CN1843345A - 1,5-di-o-caffenoylquinate solid formulation and its preparation method - Google Patents
1,5-di-o-caffenoylquinate solid formulation and its preparation method Download PDFInfo
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- CN1843345A CN1843345A CN 200510074475 CN200510074475A CN1843345A CN 1843345 A CN1843345 A CN 1843345A CN 200510074475 CN200510074475 CN 200510074475 CN 200510074475 A CN200510074475 A CN 200510074475A CN 1843345 A CN1843345 A CN 1843345A
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Abstract
The invention discloses the solid preparation of 1,5-O-dicaffeoylquinic acid and its preparing process, which is prepared from raw materials including 1,5-O-dicaffeoylquinic acid 50-500 weight parts, bulk additive 187-7400 weight parts, crumbling agent 60-2000 weight parts, lubricating agent 3-100 weight parts through the steps of raw material disintegrating, sieving, making soft material, making wet particles, sieving, drying, granulating and compressing tablets.
Description
Technical field
The present invention relates to 1, the solid preparation and the preparation technology thereof of 5-two-O-caffeoylquinic acids.
Background technology
Patent of invention international application no PCT/CN97/00087, international publication number: W098/09599 " the dicaffeoylquinic acid derivant the treatment hepatitis B and with the retrovirus diseases related in purposes and new coffeic acyl quininic acid derivative " new anti-hepatitis B medicine of a class and new antiretroviral drugs 1 disclosed, 5-two-O-caffeoylquinic acids and extraction route thereof, new coffeic acyl quininic acid derivative and contain dicaffeoylquinic acid or the pharmaceutical composition of new-caffeoylquinic acids, this pharmaceutical composition can be prepared to tablet, capsule, other suitable dosage forms such as injection, but the end discloses the technical scheme of this pharmaceutical composition different dosage form of concrete preparation.
Technical scheme
The object of the invention provide a kind of disintegration of pharmaceutical preparation and dissolution good 1, the solid preparation of 5-two-O-caffeoylquinic acids such as tablet, capsule etc. and preparation technology thereof.
1,5-two-O-caffeoylquinic acids raw material is a crystalline powder, pulverizes easily.Its Main physical chemical property that influences pharmaceutics is to become gel state rapidly after it meets water, has stoped the disintegrate of solid preparation such as tablet and the stripping of principal agent, does not reach the drug effect of treatment.Owing to 1,5-two-O-caffeoylquinic acids special physicochemical character makes soft material very sticking when water or low-concentration ethanol are made wetting agent in preparation process simultaneously, is difficult for forming granule, can't make qualified preparation.1,5-two-O-caffeoylquinic acids oral dose is bigger, be 250-500mg, so supplementary product consumption is little in the preparation at every turn, can not well disperse principal agent, causes granule or tablet not easy disintegrating and principal agent stripping; If the adjuvant amount strengthens, though can improve its disintegrate, dosage form will increase many, and inconvenience is carried and taken.
Technical scheme of the present invention is:
A kind of 1,5-two-O-caffeoylquinic acids solid preparation, it is by raw material 1 basically, 5-two-O-caffeoylquinic acids 50-500 weight portion, adjuvant filler 187-7400 weight portion, disintegrating agent 60-2000 weight portion, lubricant 3-100 weight portion are made.
Wherein filler is a kind of in starch, pregelatinized Starch, dextrin, microcrystalline Cellulose, carboxymethyl starch sodium, lactose, the mannitol or several; Consumption as filler starch can be 87-2400 weight portion, pregelatinized Starch 187-7400 weight portion, dextrin 100-1000, microcrystalline Cellulose 187-7400 weight portion, carboxymethyl starch sodium 187-2500 weight portion, lactose 187-7400 weight portion, mannitol 187-7400 weight portion.
Disintegrating agent is a kind of in interlinkage sodium carboxymethyl cellulose, polyvinylpolypyrrolidone, low-substituted hydroxypropyl cellulose sodium, the carboxymethyl starch sodium or several; As disintegrating agent wherein interlinkage sodium carboxymethyl cellulose consumption can be that 60-2000 weight portion, polyvinylpolypyrrolidone 60-2000 weight portion, low-substituted hydroxypropyl cellulose sodium 60-2000 weight portion, carboxymethyl starch sodium 60-2000 weight portion, surfactant are an amount of;
Lubricant is a kind of in magnesium stearate, micropowder silica gel, the Pulvis Talci or several; As lubricant magnesium stearate consumption wherein can be 3-100 weight portion, micropowder silica gel 6-500 weight portion, Pulvis Talci 6-500 weight portion.
Also can comprise binding agent 10-100 weight portion in the adjuvant, can be a kind of in hydroxypropyl emthylcellulose water liquid, polyvidone water liquid, starch slurry, dextrin slurry, the syrup or several.
