CN101653423A - Lacidipine tablets and preparation method thereof - Google Patents
Lacidipine tablets and preparation method thereof Download PDFInfo
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- CN101653423A CN101653423A CN200910072887A CN200910072887A CN101653423A CN 101653423 A CN101653423 A CN 101653423A CN 200910072887 A CN200910072887 A CN 200910072887A CN 200910072887 A CN200910072887 A CN 200910072887A CN 101653423 A CN101653423 A CN 101653423A
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- lacidipine
- lactose
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- magnesium stearate
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Abstract
The invention provides lacidipine tablets and a preparation method thereof. The lacidipine tablets comprise 1-4% of lacidipine, 14-32% of hydroxypropyl cellulose or microcrystalline cellulose, 1-3% ofpoloxamer or sodium dodecyl sulfate or povidone or copovidone, 0.25-2% of magnesium stearate and the balance of lactose by weight percent, and the preparation method comprises the following steps ofevenly mixing raw material of the lacidipine with the lactose according to the weight ratio of 1:1 after ultra-fine smashing, further evenly mixing the mixture with the balance of the lactose and thehydroxypropyl cellulose or the microcrystalline cellulose, adding a water solution bonding agent prepared by the poloxamer or the odium dodecyl sulfate or the povidone or the copovidone, preparing appropriate soft materials, passing a 18-mesh sieve for granulation, drying at the temperature of 40-60 DEG C, passing a 16-mesh sieve for size stabilization, adding the magnesium stearate, evenly mixingand pressing tablets, thereby preparing products. The method can effectively improve the dissolution of the lacidipine tablets and lead the evenness index to achieve the more ideal value. The methodcan further improve the bioavailability of the lacidipine tablets and has the advantages of fast absorption, convenient administration and significant efficacy.
Description
(1) technical field
The present invention relates to a kind of medicine, the present invention also relates to a kind of preparation method of medicine, specifically a kind of Lacidipine tablets and preparation method thereof.
(2) background technology
Lacidipine is a kind of dihydropyridine class calcium antagonist, this medicine energy strong inhibition calcium channel, and to blood vessel selectivity height, hypotensive effect longer duration, particularly every day are only taken once (4-6mg), have efficient and long lasting antihypertensive activity.Lacidipine has determined curative effect as the hypertensive ideal medicament of treatment, and to blood vessel selectivity height, hypotensive effect is lasting, and toxic and side effects is little, and is cheap, takes the few advantages such as (only obeying a slice every day) of number of times.
Because lacidipine belongs to low dose of, insoluble drug, adopt the dissolution and the uniformity index of the Lacidipine tablets that traditional tablet manufacturing prepared goes out all not to reach comparatively ideal numerical value.And adopt the solvent dispersion method to prepare Lacidipine tablets, and the one, just can make it molten entirely with the ethanol of q.s, but the soft material of making like this is soft excessively, the 2nd, use the solvent dispersion method, the lacidipine soluble component moves, and makes uniformity of dosage units defective, thereby influences the curative effect of product.
(3) summary of the invention
The object of the present invention is to provide a kind of bioavailability, and absorb soon the Lacidipine tablets of taking convenience.The present invention also aims to provide a kind of and can improve the dissolution of Lacidipine tablets effectively, and make uniformity index reach comparatively ideal numerical value, improve the preparation method of Lacidipine tablets of the bioavailability of Lacidipine tablets from face.
The object of the present invention is achieved like this:
Lacidipine tablets of the present invention is that percentage by weight is lacidipine 1-4%, hyprolose or microcrystalline Cellulose 14-32%, poloxamer or sodium lauryl sulphate or polyvidone or copolyvidone 1-3%, the lactose of magnesium stearate 0.25-2% and surplus, with lacidipine raw material and lactose is mix homogeneously after 1: 1 micronizing by weight, mixture again with the lactose of remainder, hyprolose or microcrystalline Cellulose mix homogeneously, the aqueous solution binding agent that adding is mixed with poloxamer or sodium lauryl sulphate or polyvidone or copolyvidone, make suitable soft material, crossing 18 mesh sieves granulates, 40-60 ℃ of drying, 16 mesh sieve granulate, add magnesium stearate, the product that mixing, tabletting are made.
Product of the present invention is to adopt following method preparation:
The percentage by weight of raw material constitutes: the lactose of lacidipine 1-4%, hyprolose or microcrystalline Cellulose 14-32%, poloxamer or sodium lauryl sulphate or polyvidone or copolyvidone 1-3%, magnesium stearate 0.25-2% and surplus;
With lacidipine raw material and lactose is mix homogeneously after 1: 1 micronizing by weight, mixture again with lactose, hyprolose or the microcrystalline Cellulose mix homogeneously of remainder; Adding is made suitable soft material with the aqueous solution binding agent that poloxamer or sodium lauryl sulphate or polyvidone or copolyvidone are mixed with, and cross 18 mesh sieves and granulate, 40-60 ℃ of drying, 16 mesh sieve granulate add magnesium stearate, mixing, tabletting is made product.
