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Phosphoric acid ligustrazine micropore permeation pump control-release tablet and preparation method thereof

A technology for the controlled release of ligustrazine phosphate and osmotic pumps, which is applied in pharmaceutical formulations, medical preparations containing active ingredients, drug delivery, etc., and can solve the problem of affecting the drug release rate of osmotic pump tablets, inapplicability of mechanical drilling, and membrane burning. Aperture and other issues, to avoid the "peak valley" phenomenon, improve the time of drug action, the effect of low equipment requirements

Active Publication Date: 2008-09-24
惠州市九惠药业有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Early mechanical drilling is not suitable for large-scale mechanized production, and the resulting damage to the coating film will affect the drug release rate of osmotic pump tablets; currently, laser drilling is often used in industrial production, but laser drilling may burn the membrane. Burning or making the pore size different, and when the drug release channel is less, the channel is easy to be blocked in the gastrointestinal tract after oral administration, resulting in irregular drug release
At present, there is no technical report on Ligustrazine Phosphate Microporous Osmotic Pump Controlled Release Tablets

Method used

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  • Phosphoric acid ligustrazine micropore permeation pump control-release tablet and preparation method thereof
  • Phosphoric acid ligustrazine micropore permeation pump control-release tablet and preparation method thereof
  • Phosphoric acid ligustrazine micropore permeation pump control-release tablet and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] Example 1 is in accordance with the following formula:

[0039]The tablet core weighs 350mg in total:

[0040] Ligustrazine Phosphate 75mg

[0041] Sodium chloride 120mg

[0042] Lactose 120mg

[0043] PVP 30mg

[0044] 20% PVP anhydrous ethanol solution

[0045] Magnesium stearate 1.8mg

[0046] Among them, the 20% PVP absolute ethanol solution can be used in accordance with the conventional use in the field to achieve the basic adhesion of the tablet core material. The sodium chloride content can range from 0 to 240 mg, and correspondingly, the lactose content can range from 240 to 0 mg.

[0047] The coating solution is according to the following formula:

[0048] Cellulose acetate 30g

[0049] PEG-400 12ml

[0050] Diethyl phthalate 9ml

[0051] Acetone 800ml

[0052] Isopropanol 200ml

[0053] Coating weight gain 3.5%

[0054] Specific preparation method:

[0055] 1. Weigh 75g of ligustrazine phosphate, 120g of sodium chloride, 120g of lactose, 30g of PVP, pass through ...

Embodiment 2

[0061] Example 2 is in accordance with the following formula:

[0062] The tablet core weighs 350mg in total:

[0063] Ligustrazine Phosphate 75mg

[0064] Sodium chloride 200mg

[0065] Sodium bicarbonate 40mg

[0066] PVP 30mg

[0067] 20% PVP anhydrous ethanol solution

[0068] Magnesium stearate 1.8mg

[0069] Among them, the 20% PVP absolute ethanol solution refers to the conventional usage in this field to achieve the basic adhesion of the core material.

[0070] The coating solution is according to the following formula:

[0071] Cellulose acetate 30g

[0072] PEG-400 12ml

[0073] Diethyl phthalate 9ml

[0074] Acetone 800ml

[0075] Isopropanol 200ml

[0076] Coating weight gain 4%

[0077] Specific preparation method:

[0078] 1. Weigh 75g of ligustrazine phosphate, 240g of sodium chloride, 30g of PVP, pass through a 60-mesh sieve and mix several times until the mixture is complete. Use 20% PVP in anhydrous ethanol as a binder, 20-mesh sieve, wet granulation Dry in an ov...

Embodiment 3

[0084] Example 3 is in accordance with the following formula:

[0085] The tablet core weighs 350mg in total:

[0086] Ligustrazine Phosphate 75mg

[0087] Sodium chloride 200mg

[0088] Mannitol 40mg

[0089] PVP 30mg

[0090] 20% PVP anhydrous ethanol solution

[0091] Magnesium stearate 1.8mg

[0092] Among them, the 20% PVP absolute ethanol solution refers to the conventional usage in this field to achieve the basic adhesion of the core material. The sodium chloride content can range from 0 to 240 mg, and correspondingly, the mannitol content can range from 240 to 0 mg.

[0093] The principle of the coating solution formulation is that the solvent uses a mixture of acetone and isopropanol in a ratio of 4:1, the cellulose acetate content is about 3mg / 100ml solvent, and diethyl phthalate accounts for 10-30 of the cellulose acetate content. %, PEG-400 accounts for 10-40% of the cellulose acetate content. The coating liquid of this embodiment is in accordance with the following sp...

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Abstract

The invention discloses a TMPP micro-osmotic pump release-control tablet and consists of a tablet core and a coating. The tablet core consists of TMPP, a penetration-promoting agent, a bonding agent, a lubricant and a right amount of absolute ethanol solution containing 20 percent of a caking agent, and the weight proportion of TMPP, the penetration-promoting agent, the bonding agent and the lubricant is 75:240:30:1.8. The coating consists of cellulose acetate, carmowax 400, diethyl phthalate and a dissolvent, and the weight volume ratio of cellulose acetate, carmowax 400, diethyl phthalate and the dissolvent is 30mg:6 to 12ml:3 to 9ml:1,000ml. The TMPP micro-osmotic pump release-control tablet prepares TMPP into a micro-osmotic pump release-control tablet capable of controlling the release for 12 hours through an optimized selection of a penetration-promoting agent, a porogen, a plasticizer and a film thickness, thereby prolonging the duration of drug action effectively, reducing the frequency of drug delivery, improving the compliance of a patient and providing experience and technology for the formulation development of similar drugs.

Description

Technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and specifically relates to a ligustrazine phosphate microporous osmotic pump controlled release tablet and a preparation method thereof. Background technique [0002] Ligustrazine is an effective ingredient extracted from the rhizomes of Ligusticum Chuanxiong, a Chinese medicine Umbelliferae plant, with molecular formula C 8 H 12 N 2 , The chemical structure is tetramethylpyrazine. Ligustrazine Phophate (Ligustrazine Phophate) is the phosphate of ligustrazine and its chemical name is Tetramethlprazine Phophate (TMPP). This product is soluble in water and ethanol, but insoluble in chloroform. The chemical structure is as follows: [0003] [0004] Molecular formula: C 8 H 12 N 2 ·H 3 PO 4 ·H 2 O [0005] Molecular weight: 252.12 [0006] Melting point: 173~177℃ [0007] Ligustrazine has the characteristics of definite curative effect, rapid action and small side effects. Modern p...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/36A61K31/4965A61P9/10A61P9/00
Inventor 高崇凯李宁刘利
Owner 惠州市九惠药业有限公司
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