The dosage form of solid preparation of the present invention can be tablet, granule, capsule etc., preferred tablet, and its oral dose can be the 250-500 milligram.
The preparation technology of solid preparation of the present invention comprises the following steps:
(1) prepares the binding agent that needs; (2) raw material 1, and 5-two-O-caffeoylquinic acids is pulverized, and crosses the 60-100 mesh sieve; (3) crude drug adds adjuvant filler, disintegrating agent mix homogeneously; (4) in above mixed powder, add binding agent and make soft material; (5) soft material is crossed the 12-30 mesh sieve and made wet granular: A, if make tablet and cross the 12-16 mesh sieve; B, if make granule cross 12-16 mesh sieve C, if make capsule, cross the 20-30 mesh sieve; 6), wet grain drying, with 60-80 ℃ of drying; (7) granulate, A, if make granule can directly pack; B, if make capsule, can be directly encapsulated; C, if make tablet, dried granule should be admixed lubricant, carry out tabletting.
The specific embodiment
Embodiment 1 tablet
Prescription:
1,5-two-O-caffeoylquinic acids 250g
Carboxymethyl starch sodium 140g
Microcrystalline Cellulose 140g
Cross-linked pvp 64g
Magnesium stearate 6g
Hydroxypropyl emthylcellulose water liquid 240ml
Total amount 600g makes 1000 altogether
More than prescription is made the tablet of 0.6g/ sheet, every content 250mg.
Method for making: hydroxypropyl emthylcellulose is made into 1% aqueous solution, and with 1,5-two-O-caffeoylquinic acids is pulverized, cross 80 mesh sieves, with 1,5-two-O-caffeoylquinic acids mixes with cross-linked pvp, add carboxymethyl starch sodium, microcrystalline Cellulose mix homogeneously again, in above mixed powder, add binding agent and make soft material, cross 30 mesh sieves and make wet granular, with 75 ℃ of temperature, dry 1 hour, granulate adds magnesium stearate, tabletting.
Embodiment 2 tablets
Prescription
1,5-two-O-caffeoylquinic acids 100g
Carboxymethyl starch sodium 215g
Microcrystalline Cellulose 215g
Cross-linked pvp 64g
Magnesium stearate 6g
Hydroxypropyl emthylcellulose water liquid 240ml
Total amount 600g makes altogether to write out a prescription more than 1000 and makes the tablet of 0.6g/ sheet, every content 100mg.
Method for making is with embodiment 1:
Embodiment 3 tablets
Prescription:
1,5-two-O-caffeoylquinic acids 125g
Carboxymethyl starch sodium 205g
Microcrystalline Cellulose 200g
Cross-linked pvp 64g
Magnesium stearate 6g
Hydroxypropyl emthylcellulose water liquid 200ml
Total amount 600g makes more than 1000 altogether, and prescription is made the tablet of 0.6g/ sheet, every content 125mg.
Method for making is with embodiment 1:
Embodiment 4 tablets
Prescription:
1,5-two-O-caffeoylquinic acids 50g
Carboxymethyl starch sodium 94g
Microcrystalline Cellulose 93g
Cross-linked pvp 60g
Magnesium stearate 3g
Hydroxypropyl emthylcellulose water liquid 200ml
Total amount 300g makes 1000, the tablet of every 0.3g/ sheet altogether.Every content 50mg
Method for making is with embodiment 1:
Embodiment 5 granules
Prescription:
1,5-two-O-caffeoylquinic acids 250g
Carboxymethyl starch sodium 140g
Microcrystalline Cellulose 140g
Cross-linked pvp 70g
Hydroxypropyl emthylcellulose water liquid 240ml
Amount to 600g and make 1000 bag 0.6g/ packet content 250mg altogether.
Method for making:
(1) preparation hydroxypropyl emthylcellulose aqueous solution,
(2) with 1,5-two-O-caffeoylquinic acids is pulverized, and crosses 80 mesh sieves,
(3) with cross-linked pvp, carboxymethyl starch sodium, microcrystalline Cellulose are crossed 100 mesh sieves respectively,
(4) with 1,5-two-O-caffeoylquinic acids is pulverized and above-mentioned adjuvant mix homogeneously,
(5) add the hydroxypropyl emthylcellulose aqueous solution and in above-mentioned mixed powder, make soft material, cross 14 mesh sieves and make wet granular,
(6) with 75 ℃ of dry wet particles, 14 mesh sieve granulate.
(7) packing.
Embodiment 6 granules
Prescription:
1,5-two-O-caffeoylquinic acids 500g
Carboxymethyl starch sodium 2500g
Microcrystalline Cellulose 6000g
Cross-linked pvp 1000g
Hydroxypropyl emthylcellulose water liquid 4000ml
Total amount 10000g makes granule, makes 1000 bags altogether, every bag 10g, content 500mg.
