CN1033441A - Method with brown algae gum to prepare enteric soluble tablet - Google Patents
Method with brown algae gum to prepare enteric soluble tablet Download PDFInfo
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- CN1033441A CN1033441A CN 87101144 CN87101144A CN1033441A CN 1033441 A CN1033441 A CN 1033441A CN 87101144 CN87101144 CN 87101144 CN 87101144 A CN87101144 A CN 87101144A CN 1033441 A CN1033441 A CN 1033441A
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- algin
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Abstract
The present invention proposes with the method for Algin as enteric coating feedstock production enteric coated tablet, have good acid-resisting and alkali solubility according to calcium alginate, the powdery Algin can be converted into calcium alginate again after moistening and make enteric coated tablet with adhering to equably after syrup combines on the plain sheet through suitable.
Description
The present invention relates to method with brown algae gum to prepare enteric soluble tablet.
In pharmaceuticals industry, many medicines as: lose drug effect in the acid medium under one's belt such as Midecamycin, erythromycin, aspirin easily or stomach had stimulation and causes feeling sick.
Therefore, seek that not collapse the enteric-coating material material that looses and collapse diffusing oral drugs rapidly in intestinal under one's belt be the problem that people explore always.Existing enteric-coating material such as Cellulose Acetate Phthalate (CAP) belong to synthetic high polymer, need use organic solvent dissolution during preparation, and its steam is toxic, and is inflammable and explosive, and quality instability behind the coating.
The present invention is intended to propose a kind of ideal enteric-coating material and is used for preparing enteric coated tablet.
Content of the present invention is to prepare enteric coated tablet with the Algin of calcification as enteric-coating material.The direct calcification of topped Algin on plain sheet can be made it to become the calcium alginate coating.
Feedstock production enteric coated tablet with Algin can preferentially adopt such technology: with the powdery Algin with adhere on the plain sheet after slurry combines, calcification is the calcium alginate coating again after moistening.
Can select for use syrup to make slurry.
Algin is the joint product of Thallus Laminariae (Thallus Eckloniae) system iodine industry, and it is sodium alginate (Na.Alg) as the active ingredient of enteric-coating material.
The principle of making enteric-coating material system enteric coated tablet with Algin is based on following three chemical reactions:
1. sodium alginate changes into the reaction of calcium alginate:
Ca.(Alg in the formula)
2It is calcium alginate.
2. medicine gulps down the chemical reaction in the stomach into:
Be that tablet is wrapped after the calcium alginate enteric coating.Do not dissolved under one's belt, be gradually transformed into alginic acid with the acid medium effect of stomach by gastric juice, under one's belt the time of staying longer, change into alignic amount the more.
H.Alg is an alginic acid in the formula.
3. tablet enters the chemical reaction behind the intestinal:
Be that Swertia Tablet enters that alkaline medium is neutralized into the water solublity sodium alginate with alginic acid in the intestinal hindgut, enteric coating is dissolving gradually in N-process, discharges medicine immediately, the performance drug effect.
Sometimes tablet under one's belt the time of staying shorter, or the abnormal people of stomach function, the gastric juice pH value is higher, calcium alginate still can disintegrate after entering small intestinal in the time of still can not being converted into alginic acid.Because of people's gland liquid bile, intestinal juice all has heavy carbonate, can make alginic acid be converted into the solubility alginate and disintegrate.
H.Alg is an alginic acid in the formula.
Adopt and proposed by the invention prepare enteric coated tablet with Algin as coating material and have following advantage:
1. Algin belongs to the carbohydrate of natural polymer, avirulence, can be soluble in water with gelatin, agar, carrageenan, sugar etc., on art for coating, can adopt dry method, manufacture process is easy to moistening and is converted into calcium alginate, so needn't use inflammablely, the organic solvent that the people is produced murder by poisoning dilutes, and has also exempted a series of safety devices such as gas defence, anti-riot, fire prevention.
2. from the disintegrate effect, Algin is comparatively ideal a kind of in the present known enteric material.The PH that its disintegrative depends primarily on human stomach, intestinal changes.The not disintegrate in the acid medium of stomach of calcium alginate enteric coating, PH increased by 5 o'clock, produced to expand, and PH is being disintegrate more than 6.
