CN1330298C - Oral liquid of metformin hydrochloride and preparation method - Google Patents
Oral liquid of metformin hydrochloride and preparation method Download PDFInfo
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- CN1330298C CN1330298C CNB2005100030807A CN200510003080A CN1330298C CN 1330298 C CN1330298 C CN 1330298C CN B2005100030807 A CNB2005100030807 A CN B2005100030807A CN 200510003080 A CN200510003080 A CN 200510003080A CN 1330298 C CN1330298 C CN 1330298C
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Abstract
The present invention discloses metformin hydrochloride oral liquid and a preparation method thereof. 25 to 100g/1000 ml of metformin hydrochloride as effective components is added, water is added, and the metformin hydrochloride and the water are heated for dissolving the metformin hydrochloride; steviosin is added, and the metformin hydrochloride, the water and the steviosin are stirred for 10 to 20 minutes for dissolving; orange essence and coconut essence are added, and the metformin hydrochloride, the water, the steviosin, the orange essence and the coconut essence are stirred for 10 to 20 minutes; finally, sodium benzoate is added, the metformin hydrochloride, the water, the steviosin, the orange essence, the coconut essence and the sodium benzoate are stirred for 10 to 20 minutes for dissolving, water is added to 1000 to 3000 ml, and then, the metformin hydrochloride, the water, the steviosin, the orange essence, the coconut essence and the sodium benzoate are stirred for 30 minutes, and the metformin hydrochloride oral liquid product is obtained by filtering, filling, moistly and heatedly sterilizing for 0.5 hour, sterilizing at 100(+/-)2 DEG C. and adding outer packing. The obtained medicament has stable properties, and the medicinal effect of the medicament is ensured. The preparation method has the advantages of simple and stable preparation process, easy control, simple equipment, low investment, simple operation, short production periodicity, etc. After the preparation is changed, patients are convenient to take, and the metformin hydrochloride oral liquid has the advantages of good mouth feel, rapid absorption and obvious curative effect.
Description
Technical field
The present invention relates to medicament preparation and preparation method thereof, specifically, relate to and treat oral liquid of metformin hydrochloride that uses in the diabetes and preparation method thereof.
Background technology
Diabetes are taking a disease of a kind of common pilosity, a kind of chronic systemic disease due to sensitivity normally absolute owing to insulin in the body or relative deficiency and the interior insulin of body reduces, classical symptom is polyuria, polydipsia, polyphagia, and loses weight, normal companion is weak, shallow complexion.Skin pruritus.Growth retardation.The patient with severe symptoms also causes complication sometimes, brings great misery and inconvenience to the patient.For the diabetes Chinese and western medicine some treatment meanss are arranged all, Chinese medicine also has the treatment proved recipe, wherein insulin-dependent (I type) mainly relies on insulinize, to non-insulin-depending type (II type) except dietetic therapy, for pharmacy variety in existing " diabetes pill ", " JIANGTANGSHU " etc. on the market, the Western medicine kind has " sulphanylureas ", " biguanides " etc., and wherein the metformin of biguanides (diformin tablet) is antidiabetic drug commonly used.Hydrochloric metformin (the C of this metformin
4H
11N
5HCl) be more than 95% of labelled amount.
In recent years, metformin hydrochloride tablet uses more for antidiabetic drug commonly used, also there is new dosage form to occur, relate to a kind of can slowly release in vivo as patent application " oral melbine hydrocloride slow-releasing preparation and preparation method thereof " (02133574.5), it is steady to keep blood drug level, and the half-life prolongs, and is used for the treatment of the hypoglycemic medicine of type ii diabetes, this slow releasing agent utilizes the imbibition of high viscosity macromolecular material to form gel, makes the slow releasing tablet of only taking every day once.This slow releasing agent be make macromolecular material that gel adds and auxiliary agent, operation is longer, production cost is higher.
