CN105213393A - A kind of niacin sustained-release preparation and preparation method - Google Patents
A kind of niacin sustained-release preparation and preparation method Download PDFInfo
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- CN105213393A CN105213393A CN201410232741.2A CN201410232741A CN105213393A CN 105213393 A CN105213393 A CN 105213393A CN 201410232741 A CN201410232741 A CN 201410232741A CN 105213393 A CN105213393 A CN 105213393A
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- lovastatin
- sustained release
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- niacin sustained
- niacin
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Abstract
The present invention relates to a kind of compound niacin sustained release tablet for blood fat reducing and preparation method, comprise niacin sustained release layer and lovastatin release layer.It is first by niacin sustained release laminate, then adds lovastatin formation lovastatin rapid release coatings by coating.The method preparation is simple, is easy to operation, and lovastatin parcel evenly, and release degree of niacin is better than ordinary preparation, is applicable to suitability for industrialized production.
Description
Technical field
The invention belongs to field of pharmaceutical preparations, specifically a kind of Lovastatin nicotinic acid slow-release preparation and preparation method.
Background technology
Nicotinic acid is also referred to as vitamin B3, or vitamin PP, and it is one of 13 kinds of vitamin of needed by human, is a kind of water soluble vitamins, belongs to vitamin B complex.Nicotinic acid is converted into nicotiamide in human body, and nicotiamide is the ingredient of cozymase and codehydrogenase Ⅱ, participates in HypercholesterolemicRats, the oxidizing process of Tissue respiration and the process of saccharide anaerobic decomposition.Be one of active drug for the treatment of hyperlipidemia, it can reduce the content of low density lipoprotein, LDL, triglyceride, the content of high density lipoprotein increasing.
Lovastatin is a kind of HMG-CoA reductase inhibitor, and it can stop the synthesis of endogenous cholesterol.Reduce low-density, extra-low density and intermediate density lipoprotein (IDL) (LDL, VLDL, TDL) in blood.Can slight high density lipoprotein increasing (HDL), few side effects and light.Be mainly used in heterozygous familial hypercholesterolemia clinically, severe primary hypercholesterolemia, light-duty primary hypercholesterolemia etc.
Clinical research proves, after two kinds of medicament mixed use, curative effect is obviously better than single preparations of ephedrine, and both are also with can totally improve blood fat situation.Apellagrin sustained-release capsule in the market has capsule-type, nicotinic acid and lovastatin two kinds of single preparationss of ephedrine are made slow release and release pills respectively, capsule preparations is made after loading in mixture, but piller coated preparation complex manufacturing, and after coating, the rate of releasing drug difficulty of pellets preparation controls.In addition, also have and adopt Double layer pellet technology, first insert lovastatin twice tabletted by after the precompressed of niacin sustained release layer granule, but the method slow release layer and release layer relative separation, can slow release effect be affected.
Summary of the invention
For the deficiency that current niacin sustained-release preparation exists, the present invention proposes a kind of compound preparation and preparation method, and preparation is simple, is easy to operation, and lovastatin parcel evenly, and release degree of niacin is better than ordinary preparation, is applicable to suitability for industrialized production.
The present invention seeks to be realized by following technical scheme: get lovastatin, nicotinic acid, adjuvant sieve for subsequent use respectively; By nicotinic acid, HPMC and PVP
k90mix homogeneously, as mixed powder, granulates with water, dries; Dry granular sieves granulate, adds the HPMC of stearic acid and surplus, mixing.Survey granule content of dispersion, calculate standard film weight.For subsequent use after granulation.Hydroxypropyl methylcellulose, PEG400, Tween 80 and lemon yellow, be dissolved in 60% ethanol, and grind the titanium dioxide of recipe quantity with this liquid, gets supernatant and namely obtain blank coating solution.Get label to weigh, put into coating pan, wrap in advance, the lovastatin sieved is distributed in coating solution, spray into coating solution continuously, reach regulation and stop coating.Measure lovastatin dissolution and release degree of niacin, qualified rear packaging, to obtain final product.
