CN112843015A - Gabapentin capsule preparation and preparation method thereof - Google Patents
Gabapentin capsule preparation and preparation method thereof Download PDFInfo
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- CN112843015A CN112843015A CN202110377440.9A CN202110377440A CN112843015A CN 112843015 A CN112843015 A CN 112843015A CN 202110377440 A CN202110377440 A CN 202110377440A CN 112843015 A CN112843015 A CN 112843015A
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- gabapentin
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- arginine
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- UGJMXCAKCUNAIE-UHFFFAOYSA-N Gabapentin Chemical compound OC(=O)CC1(CN)CCCCC1 UGJMXCAKCUNAIE-UHFFFAOYSA-N 0.000 title claims abstract description 205
- 229960002870 gabapentin Drugs 0.000 title claims abstract description 102
- 239000002775 capsule Substances 0.000 title claims abstract description 55
- 238000002360 preparation method Methods 0.000 title claims abstract description 36
- 239000003814 drug Substances 0.000 claims abstract description 39
- 239000002994 raw material Substances 0.000 claims abstract description 18
- 229940079593 drug Drugs 0.000 claims abstract description 16
- 239000002245 particle Substances 0.000 claims abstract description 15
- 238000009826 distribution Methods 0.000 claims abstract description 11
- 238000011049 filling Methods 0.000 claims description 18
- 239000004475 Arginine Substances 0.000 claims description 17
- ODKSFYDXXFIFQN-UHFFFAOYSA-N arginine Natural products OC(=O)C(N)CCCNC(N)=N ODKSFYDXXFIFQN-UHFFFAOYSA-N 0.000 claims description 17
- 239000004474 valine Substances 0.000 claims description 15
- KZSNJWFQEVHDMF-BYPYZUCNSA-N L-valine Chemical compound CC(C)[C@H](N)C(O)=O KZSNJWFQEVHDMF-BYPYZUCNSA-N 0.000 claims description 14
- KZSNJWFQEVHDMF-UHFFFAOYSA-N Valine Natural products CC(C)C(N)C(O)=O KZSNJWFQEVHDMF-UHFFFAOYSA-N 0.000 claims description 14
- CSCPPACGZOOCGX-UHFFFAOYSA-N Acetone Chemical compound CC(C)=O CSCPPACGZOOCGX-UHFFFAOYSA-N 0.000 claims description 10
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 9
- 239000007963 capsule composition Substances 0.000 claims description 8
- 238000000034 method Methods 0.000 claims description 8
- 238000007873 sieving Methods 0.000 claims description 8
- 238000001914 filtration Methods 0.000 claims description 5
- 239000002671 adjuvant Substances 0.000 claims description 4
- 238000001035 drying Methods 0.000 claims description 4
- ODKSFYDXXFIFQN-BYPYZUCNSA-P L-argininium(2+) Chemical compound NC(=[NH2+])NCCC[C@H]([NH3+])C(O)=O ODKSFYDXXFIFQN-BYPYZUCNSA-P 0.000 claims description 3
- 125000000637 arginyl group Chemical group N[C@@H](CCCNC(N)=N)C(=O)* 0.000 claims description 2
- 239000008186 active pharmaceutical agent Substances 0.000 claims 5
- 229940088679 drug related substance Drugs 0.000 claims 5
- 238000004519 manufacturing process Methods 0.000 claims 1
- 230000000694 effects Effects 0.000 abstract description 9
- 239000000463 material Substances 0.000 abstract description 7
- 231100000331 toxic Toxicity 0.000 abstract description 6
- 230000002588 toxic effect Effects 0.000 abstract description 6
- 239000007857 degradation product Substances 0.000 abstract description 2
- 238000005516 engineering process Methods 0.000 abstract description 2
- 239000000203 mixture Substances 0.000 description 14
- 238000004090 dissolution Methods 0.000 description 12
- 239000013067 intermediate product Substances 0.000 description 12
- 238000004806 packaging method and process Methods 0.000 description 12
- 238000009472 formulation Methods 0.000 description 10
- 238000012360 testing method Methods 0.000 description 9
- 239000000243 solution Substances 0.000 description 7
- 238000003756 stirring Methods 0.000 description 6
- GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 description 5
- 239000012752 auxiliary agent Substances 0.000 description 5
- BTCSSZJGUNDROE-UHFFFAOYSA-N gamma-aminobutyric acid Chemical class NCCCC(O)=O BTCSSZJGUNDROE-UHFFFAOYSA-N 0.000 description 5
- 239000008101 lactose Substances 0.000 description 5
- 239000000047 product Substances 0.000 description 5
- 239000001961 anticonvulsive agent Substances 0.000 description 4
- 230000000052 comparative effect Effects 0.000 description 4
- OGNSCSPNOLGXSM-UHFFFAOYSA-N (+/-)-DABA Natural products NCCC(N)C(O)=O OGNSCSPNOLGXSM-UHFFFAOYSA-N 0.000 description 2
- 208000024777 Prion disease Diseases 0.000 description 2
