COMPOSITION AND METHOD FOR PREPARING PAIN RELIEVING DRUG

Abstract

The present invention discloses a composition for preparing a pain relieving drug, which includes poplar bark, Ligusticum wallichii, curcumin, ambergris, processed Radix Aconiti Lateralis, ray cartilage extract, wild ginseng, fructus psoraleae, garden balsam stem, pratt mountainash root-bark, annona muricata, Arisaema heterophyllum Blume, resina draconis, frankincense, myrrh, Brazilian sapodilla and camphor. The composition can be added with an appropriate auxiliary material to be made into dosage forms suitable for oral administration or external use, such as oral liquid, a patch, a liniment, a sustained-release agent and the like.

Claims

1. A composition for preparing a pain relieving drug, wherein the composition comprises the following components in parts by weight: 50-100 parts of poplar bark, 15-20 parts of Ligusticum wallichii, 10-15 parts of curcumin, 0.1-0.3 parts of ambergris, 10-12 parts of processed Radix Aconiti Lateralis, 50-150 parts of ray cartilage extract, 35-50 parts of wild ginseng, 15-30 parts of fructus psoraleae, 30-70 parts of garden balsam stem, 25-30 parts of pratt mountainash root-bark, 100-200 parts of annona muricata, 50-100 parts of Arisaema heterophyllum Blume, 50-100 parts of resina draconis, 15-25 parts of frankincense, 15-25 parts of myrrh, 20-30 parts of Brazilian sapodilla, and 3-5 parts of camphor.

2. The composition for preparing a pain relieving drug according to claim 1, wherein the composition comprises the following components in parts by weight: 80 parts of poplar bark, 18 parts of Ligusticum wallichii, 12 parts of curcumin, 0.2 parts of ambergris, 11 parts of processed Radix Aconiti Lateralis, 100 parts of ray cartilage extract, 40 parts of wild ginseng, 20 parts of fructus psoraleae, 50 parts of garden balsam stem, 28 parts of pratt mountainash root-bark, 150 parts of annona muricata, 80 parts of Arisaema heterophyllum Blume, 80 parts of resina draconis, 20 parts of frankincense, 20 parts of myrrh, 25 parts of Brazilian sapodilla, and 4 parts of camphor.

3. A method for preparing a pain relieving drug for external use, comprising the following preparation steps: Step 1: weighing raw herbal materials according to a formula amount, taking Arisaema heterophyllum Blume, resina draconis, frankincense, myrrh at 90% of the formula amount, soaking them in 75% ethanol as a solvent for 48 hours, percolating at a speed of 1 ml/min per kilogram, collecting a filtrate, recovering the ethanol, and continually concentrating the filtrate to obtain a extractum with a relative density of 1.08-1.10; Step 2: adding 5 grams of camphor and 25 milliliters of distilled water, and adding the remaining 10% drugs of Arisaema heterophyllum Blume, curcumin, frankincense, myrrh and the like, grinding with a colloid mill to be ready for use, taking gelatin and adding water into it to dissolve it at 60 C., adding glycerol and diatomite into it, and uniformly mixing with the aforementioned ready-for-use solutions of Arisaema heterophyllum Blume and the like to prepare coating liquid; and Step 3: coating, cutting and preparing the prepared coating liquid into a patch.

4. A method for preparing a pain relieving drug for external use, comprising the following preparation steps: Step 1: weighing raw herbal materials according to a formula amount, taking poplar bark, processed Radix Aconiti Lateralis, fructus psoraleae raw material powder, annona muricata, curcumin and the like raw material powder, microcrystalline cellulose and starch at the formula amount, placing all of them into a fluidized bed, spraying a proper amount of distilled water onto them for binding, stop spraying when pellets are controlled to be about 0.18-0.22 grams, and drying the pellets at 60 C. for 2 hours, sieving to select 30-mesh and 60-mesh pellets; Step 2: placing the drug-loaded pellets into a fluidized bed, and spraying slow-release coating liquid onto the surface of the pellets for surface sealing, stop spraying after the coating weight is increased by 5%, continually drying at 55-60 C. for 0.5 h to obtain film-coated sustained-release pellets; and Step 3: encapsulating the 30-mesh pellets into capsules, and packaging the 60-mesh pellets to obtain traditional Chinese medicine of sustained-release capsules and pellets.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0036] The present invention will be further described below with reference to specific examples:

