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Rectal administration composition containing tamsulosin

A technology of rectal administration and tamsulosin, applied in the application of urination disorder drugs, the field of preparation and treatment of urination disorders, can solve the problems that drugs are difficult to penetrate into prostatic fluid, difficult to achieve therapeutic effects, poor body fluid circulation, etc. High compliance, long duration of drug efficacy, and the effect of avoiding degradation

Inactive Publication Date: 2010-11-24
张立英 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Due to the existence of this layer of phospholipid membrane (blood-prostate barrier), it is difficult for most drugs to penetrate into the prostatic fluid and tissue; and because the blood perfusion of the prostate is relatively poor, if the prostatic hyperplasia or inflammation occurs, its secretion Poor drainage leads to poor fluid circulation
Therefore, simple systemic administration is difficult to achieve the desired therapeutic effect

Method used

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  • Rectal administration composition containing tamsulosin
  • Rectal administration composition containing tamsulosin
  • Rectal administration composition containing tamsulosin

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] Example 1 Preparation of suppository A

[0037] 1. Prescription A (amount of 100 suppositories)

[0038]

[0039]

[0040] 2. Preparation method of suppository A

[0041] 1) Take the main drug tamsulosin hydrochloride in prescription A and go through a 200-mesh sieve, and other solid materials through a 100-mesh sieve;

[0042] 2) The substrate is melted, filtered and sterilized at 45~60℃;

[0043] 3) Weigh the above-mentioned melted matrix of the prescription amount and heat it at 45~55℃, add the prescription amount of other excipients under stirring and mix well, continue to add the prescription amount of the main drug under stirring, and mix well under the insulation condition to obtain mixture;

[0044] 4) Injection molding of the above mixture at 40~45℃, and the prepared suppository is cooled at 5~20℃ for 30 minutes;

[0045] 5) Seal the obtained suppository, inspect, package and store the finished product.

Embodiment 2

[0046] Example 2 Preparation of suppository B

[0047] 1. Prescription B (amount of 100 suppositories)

[0048]

[0049] 2. Preparation method of suppository B

[0050] The same as in Example 1.

Embodiment 3

[0051] Example 3 Preparation of suppository C

[0052] 1. Prescription C (amount of 100 suppositories)

[0053]

[0054] 2. Preparation method of suppository C

[0055] The same as in Example 1.

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PUM

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Abstract

The invention relates to a rectal administration composition containing tamsulosin, which comprises effective quantities of tamsulosin or pharmaceutically acceptable salts or derivatives thereof, solubilizer and sorbefacient, wherein the effective quantity of tamsulosin or pharmaceutically acceptable salts or derivatives thereof is metered according to the equivalence tamsulosin hydrochloride; the content of the tamsulosin or pharmaceutically acceptable salts or derivatives thereof is equivalent to 0.025-1.6 mg of tamsulosin hydrochloride; and the preparation per unit weighs 0.8-4 g. The rectal administration composition containing tamsulosin can overcome the defects of poor curative effect and great toxic or side effect in oral administration and systemic injection administration, and the defects of great side effect and poor patient dependence in partial injection administration, and can prolong the duration of drug actions, thereby providing a better treatment means for medical care personnel and patients. The production technology is simple and suitable for industrial mass production.

Description

Technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and specifically relates to a pharmaceutical composition containing tamsulosin and its application in preparing a medicine for treating urination disorders, especially urination disorders caused by prostate hyperplasia. Background technique [0002] Tamsulosin (Tamsulosin) is α 1a -Receptor blockers, developed by Japan's Yamanouchi Pharmaceutical Company. The molecular formula of tamsulosin is C 20 H 28 N 2 O 5 S, molecular weight is 444.965, chemical name: (R)-5-{2-[2(2-ethoxyphenoxy)ethylamino]-2-methylethyl}-2-methoxybenzene Sulfonamide ((R)-5-{2-[2(2-ethoxyphenoxy)ethylamino]-2-methylethyl)-2-methoxybenzenes ulfonamide). The compound of tamsulosin and its pharmaceutically acceptable salt were first disclosed in Japanese Patent Publication No. 56-110665. [0003] The structural formula of tamsulosin is as follows: [0004] [0005] The pharmacological effects of tamsulosin or its...

Claims

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Application Information

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IPC IPC(8): A61K31/18A61K47/34A61K47/08A61K47/12A61K47/22A61K47/28A61K47/26A61K47/20A61K9/02A61P13/00A61K47/14
Inventor 张立英陈凤仪
Owner 张立英
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