Methionine folic acid compound preparation and its preparation method and use

A compound preparation, the technology of methamphetamine folic acid, which is applied in anti-inflammatory agents, pill delivery, non-central analgesics, etc., can solve the problems of poor compliance, missed doses, and easy to take by mistake

Active Publication Date: 2017-07-14
CINKATE PHARMA INTERMEDIATES +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

It can be seen that the combination of methotrexate and folic acid has disadvantages such as poor compliance, easy misuse, and missed doses.

Method used

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  • Methionine folic acid compound preparation and its preparation method and use
  • Methionine folic acid compound preparation and its preparation method and use
  • Methionine folic acid compound preparation and its preparation method and use

Examples

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Effect test

preparation example Construction

[0073] Both the methotrexate part and the folic acid part in the methotrexate compound preparation can be made into medicinal pellets. The preparation method of pharmaceutical pellets mainly includes two steps: drug loading and coating. Drug loading is to directly coat the drug micropowder on the surface of the round core particle (also known as drug application) or use different techniques to mix the drug and excipients and directly make round pellets. The methods of drug loading of the present invention mainly include: 1. the method of adding medicine to the core of the pill, and 2. the method of directly forming a pill.

[0074] In the present invention, when adopting the drug-on-ball method to prepare methotrexate pellets and folic acid pellets, the methotrexate pellets include blank pellet cores, drug layers and protective layers sequentially from inside to outside; It includes a blank pellet core, a drug layer, an isolation layer and a functional layer in turn. The bla...

Embodiment 1

[0087] 1.1 Prescription of methotrexate pellets (10000 capsules)

[0088] (0.9-1.12mm) sucrose core 1160.5g

[0089] Methotrexate 36.2g

[0090] PVP S630 27.5g

[0091] HPMC 24.9g

[0092] Water 2049ml

[0093] Preparation process: add 27.5g of PVP S630 and 36.2g of methotrexate to 1500ml of water to make the upper drug solution; add 24.9g of HPMC to 549ml of water to make the protective layer liquid. 1160.5g average particle diameter is 0.9-1.12mm sucrose blank pellet core is placed in the fluidized bed and fluidized for 10 minutes, sprayed with liquid medicine, protective layer liquid successively, obtains methotrexate pellets (medicine liquid and protective layer The liquid is continuously stirred during the whole drug application and coating process). This process adopts the fluidized bed bottom spraying process.

[0094] 1.2 Prescription of folic acid pellets (10000 capsules)

[0095] (0.9-1.12mm) sucrose core 105.3g

[0096] Folic acid 9.1g

[0097] PVP S630 1.8...

Embodiment 2

[0108] 2.1 Prescription of methotrexate pellets (10000 capsules)

[0109] 0.8-1.0mm starch ball core 99.6g

[0110] Methotrexate 21.8g

[0111] PVP VA64 6.8g

[0112] HPC 14.2g

[0113] water 85ml

[0114] Preparation process: add 6.8g of PVP VA640 and 21.8g of methotrexate to 40ml of water to make the upper drug solution; add 14.2g of HPC to 45ml of water to make the protective layer liquid. Put 99.6g of starch blank cores with an average particle size of 0.8-1.0mm in a fluidized bed for 10 minutes, spray the drug solution and the protective layer liquid successively to obtain the methotrexate pellets (the drug solution and the protective layer The liquid is continuously stirred during the whole drug application and coating process). This process adopts the fluidized bed bottom spraying process.

[0115] Same as Example 1.1

[0116] 2.2 Prescription of folic acid pellets (10000 capsules)

[0117] 0.6-0.8mm starch ball core 607.5g

[0118] Folic acid 21.8g

[0119] P...

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Abstract

The invention relates to a methotrexate-folic acid compound preparation and a preparation method and applications thereof. The compound preparation comprises (a) a methotrexate portion and (b) a folic acid portion; wherein the methotrexate portion comprises (a1) methotrexate and (a2) any pharmacologically acceptable carrier or excipient; the folic acid portion comprises (b1) folic acid and (b2) any pharmacologically acceptable carrier or excipient; and the weight ratio of (a1) to (b1) is between 1:1 and 4:1, preferably 2:1. The invention also provides a method for preparing the compound preparation and applications of the compound preparation in treating autoimmune diseases.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to a methionine folic acid compound preparation for treating autoimmune diseases and a preparation method thereof. Background technique [0002] Methotrexate (Methotrexate, MTX) is very similar to the substrate folic acid of dihydrofolate reductase, and its affinity with dihydrofolate reductase is 100,000 times higher than that of dihydrofolate to the enzyme, so it competitively inhibits Dihydrofolate reductase, which prevents the reduction of dihydrofolate to active tetrahydrofolate, depletes the raw materials for synthesis of thymine and purine nucleotides, inhibits the synthesis of DNA and RNA, thereby inhibiting cellular immunity and humoral immunity, and is widely used It is used in the treatment of autoimmune diseases such as rheumatoid arthritis and psoriasis. Unfortunately, the treatment of patients with this drug involves serious side effect...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/519A61K9/20A61K9/48A61P37/00A61P29/00A61P19/02
Inventor 刘丽媛李秋实袁西伦肖飞
Owner CINKATE PHARMA INTERMEDIATES
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