Example 1: Preparing a Composition into Oral Liquid

[0037] 50-100 parts of poplar bark, 15-20 parts of Ligusticum wallichii, 10-15 parts of curcumin, 0.1-0.3 parts of ambergris, 10-12 parts of processed Radix Aconiti Lateralis, 50-150 parts of ray cartilage extract, 35-50 parts of wild ginseng, 15-30 parts of fructus psoraleae, 30-70 parts of garden balsam stem, 25-30 parts of pratt mountainash root-bark, 100-200 parts of annona muricata, 50-100 parts of Arisaema heterophyllum Blume, 50-100 parts of resina draconis, 15-25 parts of frankincense, 15-25 parts of myrrh, 20-30 parts of Brazilian sapodilla, and 3-5 parts of camphor were prepared into oral liquid.

[0038] The preparation method is as follows: (1) the poplar bark, Ligusticum wallichii, curcumin, ambergris, processed Radix Aconiti Lateralis, ray cartilage extract, wild ginseng, fructus psoraleae, garden balsam stem, pratt mountainash root-bark, annona muricata, Arisaema heterophyllum Blume, resina draconis, frankincense, myrrh, Brazilian sapodilla, and camphor are crushed.

[0039] (2) the raw material powder was weighed at the aforementioned weight, added with distilled water under stirring, and extracted at a controlled temperature of 80 C. for 1 hour, and filtered, the filter residue was added with water, extracted at 80 C. for 0.5 h, and filtered, and the filtrates were combined and concentrated at 80 C. under reduced pressure.

[0040] (3) Formulating: the above concentrated solutions were uniformly mixed, added with maltooligosaccharide and glucose, filtered, sterilized, and encapsulated to obtain the product.

Example 2: Preparing a Composition into a Patch, a Liniment

[0041] The poplar bark, Ligusticum wallichii, curcumin, ambergris, processed Radix Aconiti Lateralis, ray cartilage extract, wild ginseng, fructus psoraleae, garden balsam stem, pratt mountainash root-bark, annona muricata, Arisaema heterophyllum Blume, frankincense, myrrh, and Brazilian sapodilla were taken at 90% of the formula amount, soaked in 75% ethanol as a solvent for 48 hours, percolated at a speed of 1 ml/min per kilogram, a filtrate was collected, the ethanol was recovered, and the filtrate was continually concentrated to obtain a extractum with a relative density of 1.08-1.10. The extractum was added with resina draconis, camphor and water, and added with the remaining 10% drugs of poplar bark, Ligusticum wallichii, curcumin, ambergris and the like, grinded with a colloid mill to be ready for use, gelatin was taken and dissolved at 60 C. by adding water into it, added with glycerol and diatomite, and uniformly mixed with the aforementioned ready-for-use solutions of Arisaema heterophyllum Blume and the like to prepare coating liquid, coated and cut to obtain the patch.

[0042] This product adopted a water-soluble transdermal matrix, was externally applied onto a cancer pain part for percutaneous absorption, which was beneficial for the drug to exert its functions of effectively relieving pain and swelling and could effectively improves the pain for a patient with an advanced cancer.

[0043] The preparation method of the liniment: the aforementioned raw herbal materials were weighed in proportion according to proportion parameters, added with 9 times amount of water and decocted for 2-3 hours, extracted for 3 times, and filtered. The filter residue was added with another 3 times amount of water and decocted for 2 hours, and filtered. The filtrates were combined, and concentrated under reduced pressure to a thick paste with a relative density of 1.13-1.17 (85 C.). The thick paste was added with ethanol to make the ethanol content of the drug solution reach 75%, added with polyvinyl formal-acetal, completely dissolved after added with 75% ethanol for soaking and expanding, mixed well, and then ready for use. The alcohol deposit fluid was added with the pratt mountainash root-bark extract, fully stirred with the matrix to uniform, added with 75% ethanol to adjust the total amount to 1,000 grams, and packaged to obtain the liniment.

[0044] This product adopted a water-soluble transdermal matrix, was externally applied onto a cancer pain part for percutaneous absorption, which was beneficial for the drug to exert its functions of effectively relieving pain and swelling and could effectively improves the pain for a patient with an advanced cancer.

