[CHINESE MEDICINES] * [ETHICAL MEDICINES] [DRUG DELIVERY] * [READING COMPREHENSION] * [CLINICAL TESTING]

Clinical refers to any use or testing in human subjects; new drugs continue to come from traditional sources, and a variety of drug combinations can yield improved activity and reduced side effects of drugs; other clinical discoveries reported here pertain to improving reading abilities of those suffering from dyslexia and ADHD and new methods of testing generic and biosimilar drugs for equivalence of similarity with reference products.

Chinese Medicines

Natural products remain one of the largest source of new drugs; for millions of years, we have relied on natural products, even in their crudest form, to treat a variety of ailments, from heart disease to skin warts. Chinese herbal medicines, particularly for the treatment of skin disorders have been in use for a long time. The inventions shown below are based on converting anecdotal use of Chinese medicine into a scientific portfolio, to make them better acceptable to regulatory agencies such as FDA that has recently started a new Division of Complimentary and Alternate Medicines to approve these drugs.

US 6,555,118 | Pharmaceutical Preparation for The Treatment of Topical Wounds and Ulcers.

Pharmaceutical preparations for the treatment of wounds and ulcers in humans and animals and a method of preparation of the same are provided here. The composition consists of an alcoholic extract of Huangqin, Huanglian, Huangbai, Opuntia, Dilong, and ß-sitosterol (from Soybean extract), in a vegetable oil-wax base, from where the alcohol is essentially removed by evaporation. The composition is used as a topical ointment for the treatment of wounds in its preferred embodiment. Wounds, those occurring in the skin as second and third degree burns, stasis ulcers, trophic lesions, such as decubitus ulcers, diabetic ulcers, surgical wounds, severe cuts, diaper rash, cracked nipples and abrasions which are commonly resistant to the natural healing process, may be treated with this composition. The application of this combination to wounds greatly accelerates the rate of healing and reduces scarring as the mechanism of action proposed here involves regeneration of skin through stimulation of stem cells that allows healing without substantial scar formation. composition for topical medicinal application to a body surface to treat surface wounds in humans and animals free of poppy capsule consisting essentially of the following ingredients in the percentages by weight indicated; an alcoholic extract of Huangbai 1-20% an alcoholic extract of Huanglin 1-20% an alcoholic extract of Huangqin 1-20% an alcoholic extract of Dilong 1-20% an alcoholic extract of Opuntia 1-20% an alcoholic extract of ß-sitosterol 1-20%; and Canola oil QS to Volume. PDF 

US 6,495,174 | Herbal Composition for The Treatment of Alopecia.

Pharmaceutical compositions for the topical treatment of alopecia in humans and animals, consisting essentially of effective quantities of alcoholic extracts of Rhizoma zingiberis recens, Rhizoma pinelliae, Flos carthami, Radix rehmanniae, Radix angelicae sinesis, Radix paenoiae rubra, Cacumen biotae, Semen sesami nigrum, Radix polygoni multiflori, Fructus mori, Capsicum, Cantharidin, and Oleum ricini in a pharmaceutical carrier. PDF

US 6,447,820 | Pharmaceutical Composition for The Prevention and Treatment of Scar Tissue.

Compositions for treatment of existing and prevention of new skin scars in humans and animals using a topical application containing alcoholic extracts of Cortex Phellodendri and Opuntia ficus indica in a specific combination. 1. A method of the removal of scar tissue in humans and animals comprising applying to a skin surface a composition having: 1.0 to 25% of Cortex phellodendri 1.0 to 25% of Opuntia ficus-indica 5.0 to 20.0% of a wax; and 83%-87% olive oil thereby removing the scar tissue from the skin surface. PDF

US 6,419,963 | Composition and Method for The Treatment of Diaper Rash Using Natural Product.

This product is marketed for the treatment of diaper rash in the US. Pharmaceutical composition containing beeswax, olive oil, ß-sitosterol and the herb Coptis chinesis Franch for safe and quick treatment for infant and adult diaper rash. Also, provided here is a methodology for the treatment of diaper rash wherein the treatment consists of compositions that contain naturally derived anti-inflammatory agents, antimicrobial agents and such components that they provide an occlusive coating when applied to the afflicted surface. A pharmaceutical composition for the treatment of diaper rash consisting essentially of beeswax, olive oil, ß-sitosterol and the herb Coptis chinensis Franch. PDF

US 6,365,198 | Pharmaceutical Preparation for The Treatment of Gastrointestinal Ulcers and Hemorrhoids.

