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Dripping pills of lofexidine hydrochloride and its preparation method

A technology of lofexidine hydrochloride and dropping pills, which is applied in the field of pharmaceutical preparations and its preparation, can solve the problems affecting the therapeutic effect of lofexidine hydrochloride, low dissolution rate and dissolution rate, and large proportion of excipients, and achieve the goal of carrying And the effect of taking convenience, improving dissolution rate and dissolution rate, and reducing the amount of excipients

Inactive Publication Date: 2005-01-26
HONGYI SCI & TECH CO LTD NANCHANG
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Lofexidine hydrochloride is easily soluble in water, but its tablet disintegration time is long, the dissolution rate and dissolution rate are low, the absorption is poor, the bioavailability is low, and the proportion of excipients is large. Children, the elderly, bedridden patients and patients with dysphagia Inconvenient to take, poor compliance, affecting the therapeutic effect of lofexidine hydrochloride

Method used

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  • Dripping pills of lofexidine hydrochloride and its preparation method

Examples

Experimental program
Comparison scheme
Effect test

example 1

[0054] prescription:

[0055] Lofexidine Hydrochloride 0.2g

[0056] Macrogol 6000 20g

[0057] Makes 1000 capsules

[0058] Preparation method: Take lofexidine hydrochloride fine powder that has been ultrafinely pulverized and passed through a 200-mesh sieve, add it to the molten polyethylene glycol 6000 matrix, stir well, use simethicone as a coolant, make pellets by drop method, dry, Instantly.

example 2

[0060] prescription:

[0061] Lofexidine Hydrochloride 0.2g

[0062] Macrogol 4000 20g

[0063]Makes 1000 capsules

[0064] Preparation method: Take lofexidine hydrochloride fine powder that has been superfinely pulverized and passed through 200 sieves, add it to the molten polyethylene glycol 4000 matrix, stir well, use simethicone as coolant, make pellets by drop method, and dry, that is have to.

example 3

[0066] prescription:

[0067] Lofexidine Hydrochloride 0.2g

[0068] Macrogol 6000 10g

[0069] Macrogol 4000 10g

[0070] Makes 1000 capsules

[0071] Preparation method: Take lofexidine hydrochloride fine powder that has been ultrafinely pulverized and passed through 200 sieves, add it to the molten mixed matrix of polyethylene glycol 4000 and polyethylene glycol 6000, stir well, use simethicone as coolant, drop The preparation method is to make pills, dry them, and obtain them.

[0072] 4. Example 4

[0073] prescription:

[0074] Lofexidine Hydrochloride 0.2g

[0075] Glyceryl monostearate 20g

[0076] Makes 1000 capsules

[0077] Preparation method: Take lofexidine hydrochloride fine powder that has been ultrafinely pulverized and passed through a 200-mesh sieve, add it to the molten glyceryl monostearate matrix, mix well, use ice water as a coolant, make pellets by dropping, dry, and have to.

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Abstract

The invention relates to an Lofexidine Hydrochloride drop pill prepared by utilizing ultramicro disintegration and drop pill manufacturing process, which has the advantages of improving collapse and dissolving speed, dissolving out speed and degree, quick effect, increased medicament stability, reduced adjuvant consumption, lowered production costs, and easiness in carrying and use. oral or swallow administration, it has good compliance, thus is especially suitable for children, the elderly, bedridden patients and dysphagia patients.

Description

technical field [0001] The invention relates to a pharmaceutical preparation and a preparation method thereof, in particular to lofexidine hydrochloride dropping pills and a preparation method thereof. Background technique [0002] Lofexidine hydrochloride is an imidazoline derivative, similar in structure and effect to clonidine, and selectively stimulates the central nervous system α 2 Receptors, reduce the activity of peripheral sympathetic nerves, inhibit the release of norepinephrine, relax vascular smooth muscle, and produce blood pressure lowering effects. [0003] Opioids can inhibit the activity of central noradrenergic neurons. When quitting opioids or narcotics, the inhibition of this neuron is suddenly removed, resulting in hyperactivity, resulting in opioid withdrawal syndrome. Lofexidine hydrochloride can counteract this effect, so the use of lofexidine hydrochloride can reduce the intensity and duration of heroin withdrawal syndrome. [0004] use 14 C The ...

Claims

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Application Information

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IPC IPC(8): A61K9/20A61K31/4164A61P9/12
Inventor 钱进许军彭红李平朱丹刘孝乐
Owner HONGYI SCI & TECH CO LTD NANCHANG