- 208000018756 Variant Creutzfeldt-Jakob disease Diseases 0.000 description 2
- 238000010171 animal model Methods 0.000 description 2
- 229960003965 antiepileptics Drugs 0.000 description 2
- 208000005881 bovine spongiform encephalopathy Diseases 0.000 description 2
- 239000003153 chemical reaction reagent Substances 0.000 description 2
- 230000001186 cumulative effect Effects 0.000 description 2
- 206010015037 epilepsy Diseases 0.000 description 2
- 239000003797 essential amino acid Substances 0.000 description 2
- 235000020776 essential amino acid Nutrition 0.000 description 2
- 229960003692 gamma aminobutyric acid Drugs 0.000 description 2
- 208000010544 human prion disease Diseases 0.000 description 2
- 239000012535 impurity Substances 0.000 description 2
- 238000012986 modification Methods 0.000 description 2
- 230000004048 modification Effects 0.000 description 2
- 239000002244 precipitate Substances 0.000 description 2
- 239000008213 purified water Substances 0.000 description 2
- 238000004513 sizing Methods 0.000 description 2
- 206010067484 Adverse reaction Diseases 0.000 description 1
- 102100026189 Beta-galactosidase Human genes 0.000 description 1
- 229920002261 Corn starch Polymers 0.000 description 1
- 108090000790 Enzymes Proteins 0.000 description 1
- 102000004190 Enzymes Human genes 0.000 description 1
- 108010059881 Lactase Proteins 0.000 description 1
- 201000010538 Lactose Intolerance Diseases 0.000 description 1
- 206010027476 Metastases Diseases 0.000 description 1
- 241001465754 Metazoa Species 0.000 description 1
- 229920000881 Modified starch Polymers 0.000 description 1
- 208000008238 Muscle Spasticity Diseases 0.000 description 1
- 206010036376 Postherpetic Neuralgia Diseases 0.000 description 1
- 238000010521 absorption reaction Methods 0.000 description 1
- 239000004480 active ingredient Substances 0.000 description 1
- 230000006838 adverse reaction Effects 0.000 description 1
- 150000001413 amino acids Chemical class 0.000 description 1
- 206010002026 amyotrophic lateral sclerosis Diseases 0.000 description 1
- 230000036592 analgesia Effects 0.000 description 1
- 229940125681 anticonvulsant agent Drugs 0.000 description 1
- 230000004888 barrier function Effects 0.000 description 1
- 230000003542 behavioural effect Effects 0.000 description 1
- 108010005774 beta-Galactosidase Proteins 0.000 description 1
- 239000008280 blood Substances 0.000 description 1
- 210000004369 blood Anatomy 0.000 description 1
- 210000005013 brain tissue Anatomy 0.000 description 1
- YZBQHRLRFGPBSL-RXMQYKEDSA-N carbapenem Chemical compound C1C=CN2C(=O)C[C@H]21 YZBQHRLRFGPBSL-RXMQYKEDSA-N 0.000 description 1
- 238000006243 chemical reaction Methods 0.000 description 1
- 238000011109 contamination Methods 0.000 description 1
- 239000008120 corn starch Substances 0.000 description 1
- 235000013365 dairy product Nutrition 0.000 description 1
- 238000007865 diluting Methods 0.000 description 1
- 239000012738 dissolution medium Substances 0.000 description 1
- 230000002526 effect on cardiovascular system Effects 0.000 description 1
- 238000005538 encapsulation Methods 0.000 description 1
- 229940088598 enzyme Drugs 0.000 description 1
- 239000000706 filtrate Substances 0.000 description 1
- 235000013305 food Nutrition 0.000 description 1
- 238000004128 high performance liquid chromatography Methods 0.000 description 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 description 1
- 238000007689 inspection Methods 0.000 description 1
- 230000003993 interaction Effects 0.000 description 1
- 210000000936 intestine Anatomy 0.000 description 1
- 229940116108 lactase Drugs 0.000 description 1
- 239000007788 liquid Substances 0.000 description 1
- 210000004185 liver Anatomy 0.000 description 1
- 238000005259 measurement Methods 0.000 description 1
- 238000000691 measurement method Methods 0.000 description 1
- 230000004060 metabolic process Effects 0.000 description 1
- 208000004296 neuralgia Diseases 0.000 description 1
- 229940072228 neurontin Drugs 0.000 description 1
- 208000021722 neuropathic pain Diseases 0.000 description 1
- 238000011056 performance test Methods 0.000 description 1
- 230000000144 pharmacologic effect Effects 0.000 description 1
- 229920000642 polymer Polymers 0.000 description 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 description 1
- 230000008569 process Effects 0.000 description 1
- 102000004169 proteins and genes Human genes 0.000 description 1
