A kind of Chinese medicinal soft capsule for the treatment of chronic cholecystitis, cholelithiasis and preparation method thereof
Technical field:
The present invention relates to a kind of is the soft capsule preparation and preparation method thereof of active component with the Oleum menthae, belongs to medical technical field.
Background technology:
Chronic cholecystitis is a common clinical, and frequently-occurring disease belongs to the traditional Chinese medical science " gallbladder-distention ", " hypochondriac pain " category.Pathogenesis is smooth or unhygienic diet because of the melancholy of feelings will, disturbs on the greasy or blood of surfeit, causes the stagnation of QI knot of liver and gall.Hyperamization is become silted up by the stagnation of QI, becomes silted up and heat-transformation, and heat is pented up with spleen is wet, becomes the disease of dampness-heat in the liver and gallbladder.Courage stagnation of QI and blood may bring about pain, bile flow backwards then yellow, do not loose if heat is long-pending, and the fire-transformation that then suppurates, excessive noxious heat expands and goes into blood vessel.If it is not smooth that bile becomes silted up for a long time, condensing forms sandstone.Work as QI stagnation of the liver and galibladder, during damp and hot heap soil or fertilizer over and around the roots resistance, the liver failing to maintain the normal flow of QI then, the gallbladder disalignment is clear, makes pathogenic fire derived from stagnation of liver-QI, decocts the bile of pent-up, forms sandstone, burn gallbladder film.Mainly be summed up as: the stagnation of QI, damp and hot, the stasis of blood is turbid.Cholelithiasis also can belong to Chinese medicine " hypochondriac pain ", " yellow cellulitis " category.Traditional Chinese medical science ancient literature has the record of many similar cholelithiasis.The gallbladder being attached to the liver, liver and gall are the exterior and the interior each other, and gallbladder is " mansion of middle essence ", and bile is borrowed " gas after the liver overflows in gallbladder, builds up to form ".In China, along with improving constantly of people's living standard, the change of dietary habit, the relative incidence rate of cholelithiasis has been the tendency of obvious change, and in China, the relative incidence rate of cholelithiasis rises year by year in some big cities, and is existing near level of developed countries.
The etiology that modern medicine proposes chronic cholecystitis mainly contains at present: gallbladder stream stasis, bacterial infection, Metabolic disorder, neurological disorders and the change of bile chemical analysis etc.Also can delay outbreak repeatedly by acute cholecystitis.In recent years propose adiposis patient again and do not eat the cause of disease that breakfast is chronic cholecystitis.In addition, clinical confirmation has 70% patient to merge cholelithiasis.
Western medicine is by antiinflammatory, and expansion gallbladder, biliary tract and the about flesh of expansion are treated cholecystitis or calculus, serious armrest art.But Western medicine is taken for a long time, and side effect is big, and patient is difficult to tolerance.Clinical practice proves, uses the western medicine effect undesirable merely.Treat one of this sick main method and Chinese medicine is China, advantage more and more is subjected to attracting attention of common people to Chinese medicine because of its special effect, toxic and side effects be little etc.
Herba Menthae is the dry aerial parts of labiate Herba Menthae Mentha haplocalyxBriq., and is cool in nature, and acrid in the mouth is returned lung, Liver Channel, now records in " one one of Chinese pharmacopoeia version in 2000, Oleum menthae is the volatile oil that extracts from Herba Menthae.The modern pharmacology effect studies show that Herba Menthae Haplocalycis volatile oil and wherein main component more powerful function of gallbladder promoting, lithodialysis, analgesia and antiinflammatory action are arranged.The main component menthol of Herba Menthae Haplocalycis volatile oil and menthone 260mM/kg give rat oral, show as more powerful choleretic effect.Give menthol after 3 ~ 4 hours, the bile output, increase by 4 times approximately, and effect subsequently weakens.Menthone has similar action and more lasting, and the bile output increases by 50~100% approximately after taking medicine 5 hours.Have experiment to show, pure Oleum menthae can be that to be dissolved into diameter be about 2mm to the mixed type cholelithiasis of 7mm with diameter.There is bibliographical information Oleum menthae Dichlorodiphenyl Acetate to cause the mouse writhing reaction obvious suppression effect is arranged.Be the compound menthol injection of main component according to another report with the Mentholum, be used to local postoperative analgesia clinically as long-acting local anaesthesia preparation, respond well, and effect is lasting.Folium Menthae extract 250mg/ml lumbar injection is 60%~100% to the bullate suppression ratio of rat carrageenan foot, and main effective ingredient is a menthol.
