension solution;

[0062] c. Degas the above solution;

[0063] d. Inject the degassed solution into the mold, put it into a freeze dryer, and pre-freeze at -30°C for 3...

Embodiment 2

[0069] See Table 2, prescription for 10,000 tablets:

[0070] Table 2 Prescription 2 Raw Material Ratio

[0071] Prescription amount percentage agomelatine 19.8g 2.2％ Mannitol 417.6g 46.4％ Purulan 168.3g 18.7％ Hydroxypropylmethylcellulose 206.1g 22.9％ Guar Gum 7.2g 0.8％ Oleic acid 16.2g 1.8％ stevioside 19.8g 2.2％ Ethyl cellulose 45g 5％ sunset yellow 0.27g 0.03％

[0072] Preparation steps:

[0073] a. Grinding the agomelatine bulk drug, the D90 is about 5 μm;

[0074] b. Put hydroxypropyl methylcellulose and guar gum in an emulsification tank, fully swell in advance, and then add agomelatine, mannitol, pullulan, polysorbate and stevioside to the above solution, Start the stirring and shearing device to make a homogeneous suspension solution;

[0075] c. Degas the above solution;

[0076] d. Inject the degassed solution into the mold, put it into a freeze dryer, and pre-freeze at -50°C for 15 mi...

Embodiment 3

[0082] See Table 3, prescription for 10,000 tablets:

[0083] Table 3 Prescription 3 Raw Material Ratio

[0084] Prescription amount percentage agomelatine 19.8g 2.2％ Mannitol 327.6g 36.4％ Purulan 213.3g 23.7％ Hydroxypropylmethylcellulose 251.1g 27.9％ Guar Gum 7.2g 0.8％ Oleic acid 16.2g 1.8％ stevioside 19.8g 2.2％ Ethyl cellulose 45g 5％ sunset yellow 0.27g 0.03％

[0085] Preparation steps:

[0086] a. Grinding the agomelatine bulk drug, the D90 is about 30 μm;

[0087] b. Put hydroxypropyl methylcellulose and guar gum in an emulsification tank, fully swell in advance, and then add agomelatine, mannitol, pullulan, polysorbate and stevioside to the above solution, Start the stirring and shearing device to make a homogeneous suspension solution;

[0088] c. Degas the above solution;

[0089] d. Inject the degassed solution into the mold, put it into a freeze dryer, and pre-freeze at -10°C for 60 m...

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Abstract

The present invention discloses an agomelatine and agomelatine derivative oral patch preparation and the preparation method thereof, the bioavailability of agomelatine is improved through oral mucosa absorption. According to the preparation, through adoption of a vacuum freeze-drying molding method, the patch preparation has certain porosity and hardness, it is guaranteed that the patch preparation can be better attached to oral mucosa for drug release, meanwhile, a high polymer material is added in the preparation process to form inclusion with active substances, the active ingredients can be slowly released, and therefore, a certain concentration of agomelatine in a human body at night is kept, and the agomelatine has the effects of remarkably improving sleep and resisting depression.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to an oral patch preparation of agomelatine and its derivatives and a preparation method thereof. Background technique [0002] Agomelatine is a drug for the treatment of depression in adults. Its original research company is Servier, France, with a specification of 25 mg and a dosage form of tablets. The drug was launched in the EU in 2009 and imported to China in 2011. Dosage of the drug: The recommended dose is 25mg, once a day, orally before bedtime. If the symptoms do not improve after two weeks of treatment, the dose can be increased to 50mg once a day, that is, two 25mg tablets each time, before bedtime. [0003] The drug is rapidly and well absorbed (greater than 80%) when administered orally, but has very little bioavailability (less than 5%) because agomelatine has a significant hepatic first-pass effect. [0004] The original research com...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/36A61K9/22A61K31/165A61K47/38A61K47/36A61K47/42A61K47/26A61K47/10A61K47/18A61P25/24A61P25/20
CPCA61K9/2054A61K9/2063A61K9/205A61K9/2031A61K9/2018A61K9/2013A61K9/2866A61K9/2095A61K9/006A61K31/165A61P25/24A61P25/20
Inventor 汤进黄伟棠张倩立高仁超林萍王磊
Owner SHENZHEN FONCOO PHARMACEUTICAL CO LTD