Lactose among the present invention is a filler, and hyprolose or microcrystalline Cellulose are disintegrating agent, and poloxamer or sodium lauryl sulphate or polyvidone or copolyvidone are surfactant, and magnesium stearate is a lubricant.
Solid preparation all needed the process through stripping before the arrival biomembrane is absorbed, the speed and the degree of this process decision medicine absorption in vivo.The dissolution rate of the oral solid formulation of the insoluble drug that lacidipine is such is just bigger to the absorption and the curative effects of medicine.According to Nernst-Noyes-Whitney equation: dc/dt=KS (Cs-C)=DS (Cs-C)/V δ, (K is the dissolution rate constant, D is the diffusion coefficient of stripping medicine, V is the volume of dissolution medium, δ is for being the thickness of diffusion layer the solution of C from the saturated solution surface to concentration, and S is the contact area between solid drugs and the body fluid, and Cs is the concentration of the saturated solution that forms of solid surface layer, be the dissolubility of solid drugs, the concentration of medicine in bulk solution when C is time t).From then on can promptly use the big fine drug powder of dispersion with the method for the solubility property that improves medicine and increase medicine and body fluid contact surface to the slightly solubility solid drugs as can be seen in the equation, can improve dissolution rate, thereby increase medicine absorption in vivo amount.From the micromeritis angle is exactly the specific surface area that increases medicine, and the little then specific surface area of particle is big, and solubility property is good.In other words, the dissolving release of solid drugs, body absorb and bioavailability all with the preparation processing process in the miniaturization of powder body substantial connection is arranged.Therefore, concerning the medicine of poorly water-solubles such as lacidipine, the ultra micro efflorescence is to improve one of effective way of its bioavailability.
The main body of method of the present invention is to adopt micronizing equipment, and in the process of pulverizing, adds the special adjuvant of specific composition, with lacidipine raw material micronization.
The principle of micronizing is in micronizing equipment in the lacidipine piece preparation method, and the lacidipine raw material is fully ground, mixes with the special formulation adjuvant.The adjuvant of special formulation can form hydrogen bonded with lacidipine, stops reassociating of drug particle, makes medicine then moistening or disintegrate rapidly when contacting with water or gastric juice, improves drug solubility, improves the dissolution of medicine greatly.This technology make the Lacidipine tablets dissolution by 80% original (average number) be increased to after the improvement more than 85%, part batch reaches more than 89%.
Adopt superfine communication technique with lacidipine and the common micropowder of adjuvant, solved the phenomenon that light, thermo-responsive raw material pulverizing process content are reduced, effectively kept pharmaceutically active, made the key index dissolution that affects the treatment, the uniformity all improves a lot, and has improved the curative effect of medicine.
The inventive method can improve the dissolution of Lacidipine tablets effectively, and makes uniformity index reach comparatively ideal numerical value.Improved the bioavailability of Lacidipine tablets from face, and absorbed soon, taking convenience, evident in efficacy.
(4) specific embodiment
For example the present invention is done in more detail below and describes:
Embodiment one:
Proportioning raw materials:
Lacidipine 4g
Lactose 133g
Hyprolose 62g
Poloxamer 4.4g
Magnesium stearate 0.6g
Preparation method:
1, takes by weighing poloxamer 4.4g, be dissolved in the 50-70g purified water, be prepared into binding agent;
2, be 1: 1 micronizing by weight with lacidipine raw material and lactose, mix homogeneously, mixture again with lactose, the hyprolose mix homogeneously of remainder, add the binding agent made from poloxamer, make suitable soft material, crossing 18 mesh sieves granulates, 40-60 ℃ of drying, 16 mesh sieve granulate add magnesium stearate, mixing is pressed into 1000.
Embodiment two:
Proportioning raw materials:
Lacidipine 6g
Lactose 98g
Hyprolose 93g
Poloxamer 6.1g
Magnesium stearate 0.9g
Preparation method is with the specific embodiment one.
Embodiment three:
Proportioning raw materials:
Lacidipine 2g
Lactose 168g
Hyprolose 31g
Poloxamer 2.4g
Magnesium stearate 0.6g
Preparation method is with the specific embodiment one.
Embodiment four:
Proportioning raw materials:
Lacidipine 4g
Lactose 140g
Hyprolose 56g
Sodium lauryl sulphate 3g
Magnesium stearate 1g
Preparation method is with the specific embodiment one.
Embodiment five:
Proportioning raw materials:
Lacidipine 6g
Lactose 128g
Hyprolose 64g
Sodium lauryl sulphate 5g
Magnesium stearate 1g
Preparation method is with the specific embodiment one.
Embodiment six:
Proportioning raw materials:
Lacidipine 4g
Lactose 136g
Microcrystalline Cellulose 60g
Poloxamer 3g
Magnesium stearate 1g
Preparation method is with the specific embodiment one.
