Water-soluble medicine particle-type slow-release composition, preparation and its preparing method

A technology for water-soluble drugs and compositions, applied in the directions of drug combinations, pharmaceutical formulations, pill delivery, etc., can solve the problems of increasing the rate of drug absorption, unable to adjust the dose, and increasing the side effects of drugs, so as to improve the stability and process production. The process is simple and easy to operate, and the effect of strong operability

Inactive Publication Date: 2005-11-23
SHANGHAI INST OF PHARMA IND CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] However, there are still some disadvantages in common sustained-release preparations, especially most oral tablets, which cannot be broken apart when taking, and cannot be used for dose adjustment; they must be swallowed whole, and cannot be chewed or dissolved and dispersed, which is not conducive to swallowing. Difficult drug administration in elderly and pediatric patients; pharmacokinetics are susceptible to gastrointestinal environment (such as gastrointestinal motility, emptying rate, gastrointestinal pH, food, patient age); can cause The phenomenon of "drug dumping" greatly increases the rate of drug absorption, causing a sharp rise in blood concentration and increasing drug side effects

Method used

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  • Water-soluble medicine particle-type slow-release composition, preparation and its preparing method
  • Water-soluble medicine particle-type slow-release composition, preparation and its preparing method
  • Water-soluble medicine particle-type slow-release composition, preparation and its preparing method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0044] Preparation of albuterol sulfate controlled-release microspheres

[0045] prescription:

[0046] Salbutamol Sulfate 5.0g

[0047] Amberlite-IRP88 5.0g

[0048] EUDRAGIT® RSPO 37.5g

[0049] EUDRAGIT® L100 6.25g

[0050] Triethyl citrate 5.0g

[0051] Magnesium Stearate 2.5g

[0052] Absolute ethanol 200ml

[0053] Liquid paraffin 600ml

[0054] Preparation:

[0055] (1) preparation of medicine resin: the salbutamol sulfate water is made into the solution that concentration is 50~150mg / ml, drips in the glass exchange column that the ion exchange resin Amberlite-IRP88 of recipe quantity is housed, adopts dynamic adsorption method to carry out medicine, After the exchange is complete, rinse with deionized water until the drug concentration cannot be detected, dry and set aside;

[0056] (2) Preparation of microspheres: Dissolve acrylic resin EUDRAGIT® RSPO, EUDRAGIT® L100 and triethyl citrate in absolute ethanol, add medicinal resin and magnesium stearate to make ...

Embodiment 2

[0080] Preparation of albuterol sulfate sustained-release microspheres: (preparation of sustained-release granules and suspensions)

[0081] Preparation of microspheres:

[0082] prescription:

[0083] Salbutamol Sulfate 5.0g

[0084] Amberlite-IRP88 5.0g

[0085] EUDRAGIT  RSPO 60.0g

[0086] EUDRAGIT  L100 10.0g

[0087] Dimethyl phthalate 6.0g

[0088] Magnesium Stearate 3.0g

[0089] Absolute ethanol 200ml

[0090] Simethicone 600ml

[0091] The preparation method is the same as in Example 1.

[0092] In vitro release of microspheres: the effects of rotational speed, pH value, salt ionic strength, and particle size on the release of microspheres are the same as in Example 1. Depending on the particle size, it can provide sustained release for 3-8 hours. The sphericity, particle size and distribution measurements of the microspheres were similar to Example 1.

[0093] Sustained-release granules are prepared by conventional methods in the art:

[0094] Sustai...

Embodiment 3

[0098] prescription:

[0099] Salbutamol Sulfate 5.0g

[0100] Amberlite IRP88 5.0g

[0101] EUDRAGIT  RSPO 36g

[0102] EUDRAGIT  L100 12g

[0103] Triethyl citrate 2.5g

[0104] Magnesium Stearate 1.0g

[0105] Dichloromethane 200ml

[0106] Corn Oil 600ml

[0107] In vitro release of microspheres: the effects of rotational speed, pH value, salt ionic strength, and particle size on the release of microspheres are the same as in Example 1. Depending on the particle size, it can provide sustained release for 4-10 hours. The sphericity, particle size and distribution determination of the microspheres are similar to Example 1.

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PUM

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Abstract

The invention discloses a water-soluble drug particulate sustained-controled release composition, preparation and the preparing method. The composition components according to weigh percent include: water-soluble drug 1-10%, ion-exchange resin 3-50%, retarder 40-80%, plasticizer 1-10%, and dispersant 2-5%. Said water-soluble drug's constitutional formula contains -N- part able to protonize. The drug has good stability, the carrier drug quantity and obtaining rate are high, the needed equipment is simple, the technical process is simple and easy to apply, maneuverability is strong, the release of this frame microsphere all the more approaches zero level relativly to other common microspheres, the final cumulative drug-releasing quantity is also higer than common microspheres, the effect of gastrointestinal tract environment is lower, the absorption is stable and the individual difference is small.

Description

technical field [0001] The invention relates to a water-soluble drug microparticle sustained-control release preparation and a preparation method thereof. Background technique [0002] Oral dosage forms are popular because of their convenient administration and portability. However, common oral preparations bring inconvenience to patients because they need to be administered several times a day, and are easy to miss and use, and the drug concentration in the blood fluctuates greatly with peaks and valleys. When the blood concentration is high (peak concentration), it will exceed the therapeutic concentration range and increase the side effects. When it is low (trough concentration), it is below the effective therapeutic concentration, so that it cannot show curative effect. The development of slow-release and controlled-release preparations has solved the above problems to a large extent. It is convenient to take, and only needs to be taken 1-2 times a day, which reduces ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/14A61K9/20A61K31/137A61K47/30A61P11/06
Inventor 金方王晓维闻聪
Owner SHANGHAI INST OF PHARMA IND CO LTD
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