Enteric soluble preparation of Alun phosphorate and its preparing method

A technology of alendronate and enteric-coated preparations, which can be used in pharmaceutical formulations, medical preparations containing active ingredients, organic active ingredients, etc., and can solve problems such as peptic ulcers, increased dosage, and poor patient compliance. , to reduce adverse reactions and eliminate irritation

Active Publication Date: 2005-02-23
CSPC OUYI PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] It is generally believed that when taking this type of drug, part of the active ingredients will be dissolved, and a higher concentration will be produced on the mucosal surface of the esophagus, resulting in damage to the epithelium and mucosa of the upper gastrointestinal tract, and the patient will feel pain when swallowing and burning of the esophagus , heartburn, serious peptic ulcers, etc.; in addition, because these compounds are extremely polar, it is difficult to penetrate the epithelial cells of the alimentary canal into the blood, so the bioavailability is low, such as the bioavailability of alendronate sodium Utilization is lower than 1.5%. In order to achieve effective therapeutic concentration, the dose must be increased, which is also the reason for the large oral adverse reactions of this type of drug. Foreign clinical statistics have found that compared with aspirin, alendronate sodium The incidence of gastrointestinal adverse reactions is more than less, resulting in poor compliance of patients and affecting the efficacy of drugs
[0004] At present, the alendronate on the market at home and abroad is only a common tablet of alendronate sodium, because of its strong irritation to the upper gastrointestinal tract, and the need to stand upright for more than 30 minutes, so its clinical application is limited

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0050] Component Weight Weight %

[0051] (1) Core material

[0052] Alendronate Sodium 13.3g (Containing Alendronate 10g) 5%

[0053]Lactose 172.9g 65%

[0054] Hypromellose 47.88g 18%

[0055] Povidone 13.3g 5%

[0056] 95% ethanol appropriate amount

[0057] Talc 2.66g 1%

[0058] Makes 1000 pieces

[0059] (2) Coating solution

[0060] Ethylcellulose 15.96g 6%

[0061] 95% ethanol 500ml

[0062] Weigh the alendronate sodium, diluent, and part of the disintegrant through the 80-mesh sieve according to the prescription amount, mix well, add an appropriate amount of 10% povidone, granulate, dry the remaining part of the disintegrant and dry The granules are mixed evenly, and the semi-finished product is qualified after the inspection, adding a lubricant, and then pressed into tablets after mixing.

[0063] The prepared plain tablet is weighed and placed in a coating pan, while spraying the coating solution and blowing hot air to obtain an enteric-coated tablet.

Embodiment 2

[0065] Component Weight Weight %

[0066] (1) Core material

[0067] Alendronate Sodium 93.1g (Alendronate 70g) 18.62%

[0068] Microcrystalline Cellulose 229.4g 45.88%

[0069] Hypromellose 35g 7%

[0070] Sodium starch glycolate 35g 7%

[0071] Talc 7.5g 1.5%

[0072] Povidone 30g 6%

[0073] 95% ethanol appropriate amount

[0074] Makes 1000 pieces

[0075] (2) Coating solution:

[0076] Polyacrylic resin No. II 40g 8%

[0077] Polyacrylic resin No. III 10g 2%

[0078] Macrogol 6000 20g 4%

[0079] 95% ethanol 1000ml

[0080] Take the prescribed amount of alendronate sodium, pass through a 100-mesh sieve for 3 times, add diluent and disintegrant, mix well, add appropriate amount of wetting agent or binder to granulate, dry, add lubricant after the semi-finished product is qualified, mix Press evenly.

[0081] Weigh the prepared plain tablets and place them in a coating pan, spray the coating liquid and blow hot air while blowing to obtain enteric-coated tablets...

Embodiment 3

[0083] Component Weight Weight %

[0084] (1) Core material:

[0085] Alendronate Sodium 39.9g (Containing Alendronate 30g) 13.3%

[0086] Microcrystalline Cellulose 150g 50%

[0087] Hypromellose 30g 10%

[0088] Povidone 21g 7%

[0089] 95% ethanol appropriate amount

[0090] Makes 1000 capsules

[0091] (2) Coating solution:

[0092] Polyacrylic resin No. II 48g 16%

[0093] Macrogol 1000 5.1g 1.7%

[0094] Macrogol 6000 6g 2%

[0095] 95% ethanol 1000ml

[0096] The granules prepared according to the preparation method are weighed and placed in a coating pan or a fluidized fluidized bed, while spraying the coating solution and blowing hot air to obtain enteric-coated granules.

[0097] Enteric-coated granules are filled into capsules to obtain alendronate sodium enteric-coated capsules.

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Abstract

An enteric allenphosphonate in the form of tablet or capsule is prepared from allenphosphonate, medicinal auxiliary and enteric coating.

Description

technical field [0001] The invention relates to an alendronate enteric-coated preparation and a preparation method thereof. technical background [0002] Alendronate is a third-generation bisphosphonate drug that has a strong inhibitory effect on osteoclasts and is currently widely used in the treatment of primary or secondary osteoporosis, hypercalcemia, Osteitis deformans and bone pain caused by tumor bone metastasis are the only two oral drugs in the bisphosphonate class. Its activity is 1000 times that of etidronate, so it is more effective than etidronate Safety, in 2003 the sales volume of this drug in the world was as high as 1.5 billion US dollars, and it is a class of drugs that has developed rapidly in recent years. Since the two hydrogen atoms connected to a carbon atom in the structure of alendronate are replaced by two phosphate groups, this type of compound can release more H + , thus having a strong corrosiveness, this type of comp...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/663A61P19/08A61P19/10A61P35/00
Inventor 牛占旗郭卫芹张勇智彩辉
Owner CSPC OUYI PHARM CO LTD
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