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Sustained release formulation of bilobalide-B and preparation process thereof

A ginkgolide, sustained-release preparation technology, applied in the field of pharmaceutical preparations, can solve the problem of no ginkgolide B, etc.

Inactive Publication Date: 2007-05-23
王爱民
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] At present, there is no report that Ginkgolide B is used as an active ingredient to make sustained-release preparations

Method used

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  • Sustained release formulation of bilobalide-B and preparation process thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] The preparation of embodiment 1 ginkgolide B skeleton type sustained-release tablet

[0025] prescription:

[0026] Ginkgolide B 60.0g

[0027] Hydroxypropyl methylcellulose (4000 centipoise) 51.7g

[0028] 3% ethanol solution of hydroxypropyl methylcellulose (50 centipoise) 5.3g (calculated as dry matter)

[0029] Microcrystalline Cellulose 17.5g

[0030] Magnesium stearate 0.9g

[0031] Makes 1000 pieces

[0032] Preparation method: mix ginkgolide B, hydroxypropyl methylcellulose, and microcrystalline cellulose, add 3% hydroxypropyl methylcellulose ethanol solution, mix well, granulate, and dry at 65°C for 12 Hours, add magnesium stearate, mix well, compress into tablets, and obtain.

Embodiment 2

[0033] The preparation of embodiment 2 matrix type sustained-release tablets

[0034] prescription:

[0035] Ginkgolide B 200g

[0036] Microcrystalline Fiber Cord 50.0g

[0037] Carbopol 105.0g

[0038] Polyvinylpyrrolidone K-30 10.5g (calculated as dry matter)

[0039] Magnesium stearate 1.8g

[0040] Makes 1000 pieces

[0041] Preparation method: mix ginkgolide B and polycarboxyethylene, granulate with 5% polyvinylpyrrolidone K-30 aqueous solution, dry at 55°C for 12 hours, add magnesium stearate, mix evenly, and press into tablets. Instantly.

Embodiment 3

[0042] The preparation of embodiment 3 film-controlled sustained-release capsules

[0043] prescription:

[0044] Ginkgolide B 45.0g

[0045] 2% hydroxypropyl methylcellulose (50 centipoise) aqueous solution 6.3 (based on dry matter)

[0046] Trimethylammonium ethyl methacrylate - methacrylate copolymer (Eudragit RS100) 50.0g

[0047] Microcrystalline Cellulose 43.8g

[0048] Polyvinylpyrrolidone K30 ethanol solution 12.5g

[0049]Makes 1000 capsules

[0050] Use methacrylic trimethylammonium ethyl ester-methacrylate copolymer as the coating film material, add a small amount of polyvinylpyrrolidone ethanol solution (PVP-K 30 ) as a porogen, the porogen dissolves in the digestive juice to form micropores on the coating film, and the active ingredient is slowly and steadily released from the micropores.

[0051] Preparation method: Mix the prescription amount of ginkgolide B and microcrystalline cellulose, add hydroxypropyl methylcellulose aqueous solution, mix well, extru...

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Abstract

The invention relates to a bilobalide B slow-release agent and relative production, wherein it is formed by bilobalide B, slow-release material, and other findings. The invention can stabilize blood drug density, improve treatment effect, and reduce side effect. It is portable.

Description

Technical field: [0001] The invention relates to a ginkgolide B sustained-release preparation and a preparation method thereof, belonging to the field of pharmaceutical preparations. Background technique: [0002] Ginkgolide is an effective active component extracted from the leaves of the traditional Chinese medicine Ginkgo biloba, which can be further subdivided into ginkgolide A, B, C, bilobalide, etc. in terms of structure. Modern pharmacological studies have shown that ginkgolides are currently the most promising drugs for clinical application among natural anti-platelet activating factor (PAF) receptor antagonists, and ginkgolide B has the strongest selectivity and activity in antagonizing PAF receptors. Therefore, Ginkgolide B, as a highly active platelet antagonist factor, may be developed into a clinical therapy that plays an important role in pathological processes such as thrombosis, organ transplant rejection, senile dementia, acute inflammation, cardiac allergy,...

Claims

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Application Information

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IPC IPC(8): A61K31/365A61K9/20A61K9/48A61P9/00A61P9/10A61P7/02A61P25/28A61P37/06
Inventor 王爱民刘文尧骆建成
Owner 王爱民
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