3. Algin has good water-resistance and quality stability through being converted into the coatings that calcium alginate forms, thereby storage under field conditions (factors), and difficult generation is broken, is out of shape or goes mouldy.
The quality testing of Algin enteric coatel tablets
External slaking test:
The Algin erythromycin enteric-coated tablet is pressed in Chinese Pharmacopoeia version in 1977 and the version appendix in 1985 enteric coated tablet inspection technique disintegration and is checked, the results are shown in Table
The external slaking test of Algin enteric coatel tablets
Five crowdes of Algin erythromycin casing sheet three level testing results
Assay meets 85 years version regulations of Chinese Pharmacopoeia disintegration
2. slaking test in the body:
73 tablets of Algin enteric coatel tablets disintegrate situation in gastrointestinal
Result of the test is on an empty stomach organized 73, and 2 hours 5 of gastric disintegrates, has 2 what enteral surpassed last disintegrate in 1 hour, and promptly underproof totally 7, disqualification rate is 66 of inherent enteral disintegrate disintegrates in 9.59%1 hours, and qualification rate is 90.41%.
For link up to observe tablet in stomach, intestinal the disintegrate situation and carry out X line perspective and follow the tracks of film making, its result is as table
The disintegrate in the human intestines and stomach of barium sulfate enteric coatel tablets is followed the tracks of live
Medicine stability test:
(1) accelerated test: the Algin erythromycin enteric-coated tablet that will normally pack places respectively and carries out 60 days accelerated tests under 45 ℃, carries out medicine valency, limit test of weight variation, disintegration, property determination then, all with the preceding no significant difference of accelerated test.
(2) stability of storing is naturally measured: the erythromycin tablet is by common bottled, after the mouth of sealing with wax is at room temperature preserved 2 years, measure projects such as its character, disintegration, content, the whole following tables up to specification of result are the synthesis result of institute for drug control to five batches of products measures.
Algin erythromycin enteric-coated tablet, storage quality inspection in 2 years
Find out that from last table the Algin erythromycin enteric-coated tablet is after preserving 2 years, quality still end reduces, and illustrates that medicine stability is good.
Below the embodiment that is prepared as with the erythromycin enteric tablet describes the method for preparing enteric coated tablet with Algin as coating in detail.
Fig. 1 is the process chart of preparation erythromycin enteric-coated tablet
1. fill a prescription:
(1) erythromycin tablets prescription: per 100,000 meters (100,000 units/sheet)
Erythromycin 10,000,000,000 units
5.25 kilograms of starch
1.00 kilograms of starch (dashing slurry 10%)
0.36 kilogram of magnesium stearate
0.50 kilogram of disintegrating agent (little silicon)
(2) enteric coating prescription: per 100,000 meters
3.0 kilograms of sodium alginates
0.3 kilogram in calcium chloride
Distilled water 11.4 liters
2. the art for coating condition is selected test:
(1) the Algin specification is selected:
Moisture content (%)≤15
Ash (%) 16-24
PH value 6.5-7
Water-insoluble (%)＜0.2
Heavy metal (PPM)≤20
Arsenic (A
s) (PPM)≤2
Viscosity (centipoise)＞400
Fineness (order) is more than 100
(2) coatings thickness: the thickness of tablet appearance enteric coating layer, to not directly influence of disintegration rate, will make the Algin casing sheet of different-thickness, put in the simulated gastric fluid and handle after 2 hours, in simulated intestinal fluid, carry out disintegrating method again, the result is as table
The disintegration time of different-thickness Algin enteric coating is (unit: millimeter divides) relatively
| Algin enteric coating thickness | Disintegration time in the simulated intestinal fluid |
| 0.12 | 5 |
| 0.15 | 17 |
| 0.20 | 25 |
| 0.22 | 30 |
| 0.25 | 33 |
The thick more disintegration time of last table explanation enteric coating is long more.Therefore the thickness of enteric coating preferably should not surpass 0.20 millimeter, promptly controls disintegration time and is no more than 30 minutes.
