CN104434773A - Vitamin B1 composition lyophilized tablet and preparation method thereof - Google Patents

Abstract

The invention provides a vitamin B1 composition lyophilized tablet and a preparation method thereof, and relates to the technical field of medicine and medicine production. The tablet is prepared from vitamin B1, starch and sucrose, wherein the starch and sucrose are used as auxiliary materials, and common corn starch is subjected to heat process, so that adhesion and disintegration effects of the starch in a tablet can be improved, and the moldability of the tablet can be improved; and only starch and sucrose are needed in the vitamin B1 composition lyophilized tablet. According to the preparation method, a two-decreasing two-increasing lyophilizing process is adopted for the vitamin B1 composition lyophilized tablet, the moldability of the tablet can be better by means of twice cooling and twice heating, the solubility of the tablet can be improved, and the bioavailability of the tablet can be improved; the tablet is capable of overcoming the defect of conventional vitamin B1 tablets and reducing the types and usage of auxiliaries in the vitamin B1 tablets, is high in solubility and high in bioavailability, and can be used for guaranteeing the curative effect and safety of clinical administration.

Description

A kind of vitamin B 1composition freeze-drying sheet and preparation method thereof

Technical field

The present invention relates to medicine and medical production technical field, be specifically related to a kind of vitamin B ₁composition freeze-drying sheet and preparation method thereof.

Background technology

Vitamin B ₁it is a kind of vitamin B group that pyrimidine ring and thiazole ring are combined into by methylene.

Molecular formula: C ₁₂h ₁₇clN ₄oSHCl

Molecular weight 337.27

Existing clinical common dosage forms is all the product of chemosynthesis.This product participates in catabolism of carbohydrate with co-enzyme form, has the effect of neuroprotective system; Can also enterogastric peristalsis be promoted, increase appetite.Clinical common formulations is tablet and injection.

Common vitamin B ₁in sheet containing supplementary product kind and quantity more, generally will use filler, lubricant, disintegrating agent, adhesive, correctives etc., its disintegration time reaches 12 minutes, and bioavailability is lower.And increasing research shows that impurity in the incompatibility of the toxic and side effects of adjuvant itself, adjuvant and principal agent, adjuvant etc. all can have an impact to the safety of medicine.

Therefore, provide one can overcome above-mentioned shortcoming, select suitable adjuvant and technique, reduce vitamin B ₁supplementary product kind and consumption in sheet, improve vitamin B ₁sheet bioavailability, ensures that the safety of clinical application all has positive effect.

Traditional lyophilizing tablet can improve bioavailability, but still need use the adjuvant such as mannitol, gelatin.And mannitol has certain biological activity, gelatin resource-constrained and perishable.

Starch is the basic adjuvant of oral solid formulation, and it is polymerized by glucose molecule, and be commonly used for adhesive, diluent and disintegrating agent in tablets, it is cheap and easy to get, and to human-body safety, but being used alone starch produces vitamin B as adjuvant freeze-dry process ₁lyophilizing sheet has no report.

Summary of the invention

Technical problem to be solved by this invention is the defect overcoming prior art, proposes a kind of vitamin B further ₁composition freeze-drying sheet and preparation method thereof, said preparation adjuvant is few, good stability, and bioavailability is high.

Technical problem to be solved by this invention realizes by the following technical solutions:

A kind of vitamin B ₁composition freeze-drying sheet, does adjuvant with starch and sucrose, and produce with freeze-dry process, this tablet overcomes above-mentioned usual vitamin B ₁the shortcoming of sheet, decreases vitamin B ₁supplementary product kind and consumption in sheet, this sheet dissolution is large, and bioavailability is high, ensure that curative effect and the safety of clinical application.

A kind of vitamin B ₁composition freeze-drying sheet, is prepared from by following raw material:

A preparation method for vitamin B 1 composite lyophilizing sheet, comprises step as follows:

A, take the starch of component amount, add a certain amount of purified water and stir, by pH adjusting agent, the pH value of solution is controlled between 4-5, be then heated to 72 DEG C, be incubated 20 minutes, make the corn starch solution of 5 ~ 15% (W/V);

B, measure purified water 45ml, boil, add 85g sucrose, stir, after dissolving, continue to be heated to 100 DEG C, filter with purified cotton, the appropriate hot distilled water of filter is cleaned, and washing liquid and filtrate merge, and let cool, add appropriate distilled water, make full dose become 100ml, stir evenly, obtain B solution;

The solution that C, the solution and the step B that steps A are obtained obtain mixes, and fully stirs 30 minutes, is down to room temperature and obtains Semen Maydis-sucrose solution;

D, take vitamin B ₁50 grams, add in 1L Semen Maydis-sucrose solution, stir 25 ~ 35 minutes;

E, medicinal liquid measure vitamin B ₁after content, medicinal liquid is sub-packed in drug-containing dish, each drug-containing dish dress 1.0ml;

F, the drug-containing dish that medicinal liquid is housed is put into vacuum freezing drying oven, be cooled to subzero 45 DEG C, keep 2 hours, evacuation, then 0 DEG C is warming up to gradually, keep 2 hours, then be cooled to subzero 45 DEG C, keep 2 hours, be warming up to 0 DEG C gradually again, keep 2 ~ 4 hours, then be warming up to 28 ~ 32 DEG C of dryings 4 ~ 6 hours gradually, whole process vacuum remains on 10 handkerchiefs; Finally the drug-containing dish lid of powder charge is covered tightly, and load aluminium foil bag and carry out sealing and obtain vitamin B ₁composition freeze-drying sheet.