- 108090000623 proteins and genes Proteins 0.000 description 1
- 239000012088 reference solution Substances 0.000 description 1
- 238000011160 research Methods 0.000 description 1
- 239000007787 solid Substances 0.000 description 1
- 208000018198 spasticity Diseases 0.000 description 1
- 239000000454 talc Substances 0.000 description 1
- 229910052623 talc Inorganic materials 0.000 description 1
- 238000005303 weighing Methods 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/19—Carboxylic acids, e.g. valproic acid
- A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/4841—Filling excipients; Inactive ingredients
- A61K9/4858—Organic compounds
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/08—Antiepileptics; Anticonvulsants
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Pain & Pain Management (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
The invention provides a gabapentin capsule preparation, which is a capsule directly filled with gabapentin bulk drug; the particle size distribution of the gabapentin raw material medicine is 50-70 meshes. The invention provides a simpler gabapentin capsule preparation technology, and toxic and side effects brought by auxiliary materials or degradation products are greatly reduced.
Description
Technical Field
The invention relates to the technical field of pharmacy, in particular to a gabapentin capsule preparation and a preparation method thereof.
Background
Gabapentin (Gabapentin) known as nortriptin; gabapentin; carbapenem; (ii) Neurontin; GO-3450, the antiepileptic drug first developed by Warner-Lanbert, USA, was first marketed in the United kingdom in 1993. Gabapentin is a novel antiepileptic drug, is a derivative of gamma-aminobutyric acid (GABA), has pharmacological effects different from those of the existing antiepileptic drugs, and recently researches show that gabapentin has the effect of changing GABA metabolism. Gabapentin has been shown to prevent epilepsy in various animal models, and in addition, has been shown to have effects in animal models of spasticity, analgesia, and amyotrophic lateral sclerosis. Gabapentin has a high affinity for novel binding sites of brain tissue, it passes through barriers in the body by amino acid metastases, and gabapentin has fewer behavioral and cardiovascular side effects than other anticonvulsants.
As a novel drug for effectively treating epilepsy, gabapentin is not metabolized in the body, is not bound to protein, does not induce liver drug enzymes, has no interaction with other drugs, is not affected by food when taken orally, and does not need to be monitored for blood concentration. Its domestic indications have now expanded to the treatment of post-herpetic neuralgia. Whereas in the uk gabapentin has been approved for the treatment of all neuropathic pain. Compared with the prior similar products, the medicine has the advantages of quick oral absorption, good tolerance, small toxic and side effects, good treatment effect and the like. It is expected that gabapentin is a very promising drug.
At present, most of gabapentin capsules at home and abroad comprise the following components: the main components are as follows: gabapentin; the auxiliary materials are as follows: lactose, corn starch and talc. However, lactose, like other dairy derived products, also faces the problem of contamination by Bovine Spongiform Encephalopathy (BSE) or animal Transmissible Spongiform Encephalopathy (TSE). Other adverse reactions due to lactose intolerance may also occur due to the lack of lactase in some populations' intestines. In the formula, primary amino group in gabapentin molecules is easy to have Maillard reaction with hydroxyl group in lactose to generate toxic and side gabapentin lactose polymer which is difficult to control, and the quality of gabapentin capsules is influenced. Secondly, although the pregelatinized starch is used for replacing lactose, the auxiliary materials also have little toxic and side effects, and the most ideal medicine can be prepared by adding the auxiliary materials as little as possible or not.
Disclosure of Invention
In view of the above, the technical problem to be solved by the present invention is to provide a gabapentin capsule preparation and a preparation method thereof, wherein a small amount of auxiliary agents are added, or no auxiliary agent is added, and the prepared capsule preparation has high stability.