Purpose of the present invention can not be brought into play hypoglycemic activity well to existing metformin hydrochloride ordinary tablet exactly, and take inconvenient characteristics, simultaneously for increasing the pharmacy variety of treatment diabetes, to adapt to the needs of different diabeticss, the inventor herein provides a kind of oral liquid of metformin hydrochloride through research, patient's taking convenience after changing dosage form absorbs fast, evident in efficacy.
Another purpose of the present invention provides the oral liquid of metformin hydrochloride preparation method.
Summary of the invention
The oral liquid of metformin hydrochloride preparation program that the inventor works out, its prescription is: in the cooperation ratio of metformin hydrochloride 25.0 ∽ 100g, steviosin 0.4 ∽ 1.6g, flavoring orange essence 1.25 ∽ 5.00ml, cocoanut flavour 1.25 ∽ 5.00ml, sodium benzoate 2.0 ∽ 8.0g, add an amount of purified water and be mixed with 1000 ∽ 3000ml oral administration solutions, wherein unit is according to the amount of preparation decision in producing, unit of weight can be g, kg, and volume unit can be ml, L;
Its preparation method is that the metformin hydrochloride that takes by weighing formula ratio adds in the suitable quantity of water, stirs dissolving in 10 minutes, adds steviosin again and stirs 10 ∽ dissolving in 20 minutes, adding flavoring orange essence, cocoanut flavour stirred 10 ∽ 20 minutes, add at last after sodium benzoate stirs 10 ∽ 20 minutes dissolving, add water and supply 1000 ∽ 3000ml, stirred 30 minutes, filter, fill, moist heat sterilization 0.5 hour, 100 ± 2 ℃ of sterilising temps, outer package can obtain the oral liquid of metformin hydrochloride product.
According to above-mentioned oral liquid of metformin hydrochloride, its preferable prescription is: in the cooperation ratio of metformin hydrochloride 25.0g, steviosin 0.4g, flavoring orange essence 1.25ml, cocoanut flavour 1.25ml, sodium benzoate 2.0g, add an amount of purified water and be assigned to the 1000ml oral administration solution.
According to above-mentioned at metformin hydrochloride (C
4H
11N
5HCl) in the preparation method of oral administration solution, the best is got metformin hydrochloride 25.0g, add water 100ml, being heated to 50 ℃ dissolves metformin hydrochloride fully, add steviosin 0.4g again, stir dissolving in 10 minutes,, add flavoring orange essence 1.25ml, cocoanut flavour 1.25, stirred 10 minutes, after adding sodium benzoate 2.0g stirring dissolving in 10 minutes at last, add water and supply 1000ml, stirred 30 minutes, filter, fill, moist heat sterilization 0.5 hour, 100 ± 2 ℃ of sterilising temps, outer package can obtain the oral liquid of metformin hydrochloride product.
Metformin hydrochloride (C
4H
11N
5HCl), be 1,1 dimethyl biguanide hydrochloride.Calculate its (C by dry product
4H
11N
5HCl) content must not be less than 98.5%.Metformin hydrochloride is white crystals or crystalline powder, nontoxic, odorless.Metformin hydrochloride is easily molten in water, and slightly soluble in ethanol is insoluble in chloroform or ether.Mainly it is used as antidiabetic drug in the treatment diabetes at present.
Metformin hydrochloride (C in the 1000ml oral liquid of metformin hydrochloride
4H
11N
5HCl) content is 25 ∽ 50g.
Chemical medicine preparation " metformin hydrochloride tablet " dosage changing form of the existing national standard of oral liquid of metformin hydrochloride of the present invention system and getting, because of tablet need add some excipient, and through compression forming, dissolution is slower, and the adjuvant that oral solution adds is few, and the dispersion of medicine is bigger, absorbs fast and the speed of proving effective, the dispersion of active ingredient is more even, has improved the patient's who can not or be reluctant to swallow tablet compliance.Therefore changing its dosage form is oral solution.