The DANSHU JIAONANG of present clinical use is hard capsule, and the principal agent composition is exactly an Oleum menthae in its prescription, and content is white glossy granule, the special fragrance of tool, acrid in the mouth, cold.Function is a liver-smoothing, qi-regulating, function of gallbladder promoting.DANSHU JIAONANG has been put into national basic medical insurance medicine catalogue as the Chinese patent medicine commonly used of liver-gallbladder disease.In recent years, obtained application more and more widely clinically.Though the clinical practice of DANSHU JIAONANG is fine, but as principal agent is the capsule of volatile oil, exist following significant disadvantages: (1) is owing to the Oleum menthae in the DANSHU prescription volatilizees easily, so, when being made into common hard capsule preparation, will inevitably lose its effective ingredient in the pelletization, affect the treatment.Although DANSHU JIAONANG has been controlled its content by assay, the loss in the preparation process has at least also caused the waste of resource.(2) because Oleum menthae has special fragrance, and common hard capsule preparation can not well be covered up, so, brought certain inconvenience for patient's medication.(3) the common hard capsule preparation of DANSHU is because seal is bad, and Oleum menthae is volatile, causes the medicine instability.In addition, for volatile oil, also there are shortcomings such as content distribution is inhomogeneous, bioavailability is low with making hard capsule after its granulation.
Summary of the invention:
The purpose of this invention is to provide a kind of is the treatment chronic cholecystitis of main component, the Chinese medicinal soft capsule preparation of cholelithiasis with the Oleum menthae.
It is the treatment chronic cholecystitis of main component, the preparation method of cholelithiasis Chinese medicinal soft capsule preparation with the Oleum menthae that another object of the present invention provides a kind of.
The Chinese medicinal soft capsule preparation of treatment chronic cholecystitis of the present invention, cholelithiasis, form by soft capsule shell and content, content is made up of Oleum menthae and pharmaceutic adjuvant, pharmaceutic adjuvant be can with the aqueous material of active component Oleum menthae mix homogeneously, be selected from PEG400 (PEG400), Tween 80, glycerol, propylene glycol, isopropyl alcohol, dehydrogenation soybean oil, vegetable oil, fragrant wet goods, the weight proportion of active component and pharmaceutic adjuvant, be Oleum menthae by weight: pharmaceutic adjuvant=1: 0.5-1: 5; Wherein in every soft capsule, the content of Oleum menthae is by the normal capsules grain, and every contains Oleum menthae 0.02~0.2 gram; Soft capsule shell prepares with conventional method, is generally filled a prescription in certain proportion by gelatin, G ﹠ W and makes, and by weight, gelatin, G ﹠ W preferred proportion are 10: 3.1~4.0: 7-15.
Soft capsule of the present invention is preferably filled a prescription and consisted of every soft capsule and contain: Oleum menthae 0.02~0.2 gram, PEG400 or vegetable oil are the 0.01-0.5 gram; Be more preferably Oleum menthae 0.08~0.12 gram, PEG400 or vegetable oil are the 0.05-0.3 gram; Particularly preferred is Oleum menthae 0.1 gram, and PEG400 or vegetable oil are the 0.08-0.15 gram, and even with the mixture content of adjuvant by the principal agent of this ratio preparation, good fluidity is fit to pack into, and the soft capsule loading amount of preparation is accurate, even.
Chinese medicinal soft capsule preparation of the present invention can adopt following method preparation: get gelatin, G ﹠ W respectively, make its abundant imbibition with adding an amount of water in the gelatin earlier, insert in the glue pot behind glycerol and the remaining water mixing and be heated to uniform temperature, add expansible gelatin, after fully stirring, leave standstill, insulation, standby; Get Oleum menthae and pharmaceutic adjuvant respectively, fully stir and make mix homogeneously, the medicinal liquid for preparing is poured in the pellet processing machine, regulate loading amount, the hothouse drying is put in typing, packing, promptly.