In order to achieve the aim, the invention provides a gabapentin capsule preparation, which is a capsule directly filled with gabapentin bulk drug;
the particle size distribution of the gabapentin raw material medicine is 50-70 meshes.
Further preferably, the particle size of the gabapentin bulk drug is 60 meshes.
The method for preparing the gabapentin capsule preparation of the present invention is not particularly limited, and the gabapentin capsule preparation can be prepared by a method known to those skilled in the art.
Preferably, after the gabapentin raw material medicine is granulated by a proper granulator, the particle size distribution of the gabapentin raw material medicine meets the requirement, and the gabapentin raw material medicine is directly filled into capsules.
The invention realizes the purpose of directly filling capsules by controlling the particle size distribution of the gabapentin raw material medicine and creatively not adding auxiliary materials, greatly reduces the dosage of the auxiliary materials, reduces the toxic and side effects of the medicine, and does not influence the stability and the dissolution rate of the medicine.
The invention also provides a gabapentin capsule preparation, which is filled with gabapentin bulk drug and arginine.
The arginine is added into the gabapentin capsule preparation, so that the stability of the gabapentin capsule preparation can be further improved, and meanwhile, the arginine is essential amino acid for a human body, and the arginine is used as an auxiliary agent, so that the medicine has higher safety.
According to the invention, the preferable mass ratio of the gabapentin raw material medicine to the arginine is 10: 1.
Preferably, the particle size distribution of the gabapentin raw material medicine is 50-70 meshes; more preferably 60 mesh.
In the invention, the particle size distribution of the arginine is preferably 50-70 meshes, and more preferably 60 meshes.
The invention also provides a gabapentin capsule preparation, which is filled with gabapentin bulk drug and valine.
The invention adds valine into the gabapentin capsule preparation, can further improve the stability of the gabapentin capsule preparation, and meanwhile, the valine is essential amino acid for human bodies, and the valine is used as an auxiliary agent, so that the medicine has higher safety.
According to the invention, the preferable mass ratio of the gabapentin raw material medicine to valine is 10: 1.
According to the invention, the particle size distribution of the gabapentin raw material medicine is preferably 50-70 meshes, and more preferably 60 meshes.
In the present invention, the valine preferably has a particle size distribution of 50 to 70 mesh, and more preferably 60 mesh.
The invention provides a preparation method of the gabapentin capsule preparation, which comprises the following steps:
dripping the mixed water solution of the gabapentin bulk drug and the adjuvant into an acetone solution, filtering, drying, sieving and filling capsules to obtain a gabapentin capsule preparation;
the adjuvant is arginine or valine.
In the invention, the gabapentin raw material medicine and arginine or valine are preferably mixed and then dissolved in water.
The mass-volume ratio of the gabapentin bulk drug to water is preferably 1 g: 3 ml.
And then, dropwise adding the mixed water solution of the gabapentin bulk drug and arginine or valine into the acetone solution, and standing, preferably standing for 2-4 h, and more preferably standing for 3 h.
According to the invention, the dripping temperature is preferably 2-8 ℃.
And then filtered.
The solid obtained is then preferably dried under reduced pressure.
Then sieving the mixture to ensure that the particle size of the mixture of the gabapentin bulk drug and the arginine meets the requirement.
In the invention, the sieving is preferably 50-70 mesh sieving, and more preferably 60 mesh sieving.
And finally filling the capsules.
In a preferred embodiment of the present invention, the unit dose of the above gabapentin capsule preparation is 300 mg.
Compared with the prior art, the invention provides a gabapentin capsule preparation, which is a capsule directly filled with gabapentin bulk drug; the particle size distribution of the gabapentin raw material medicine is 50-70 meshes. The invention provides a simpler gabapentin capsule preparation technology, and toxic and side effects brought by auxiliary materials or degradation products are greatly reduced.
Detailed Description
In order to further illustrate the present invention, the gabapentin capsule formulation provided in the present invention and the preparation method thereof will be described in detail below with reference to examples.
Example 1
Prescription: gabapentin 300g
Making into 1000 pieces
The preparation method comprises the following steps:
the gabapentin raw material medicine is selected, sized by a gate type sizing machine, filtered by a 60-mesh screen, and encapsulated by a capsule filling machine, and the difference of the encapsulation amount is controlled within +/-5%. And (4) after the intermediate product is detected to have qualified filling quantity difference and dissolution rate, packaging the intermediate product by aluminum-plastic packaging, and then externally packaging the intermediate product to obtain the gabapentin capsule.