Described starch selects corn starch, preferably the corn starch solution of 10% (W/V).

Beneficial effect of the present invention is:

A kind of vitamin B of the present invention ₁the preparation method of composition freeze-drying sheet, carries out heating process process to common corn starch, can improve starch bonding in tablets, disintegration, improves the mouldability of tablet, vitamin B ₁in composition freeze-drying sheet, dosage of sucrose is 8.5% (W/V), and it is the hardness reinforcer of this tablet, and plays flavored action.Vitamin B ₁composition freeze-drying sheet only needs starch and sucrose two kinds of adjuvants.Vitamin B ₁the freeze-dry process of two liters falls in composition freeze-drying sheet employing two, and twice cooling, twice intensification can make sheet mouldability better, and shorten the disintegration time of tablet, improve the bioavailability of tablet.

Detailed description of the invention

The technological means realized to make the present invention, creation characteristic, reaching object and effect is easy to understand, below in conjunction with specific embodiment, set forth the present invention further, but following embodiment being only the preferred embodiments of the present invention, and not all.Based on the embodiment in embodiment, those skilled in the art under the prerequisite not making creative work obtain other embodiment, all belong to the protection domain of this patent.

Embodiment 1

A, take the corn starch of 100g, the purified water adding 900ml stirs, and controls 6.5, is then heated to 72 DEG C, keep 120 minutes, make the corn starch solution of 9% (W/V) by pH adjusting agent by the pH value of solution.

B, measure purified water 45ml, boil, add 85g sucrose, stir, after dissolving, continue to be heated to 100 DEG C, filter with purified cotton, the appropriate hot distilled water of filter is cleaned, and washing liquid and filtrate merge, and let cool, add appropriate distilled water, make full dose become 100mL, stir evenly, obtain B solution.

The solution that C, the solution and the step B that steps A are obtained obtain mixes, and fully stirs 30 minutes, after solution be down to room temperature obtain Semen Maydis-sucrose solution.

D, take vitamin B ₁50g, adds in 1L Semen Maydis-sucrose solution, stirs 30 minutes.

E, medicinal liquid measure vitamin B ₁after content, medicinal liquid is sub-packed in drug-containing dish, each drug-containing dish dress 1.0ml.

F, the drug-containing dish that medicinal liquid is housed is put into vacuum freezing drying oven, be cooled to subzero 45 DEG C, keep 2 hours, evacuation, then 0 DEG C is warming up to gradually, keep 2 hours, then be cooled to subzero 45 DEG C, keep 2 hours, be warming up to 0 DEG C gradually again, keep 2 ~ 4 hours, then be warming up to 28 ~ 32 DEG C of dryings 4 ~ 6 hours gradually, whole process vacuum remains on 10 handkerchiefs.Finally the drug-containing dish lid of powder charge is covered tightly, and load aluminium foil bag and carry out sealing and obtain vitamin B ₁composition freeze-drying sheet.

Embodiment 2

A, take the corn starch of 130g, the purified water adding 900ml stirs, and controls at 4-5, is then heated to 72 DEG C, keep 120 minutes, make the corn starch solution of 13% (W/V) by pH adjusting agent by the pH value of solution.

B, measure purified water 45ml, boil, add 85g sucrose, stir, after dissolving, continue to be heated to 100 DEG C, filter with purified cotton, the appropriate hot distilled water of filter is cleaned, and washing liquid and filtrate merge, and let cool, add appropriate distilled water, make full dose become 100mL, stir evenly, obtain B solution.

The solution that C, the solution and the step B that steps A are obtained obtain mixes, and fully stirs 30 minutes, after solution be down to room temperature obtain Semen Maydis-sucrose solution.

D, take vitamin B ₁50 grams (by 1000 calculations), add 1L Semen Maydis-sucrose solution, stir 30 minutes.

E, medicinal liquid measure vitamin B ₁after content, medicinal liquid is sub-packed in drug-containing dish, each drug-containing dish dress 1.0ml.

