Pulsatile pellet, pulsatile orally disintegrating tablet containing same, and preparation methods and applications thereof

A technology of pulse pellets and disintegrants, which is applied in the direction of medical preparations containing active ingredients, medical preparations with inactive ingredients, pill delivery, etc., which can solve the problem that the dosage cannot be adjusted according to the needs of the disease, and the pulse tablets cannot be combined with the oral cavity. The function of disintegration, the inability of the coating material to be separated, etc.

Inactive Publication Date: 2011-11-09
SHANGHAI INST OF PHARMA IND +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The technical problem to be solved by the present invention is to overcome the fact that the existing pulse tablets cannot have the function of oral disintegration, and the coating material cannot be divided so that the dose cannot be adjusted according to the needs of the disease, and the poor compressibility of the coating can only be made into a high-cost tablet. Capsules that are not easy to swallow, or need to be coated with double-layer coating layers containing sustained-release materials to achieve the effect of regular drug delivery, provide a pulsed pellet and a preparation method thereof, and the pulsed pellet The prepared new pharmaceutical dosage form-pulse orally disintegrating tablet, its preparation method and application

Method used

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  • Pulsatile pellet, pulsatile orally disintegrating tablet containing same, and preparation methods and applications thereof
  • Pulsatile pellet, pulsatile orally disintegrating tablet containing same, and preparation methods and applications thereof
  • Pulsatile pellet, pulsatile orally disintegrating tablet containing same, and preparation methods and applications thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0046] Embodiment 1 prepares diclofenac sodium pulse pellets

[0047] 1. Pack drug layer

[0048] Add 7g of polyvinylpyrrolidone PVP VA64 and 42g of diclofenac sodium into 280ml of 75% (v / v) ethanol to make a medicinal solution, wherein the concentration of diclofenac sodium is 15g / 100ml, and the concentration of binder PVP VA64 is 2.5% (wt). Place 100 g of microcrystalline cellulose blank cores with an average particle size of 0.15 mm in a fluidized bed for 10 minutes, and slowly spray the drug solution on the surface of the cores. The operating conditions of the tangential spray fluidized bed are: the fan frequency is 20-23Hz; the material temperature is 33-35°C; the rotation frequency of the turntable is 100-150rpm; the atomization pressure of the atomizing spray gun is 0.09-0.11MPa; The liquid spray speed is 12~15g / min.

[0049] 2. Pack swelling layer

[0050]80g sodium carboxymethylcellulose, 30g hydroxypropylmethylcellulose T5 and 75% (v / v) ethanol 1000ml are added, s...

Embodiment 2

[0060] Example 2 Tablet Preparation of Diclofenac Sodium Pulse Orally Disintegrating Tablets

[0061] 1. The formula of one pulse orally disintegrating tablet is shown in Table 2, the unit is mg:

[0062] Table 2

[0063]

[0064] 2. The preparation method of pulse orally disintegrating tablets is as follows:

[0065] The diclofenac sodium pulse pellets obtained in Example 1 were passed through a 60 mesh sieve, and the formula in Table 2 was directly compressed with a tablet machine, and the tablet hardness was 3kg.

[0066] Take the pulse pellet orally disintegrating tablet, according to the "Pharmacopoeia of the People's Republic of China" (2005 edition two appendix XC first method rotating basket method, 100rpm, 37 ℃), with 0.1mol L-1HCl as the first 2 hours of release Medium, the volume of the medium is 750ml, and 250ml of 0.2mol·L-1 sodium phosphate solution is added in 2 hours. Sampling at certain time intervals (simultaneously replenishing medium at the same tempe...

Embodiment 3

[0067] Embodiment 3 prepares nifedipine pulse pellet

[0068] 1. Pack drug layer

[0069] 8.3g of polyvinylpyrrolidone PVP S630 and 25g of nifedipine were added to 300ml of water to make a drug solution, wherein the concentration of nifedipine was 8.3g / 100ml, and the concentration of binder PVP VA64 was 2.8% (wt). Place 150g of starch blank cores with an average particle size of 0.1 mm in a fluidized bed for 10 minutes, and slowly spray the drug solution on the surface of the cores. The operating conditions of the tangential spray fluidized bed are: the fan frequency is 20-23Hz; the material temperature is 33-35°C; the rotation frequency of the turntable is 100-150rpm; the atomization pressure of the atomizing spray gun is 0.09-0.11MPa; The liquid spray speed is 12~15g / min.

[0070] 2. Pack swelling layer

[0071] With 42g sodium carboxymethyl starch, 21g hydroxypropyl methylcellulose T5 and adding in 75% (v / v) ethanol 400ml, slowly spray on the upper pill core of gained in...

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Abstract

The invention relates to a pulsatile pellet which comprises 20-40% of blank pellet core, 5-30% of drug layer, 8-25% of swelling layer, 5-12% of retardant layer, 20-40% of acid layer and 15-40% of stagnant layer from the inside to the outside sequentially, wherein the stagnant layer comprises 55-75% of sustained-release material, 10-35% of anti-sticking agent and 5-20% of plasticizer; the sustained-release material is a terpolymer formed by ethyl acrylate, methyl methacrylate and trimethylamine chloride ethyl methacrylate; the average particle diameter of the blank pellet core is 0.1-0.3mm; and the acid layer comprises an organic acid and an adhesive. The invention also provides a preparation method of the pulsatile pellet, a pulsatile orally disintegrating tablet containing the pulsatile pellet, and a preparation method and application thereof. The pulsatile orally disintegrating tablet provided by the invention has both pulsatile and orally disintegrating functions, is especially suitable for administration for daily rhythmicity disease, reduces the drug side effect, has low production cost and is favorable to swallowing.

Description

technical field [0001] The present invention relates to the field of pharmaceutical preparations, in particular to a pulsed pellet and a preparation method thereof, a pulsed orally disintegrating tablet prepared by using the pulsed pellet and a preparation method thereof, and the pulsed orally disintegrating tablet in the preparation of treatment or prevention day and night Use in drugs for rhythm disorders. Background technique [0002] With the development of chronopharmacology, people have learned that many common diseases show similar diurnal fluctuations, such as asthma, arthritis, angina pectoris, hypertension, gastric ulcer, etc., have the highest attack frequency in the morning. For this circadian rhythmic disease, the traditional practice is to administer common preparations multiple times at night to maintain effective blood drug levels or to administer sustained-release preparations once. However, the disadvantage of this method is that the patient's compliance i...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K47/32A61K47/38A61K45/00A61P11/06A61P19/02A61P9/10A61P9/12A61P1/00A61P7/02
Inventor 任麒刘丽媛
Owner SHANGHAI INST OF PHARMA IND
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