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Tropisetron pharmaceutical composition

A technology of tropisetron and tropisetron hydrochloride, which is applied in the field of tropisetron pharmaceutical compositions, can solve the problems of poor patient compliance, many adverse reactions, and low bioavailability, so as to improve compliance and reduce The frequency of medication and the effect of guaranteed curative effect

Active Publication Date: 2014-07-02
SHENZHEN SOUTH CHINA PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Injections have the problems of having to be administered to patients by professionals, inconvenient medication, and short half-life of drugs that require continuous administration for a long time
However, common oral preparations have the following disadvantages: (1) low bioavailability, short half-life, requiring multiple medications; (2) poor compliance of patients, and the vomiting caused by radiotherapy and chemotherapy is very severe, which makes it impossible to use conventional oral administration. (3) There are many adverse reactions, such as headache, dizziness, constipation, dizziness, fatigue and gastrointestinal dysfunction such as abdominal pain and diarrhea.
But the weak point of this composition preparation is: although do not need to drink water when taking medicine, but tropisetron hydrochloride oral mucosa penetration rate is low, and this invention does not provide that the tropisetron hydrochloride in this composition removes complete setron oral mucosa Therefore, it is an immediate-release oral drug formulation, and it is still difficult to avoid the loss of the administered dose due to vomiting

Method used

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  • Tropisetron pharmaceutical composition
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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0043] Embodiment 1: Tropisetron hydrochloride pharmaceutical composition, the prescription is composed as follows:

[0044]

[0045] Preparation:

[0046] Take Carbomer 974P, add water and stir to disperse, continue to stir until completely dissolved, add tropisetron hydrochloride, 1-methyl-4-isopropylcyclohexan-3-ol, methylparaben, paraben After the gold propane is completely dissolved, add poloxamer and hypromellose, add water to the full amount, stir evenly, and process it through a colloid mill three times, and place it at 0~4°C until it is completely swollen. If necessary, you can use 0.1mol / l of NaOH solution and / or 0.1 mol / l of hydrochloric acid solution to adjust the pH to 3-7.

Embodiment 2

[0047] Embodiment 2: Tropisetron mesylate pharmaceutical composition, the prescription is composed as follows:

[0048]

[0049] The preparation method is the same as in Example 1, the difference is: take Carbomer 974P, add it into water and stir to disperse, keep stirring until completely dissolved, add tropisetron methanesulfonate, 1-methyl-4-isopropylcyclo After hexan-3-ol, methylparaben, and propylparaben are completely dissolved, add Poloxamer 407, hypromellose K4M, and add water to the full amount.

Embodiment 3

[0050] Embodiment 3: Tropisetron hydrochloride pharmaceutical composition, the prescription is composed as follows:

[0051]

[0052] The preparation method is the same as in Example 1, the difference is: take Carbomer 974P, add it into water and stir to disperse, keep stirring until completely dissolved, add tropisetron hydrochloride, 1-methyl-4-isopropylcyclohexyl- After 3-alcohol, methylparaben, propylparaben, and orange essence are completely dissolved, add Poloxamer 407, Poloxamer 188, and hypromellose K4M, and add water to the full amount.

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Abstract

The invention relates to a tropisetron pharmaceutical composition, which comprises tropisetron salts, carbomer, hydroxypropyl methylcellulose, poloxamer, 1-methyl-4-isopropylcyclo-3-alcohol and other additives. The tropisetron pharmaceutical composition disclosed by the invention is in the liquid state in vitro; after being used for a mouth mucosa, the tropisetron pharmaceutical composition is in the semi-solid gel state and serves as temperature-sensitive gel; the composition gel has a certain intensity and biological adhesive and can stay in a drug application position, so that drugs are continuously released; furthermore, drugs can be promoted to be absorbed through the mouth mucosa; the pharmacological effect is taken.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical preparations, in particular to a pharmaceutical composition of tropisetron. Background technique [0002] The chemical name of tropisetron is: 3-indolecarboxylic acid (8-methyl-8-azabicyclo[3.2.1]-3α-octyl) ester, which is a peripheral neuron and central nervous system serotonin A potent, highly selective competitive antagonist of the 3 (5-HT3) receptor. Certain substances, including some chemotherapeutic drugs, stimulate the release of serotonin from chromaffin-like cells in the visceral mucosa, which induces the gag reflex with nausea. This product mainly inhibits the vomiting reflex by selectively blocking the presynaptic 5-HT3 receptors of peripheral neurons. In addition, its antiemetic effect may also inhibit the area postrema by directly blocking the central 5-HT3 receptors. Stimulation of the vagus nerve. [0003] At present, there are two types of tropisetron preparations on the ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/06A61K9/12A61K31/46A61K47/38A61P1/08
Inventor 卢锦华苏宏瑞
Owner SHENZHEN SOUTH CHINA PHARMA
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