F, the drug-containing dish that medicinal liquid is housed is put into vacuum freezing drying oven, be cooled to subzero 45 DEG C, keep 2 hours, evacuation, then 0 DEG C is warming up to gradually, keep 2 hours, then be cooled to subzero 45 DEG C, keep 2 hours, be warming up to 0 DEG C gradually again, keep 2 ~ 4 hours, then be warming up to 28 ~ 32 DEG C of dryings 4 ~ 6 hours gradually, whole process vacuum remains on 10 handkerchiefs.Finally the drug-containing dish lid of powder charge is covered tightly, and load aluminium foil bag and carry out sealing and obtain vitamin B ₁composition freeze-drying sheet.

Experimental data

The vitamin B obtained by above-described embodiment ₁composition freeze-drying sheet carries out following quality research test:

1, hardness, friability contrast test

Get vitamin B prepared by above-described embodiment respectively ₁composition freeze-drying sheet and vitamin B ₁ordinary tablet (commercially available) detects friability and hardness by " Chinese Pharmacopoeia " version in 2010 two annex X G inspection techniques, contrasts, the results are shown in following table:

Sample	Hardness/N	Friability
			Embodiment 1	65	<1％
Embodiment 2	68	<1％
			Ordinary tablet	70	<1％

Experimental data shows, vitamin B ₁composition freeze-drying sheet and ordinary tablet without significant difference, meet " Chinese Pharmacopoeia " version in 2010 to the requirement of tablet on friability and hardness.

2, disintegration contrast test

Get vitamin B prepared by above-described embodiment respectively ₁composition freeze-drying sheet and vitamin B ₁ordinary tablet (commercially available) operates by Chinese Pharmacopoeia (2010 editions) second annex X A, checks its disintegration.Result is as follows:

Vitamin B ₁ordinary tablet (commercially available)

Two, vitamin B ₁composition freeze-drying sheet (No. 1 to No. 3 is embodiment 1, and No. 4 to No. 6 is embodiment 2)

Result judges:

According to Chinese Pharmacopoeia (2010 editions) second vitamin B ₁tablet quality standard and Chinese Pharmacopoeia (2010 editions) second annex X A judge about the bioassay standard in disintegration of tablet time limit, vitamin B ₁sheet is no more than 15 minutes for qualified disintegration, and actual measurement is 12 minutes, and vitamin B ₁composition freeze-drying sheet (embodiment 1 and embodiment 2) disintegration is 6 minutes.It can thus be appreciated that vitamin B ₁composition freeze-drying sheet compares vitamin B disintegration ₁reduce by 50% (6 minutes) sheet (commercially available) disintegration, so vitamin B ₁composition freeze-drying sheet absorption of human body is faster, and the blood drug level peaking time compares vitamin B ₁ordinary tablet (commercially available) is short, and its bioavailability is higher, better efficacy.

More than show and describe ultimate principle of the present invention, principal character and advantage of the present invention.The technical staff of the industry should understand; the present invention is not restricted to the described embodiments; what describe in above-described embodiment and description is only preference of the present invention; be not used for limiting the present invention; without departing from the spirit and scope of the present invention; the present invention also has various changes and modifications, and these changes and improvements all fall in the claimed scope of the invention.Application claims protection domain is defined by appending claims and equivalent thereof.

Claims (2)

1. a vitamin B ₁composition freeze-drying sheet, is characterized in that, is prepared from by following raw material:

2. a vitamin B according to claim 1 ₁the preparation method of composition freeze-drying sheet, is characterized in that, comprises step as follows:

A, take the starch of component amount, add a certain amount of purified water and stir, by pH adjusting agent, the pH value of solution is controlled between 4-5, be then heated to 72 DEG C, be incubated 20 minutes, make the corn starch solution of 5 ~ 15% (W/V);

B, measure purified water 45ml, boil, add 85g sucrose, stir, after dissolving, continue to be heated to 100 DEG C, filter with purified cotton, the appropriate hot distilled water of filter is cleaned, and washing liquid and filtrate merge, and let cool, add appropriate distilled water, make full dose become 100ml, stir evenly, obtain B solution;

The solution that C, the solution and the step B that steps A are obtained obtain mixes, and fully stirs 30 minutes, is down to room temperature and obtains Semen Maydis-sucrose solution;

D, take vitamin B ₁50 grams, add in 1L Semen Maydis-sucrose solution, stir 25 ~ 35 minutes;

E, medicinal liquid measure vitamin B ₁after content, medicinal liquid is sub-packed in drug-containing dish, each drug-containing dish dress 1.0ml;

F, the drug-containing dish that medicinal liquid is housed is put into vacuum freezing drying oven, be cooled to subzero 45 DEG C, keep 2 hours, evacuation, then 0 DEG C is warming up to gradually, keep 2 hours, then be cooled to subzero 45 DEG C, keep 2 hours, be warming up to 0 DEG C gradually again, keep 2 ~ 4 hours, then be warming up to 28 ~ 32 DEG C of dryings 4 ~ 6 hours gradually, whole process vacuum remains on 10 handkerchiefs; Finally the drug-containing dish lid of powder charge is covered tightly, and load aluminium foil bag and carry out sealing and obtain vitamin B ₁composition freeze-drying sheet.