The content of Chinese medicinal soft capsule of the present invention is a volatility oily liquid, so the content and the stability of control medicine are particularly important.Because the content of Chinese medicinal soft capsule of the present invention is by Oleum menthae and the mixed uniformly liquid of oily adjuvant, so uniformity of dosage units will be better than the hard capsule preparation with solid adjuvant material absorption far away.Stability test also shows in addition, originally the main component Mentholum content in the Oleum menthae is the Chinese medicinal soft capsule of the present invention of 32.8mg/ grain, through the investigation that keeps sample of 12 months room temperatures, content still has the 32.7mg/ grain, content does not almost change, and DANSHU YINGJIAONANG through 12 months room temperature keep sample investigate after, Mentholum content is then reduced to the 26.5mg/ grain by original 30.6mg/ grain, content has descended about 13.4%.Show that more than the content of Chinese medicinal soft capsule of the present invention is even, good stability.
The present invention makes the appropriate soft capsule of proportioning with new preparation technique with Oleum menthae, compares with existing hard capsule, has following tangible advantage: (1) has effectively controlled the volatilization of the Oleum menthae in the prescription, and quality is more stable.(2) well covered up the special fragrance of Oleum menthae, so brought very big convenience for patient's medication.(3) dispersion of medicine, stripping is fast, the bioavailability height.(4) side effect is little.(5) soft capsule with method preparation provided by the invention can reduce irritating abnormal smells from the patient in preparation process, reduces and pollutes.(6) overcome the difficulty that volatility big product is difficult to make soft capsule.(7) prolonged the storage life.(8) easier absorption.(9) better efficacy.
The specific embodiment:
The following example is intended to further describe for example the present invention, rather than limits the present invention by any way.Principal agent in following examples, adjuvant source:
Title | The source | Specification (standard) |
Oleum menthae | Nantong Herba Menthae factory | Meet Chinese Pharmacopoeia version regulation in 2000 |
Gelatin | Qingdao gelatin Co., Ltd | Meet Chinese Pharmacopoeia version regulation in 2000 |
Vegetable oil | Grain and oil company limited in Shanghai is good | Q/TEFO?5 |
Glycerol | HeFei University of Technology's chemical reagent | Meet Chinese Pharmacopoeia version regulation in 2000 |
Embodiment 1:
Get gelatin 1000g, glycerol 400g, water 1000g makes its abundant imbibition with the water that adds 300g in the gelatin earlier, insert in the glue pot behind glycerol and the remaining water mixing and be heated to 70 ~ 80 ℃, add expansible gelatin, after fully stirring, leave standstill, 60 ℃ of insulations, standby; Get each 100g of Oleum menthae and vegetable oil respectively, fully stir and make mix homogeneously, the medicinal liquid for preparing is poured in the pellet processing machine, the adjusting loading amount is 0.2g, and the hothouse drying is put in typing, packing, promptly.
Embodiment 2:
Get gelatin 1000g, glycerol 300g, water 800g makes its abundant imbibition with the water that adds 300g in the gelatin earlier, insert in the glue pot behind glycerol and the remaining water mixing and be heated to 70 ~ 80 ℃, add expansible gelatin, after fully stirring, leave standstill, 60 ℃ of insulations, standby; Get each 100g of Oleum menthae and vegetable oil respectively, fully stir and make mix homogeneously, the medicinal liquid for preparing is poured in the pellet processing machine, the adjusting loading amount is 0.3g, and the hothouse drying is put in typing, packing, promptly.
Embodiment 3:
Get gelatin 1000g, glycerol 400g, water 900g makes its abundant imbibition with the water that adds 300g in the gelatin earlier, insert in the glue pot behind glycerol and the remaining water mixing and be heated to 70 ~ 80 ℃, add expansible gelatin, after fully stirring, leave standstill, 60 ℃ of insulations, standby; Get Oleum menthae 100g and vegetable oil 200g respectively, fully stir and make mix homogeneously, the medicinal liquid for preparing is poured in the pellet processing machine, the adjusting loading amount is 0.3g, and the hothouse drying is put in typing, packing, promptly.
Embodiment 4:
Get gelatin 1000g, glycerol 300g, water 1000g makes its abundant imbibition with the water that adds 300g in the gelatin earlier, insert in the glue pot behind glycerol and the remaining water mixing and be heated to 70 ~ 80 ℃, add expansible gelatin, after fully stirring, leave standstill, 60 ℃ of insulations, standby; Get Oleum menthae 100 and 100g PEG400 respectively, fully stir and make mix homogeneously, the medicinal liquid for preparing is poured in the pellet processing machine, the adjusting loading amount is 0.2g, and the hothouse drying is put in typing, packing, promptly.