Zolmitriptan tongue tablet

A zolmitriptan and sublingual tablet technology, which is applied in the direction of non-active ingredient medical preparations, pill delivery, organic active ingredients, etc., can solve the problem of unsatisfactory drug absorption, nasal cavity irritation, and low bioavailability and other problems to achieve the effect of avoiding the first-pass effect, taking and carrying convenience, and high bioavailability

Inactive Publication Date: 2008-05-21
重庆医科大学医药研究所
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But there are following deficiencies: 1. Oral tablets, capsules and dispersible tablets are easy to use and low in cost, but their effects are slow, and it is difficult for patients with nausea symptoms to take, and they need to be absorbed into the blood through the gastrointestinal tract to take effect. Therefore, the onset of action is slow; and due to the first-pass effect, the absorption rate is not high; ② orally disintegrating tablets do not need to be taken with water after administration, but they also need to be absorbed through the gastrointestinal tract, and the onset of action is also slow. There will also be a first-pass effect; ③nasal spray has an irritating effect on the nasal cavity and a bitter taste in the mouth. When used improperly, the drug absorption effect is not satisfactory and it is relatively expensive
However, studies have shown that zolmitriptan is poorly absorbed orally and has low bioavailability, greatly reducing its effectiveness in clinical use

Method used

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  • Zolmitriptan tongue tablet

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Embodiment 1: a kind of zolmitriptan sublingual tablet, it is made by zolmitriptan 2.5, powdered sugar 40, lactose 20, sodium carboxymethyl starch 2, magnesium stearate 1, all in parts by weight count.

[0029] The specific preparation method is as follows: the above-mentioned main drug zolmitriptan, filler sugar powder, lactose, disintegrant sodium carboxymethyl starch and lubricant magnesium stearate are dried, pulverized, and sieved for pretreatment; Mix the pretreated main ingredients, fillers and disintegrants, use pure water as a binder to make the mixed material into a soft material, and granulate it with a 20-mesh sieve; and dry it at 60°C until it meets the moisture content ≤3%; then add the lubricant to the dry granules obtained above, carry out total mixing, and finally compress into tablets to obtain zolmitriptan sublingual tablets.

Embodiment 2

[0030] Embodiment 2: a zolmitriptan sublingual tablet, which consists of zolmitriptan 2.5, lactose 30, microcrystalline cellulose 30, sucralose 2, cross-linked polyvinylpyrrolidone 3, magnesium stearate 1, Micronized silica gel 1 is made, and all count parts by weight.

[0031] The specific preparation method: the above-mentioned components are pretreated by drying, pulverizing, and sieving, and then directly compressed into tablets after mixing to obtain zolmitriptan sublingual tablets.

Embodiment 3

[0032] Example 3: A zolmitriptan sublingual tablet, composed of zolmitriptan 5, xylitol 20, microcrystalline cellulose 30, stevioside 3, lactose 40, low-substituted hydroxypropyl cellulose 3, poly Ethylene glycol 6000 1, all in parts by weight.

[0033] The specific preparation method is as follows: dry, pulverize, and sieve the above components for pretreatment, then mix the components except polyethylene glycol 6000 evenly, use a dry granulator to make 20-mesh granules, and then add polyethylene glycol Alcohol 6000, tableted, made zolmitriptan sublingual tablet.

[0034] Components and consumptions selected in Table 1 Examples 4-16 (by weight)

[0035]

[0036] Microcrystalline Cellulose-

[0037] Talc powder

[0038] The invention utilizes the non-keratinized sublingual mucosa, rich capillaries and fast blood flow, and is an ideal site for drug absorption. Due to the slow onset of oral administration of zolmitriptan, the bioavailability is not high. ...

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PUM

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Abstract

The invention provides a zolmitriptan sublingual tablet, which is characterized in that it contains the main drug zolmitriptan, a disintegrating agent and a filler. In every 1000 sublingual tablets, the content of zolmitriptan is 1 -50g, the content of disintegrating agent is 2-20g, the content of filler is 40-200g; it also contains 0-20g of corrective agent, 10-60g of binder and 0.5-5g of lubricant. The present invention utilizes the characteristics of non-keratinized sublingual mucosa, rich capillaries, and fast blood flow, aiming at the absorption of zolmitriptan ordinary tablets through the gastrointestinal tract, slow onset of action, first-pass effect, and low bioavailability. The deficiencies of advanced prior art, zolmitriptan is made into sublingual tablet, can make it absorb through sublingual mucosa, directly enter blood circulation through jugular vein and superior vena cava, take effect rapidly; Avoid oral administration The first-pass effect improves bioavailability and ensures curative effect. Moreover, water is not needed when taking the medicine, and it is placed under the tongue to contain it, so it is convenient to take and has a good taste. With the characteristics of rapid onset of action, convenient administration and high bioavailability, it can provide patients with a new treatment option and fill the gap in the market.

Description

technical field [0001] The invention relates to a zolmitriptan sublingual tablet, in particular to a zolmitriptan sublingual tablet preparation and a preparation method thereof which are used for treating migraine and mainly absorb quickly through sublingual mucosa. Background technique [0002] Zolmitriptan is a selective serotonin (5-HT 1 ) receptor agonist, which is a new generation of triptan drugs after sumatriptan. In addition, pharmacological studies have confirmed that zolmitriptan can act on extracerebral arteries and intracranial arteries, and inhibit the excessive expansion of these blood vessels. When migraine attacks, the patient is very painful and can seriously affect the social life of the patient. Therefore, Western pathologists call it "a mental torture disease". Therefore, proper treatment is critical. The etiology of migraine is complex. At present, the academic community generally believes that the dysfunction of the trigeminal nerve and blood vessels...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/422A61K9/28A61K47/38A61P25/06
Inventor 黄华
Owner 重庆医科大学医药研究所
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