Embodiment seven:
Proportioning raw materials:
Lacidipine 6g
Lactose 135g
Microcrystalline Cellulose 58g
Poloxamer 3g
Magnesium stearate 2g
Preparation method is with the specific embodiment one.
Embodiment eight:
Lacidipine 4g
Lactose 139g
Microcrystalline Cellulose 56g
Sodium lauryl sulphate 4g
Magnesium stearate 1g
Preparation method is with the specific embodiment one.
Embodiment nine:
Proportioning raw materials:
Lacidipine 6g
Lactose 141g
Microcrystalline Cellulose 52g
Sodium lauryl sulphate 3g
Magnesium stearate 2g
Preparation method is with the specific embodiment one.
Embodiment ten:
Proportioning raw materials:
Lacidipine 4g
Lactose 153g
Hyprolose 42g
Polyvidone 4g
Magnesium stearate 1g
Preparation method is with the specific embodiment one.
Embodiment 11:
Proportioning raw materials:
Lacidipine 6g
Lactose 143g
Hyprolose 52g
Polyvidone 2.2g
Magnesium stearate 0.8g
Preparation method is with the specific embodiment one.
Embodiment 12:
Proportioning raw materials:
Lacidipine 6g
Lactose 145g
Microcrystalline Cellulose 48g
Copolyvidone 3.2g
Magnesium stearate 1.8g
Preparation method is with the specific embodiment one.
Claims (2)
1, a kind of Lacidipine tablets, it is characterized in that: be that percentage by weight is lacidipine 1-4%, hyprolose or microcrystalline Cellulose 14-32%, poloxamer or sodium lauryl sulphate or polyvidone or copolyvidone 1-3%, the lactose of magnesium stearate 0.25-2% and surplus, with lacidipine raw material and lactose is mix homogeneously after 1: 1 micronizing by weight, mixture again with the lactose of remainder, hyprolose or microcrystalline Cellulose mix homogeneously, the aqueous solution binding agent that adding is mixed with poloxamer or sodium lauryl sulphate or polyvidone or copolyvidone, make suitable soft material, crossing 18 mesh sieves granulates, 40-60 ℃ of drying, 16 mesh sieve granulate, add magnesium stearate, the product that mixing, tabletting are made.
2, a kind of preparation method of Lacidipine tablets is characterized in that:
The percentage by weight of raw material constitutes: the lactose of lacidipine 1-4%, hyprolose or microcrystalline Cellulose 14-32%, poloxamer or sodium lauryl sulphate or polyvidone or copolyvidone 1-3%, magnesium stearate 0.25-2% and surplus;
With lacidipine raw material and lactose is mix homogeneously after 1: 1 micronizing by weight, mixture again with lactose, hyprolose or the microcrystalline Cellulose mix homogeneously of remainder, the aqueous solution binding agent that adding is mixed with poloxamer or sodium lauryl sulphate or polyvidone or copolyvidone, make suitable soft material, cross 18 mesh sieves and granulate 40-60 ℃ of drying, 16 mesh sieve granulate, add magnesium stearate, mixing, tabletting is made product.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN200910072887A CN101653423A (en) | 2009-09-15 | 2009-09-15 | Lacidipine tablets and preparation method thereof |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN200910072887A CN101653423A (en) | 2009-09-15 | 2009-09-15 | Lacidipine tablets and preparation method thereof |
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| CN101653423A true CN101653423A (en) | 2010-02-24 |
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| CN200910072887A Pending CN101653423A (en) | 2009-09-15 | 2009-09-15 | Lacidipine tablets and preparation method thereof |
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Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102198107A (en) * | 2011-05-18 | 2011-09-28 | 浙江贝得药业有限公司 | Lacidipine dispersible tablets and preparation method thereof |
| CN104224736A (en) * | 2013-06-21 | 2014-12-24 | 哈药集团三精制药股份有限公司 | Preparation method of simvastatin tablet |
| CN106822005A (en) * | 2015-12-03 | 2017-06-13 | 江苏先声药业有限公司 | Shellfish cholic acid composition difficult to understand and preparation method thereof |
-
2009
- 2009-09-15 CN CN200910072887A patent/CN101653423A/en active Pending
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102198107A (en) * | 2011-05-18 | 2011-09-28 | 浙江贝得药业有限公司 | Lacidipine dispersible tablets and preparation method thereof |
| CN102198107B (en) * | 2011-05-18 | 2012-11-21 | 浙江贝得药业有限公司 | Lacidipine dispersible tablets and preparation method thereof |
| CN104224736A (en) * | 2013-06-21 | 2014-12-24 | 哈药集团三精制药股份有限公司 | Preparation method of simvastatin tablet |
| CN106822005A (en) * | 2015-12-03 | 2017-06-13 | 江苏先声药业有限公司 | Shellfish cholic acid composition difficult to understand and preparation method thereof |
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Application publication date: 20100224 |