Slow release Core formulation:
Coating fluid prescription
The niacin slow-release tablet prepared as stated above, detects according to the requirement of state-promulgated pharmacopoeia.(sodium dihydrogen phosphate 1.38g is got with the phosphate buffer of 0.5% sodium dodecyl sulfate solution, sodium lauryl sulphate 5g, the 900ml that adds water dissolves, pH7.0 is regulated with 1mol/L sodium hydroxide, thin up is to 1000ml, mixing) 900ml is dissolution medium, with Rotating shaker, carries out lovastatin dissolution test under 100 revs/min.Select the high performance liquid chromatography highly sensitive, specificity is strong, measure dissolution.Adopt basket method, 100 revs/min, carry out release degree of niacin experiment with 900ml water for solvent, select determined by ultraviolet spectrophotometry release degree of niacin.
Measurement result shows, dissolution when 30 minutes has on average reached more than 88.0% of labelled amount, and stripping homogeneity is better, and the stripping curve of three batch samples is similar, illustrates that technique is more stable.
The every sheet of the present invention is respectively 22.4%, 51.9% and 87.6% 3,9,20 hours releases, all conforms with the regulations.
Select the high performance liquid chromatography highly sensitive, specificity is strong, respectively the related substance of nicotinic acid in the present invention and lovastatin is checked.Through accelerating and long term test examination, the related substance of nicotinic acid, lovastatin, without obvious increase, illustrates that lovastatin has good stability.
Specific implementation method
Embodiment
Lovastatin and nicotinic acid are crossed No. 7 sieves, adjuvant HPMC, PVP
k90, stearic acid respectively cross No. 7 sieves.
Take the nicotinic acid of 500,17.2gPVP
k90with the HPMC of 185.0g31%, mix homogeneously, as mixed powder, granulates with water.Wet grain puts 60 DEG C of 7 DEG C of dryings of ventilating, and dry granule, after No. 2 sieve granulate, adds the stearic acid of 7.0g and the HPMC of surplus, mixing.The stamping of 13mm scrobicula, tablet hardness controls at 5 ~ 6kg.
Take 86.4g hydroxypropyl methylcellulose, 2.4ml PEG400,3.2ml Tween 80 and 8.0g lemon yellow, be dissolved in 3200ml60% ethanol, and with this liquid grinding 8.0g titanium dioxide, get supernatant and namely obtain not pastille coating solution.
Get label to weigh, put into coating pan, temperature controls at 40 ± 2 DEG C, and rotating speed is 30 revs/min, wraps a few minutes in advance to nicotinic acid label, is distributed in coating solution, sprays into coating solution continuously by the lovastatin crossing No. 7 sieves, to tablet weightening finish 9.87%, both obtains finished product.
The coated tablet that this method is obtained, unilateral smooth, lovastatin content, lovastatin dissolution and release degree of niacin are carried out respectively to this tablet and investigates.
Table 145 minute lovastatin dissolution determination result
Table 2 coated tablet release degree of niacin is investigated
| Time (h) | 1 | 3 | 6 | 9 | 12 | 16 | 20 | 24 |
| Release | 7.9 | 22.4 | 38.1 | 51.9 | 63.1 | 76.9 | 87.6 | 97.6 |
The coated tablet lovastatin dissolution that this prescription is obtained and release degree of niacin all conform with the regulations, and carry out different pH value medium release degree of niacin and investigate, refer to table 3 with this compound niacin sustained release tablet.
Table 3 compound niacin sustained release tablet different pH value medium release degree of niacin is investigated
Above-mentioned experiment proves that compound niacin sustained release tablet release under different PH condition is better, and sample is under high temperature, high humidity and intense light conditions, and character, release, content and related substance have no significant change, and technique favorable reproducibility is simple to operate, is easy to suitability for industrialized production
Above-described specific embodiment; object of the present invention, technical scheme and beneficial effect are further described; be understood that; the foregoing is only specific embodiments of the invention; be not limited to the present invention; within the spirit and principles in the present invention all, any amendment made, equivalent replacement, improvement etc., all should be included within protection scope of the present invention.
Claims (6)
1. a compound niacin sustained release tablet, is made up of niacin sustained release part and lovastatin rapid release coatings, it is characterized in that: niacin sustained release part is made up of the material composition of following weight portion:
Make 1000.