Oral liquid of metformin hydrochloride of the present invention is patient's taking convenience after changing dosage form, and mouthfeel is good, absorption is fast, and curative effect is still remarkable, and the adjuvant that preparation technology adds does not have adverse influence to the medicament stable in properties, guarantees the drug effect of medicament.It is simple, stable and be easy to grasp that its preparation technology also has preparation technology, and equipment is simple, reduced investment, advantage such as simple to operate, with short production cycle.
The specific embodiment
The effective ingredient metformin hydrochloride of oral liquid of metformin hydrochloride of the present invention has blood sugar lowering to diabetes in treatment in the diabetes, alleviates and eliminates effect such as diabetes condition of illness gradually.Through clinical research confirmation, on former treatment (diet control and sulfonylureas drugs for diabetes treatment) basis, add with oral liquid of metformin hydrochloride (I) by 23 examples.The above person of fasting glucose 10mmol/L, (0.5g in metformin hydrochloride) 3 times/day, be the A group, the following person of fasting glucose 10mmol/L, (0.25g in metformin hydrochloride) 3 times/day, be the B group, add survey respectively around (I) preceding and back the empty stomach and 2 hours after the meal hemoglobin (HbA, C), cholesterol (ch), triglyceride (TG), creatinine (Cr), blood urea nitrogen (BUN), ALT and body weight, blood pressure.Observation shows: type i diabetes patient blood glucose and blood fat there are the reduction effect, and especially obvious to the post-prandial glycemia effect, obvious when heavy dose of.
The toxicity research situation of oral liquid of metformin hydrochloride: by to 64 routine patient's clinical observations, just select the oral liquid of metformin hydrochloride of various dose for use according to blood glucose, every day, dosage was equivalent to metformin hydrochloride 0.5g ∽ 5g, gradation is oral, the carbohydrate tolerance of back check all around, insulin release test.The result treats back and the preceding relatively P of treatment
All＜0.001, insulin level does not have significant change before and after the treatment; No obvious toxic-side effects.In conjunction with former metformin hydrochloride tablet long-term toxicity test for animals situation: 50 times, 30 times and 10 times of clinical dosage, the no abnormal performance of each dosage group experimental animal, compare no significant difference (P＜0.05) with the blank group, 2 weeks of drug withdrawal, do not find the retardance toxic reaction, show that the clinical maximum consumption per day toxicity of this oral liquid of metformin hydrochloride is lower, clinical practice safety.
The oral liquid of metformin hydrochloride clinical practice is to treating the anovulatory clinical trial situation of hyperinsulinemia: to 29 routine hyperinsulinemia patients, carry out 12 all oral liquid of metformin hydrochloride treatments, wherein 19 examples are all accepted clomifene 1 cycle of treatment before and after the oral liquid of metformin hydrochloride treatment.Observe the variation of treatment front and back plasma testosterone level and ovulation function.The result: the plasma testosterone level before the oral liquid of metformin hydrochloride treatment is (2.7 ± 1.0) nmol/L., treats 4 Zhou Houwei (1.9 ± 1.0) nmol/L., and both compare, and difference has significance (P＜0.05).Spontaneous ovulation has 3 examples before the oral liquid of metformin hydrochloride treatment, and 10 examples (wherein 8 examples are former anovulation person) (P＜0.05) are arranged after the treatment; 19 examples were all taken clomifene at oral liquid of metformin hydrochloride before and after treatment, the induced ovulation success has 8 examples before the metformin hydrochloride treatment, 15 examples (P＜0.05) are arranged after the treatment.Conclusion: hyperinsulinemia causes that plasma testosterone level descends, and ovulation function has improvement.
Following examples can further specify preparation method of the present invention:
Embodiment 1: take by weighing metformin hydrochloride 100kg, add water 120L, place 50 ℃ of stirrings dissolving in 20 minutes that metformin hydrochloride is dissolved fully, add steviosin 1.3kg again and stir dissolving in 15 minutes, add flavoring orange essence 5L, cocoanut flavour 5L, stirred 10 minutes, after adding sodium benzoate 5kg stirring dissolving in 10 minutes at last, add water and supply 4000L, stirred 30 minutes, filter, fill, moist heat sterilization 0.5 hour, 100 ± 2 ℃ of sterilising temps, add outer package, can obtain the oral liquid of metformin hydrochloride product.