Pharmaceutical preparations for the treatment of gastrointestinal ulcers and hemorrhoids in humans and animals and a method of preparation for this composition are provided here. The preferred composition consists of an alcoholic extract of Huangqin, Huanglian, Huangbo, Opuntia and Pheretima dissolved in vegetable oil from where alcohol is essentially removed by evaporation. The composition is then packaged in a soft gelatin capsule for oral administration or mixed with wax to make an ointment suitable for rectal administration. An oral composition for the amelioration or treatment of gastrointestinal ulcers and hemorrhoids comprising effective amounts of extracts of Huanglian, Huangqin, Huangbo, Pheretima, and Opuntia. PDF

US 6,312,735 | Method for Instantaneous Removal of Warts and Moles.

A method for the removal of all types of human and animal skin warts using a technique of cauterization wherein slaked lime is applied to wart and then the surface of wart is scratched by using the stem of betel leaf. A method of removing warts and moles comprising application of a composition comprising slaked lime to the surface of a wart or mole followed by rupture of the surface of the wart with the stub of the stem of betel leaf. PDF

US 10/604,424 | Pharmaceutical Composition for The Treatment of Itch.

Topical preparations for the treatment of topical itch in humans and animals. The said composition consists of Opuntia, Propolis, Stearic Acid, Beeswax, Vegetable Oil and ß-sitosterol. Itch includes scratch reaction itch, anal itch, or irritant itch due to plants (e.g., poison ivy), insect bite, sunburn, chemical itch, eczema, pruritis dermatitis, diabetic skin itch, aging skin itch, foot-itch, chickenpox, jock itch, hives, itch of healing burns and wounds, dry winter skin itch, and stress-related scalp itch, etc. A composition for topical application to a body surface to treat itch in humans and animals comprising of Bee Propolis, 0.10-10%; Stearic Acid, 1-10%,; Opuntia Ficus-indica, 1-10%; .beta.-sitosterol, 1-10%; Natural Beeswax, 2-20%; Vegetable Oil QS to Volume. PDF

US 10/250197 | Compositions and Methods for Reducing or Controlling Blood Cholesterol, Lipoproteins, Triglycerides, And Sugar and Preventing or Treating Cardiovascular Diseases.

Compositions and methods related to the administration of psyllium husk, ß-sitosterol, guggul tree extract, guar gum and chromium as a combination to reduce or control blood cholesterol, triglycerides, low density lipoproteins, blood sugar or increasing or controlling high density lipoproteins in a mammal, to reduce arterial plaque build-up, atherosclerosis, in a mammal which may be associated with cardiovascular, cerebrovascular, peripheral vascular, or intestinal vascular disorders. A method of reducing or controlling blood cholesterol, triglycerides or sugar in a mammal comprising the administration to said mammal a composition of between 2 g and 10 g of psyllium husk, 0.05 g to 0.2 g of simethicone (30%), 0.1 g to 0.5 g of ß-sitosterol, 0.1 g to 5 g of guggul tree (Commiphora mukul) extract, 0.1 g to 0.5 g of guar (Cyamopis tetragonoloba) gum, and 10 to 500 mcg of chromium. PDF

US 10/077,289 | Pharmaceutical composition for the treatment of alopecia.

Pharmaceutical compositions containing phystosterols and/or blood flow stimulants are described to promote hair growth through stimulation of follicular cells, bulb cells and stem cells in the scalp to treat the condition of alopecia in humans and animals. A composition for stimulating the growth of hair by enhancing blood flow to scalp, comprising, in a pharmaceutically acceptable carrier, a solution of a potent rubefacient or a vasodilator compound, preferably capsaicin, methyl nicotinate or a known vasodilator in concentrations suitable to produce and maintain enhanced blood flow to scalp area. 3. A composition for stimulating the growth of human and animal hair by enhancing the growth of stem cells or bulb cells and enhancing blood flow to scalp, in a pharmaceutical acceptable carrier, such as an alcoholic solution of a ß-sitosterol with a known vasodilator or rubefacient compound. PDF

US 09/957,773 | Composition and Method for The Treatment of Hypercholesterolemia and Hyperlipidemia in Mammals.

Pharmaceutical compositions suitable for the treatment of a condition selected from the group consisting of atherosclerosis, post-angioplasty restenosis, coronary artery disease, angina, small artery disease and other diseases caused by or are the result of hypercholesterolemia, or combination thereof comprising of a specific botanical plant. Specifically, the present invention relates to compositions comprising the herb or botanical Zizyphus jujube or extract thereof, which is useful in treating cardiovascular disorders, particularly those associated with elevated LDL and overall serum cholesterol levels. A method of preparing the pharmaceutical compositions of the invention and a method for treating a patient therewith are also disclosed. A method for treating a patient comprising, administering a therapeutic amount of the herbal composition of the Zizyphus jujube effective to prevent or ameliorate the effects of a condition selected from the group consisting of atherosclerosis, post-angioplasty restenosis, coronary artery disease, angina, and small artery disease or other disease caused by or because of hypercholesterolemia and hyperlipidemia. PDF

US 09/949,445 | Method and Composition for Reducing Sebum Secretion in Mammals.

