Medicinal composition for increasing dissolution rate of racanisodamine and preparation method thereof

A technology of anisodamine and its composition, which is applied in the field of pharmaceutical composition and its preparation for improving the dissolution rate of racemic anisodamine, which can solve the problem of poor dissolution rate and stability, non-compliance of drug dissolution rate, and influence on bioavailability issues such as high yield and clinical use effect, to achieve the effect of high yield and high economic value

Inactive Publication Date: 2015-03-11
HENAN PURUI PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The oral solid preparation prepared by the existing common preparation process, even if it can be completely disintegrated, it is difficult to achieve complete dissolution, and the dissolution rate is basically about 70%.
Especially in the storage process, long-term storage often leads to drug dissolution that does not meet the requirements
And racemic anisodamine tablets are small-scale preparations, the specifications are: 5mg, 10mg, if the dissolution is not good, it will directly affect the bioavailability and clinical use effect
In order to solve the problem of poor dissolution and stability of racemic anisodamine tablets, the study of the pharmaceutical composition was carried out

Method used

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  • Medicinal composition for increasing dissolution rate of racanisodamine and preparation method thereof
  • Medicinal composition for increasing dissolution rate of racanisodamine and preparation method thereof
  • Medicinal composition for increasing dissolution rate of racanisodamine and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0045] The components and the proportioning ratio of the improved racemic anisodamine pharmaceutical composition of the present invention are as follows:

[0046] Formula quantity (1000 tablets / batch), the specification is 5mg tablet.

[0047] components particle size Proportion Feeding amount racemic anisodamine 50μm 6.25％ 5g lactose 115μm 27.5％ 22g microcrystalline cellulose 115μm 27.5％ 22g starch 115μm 28.6％ 22.9g

[0048] Croscarmellose Sodium 115μm 5％ 4g purified water ---- 0 0 (dry removal) Croscarmellose sodium (step e plus) 115μm 5％ 4g Magnesium stearate 115μm 0.1％ 0.08g total ---- 100％ 80g

[0049] The pharmaceutical composition containing the dissolution rate of 6.25% of the total component weight in the table above is prepared into a tablet by the following method:

[0050] (a) the active compound racemic anisodamine is micronized to control particle size;

...

Embodiment 2

[0061] The components and the proportioning ratio of the improved racemic anisodamine pharmaceutical composition of the present invention are as follows:

[0062] Tablet production (1000 tablets / batch), the specification is 10mg tablet,

[0063] components particle size Proportion Feeding amount racemic anisodamine 25μm 12.5％ 10g sucrose 75μm 7.5％ 6g Mannitol 75μm 17.5％ 14g pregelatinized starch 75μm 12.5％ 10g Crospovidone 75μm 15％ 12g syrup ---- 10％ 8g Croscarmellose sodium (step e plus) 75μm 15％ 12g Calcium stearate 75μm 10％ 8g

[0064] total ---- 100％ 80g

[0065] The pharmaceutical composition of the dissolution rate of racemic anisodamine in the above table is compressed into a tablet by the preparation method of Example 1.

[0066] Experimental Test 2:

[0067] Under simulated gastrointestinal conditions, 6 tablets were randomly selected from the tablets prepared...

Embodiment 3

[0071] The components and the proportioning ratio of the improved racemic anisodamine pharmaceutical composition of the present invention are as follows:

[0072] Tablet production (10000 tablets / batch), the specification is 5mg tablets,

[0073] components particle size Proportion Feeding amount racemic anisodamine 75μm 6.25％ 50g lactose 150μm 22％ 176g calcium carbonate 150μm 22％ 176g dextrin 150μm 23.75％ 190g Sodium carboxymethyl starch 150μm 8％ 64g Starch slurry ---- 5％ 40g Low-substituted hydroxypropyl cellulose (step e added) 150μm 8％ 64g Micropowder silica gel 150μm 5％ 40g total ---- 100％ 800g

[0074] The pharmaceutical composition of the dissolution rate of racemic anisodamine in the above table is compressed into a tablet by the preparation method of Example 1.

[0075] Experimental Test 3:

[0076] Under simulated gastrointestinal conditions, 6 tablets were randomly se...

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Abstract

The invention relates to a medicinal composition for increasing dissolution rate of racanisodamine and a preparation method thereof. The medicinal composition and the preparation method thereof can effectively improve the dissolution rate of racanisodamine. Through a micronization technology and pharmaceutically acceptable diluents or carriers, a racanisodamine solid preparation, such as tablet, is prepared, so that the racanisodamine rapidly releases from the preparation to improve the bioavailability. The process of the invention is simple and easy, does not use organic solvent in the process, and has low production cost and little environmental pollution.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparation technology, and in particular relates to a pharmaceutical composition for improving the dissolution rate of racemic anisodamine and a preparation method thereof. Background technique [0002] Racemic anisodamine, its chemical name is (±)-6β-hydroxyl-1αH, 5αH-tropane-3α-ol tropic acid ester, this compound has peripheral anti-M choline receptor effect, and can relieve the effect caused by acetylcholine Smooth muscle spasm, has a relaxing effect on the smooth muscle of the gastrointestinal tract and inhibits its peristalsis. This product is white crystal or crystalline powder, odorless and bitter. Soluble in ethanol or hydrochloric acid, dissolved in water. [0003] Before the 2005 edition of "Chinese Pharmacopoeia", the dissolution rate of racemic anisodamine tablets was not checked, and the 2010 edition of "Chinese Pharmacopoeia" began to check the dissolution rate of racemic anisodamine...

Claims

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Application Information

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IPC IPC(8): A61K31/46A61K47/38A61K9/20A61P1/00
CPCA61K9/2018A61K9/2054A61K9/2059A61K31/46
Inventor 栗金梁黄普广左辉辉刘兰君
Owner HENAN PURUI PHARMA
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