Claims (3)
1, a kind of oral liquid of metformin hydrochloride, be characterised in that its prescription is: metformin hydrochloride adds the oral administration solution that an amount of purified water is mixed with 1000～3000ml in the cooperation ratio of 25.0～100g, steviosin 0.4～1.6g, flavoring orange essence 1.25～5.00ml, cocoanut flavour 1.25～5.00ml, sodium benzoate 2.0～8.0g;
Its preparation method is that the metformin hydrochloride that takes by weighing formula ratio adds in the suitable quantity of water, stirs dissolving in 10 minutes, adds steviosin again and stirs dissolving in 10～20 minutes, add flavoring orange essence, cocoanut flavour stirring 10～20 minutes, after adding sodium benzoate stirring dissolving in 10～20 minutes at last, add water and supply 1000～3000ml, stirred 30 minutes, filter, fill, moist heat sterilization 0.5 hour, 100 ± 2 ℃ of sterilising temps, add outer package, can obtain the oral liquid of metformin hydrochloride product.
2, oral liquid of metformin hydrochloride according to claim 1, its feature at its prescription is: cooperate ratio in metformin hydrochloride 25.0g, steviosin 0.4g, flavoring orange essence 1.25ml, cocoanut flavour 1.25ml, sodium benzoate 2.0g, add an amount of purified water and be assigned to the 1000ml oral administration solution.
3, the preparation method of oral liquid of metformin hydrochloride according to claim 1, it is characterized in that getting metformin hydrochloride 25.0g, add water 100ml, be heated to 50 ℃, metformin hydrochloride is dissolved fully, add steviosin 0.4g again, stir dissolving in 10 minutes, add flavoring orange essence 1.25ml, cocoanut flavour 1.25ml stirred 10 minutes, add sodium benzoate 2.0g at last, after stirring dissolving in 10 minutes, add water and supply 1000ml, stirred 30 minutes, filter, fill, moist heat sterilization 0.5 hour, 100 ± 2 ℃ of sterilising temps, add outer package, can obtain the metformin hydrochloride oral liquid product.
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNB2005100030807A CN1330298C (en) | 2005-05-26 | 2005-05-26 | Oral liquid of metformin hydrochloride and preparation method |
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|---|---|---|---|
| CNB2005100030807A CN1330298C (en) | 2005-05-26 | 2005-05-26 | Oral liquid of metformin hydrochloride and preparation method |
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|---|---|
| CN1695602A CN1695602A (en) | 2005-11-16 |
| CN1330298C true CN1330298C (en) | 2007-08-08 |
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| CNB2005100030807A Active CN1330298C (en) | 2005-05-26 | 2005-05-26 | Oral liquid of metformin hydrochloride and preparation method |
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| US9101160B2 (en) | 2005-11-23 | 2015-08-11 | The Coca-Cola Company | Condiments with high-potency sweetener |
| US8017168B2 (en) | 2006-11-02 | 2011-09-13 | The Coca-Cola Company | High-potency sweetener composition with rubisco protein, rubiscolin, rubiscolin derivatives, ace inhibitory peptides, and combinations thereof, and compositions sweetened therewith |
| US20080107787A1 (en) * | 2006-11-02 | 2008-05-08 | The Coca-Cola Company | Anti-Diabetic Composition with High-Potency Sweetener |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1391890A (en) * | 2002-08-05 | 2003-01-22 | 成都恒瑞制药有限公司 | Oral melbine hydrocloride slow-releasing prepn and its preparing method |
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Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1391890A (en) * | 2002-08-05 | 2003-01-22 | 成都恒瑞制药有限公司 | Oral melbine hydrocloride slow-releasing prepn and its preparing method |
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