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Drug composite containing limaprost and preparation method thereof

A technology for limaprost and a composition, which is applied to the field of oral limaprost tablets and their preparation, can solve the problem of no patent application for limaprost, and achieves improved bioavailability, stable dissolution curve, and stable release. effect of medicine

Active Publication Date: 2012-03-21
BEIJING TIDE PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, there is no patent application for limaprost in China

Method used

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  • Drug composite containing limaprost and preparation method thereof
  • Drug composite containing limaprost and preparation method thereof
  • Drug composite containing limaprost and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] Pharmaceutical composition of the present invention--the prescription composition of limatoprost tablet:

[0042] Limaprost Hydroxypropyl-α-CD Inclusion Complex 0.17g

[0043] Mannitol 0.72g

[0044] Sorbitol 1.78g

[0045] Starch slurry 7.00g

[0046] Povidone 4.50g

[0047] Lactose 70.23g

[0048] Talc powder 0.60g

[0049] Made into tablets 85mg / tablet, made into 1000 pieces

[0050] Preparation:

[0051] a. Weigh 0.72g mannitol, 1.78g sorbitol and 0.17g limaprost hydroxypropyl-α-CD inclusion compound, dissolve with appropriate amount of water, freeze-dry, and pre-freeze at -40°C, 200Pa, - Vacuum at 20°C, dry at 100Pa and 20°C to obtain lyophilized mixture I;

[0052] b. Pulverize the freeze-dried mixture I, pass through a 100-mesh sieve, add 7.00g starch slurry, 4.50g povidone, and 70.23g lactose according to the prescription ratio, mix for more than 5 minutes, then add 0.30g of talcum powder, and mix for more than 1 minute , to obtain mixture II;

[0053]...

Embodiment 2

[0064] The prescription composition of Limaprost tablet:

[0065] Limaprost Hydroxypropyl-γ-CD Inclusion Complex 0.0125g

[0066] Mannitol 0.70g

[0067] Trehalose 0.70g

[0068] Pectin 4.50g

[0069] Sodium carboxymethyl starch 8.00g

[0070] Maltose 70.08g

[0071] Magnesium Stearate 1.00g

[0072] Made into tablets 85mg / tablet, made into 1000 pieces

[0073] Preparation:

[0074] a. Weigh 0.70g of mannitol, 0.70g of trehalose and 0.0125g of limatoprost hydroxypropyl-γ-CD inclusion compound, dissolve with an appropriate amount of water, freeze-dry, and pre-freeze at -30°C, 300Pa , Vacuum at -20°C, and dry at 200Pa at 20°C to obtain freeze-dried mixture I;

[0075] B, freeze-dried mixture I is pulverized, crosses 100 mesh sieves, adds 4.50g pectin, 8.00g carboxymethyl starch sodium, 70.08g maltose according to prescription ratio, mixes more than 5 minutes, then adds the magnesium stearate of 0.50g, Mix for more than 1 minute to obtain mixture II;

[0076] c. Put mix...

Embodiment 3

[0084] The prescription composition of Limaprost tablet:

[0085] Limaprost-α-CD inclusion complex 0.25g

[0086] Mannitol 0.75g

[0087] Sucrose 0.25g

[0088] Hypromellose 10.00g

[0089] Low-substituted hydroxypropyl cellulose 10.00g

[0090] Sorbitol 63.25g

[0091] Micronized silica gel 0.50g

[0092] Made into tablets 85mg / tablet, made into 1000 pieces

[0093] Preparation:

[0094] a. Weigh 0.75g of mannitol, 0.25g of sucrose and 0.25g of limatoprost-α-CD inclusion compound, dissolve with an appropriate amount of water, freeze-dry, and pre-freeze at -20°C, 65Pa, -30°C Under vacuum, 90Pa, 30°C drying to obtain freeze-dried mixture I;

[0095] b. Pulverize the freeze-dried mixture I, pass through a 100-mesh sieve, add 10.00g hydroxypropylmethylcellulose, 10.00g low-substituted hydroxypropylcellulose, and 63.25g sorbitol according to the prescription ratio, mix for more than 5 minutes, and then add 0.25g Micropowder silica gel, mixed for more than 1 minute to obta...

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Abstract

The invention provides a drug composite containing limaprost and a preparation method thereof, wherein the drug composite of the invention contains 0.01-1% (weight) of the cyclodextrin inclusion compound of limaprost, 0.5-10% (weight) of freeze-drying stabilizer and other pharmaceutically acceptable excipients, wherein the free-drying stabilizer contains mannitol. The drug composite adopts a freeze drying and dry granulating combined preparation technology, greatly overcomes the defects of easy moisture adsorption and extremely bad stability of limaprost which is the main drug, and simultaneously cannot influence the slaking characteristic and the dissolution of the main drug, in addition, the product is not a coated tablet, and thereby the invention prevents the defect of slower dissolution of the conventional coated tablets.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to a pharmaceutical composition and a preparation method thereof, in particular to a limatoprost tablet for oral administration and a preparation method thereof. Background technique [0002] The chemical name of Limaprost is: (E)-7-[(1R, 2R, 3R)-3-hydroxy-2-[(3S, 5S)-(E)-3-hydroxy-5-methanol Base-1-nonenyl]-5-oxocyclopentyl]-2-heptanoic acid ((E)-7-[(1R, 2R, 3R)-3-hydroxy-2-[(3S, 5S) -(E)-3-hydroxy-5-methyl-1-nonenyl]-5-oxocyclopenty1]-2-heptenoic acid), the structural formula is as follows: [0003] [0004] This product is a derivative of prostaglandin E1, which can increase the content of cyclic adenosine monophosphate (cAMP) and inhibit the generation of thromboxane A2 (TXA2). It has the functions of dilating blood vessels, increasing blood flow and inhibiting platelet aggregation and adhesion. Animal experiments also show that It can increase the blo...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/5575A61K9/20A61P7/02A61P9/08A61J3/10
Inventor 刘红星张扬李学广杨青松肖萱周丽莹
Owner BEIJING TIDE PHARMA
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