Example 3: Preparing the Composition into a Sustained-Release Preparation

[0045] The above poplar bark, processed Radix Aconiti Lateralis, fructus psoraleae, annona muricata, curcumin and the like raw material extract powder, microcrystalline cellulose and starch were all placed in a fluidized bed, sprayed with a proper amount of distilled water according to parameters in an operation parameter list, spraying was stopped when the pellets were controlled at about 0.18-0.22 grams, and appropriate drying was conducted. Sieving was conducted to select pellets between 30 meshes and 60 meshes;

[0046] (3) The drug-loaded pellets were placed into a fluidized bed, and according to parameters on an operation parameter list, slow-release coating liquid was sprayed onto the surface of the drug-loaded pellets for surface sealing, Spraying was stopped after the coating weight was increased by 5%. Drying was continually done at 55-60 C. for 0.5 h to obtain film-coated sustained-release pellets. The 30-mesh pellets were encapsulated into capsules, and the 60-mesh pellets were packaged to obtain traditional Chinese medicines of sustained-release capsules and pellets.

[0047] Characteristics: the sustained-release technology for preparing this product could effectively control the drug to be released within a certain period of time, maintain an effective blood drug concentration for 24 hours, has no burst release phenomenon, and has no irritation and adverse reactions to stomach, intestine, liver and spleen.

[0048] Observation of therapeutic effects:

[0049] Referring to the liniment of Example 2, the liniment was respectively applied to the first group and the second group. The liniment was applied to the pain part 2-3 times a day (for a patient with a severe pain, administration for 5-6 times was allowed within 24 hours). 20 days was one course of treatment. After two courses of treatment, the pains of all patients were obviously alleviated, without any adverse reaction found in the medication process. In six years, 42 patients had improved walking, no longer suffered from pain, and had no relapse reaction after drug withdrawal.

[0050] In 10 years, of 8 patients, 7 were basically cured after 4 courses of treatment, and 1 had other symptoms obviously alleviated except a leg pain due to prolapse of lumbar intervertebral disc. Summary of effects: a significant effect of 85%, an effective rate of 98%, and no obvious effect of 3% were achieved. It could be seen from the examples that this traditional Chinese medicine formula had the advantages of quick effect, low cost, safety and reliability, small toxic and side effects and the like.

[0051] Observation of recipe cases:

[0052] It was used in 46 cases of advanced-cancer pains (statistics of some outpatients). The results showed a marked effect (pain disappeared) in 37 cases, improvement (pain relief) in 19 cases, ineffectiveness in 2 cases, with a total effective rate of 98%.

[0053] A typical case was Mrs. Lu, who was 56 years old and went to see a doctor at 9:00 p.m. on Mar. 5, 2018. She complained that she had a severe abdominal pain in the past two days, was unable to eat or drink, and the pain was even more severe at night. She had gone to two tumor hospitals for examination and was diagnosed as massive hepatocellular carcinoma and was not given treatment. Current conditions: the patient had a face that was as yellow as paper, had thin muscle, was skinny, had yellow skin and sclera, and was extremely poor in spirit. Auscultation: the patient had normal heart and lung, a large liver below umbilicus with a harder texture and a nodular shape. Upon abdominal CT, the patient was reported to have a massive hepatocellular carcinoma. According to the diagnosis of the pulse condition of the patient, the six pulses were deep and stagnating, the tongue was light-colored with a white coating that was gray and had ecchymosis. The patient was thus diagnosed as having Qi-stagnation and blood stasis, phlegm accumulation and damp obstruction. Seeing the patient's unbearable pain, she was given an external patch (Example 2) and pellets for oral administration (Example 3), and the pain began to decrease in about 35 minutes. The patch was replaced every 3-5 days. The pellets were administrated 1-2 times a day, with 5-7 pellets each time. The treatment was conducted for 58 days in total. Then the liver was reduced from 5 cm below the navel to 7 cm above the navel. The patient had a normal diet. The body weight of the patient was 53 kilograms before the treatment, and increased to 69 kilograms after the 58 days of treatment. The patient could not move before the treatment, and could walk in the park and drive for 1 hour without feeling tired after the treatment. The tumor-bearing patient had survived for more than 5 years, and was still healthy without relapse after follow-up.