Compositions for to reducing sebum production on the skin using methods and compositions containing a surfactant, a chylomicron disrupter, a skin penetration enhancer, and an anti-androgenic compound. In a preferred embodiment, the composition contains the surfactant as a mixture of polyoxyethylene compounds and the anti-androgenic agent as a mixture of saw palmetto extract and nettle extract. A method for reducing sebum secretion in mammals by applying to skin a topical composition containing a carrier or mixtures thereof, a surfactant or mixtures thereof, a chylomicron disrupter or mixtures thereof, a skin penetration enhancer or mixtures thereof, and an anti-androgenic compound or mixtures thereof. PDF

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Ethical medicines

 Development of new ethical drugs is a multi-billion-dollar feat; however, as science develops and our understanding of the nature of drugs improves, there are many opportunities of expanding the utility of proven safe drugs, reduce their side-effects and provide new opportunities that require less capital investment to provide additional options to patients. Categories of drugs developed include weight loss, analgesic, sebum and war removal, burn treatment, rash and stretch mark removal, etc.

US 6,338,862 | Composition and Method of Use in Treating Sexual Dysfunction Using C-GMP-Specific Phosphodiesterase Type 5 Inhibitors.

 The inhibitors of cyclic guanosine monophosphate (cGMP) phosphodiesterases type 5 (cGMP-PDE5) such as sildenafil citrate (Viagra®) act by increasing the level of cGMP in sexual organs to produce enhanced blood flow and an erectile response of sexual organs. Though sildenafil citrate is a specific inhibitor of cGMP-PDE5, its effects on other body organs produce many side effects including fatalities. Described here is a method of combining cGMP-PDE5 inhibitors with natural sources of nutrients that instantly enhance the levels of endogenous cGMP and thus reduce the therapeutic dose and therefore the side effects of cGMP-PDE5 inhibitors. We have discovered that if sildenafil citrate, as a prototype of cGMP-PDE5, is combined with L-arginine, ginseng, vitamin B6, vitamin B12, and folic acid, all natural and safe ingredients, the dose requirements for sildenafil citrate can be reduced substantially. The specific composition described here assists in the action of sildenafil primarily by increasing the production of cGMP through modulation of nitric oxide pathway (L-arginine to nitric oxide to cGMP) and secondarily by having its own effect on improving blood circulation to sexual organs. A composition for treating sexual dysfunction comprising effective amounts of an inhibitor of cGMP-specific phosphodiesterase type 5 enzyme, a natural amino acid, ginseng, vitamin B6, vitamin B12 and folic acid. PDF

US 6,251,421 | Pharmaceutical Composition Containing Psyllium Fiber and a Lipase Inhibitor

Pharmaceutical compositions containing an inhibitor of gastrointestinal lipase, and at least one compound selected from the group consisting of psyllium husk, its seeds and leaves thereof. Methods are provided for preventing and treating anal leakage of oil in a patient to whom a composition containing an inhibitor of gastrointestinal lipase is orally administered. A pharmaceutical composition in oral dosage form for humans, said composition comprising an inhibitor of gastrointestinal lipase, said gastrointestinal lipase is present in an amount of from about 10 mg to about 500 mg, and a compound comprising psyllium husk, seeds or leaves thereof, said compound is present in an amount of from about 500 mg to about 20 g, wherein said composition contains 10 to 50 parts by weight of the compound per 1 part by weight of the inhibitor of gastrointestinal lipase. PDF

US 6,235,796 | Use of Fluorocarbons for The Prevention of Surgical Adhesions.

Method for the prevention and inhibition of adhesion between tissues comprising the use of fluorocarbons are disclosed. The method provides for the introduction of a fluorocarbon into the surgical site of a mammalian body, such as a human, to minimize friction and enhance the mobility of the surrounding tissues and organs. The fluorocarbons introduced may be in various forms including liquid and emulsions, and provides a coating, film or barrier thereby reducing the surface tension associated after surgery. The subject invention further discloses the use of perfluorodecalin as a preferred fluorocarbon compound used as the primary anti-adhesion agent. A method for preventing or inhibiting the formation of adhesions in a surgical site comprising the step of locally administering to said surgical site on internal surfaces within said surgical site an effective adhesion preventing amount of an inert and non-toxic polycyclic fluorocarbon forming a lubricated barrier between said internal surfaces. PDF

US 6,235,314 | Analgesic, Anti-Inflammatory and Skeletal Muscle Relaxant Compositions.

