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Isoniazid lipid derivate and compositions thereof

A lipid derivative, isoniazid technology, applied in the fields of chemistry and biomedicine, can solve the problems of low encapsulation rate, poor stability, easy leakage of drugs, etc.

Inactive Publication Date: 2010-03-31
INST OF RADIATION MEDICINE ACAD OF MILITARY MEDICAL SCI OF THE PLA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Because most anti-tuberculosis drugs are water-soluble, their encapsulation rate in liposomes is all low, and the stability is poor, and the medicine in vitro or in vivo is easy to leak, and for example the encapsulation rate of isoniazid is only 2%~15% (Pandey R, Sharma S, Khuller GK. Liposome-based antitubercular drug therapy in a guinea pig model of tuberculosis. Int J Antimicrob Agents, 2004, 23: 414-415)

Method used

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  • Isoniazid lipid derivate and compositions thereof
  • Isoniazid lipid derivate and compositions thereof
  • Isoniazid lipid derivate and compositions thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] Example 1, the preparation of N-[5-hexadecane-6-thio-(1,3,5)thiadiazin-3-yl]-isonicotinamide

[0033] Put 6.04g (25mmol) hexadecylamine in a flask, add 90mL of toluene, heat to dissolve at 40°C, add 10mL of 20% KOH solution and stir for about 3 minutes, then drop in 10mL of carbon disulfide, react at 35°C for 6 hours, cool After reaching room temperature, 6 mL of formaldehyde was added, and stirring was continued for 0.5 hours. 3.43g (25mmol) of isoniazid was dissolved in 15mL of pH7.8 phosphate buffer solution and 25mL of absolute ethanol, and dropped into the above reaction solution, and reacted for 6 hours. The layers were separated, the upper layer was poured out, the lower layer was extracted three times with toluene, the extracts were combined, and the toluene was evaporated under reduced pressure at 40°C to obtain a light yellow crude product, which was recrystallized from chloroform / methanol (1:1) to obtain a white solid powder with a yield of 50 %. TLC of th...

Embodiment 2

[0035] Embodiment 2, isoniazid hexaalkyl derivative injection

[0036] The isoniazid hexaalkyl derivative in this example means that R in the molecular structural formula in the specification is a hexacarbon alkyl group (hexyl group).

[0037] prescription:

[0038] Isoniazid Hexaalkyl Derivatives 10g

[0039] Tween 80 10ml

[0040] Ethanol 25ml

[0041] Add water for injection to 100ml

[0042] Take isoniazid hexaalkyl derivatives, Tween 80, and ethanol and stir to dissolve, and slowly add water for injection under stirring to obtain a clear solution. Packed into 100 brown glass ampoules, sterilized after filling. Each injection contains 100mg of isoniazid hexaalkyl derivatives.

[0043] Injections of other isoniazid lipid derivatives can be obtained with similar prescriptions and techniques.

Embodiment 3

[0044] Embodiment 3, isoniazid lauryl derivative tablet

[0045] The isoniazid dodecyl derivative in this example means that R in the molecular structural formula in the specification is dodecyl.

[0046] prescription:

[0047] Isoniazid lauryl derivative 10g

[0048] Lactose 150g

[0049] Starch 25g

[0050] Cross-linked polyvinylpyrrolidone 10g

[0051] Polyvinylpyrrolidone 4g

[0052] Magnesium stearate 0.6g

[0053] Grind isoniazid dodecyl derivatives and lactose together, pass through a 100-mesh sieve, then mix evenly with cornstarch and half the amount of carboxymethyl starch sodium, take 15% polyvinylpyrrolidone aqueous solution to make a soft material, pass through a 20-mesh sieve Prepare wet granules, dry at 60°C, sieve the dry granules with a 20-mesh sieve, mix them with the other half of sodium carboxymethyl starch and magnesium stearate, and punch tablets with 8mm dimples, with an average tablet weight of 200mg. Each tablet contains 100mg of isoniazid laur...

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Abstract

The invention discloses an isoniazid lipid derivate and compositions thereof. The isoniazid lipid derivate is characterized by having an INH-THTT-R structure, wherein INH is isoniazid, THTT is thiadiazine thione, and R is a long fatly chain having 6-20 carbon atoms. The isoniazid lipid derivate can be used for preparing tablets, capsules, injections, aerosols, dry powder inhalers and strong dispersant excipients, wherein the strong dispersant excipients comprise selected liposome, nonionic surface active agent vesicles, particles, nanometer grains, emulsions, self-emulsification systems, micelles and nanometer gel.

Description

technical field [0001] The invention relates to the fields of chemistry and biomedicine, in particular to an isoniazid lipid derivative and its composition, wherein the composition includes a highly dispersed dosage form. Background technique [0002] Tuberculosis is an infectious disease that seriously endangers human life and health, and is a major public health and social problem. At present, 2 billion people in the world are infected with tuberculosis, 20 million active tuberculosis patients, 8 to 10 million new cases every year, and 3 million people die of tuberculosis every year. There are about 4.51 million active tuberculosis patients in my country, about 2 million people are infected, and 130,000 people die every year, ranking second in the world. According to the survey, 400 million people in the whole country have been infected by tuberculosis, and 10% of them are ill. According to the 2004 National Statutory Reportable Infectious Diseases Ranking published by t...

Claims

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Application Information

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IPC IPC(8): C07D417/12A61K31/549A61K9/127A61P31/06
Inventor 金义光杜丽娜陈书峰
Owner INST OF RADIATION MEDICINE ACAD OF MILITARY MEDICAL SCI OF THE PLA
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