(3) the calcium alginate transforming degree influences disintegrate: when the sodium alginate coatings changes into calcium alginate, used calcium concentration will influence the disintegration rate in intestinal juice.The casing sheet of same thickness, when adopting the calcium chloride processing of variable concentrations respectively, its dissolution time sees the following form
The disintegrate effect that table variable concentrations calcium is handled Brown algae gel coat film compares (unit: the grams per liter branch)
| Calcium concentration | Disintegration time in the simulated intestinal fluid |
| 3.6 | 12 |
| 7.2 | 25 |
| 10.8 | 40 |
| 14.4 | 58 |
| 18.0 | 62 |
Last table is found out: calcium concentration is bigger, and enteric coating disintegrate required time in simulated intestinal fluid is longer, and by long, according to the disintegration time requirement, calcium concentration is preferably less than 10 grams per liters.
(4) viscosity of Algin is to the enteric coating intensity effect: Algin belongs to the natural polymer product.Molecular weight is 14,000～200,000, generally just select for use with viscosity, the following person of 200 centipoises is a low viscosity, and 200～400 centipoises are medium viscosity, and 1000 centipoises are above to be hyperviscosity, the clothing film that low viscosity is made breaks easily, pretends to the enteric coatel tablets clothing and should select medium viscosity Algin about 400 centipoises for use.
(5) fineness of Algin influences the clothing film quality: the Algin granule too slightly can influence the fastness and the outward appearance of clothing film.So preferably adopting the above fineness of 100 orders is advisable.
Can make erythromycin tablets by prescription (1), with the powdery Algin with adhere to the plain sheet of erythromycin after syrup combines on, reuse calcium chloride changes into the calcium alginate coating with the sodium alginate on the plain sheet after moistening, can make the erythromycin enteric tablet of finished product again through last sugar layer and polishing operation.
Replace to stew in shallow water with the plain sheet of Midecamycin and turn round and look at the pure Chinese herbaceous peony of the narrow of the male servant earthworm comet of sleeping frequently and turn round and look at line in the Eight Diagrams θ root of Dahurian angelica
Claims (7)
1, a kind of method for preparing enteric coated tablet is characterized in that doing with the Algin of calcification the material of enteric coating.
2, according to the method for claim 1, it is characterized in that with the brown glue of powdery algae with adhere on the plain sheet after slurry combines, calcification is the calcium alginate coating again after moistening.
3,, it is characterized in that the thickness of coating is no more than 0.2 millimeter according to the method for claim 1 or 2.
4, according to the method for claim 1 or 2, the concentration of calcium is less than 10 grams per liters when it is characterized in that the calcification Algin.
5, according to the method for claim 1 or 2, the viscosity that it is characterized in that Algin is the 200-400 centipoise.
6, according to the method for claim 1 or 2, the granularity that it is characterized in that Algin is more than 100 orders.
7,, it is characterized in that the slurry of selecting for use is a syrup according to the method for claim 2.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 87101144 CN1033441A (en) | 1987-12-11 | 1987-12-11 | Method with brown algae gum to prepare enteric soluble tablet |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 87101144 CN1033441A (en) | 1987-12-11 | 1987-12-11 | Method with brown algae gum to prepare enteric soluble tablet |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN1033441A true CN1033441A (en) | 1989-06-21 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN 87101144 Pending CN1033441A (en) | 1987-12-11 | 1987-12-11 | Method with brown algae gum to prepare enteric soluble tablet |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN1033441A (en) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1997046224A1 (en) * | 1996-06-06 | 1997-12-11 | Bifodan A/S | Enteric coating, comprising alginic acid, for an oral preparation |
-
1987
- 1987-12-11 CN CN 87101144 patent/CN1033441A/en active Pending
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1997046224A1 (en) * | 1996-06-06 | 1997-12-11 | Bifodan A/S | Enteric coating, comprising alginic acid, for an oral preparation |
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| C01 | Deemed withdrawal of patent application (patent law 1993) | ||
| WD01 | Invention patent application deemed withdrawn after publication |