Morphine sulfate sustained/controlled-release suppository and preparation method thereof

A morphine sulfate and suppository technology, which is applied in the directions of suppository delivery, pharmaceutical formulations, and non-active ingredients medical preparations, etc., can solve the problems of inability to achieve sustained and controlled release, unstable blood drug concentration, and short effect time, and achieve reliable curative effect. , the effect of reducing the frequency of administration and reducing the dosage of administration

Active Publication Date: 2012-06-27
MAYINGLONG PHARMA GROUP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The prior art discloses a morphine sulfate suppository (patent 200810197059.9), which uses 0.5-5% by weight of morphine sulfate as the main ingredient, 70-93.49% of 36-type mixed fatty acid glycerides, and 2-20% of 38-type Mixed fatty acid glycerides, 1-6% Tween-80, 1-3% micronized silica gel, 2-8% microcrystalline cellulose, 0.005-0.05% tert-butyl-p-hydroxyanisole and 0.005-0.05 % of 2,6-di-tert-butyl-p-cresol is prepared as an auxiliary material. Due to the auxiliary material and its proportioning ratio, the above-mentioned morphine sulfate suppository is a common suppository, which cannot achieve the effect of sustained and controlled release. After the drug is used in clinical trials, its The effective pain relief time is only about 7 hours, and the effective time is short, which will make the number of administrations per unit time more, and the dosage will be large, which will easily lead to unstable blood drug concentration

Method used

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  • Morphine sulfate sustained/controlled-release suppository and preparation method thereof
  • Morphine sulfate sustained/controlled-release suppository and preparation method thereof
  • Morphine sulfate sustained/controlled-release suppository and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0046] The morphine sulfate sustained-release suppository provided in this embodiment contains the following percentages by weight:

[0047] Morphine sulfate 3.48%;

[0048] Poloxamer 188 24.00%;

[0049] Poloxamer 407 26.40%;

[0050] BHT 0.02%;

[0051] Glycerin 40.50%

[0052] Azone 4.80%;

[0053] Carbomer 0.80%.

[0054] The preparation method of above-mentioned morphine sulfate suppository, comprises the steps:

[0055] A. Pass the main drug morphine sulfate through a 180 or more mesh sieve; the auxiliary materials include F68, F127, carbomer, 2,6-di-tert-butyl p-cresol (BHT), and the auxiliary materials pass through a 100 mesh or more mesh sieve respectively ,spare;

[0056] B. F68, F127, BHT, morphine sulfate, carbomer, stir and mix well, heat to 60-80°C to melt, stir and mix well;

[0057] C. Stir the molten substrate in step B at 60-75°C, add glycerin and azone and keep warm and stir evenly;

[0058] D. Stir the mixture in step C at a constant temperature of 6...

Embodiment 2

[0075] The morphine sulfate sustained-release suppository provided in this embodiment contains the following percentages by weight:

[0076] Morphine sulfate 5.94%;

[0077] Poloxamer 188 28.05%;

[0078] Poloxamer 407 25.25%;

[0079] BHT 0.02%;

[0080] Glycerin 35.84%

[0081] Azone 4.20%;

[0082] Carbomer 0.70%.

[0083] The preparation method of above-mentioned morphine sulfate suppository, comprises the steps:

[0084] A. Pass the main drug morphine sulfate through a 180 or more mesh sieve; the auxiliary materials include F68, F127, carbomer, 2,6-di-tert-butyl p-cresol (BHT), and the auxiliary materials pass through a 100 mesh or more mesh sieve respectively ,spare;

[0085] B. F68, F127, BHT, morphine sulfate, and carbomer are stirred and mixed, then heated to 70°C to melt, and stirred again;

[0086] C. Add glycerin and azone to the melted substrate in step B under stirring at 40-45°C and keep warm and stir evenly;

[0087] D. Stir the mixture in step C to a ...

Embodiment 3

[0106] The morphine sulfate sustained-release suppository provided in this embodiment contains the following percentages by weight:

[0107] Morphine sulfate 7.70%;

[0108] Poloxamer 188 21.76%;

[0109] Poloxamer 407 28.29%;

[0110] BHT 0.02%;

[0111] Glycerin 37.16%

[0112] Azone 4.35%;

[0113] Carbomer 0.72%

[0114] The preparation method of above-mentioned morphine sulfate suppository, comprises the steps:

[0115] A. Pass the main drug morphine sulfate through a 180 or more mesh sieve; the auxiliary materials include F68, F127, carbomer, 2,6-di-tert-butyl p-cresol (BHT), and the auxiliary materials pass through a 100 mesh or more mesh sieve respectively ,spare;

[0116] B. F68, F127, BHT, morphine sulfate, and carbomer are stirred and mixed, then heated to 70°C to melt, and stirred again;

[0117] C. Add glycerin and azone to the melted substrate in step B under stirring at 40-45°C and keep warm and stir evenly;

[0118] D. Stir the mixture in step C at a c...

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Abstract

The invention discloses a morphine sulfate sustained / controlled-release suppository, which comprises the following compositions in percentage by weight: 1 to 10 percent of morphine sulfate, 20 to 35 percent of poloxamer 188, 20 to 35 percent of poloxamer 407, 0.004 to 0.02 percent of antioxidant, and 25 to 48 percent of water absorbent. The morphine sulfate sustained-release / controlled-release suppository can make the effective blood concentration maintain more than 24 hours, show a good blood platform, and fully display the sustained / controlled-release characteristics.

Description

technical field [0001] The invention relates to a morphine sulfate sustained and controlled release suppository and a preparation method thereof. Background technique [0002] Morphine, as a classic narcotic analgesic, is the third-level basic drug in the three-step cancer pain relief principle recommended by the World Health Organization. It is mainly used for severe pain, and small doses can also be used for pain relief in patients with moderate pain. [0003] Morphine is an opioid receptor agonist, which has strong analgesic effect, obvious sedative effect, and antitussive effect. Morphine acts on the morphine receptors in the posterior cutin of the spinal cord and the ventroposterolateral nucleus of the thalamus, and has an analgesic effect on sharp pain; it acts on the morphine receptors in the gray matter of the midbrain aqueduct, hypothalamus, and thalamus, and has an analgesic effect on dull pain and visceral pain. The effect is particularly obvious; acting on the m...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/02A61K31/485A61K47/34A61P25/04A61K47/10A61K47/32
Inventor 陈平丁明和
Owner MAYINGLONG PHARMA GROUP
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