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Sarpogrelate hydrochloride sustained release pellet and preparation method thereof

A technology of sarpogrelate hydrochloride and sustained-release pellets is used in pharmaceutical formulations, medical preparations containing active ingredients, and devices for making medicines into special physical or taking forms, etc. problems such as pellet processing properties, to achieve the effect of low friability, controllable quality and high yield

Active Publication Date: 2012-07-11
JINLING PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0018] At present, there is no report on the addition of surfactants to the pellet formula to improve the processing properties of the pellets and further coating to prepare sagrelate hydrochloride sustained-release pellets

Method used

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  • Sarpogrelate hydrochloride sustained release pellet and preparation method thereof
  • Sarpogrelate hydrochloride sustained release pellet and preparation method thereof
  • Sarpogrelate hydrochloride sustained release pellet and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0083] Embodiment 1: the main factor that affects the forming of pill core containing medicine

[0084] In this example, in the case of the selected drug, the solubility of the active ingredient (vitamin C (0.2g / ml, easily soluble), sarcogrelate hydrochloride (0.02g / ml, slightly soluble)), the excipient (microcrystalline cellulose), wetting agent (20% ethanol), surfactant (polysorbate 80), wetting time of soft material (min), extrusion frequency (HZ), sieve aperture (mm), 9 variables such as spheronization time (min), drying temperature (°C), and 2 dummy variables (Dummy) were designed in P-B experiment (N=12) to investigate the main factors affecting the formation of drug-containing pellet cores. Wherein, the amount of the active ingredient is the weight ratio of the active ingredient to (the sum of the active ingredient and the excipient), and the amount of the excipient is the weight ratio of the excipient to the (the sum of the active ingredient and the excipient). The am...

Embodiment 2

[0097] Embodiment 2: Surfactant is to the influence of important procedure in the processing of core containing pill

[0098] In this embodiment, vitamin C (easy to dissolve), taurine (dissolved), and bromamide hydrochloride (slightly soluble) were respectively used as active ingredients with microcrystalline cellulose (excipient), 20% ethanol (moisturized wet agent) to form the basic formula, adding and (active substance+excipient) weight percent is 0, 1, 2, 3, 4, 6, 7% surfactant (polysorbate 80 ) to form a series of formulas (the active ingredient of formula 1 is vitamin C, the active ingredient of formula 2 is taurine, and the active ingredient of formula 3 is bromamide hydrochloride), according to the "preparation method" and "process parameters" in the "example description" Prepare the bar, observe and calculate the shape of the bar and the yield per unit time, and drop the bar naturally into a 1-meter square plate, shake it gently and transfer it to an electric blast dr...

Embodiment 3

[0112] Containing pill core formula: parts by weight

[0113] Active ingredient: 79.5 parts of sarcogrelate hydrochloride

[0114] Excipient 1: 20 parts of microcrystalline fiber

[0115] Excipient 2: Hypromellose 0.5 parts

[0116] Surfactant: 2.5 parts of polyoxyethylene (40) hydrogenated castor oil

[0117] Wetting agent: 20% ethanol 20 parts

[0118] Coating solution formula (according to 100 parts by weight containing pill core):

[0119] 10% Surelease Water dispersion 100 parts

[0120] Note: 10% Surelease Aqueous dispersion Ethyl cellulose aqueous dispersion.

[0121] Preparation process: Prepare three batches of micropills according to the "Example Description" and the above formula. The quality evaluation results are shown in Table 6 below, and the properties of the micropills are shown in Table 6. diagram 2-1 , 2-2 , 2-3.

[0122] Table 6: Ball core quality evaluation

[0123] Evaluation index / batch

[0124] Comprehensive form factor (e...

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Abstract

The invention belongs to the field of medicinal preparation and discloses a sarpogrelate hydrochloride sustained release pellet and a preparation method thereof. The pellet is prepared by coating a sustained release coat on a medicine contained pellet core, wherein the formula of the medicine contained pellet core comprises the following raw materials in parts by weight: 75-100 parts of sarpogrelate hydrochloride and 0-25 parts of excipient, wherein the total weight part of the sarpogrelate hydrochloride and the excipient is 100 or the weight parts of the sarpogrelate hydrochloride and the excipient are increased or reduced by the same ratio; a surfactant accounts for 0.1-8% of the total weight of the sarpogrelate hydrochloride and the excipient; and a wetting agent accounts for 0.1-30% of the total weight of the sarpogrelate hydrochloride and the excipient. By using the preparation method disclosed by the invention, the medicine contained pellet core with low friability, higher yield, smaller particle size and smooth surface can be obtained; the pellet core is convenient to be further processed; according to the invention, the medicine contained pellet core is coated with the sustained release coat so as to obtain a potassium citrate sustained release pellet; and the pellet has the advantages of controllable and stable quality in vitro and sustained release characteristics in vivo.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to sargrelate hydrochloride sustained-release pellets and a preparation method thereof. Background technique [0002] Pellets generally refer to spherical or spherical preparations with a diameter between 0.5-1.5 mm. As a multi-unit drug delivery system, compared with traditional single-dose drug delivery systems such as ordinary tablets, pellets, especially sustained-release pellets, have the following advantages: ①After entering the body, they are quickly distributed throughout the gastrointestinal tract. The dose is evenly dispersed in a single pellet, and the contact area between the drug and the gastrointestinal tract is greatly increased, thereby improving the bioavailability and reducing the irritation of some drugs to the gastrointestinal tract; ②The gastric emptying time of ordinary tablets is generally between 120-640min, while the micropill is 120-180min, so the ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K31/225A61J3/06A61J9/00A61P7/02
Inventor 黄春玉戴银娣邢芸薛斐张庆晓万辉姬晓燕
Owner JINLING PHARMA
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