2. compound niacin sustained release tablet as claimed in claim 1, is characterized in that: lovastatin rapid release coatings is made up of the material composition of following weight portion:
。
3. the preparation method of compound niacin sustained release tablet as claimed in claim 1, is characterized in that: get lovastatin, nicotinic acid, adjuvant sieve for subsequent use respectively; By nicotinic acid, HPMC and PVP
k90mix homogeneously, as mixed powder, granulates with water, dries; Dry granular sieves granulate, adds the HPMC of stearic acid and surplus, mixing, for subsequent use after granulation.Hydroxypropyl methylcellulose, PEG400, Tween 80 and lemon yellow, be dissolved in 60% ethanol, and grind the titanium dioxide of recipe quantity with this liquid, gets supernatant and namely obtain blank coating solution.Get label to weigh, put into coating pan, wrap in advance, the lovastatin sieved is distributed in coating solution, spray into coating solution continuously, reach regulation and stop coating.Measure lovastatin dissolution and release degree of niacin, qualified rear packaging, to obtain final product.
4. the preparation method of compound niacin sustained release tablet as claimed in claim 3, is characterized in that: lovastatin and nicotinic acid are crossed No. 7 sieves, adjuvant HPMC, PVP
k90, stearic acid respectively cross No. 7 sieves.Take the nicotinic acid of 500,17.2gPVP
k90with the HPMC of 185.0g31%, mix homogeneously, as mixed powder, granulates with water.Wet grain puts 60 DEG C of 7 DEG C of dryings of ventilating, and dry granule, after No. 2 sieve granulate, adds the stearic acid of 7.0g and the HPMC of surplus, mixing.The stamping of 13mm scrobicula, tablet hardness controls at 5 ~ 6kg.Take 86.4g hydroxypropyl methylcellulose, 2.4ml PEG400,3.2ml Tween 80 and 8.0g lemon yellow, be dissolved in 3200ml60% ethanol, and with this liquid grinding 8.0g titanium dioxide, get supernatant and namely obtain not pastille coating solution.Get label to weigh, put into coating pan, temperature controls at 40 ± 2 DEG C, and rotating speed is 30 revs/min, wraps a few minutes in advance to nicotinic acid label, is distributed in coating solution, sprays into coating solution continuously by the lovastatin crossing No. 7 sieves, to tablet weightening finish 9.87%, both.
5. the preparation method of compound niacin sustained release tablet as claimed in claim 3, is characterized in that: compound niacin sustained release tablet is first by niacin sustained release laminate, then adds lovastatin formation lovastatin rapid release coatings by coating.
6. the preparation method of compound niacin sustained release tablet according to claim 4, is characterized in that: the weight proportion of blocker, filler, lubricant is: HPMC185g, filler PVP
k9017.2g, stearic acid 7.0g.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201410232741.2A CN105213393A (en) | 2014-05-28 | 2014-05-28 | A kind of niacin sustained-release preparation and preparation method |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201410232741.2A CN105213393A (en) | 2014-05-28 | 2014-05-28 | A kind of niacin sustained-release preparation and preparation method |
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| CN105213393A true CN105213393A (en) | 2016-01-06 |
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| Application Number | Title | Priority Date | Filing Date |
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| CN201410232741.2A Pending CN105213393A (en) | 2014-05-28 | 2014-05-28 | A kind of niacin sustained-release preparation and preparation method |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN107854448A (en) * | 2017-11-06 | 2018-03-30 | 广州市桐晖药业有限公司 | A kind of nicotinic acid tablet and preparation method thereof |
-
2014
- 2014-05-28 CN CN201410232741.2A patent/CN105213393A/en active Pending
Non-Patent Citations (1)
| Title |
|---|
| 杨春光: "复方烟酸和洛伐他汀缓释片的研究", 《中国优秀博硕士学位论文全文数据库 (硕士)工程科技Ⅰ辑》 * |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN107854448A (en) * | 2017-11-06 | 2018-03-30 | 广州市桐晖药业有限公司 | A kind of nicotinic acid tablet and preparation method thereof |
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