CN104523614A - Vitamin B6 composition freeze-dried tablet and preparation method thereof - Google Patents

Abstract

Relating to the technical field of medicine and medicine production, the invention provides a vitamin B6 composition freeze-dried tablet and a preparation method thereof. The freeze-dried tablet contains vitamin B6, starch and sucrose. The starch and sucrose are used as auxiliary materials. Heating process treatment is carried out on ordinary corn starch to improve the bonding and disintegrating effects of starch in the tablet and improve the formability of the tablet. The vitamin B6 composition freeze-dried tablet only needs starch and sucrose as the auxiliary materials. The vitamin B6 composition freeze-dried tablet adopts a freeze-drying process of two-cooling and two-heating. Two cooling and two heating enable better formability of the tablet, and enhance the dissolution of the tablet, thereby improving the bioavailability of the tablet. The tablet overcomes the disadvantages of common vitamin B6 tablets, and reduces the variety and dosage of auxiliary materials in vitamin B6 tablets. The tablet provided by the invention has high dissolution and bioavailability, and ensures the efficacy and safety of clinical medication.

Description

A kind of vitamin B 6composition 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 ₆composition freeze-drying sheet and preparation method thereof.

Background technology

Molecular formula C ₈h ₁₁nO ₃hCl

Molecular weight 205.64

Mainly participate in nearly hundred kinds of enzyme reactions with phosphoric acid Vitamin B6 (PLP) form.Most relevant with amino acid metabolism: to comprise turn amino, decarboxylation, a side chain cleavage, dewater and turn sulfurization.Participate in the conversion of homocysteine to methionine, have the effect reducing chronic disease, slight hyperhomocysteinemiainjury is considered to a kind of potentially dangerous factor of angiopathy, vitamin B ₆intervention can reduce homocysteine in plasma content.Clinical common formulations is tablet and injection.

Common vitamin B ₆in 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 ₆supplementary product kind and consumption in sheet, improve vitamin B ₆sheet 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 ₆sheet lyophilizing 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 ₆composition 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 ₆composition freeze-drying sheet, does adjuvant with starch and sucrose, and produce with freeze-dry process, this tablet overcomes above-mentioned usual vitamin B ₆the shortcoming of sheet, decreases vitamin B ₆supplementary 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 ₆composition freeze-drying sheet, is prepared from by following raw material:

A kind of vitamin B ₆the preparation method of composition freeze-drying 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 ₆10 grams, add in 1L Semen Maydis-sucrose solution, stir 25 ~ 35 minutes;

E, medicinal liquid measure vitamin B ₆after 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 ₆composition 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 ₆the 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 ₆in 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 ₆composition freeze-drying sheet only needs starch and sucrose two kinds of adjuvants.Vitamin B ₆the 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 with the pH value of pH adjusting agent by solution 6.5, be then heated to 72 DEG C, keep 120 minutes, make the corn starch solution of 9% (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, after solution be down to room temperature obtain Semen Maydis-sucrose solution.

D, take vitamin B ₆10g, adds in 1L Semen Maydis-sucrose solution, stirs 30 minutes.

E, medicinal liquid measure vitamin B ₆after 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 ₆composition freeze-drying sheet.

Embodiment 2

A, take the corn starch of 130g, the purified water adding 900ml stirs, and controls with the pH value of pH adjusting agent by solution 4-5, be then heated to 72 DEG C, keep 120 minutes, make the corn starch solution of 13% (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, after solution be down to room temperature obtain Semen Maydis-sucrose solution.

D, take vitamin B ₆10 grams (by 1000 calculations), add 1L Semen Maydis-sucrose solution, stir 30 minutes.

E, medicinal liquid measure vitamin B ₆after 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 ₆composition freeze-drying sheet.

Experimental data

The vitamin B6 composition freeze-drying sheet that above-described embodiment is obtained carries out following quality research test:

1, hardness, friability contrast test

Get vitamin B prepared by above-described embodiment respectively ₆composition freeze-drying sheet and vitamin B ₆ordinary 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	64.5	<1％
Embodiment 2	69.6	<1％
			Ordinary tablet (commercially available)	72	<1％

Experimental data shows, vitamin B ₆composition 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 ₆composition freeze-drying sheet and vitamin B ₆ordinary tablet (commercially available) operates by Chinese Pharmacopoeia (2010 editions) second annex X A, checks its disintegration.Result is as follows:

One, vitamin B ₆ordinary tablet (commercially available)

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

2. a vitamin B according to claim 1 ₆the 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 ₆10 grams, add in 1L Semen Maydis-sucrose solution, stir 25 ~ 35 minutes;

E, medicinal liquid measure vitamin B ₆after 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 ₆composition freeze-drying sheet.