Comparative example 1
Prescription: gabapentin 300g
Making into 1000 pieces
The preparation method comprises the following steps:
the gabapentin raw material medicine is selected, sized by a gate type sizing machine, sieved by a 80-mesh screen, and encapsulated by a capsule filling machine, and the difference of the filling amount is controlled within +/-5%. And (4) after the intermediate product is detected to have qualified filling quantity difference and dissolution rate, packaging the intermediate product by aluminum-plastic packaging, and then externally packaging the intermediate product to obtain the gabapentin capsule.
Example 2
Prescription: gabapentin 300g
Arginine 30g
Making into 1000 pieces
The preparation method comprises the following steps:
taking 300g of gabapentin raw material medicine, adding 900ml of purified water, stirring and dissolving, adding 30g of arginine, stirring and dissolving, slowly dripping the solution into acetone, continuously stirring, standing for 3 hours after dripping is finished, filtering to obtain white crystalline precipitate, drying under reduced pressure, sieving the gabapentin arginine mixture with a 60-mesh sieve, filling capsules by a capsule filling machine, and controlling the filling quantity difference within +/-5%. And (4) after the intermediate product is detected to have qualified filling quantity difference and dissolution rate, packaging the intermediate product by aluminum-plastic packaging, and then externally packaging the intermediate product to obtain the gabapentin capsule.
Example 3
Prescription: gabapentin 300g
Valine 30g
Making into 1000 pieces
The preparation method comprises the following steps:
taking 300g of gabapentin raw material medicine, adding 900ml of purified water, stirring and dissolving, then adding 30g of valine, stirring and dissolving, slowly dripping the solution into acetone, continuously stirring, standing for 3 hours after dripping is finished, filtering to obtain white crystalline precipitate, drying under reduced pressure, sieving the gabapentin-valine mixture with a 60-mesh sieve, filling capsules by a capsule filling machine, and controlling the filling amount difference within +/-5%. And (4) after the intermediate product is detected to have qualified filling quantity difference and dissolution rate, packaging the intermediate product by aluminum-plastic packaging, and then externally packaging the intermediate product to obtain the gabapentin capsule.
Example 4 Performance testing
The gabapentin capsules prepared in the above examples and comparative examples were examined, and the results are shown in the following table 1:
TABLE 1 Performance test results
The inspection results show that the gabapentin capsule preparation prepared by the invention meets the quality requirements, the prescription is simple, the process is easy to operate, the product quality is stable and controllable, the content of single impurities and total impurities is small, and the content of active ingredients is high.
EXAMPLE 5 dissolution determination
Test formulation 1: gabapentin capsules prepared in example 1 of the present invention.
Test formulation 2: gabapentin capsules prepared in example 2 of the present invention.
Test formulation 3: gabapentin capsules prepared in example 3 of the present invention.
Test reagent 4: gabapentin capsules prepared in comparative example 1 of the present invention.
Reference formulation: gabapentin capsules (specification: 300mg) produced by Pfizer Pharma PFE GmbH (Germany).
Measurement method
Taking the product, according to determination method of dissolution rate and release rate (first method of 0931 of the general rule of the four parts of the 2020 edition of Chinese pharmacopoeia), using 900ml of water as dissolution medium, rotating speed of 100 r/min, operating according to the method, taking dissolution liquid at 5, 10, 15 and 30 minutes, filtering, and taking subsequent filtrate.
The reference solution is prepared by precisely weighing a proper amount of gabapentin reference, dissolving in water, quantitatively diluting to obtain a solution containing 0.3mg (0.3 g) per 1ml, and measuring by high performance liquid chromatography (0512 in the four ministry of general regulation of China pharmacopoeia 2020 edition) to calculate the cumulative dissolution amount. The results are shown in Table 2.
TABLE 2 dissolution rate measurement results
| Product(s) | 5min | 10min | 15min | 30min |
| Test formulation 1 | 73.6 | 98.8 | 99.4 | 100.1 |
| Test formulation 2 | 87.6 | 98.8 | 99.4 | 100.1 |
| Test formulation 3 | 88.3 | 98.5 | 99.6 | 100.2 |
| Test reagent 4 | 80.9 | 94.2 | 97.3 | 99.7 |
| Reference formulation | 85.5 | 97.3 | 99.2 | 99.8 |
From the above results, it can be seen that the tested formulations 1 to 3, i.e., gabapentin capsule formulations prepared in examples 1 to 3 of the present invention, had an equivalent cumulative dissolution rate to the reference formulation.