Method for making is with embodiment 5:
Embodiment 7 capsules
Prescription:
1,5-two-O-caffeoylquinic acids 250g
Pregelatinized Starch 140g
Microcrystalline Cellulose 142g
Interlinkage sodium carboxymethyl cellulose 64g
Magnesium stearate 4g
Hydroxypropyl emthylcellulose water liquid 200ml
Total amount 600g makes 1000 of capsules, 0.6g/ grain, content 250mg.
Method for making:
(8) preparation hydroxypropyl emthylcellulose aqueous solution;
(9) with 1,5-two-O-caffeoylquinic acids is pulverized, and crosses 80 mesh sieves;
(10) with cross-linking sodium carboxymethyl cellulose, pregelatinized Starch, microcrystalline Cellulose is crossed 100 mesh sieves respectively;
(11) with 1,5-two-O-caffeoylquinic acids is pulverized and above-mentioned adjuvant mix homogeneously;
(12) in above-mentioned mixed powder, slowly add the hydroxypropyl emthylcellulose aqueous solution and in above-mentioned mixed powder, make soft material, cross 14 mesh sieves and make wet granular,
(13) with 75 ℃ of dry wet particles 1 hour, with 14 mesh sieve granulate;
(14) filled capsules.
Claims (7)
1, a kind of 1,5-two-O-caffeoylquinic acids solid preparation, it is characterized in that: it is by crude drug 1 basically, and 5-two-O-caffeoylquinic acids 50-500 weight portion, adjuvant filler 187-7400 weight portion, disintegrating agent 60-2000 weight portion, lubricant 3-100 weight portion are made.
2, solid preparation according to claim 1 is characterized in that: filler is a kind of in starch, pregelatinized Starch, dextrin, microcrystalline Cellulose, carboxymethyl starch sodium, lactose, the mannitol or several.
3. solid preparation according to claim 1 is characterized in that disintegrating agent is a kind of in interlinkage sodium carboxymethyl cellulose, interlinkage polyvidone, low-substituted hydroxypropyl cellulose sodium, surfactant, the carboxymethyl starch sodium or several.
4. solid preparation according to claim 1 is characterized in that lubricant is a kind of in magnesium stearate, micropowder silica gel, the Pulvis Talci or several.
5. solid preparation according to claim 1 is characterized in that: also comprise binding agent 10-100 weight portion in the adjuvant.
6, solid preparation according to claim 5 is characterized in that binding agent is: a kind of in hydroxypropyl cellulose water liquid, polyvidone water liquid, starch slurry, dextrin slurry, the syrup or several.
7,, it is characterized in that comprising the following steps: the binding agent of (1) preparation needs according to the production technology of the arbitrary described solid preparation of claim 1-6; (2) crude drug 1, and 5-two-O-caffeoylquinic acids is pulverized, and crosses the 60-100 mesh sieve; (3) crude drug adds adjuvant filler, disintegrating agent mix homogeneously; (4) in above mixed powder, add binding agent and make soft material; (5) soft material is crossed the 10-30 mesh sieve and made wet granular: A, if make tablet and cross the 12-16 mesh sieve; B: cross the 12-16 mesh sieve if make granule; C, if make capsule, cross the 20-30 mesh sieve: (6), wet grain drying, with 60-80 ℃ of drying, (7) granulate, A, if make granule can directly pack; B, if make capsule, can be directly encapsulated; C, if make tablet, dried granule should be admixed lubricant, carry out tabletting.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200510074475 CN1843345A (en) | 2005-06-07 | 2005-06-07 | 1,5-di-o-caffenoylquinate solid formulation and its preparation method |
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| Application Number | Priority Date | Filing Date | Title |
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| CN 200510074475 CN1843345A (en) | 2005-06-07 | 2005-06-07 | 1,5-di-o-caffenoylquinate solid formulation and its preparation method |
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| CN1843345A true CN1843345A (en) | 2006-10-11 |
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| CN 200510074475 Pending CN1843345A (en) | 2005-06-07 | 2005-06-07 | 1,5-di-o-caffenoylquinate solid formulation and its preparation method |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105769841A (en) * | 2014-08-12 | 2016-07-20 | 烟台市华文欣欣医药科技有限公司 | Application of syringic acid/4-hydroxy-3,5-dimethoxybenzoic acid in preparing drug for pregnancy termination |
-
2005
- 2005-06-07 CN CN 200510074475 patent/CN1843345A/en active Pending
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105769841A (en) * | 2014-08-12 | 2016-07-20 | 烟台市华文欣欣医药科技有限公司 | Application of syringic acid/4-hydroxy-3,5-dimethoxybenzoic acid in preparing drug for pregnancy termination |
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Open date: 20061011 |