As can be seen from the above examples and comparative examples, the gabapentin capsule preparation prepared by the invention without adding any auxiliary agent or with a small amount of arginine has high stability and dissolution rate.
The above description of the embodiments is only intended to facilitate the understanding of the method of the invention and its core idea. It should be noted that, for those skilled in the art, it is possible to make various improvements and modifications to the present invention without departing from the principle of the present invention, and those improvements and modifications also fall within the scope of the claims of the present invention.
Claims (10)
1. A gabapentin capsule preparation is a capsule directly filled with gabapentin bulk drug;
the particle size distribution of the gabapentin raw material medicine is 50-70 meshes.
2. The gabapentin capsule formulation of claim 1, wherein the particle size of the gabapentin drug substance is 60 mesh.
3. A gabapentin capsule is prepared from gabapentin and arginine.
4. The gabapentin capsule formulation of claim 3, wherein the mass ratio of the gabapentin drug substance to arginine is 10: 1.
5. a gabapentin capsule preparation is prepared from gabapentin raw material and valine by filling into capsule.
6. The gabapentin capsule formulation of claim 5, wherein the mass ratio of gabapentin drug substance to valine is 10: 1.
7. the gabapentin capsule formulation according to any one of claims 3 to 6, wherein the particle size distribution of the gabapentin drug substance is 50 to 70 mesh.
8. The gabapentin capsule formulation of claim 7, wherein the particle size of the gabapentin drug substance is 60 mesh.
9. A method of preparing a gabapentin capsule formulation as claimed in any one of claims 1 to 8, comprising the steps of:
dripping the mixed water solution of the gabapentin bulk drug and the adjuvant into an acetone solution, filtering, drying, sieving and filling capsules to obtain a gabapentin capsule preparation;
the adjuvant is arginine or valine.
10. The production method according to claim 9, wherein the temperature of the dropwise addition is 2 to 8 ℃.
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN202110377440.9A CN112843015A (en) | 2021-04-08 | 2021-04-08 | Gabapentin capsule preparation and preparation method thereof |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN202110377440.9A CN112843015A (en) | 2021-04-08 | 2021-04-08 | Gabapentin capsule preparation and preparation method thereof |
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| CN112843015A true CN112843015A (en) | 2021-05-28 |
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|---|---|---|---|---|
| FR2781793A1 (en) * | 1998-08-03 | 2000-02-04 | Prographarm Lab | PROCESS FOR PRODUCING COATED GABAPENTINE GRANULES |
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| CN103385869A (en) * | 2012-05-09 | 2013-11-13 | 鲁南制药集团股份有限公司 | Medical application of gabapentin |
| CN104352476A (en) * | 2014-10-21 | 2015-02-18 | 齐宏 | Gabapentin capsule and preparation method thereof |
| CN105949042A (en) * | 2016-06-07 | 2016-09-21 | 王昌荣 | Gabapentin pharmaceutical composition and medical application thereof |
| CN112321442A (en) * | 2020-11-06 | 2021-02-05 | 中国药科大学 | Salt of gabapentin and 2, 6-pyridinedicarboxylic acid, preparation method and application thereof |
-
2021
- 2021-04-08 CN CN202110377440.9A patent/CN112843015A/en active Pending
Patent Citations (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1301155A (en) * | 1998-05-15 | 2001-06-27 | 沃尼尔·朗伯公司 | Stabilized pharmaceutical preparations of gamma-aminobutyric acid derivative process for preparing the same |
| FR2781793A1 (en) * | 1998-08-03 | 2000-02-04 | Prographarm Lab | PROCESS FOR PRODUCING COATED GABAPENTINE GRANULES |
| CN103385869A (en) * | 2012-05-09 | 2013-11-13 | 鲁南制药集团股份有限公司 | Medical application of gabapentin |
| CN104352476A (en) * | 2014-10-21 | 2015-02-18 | 齐宏 | Gabapentin capsule and preparation method thereof |
| CN105949042A (en) * | 2016-06-07 | 2016-09-21 | 王昌荣 | Gabapentin pharmaceutical composition and medical application thereof |
| CN112321442A (en) * | 2020-11-06 | 2021-02-05 | 中国药科大学 | Salt of gabapentin and 2, 6-pyridinedicarboxylic acid, preparation method and application thereof |
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