 Disclosed is a local skeletal muscle relaxant and a non-steroidal anti-inflammatory drug in a topical composition for topical application to a patient for relief of pain. More particularly and in its preferred form, the invention involves a combination of diazepam and diclofenac in a composition for topical application to the skin of a patient as a colorless transparent gel. A composition for topical application to a body surface, comprising: 0.5% to 2.5% carbomer, 50% to 65% H2 O, 1.5% to 3.5% paraffin, 1.5% to 3.0% emollient, 1.0% to 3.0% emulsifier, 0.5% to 2.0% diethylamine, 0.5% to 3.0% pharmaceutically acceptable neutralizing base, 20% to 30% alcohol, 1.5% to 5.0% propylene glycol, 0.1% to 5.0% diazepam, 0.1% to 5.0% nonsteroidal anti-inflammatory drug in a homogenized mixture. PDF

US 4,530,936 | Composition and Method for Inhibiting the Absorption of Nutritional Elements from The Upper Intestinal Tract.

A method of inhibiting the absorption of nutritional elements, principally food, from the gastrointesinal tract is disclosed which comprises ingesting perfluorodecalin in an amount sufficient to form a nutritional element-impermeable film thereof on at least a substantial part of the inner wall of the upper intestine and maintaining the film for a time long enough to inhibit the absorption from the gastrointestinal tract of a significant proportion of the ingested nutritional elements. An emulsion dosage form is preferred for carrying out this method, which emulsion contains perfluorodecalin, water, and a non-toxic emulsifier, preferably Pluronic F-68, and optionally flavoring and/or coloring agents. The method of inhibiting or preventing the absorption of at least one nutritional elements selected from the group consisting of carbohydrates, fats, proteins, vitamins, and minerals from the gastrointestinal tract which comprises ingesting perflorodecalin in an amount sufficient to form a nutritional element-impermeable film thereof on at least a substantial part of the inner wall of the upper intestine and maintaining said film for a time long enough to inhibit absorption of nutritional elements from the gastrointestinal tract. PDF

US 11/306155 | Alleviation of Pain in Osteoarthritis by Means of Intra-Articular Implantation of Perfluorodecalin.

A method of alleviating pain in osteochondral lesions by means of intra-articular implantation of perfluorodecalin, a fully fluorinated fluorocarbon. The main objective of the invention is to introduce the new medical use of perfluorodecalin for the alleviation of pain when injected into joints wherein perfluorodecalin provides a lubrication and viscoelastic function that allows smooth movement of joints without appreciable pain. PDF

US 11/053,400 | Formula, a system and a method for treating urushiol induced contact dermatitis.

A formula, a system and a method is provided for treating urushiol induced contact dermatitis, chemical irritants and/or microbiological irritants on an affected area of skin of a user. The formula and/or the system is applied to an area of the skin of the user affected with urushiol, the chemical irritants and/or the microbiological irritants. The formula and/or the system have a cleansing agent, one or more surfactants and/or one or more abrasive agents for treating the urushiol induced contact dermatitis, the chemical irritants and/or the microbiological irritants. One or more abrasive agents separates the urushiol, the chemical irritants and/or the microbiological irritants from the skin of the user at the affected area. The cleansing agent bonds to the urushiol, the chemical irritants and/or the microbiological irritants at the affected area and withdraws the urushiol, the chemical irritants and/or the microbiological irritants from the tissue under the affected area of the skin of the user. The formula, the system, the urushiol, the chemical irritants and/or the microbiological irritants may be rinsed away from and/or may be removed from the affected area of the skin of the user. As a result, the urushiol induced contact dermatitis, the chemical irritants and/or the microbiological irritants is treated and/or is terminated by the formula, the system, the cleansing agent and/or one or more surfactants. A formula for treating dermatitis on an area of skin of a user wherein the area of the skin is affected with urushiol wherein the formula is applied to the area of the skin of the user, the formula comprising: a cleansing agent to bind to the urushiol at the area of the skin of the user; a first surfactant to remove the urushiol from the area of the skin of the user; and a first abrasive agent to separate the urushiol from the skin of the user wherein the formula and the urushiol are rinsed from the area of the skin of the user. PDF

US 09/681254 | Combination of multiple non-steroidal anti-inflammatory drugs and muscle relaxants for local treatment of musculoskeletal pain. 

This discovery is for a novel topical application of non-steroidal anti-inflammatory drug administered in a specific combination to treat osteoarthritic pain, skeleto-muscular pains, sports injuries, a variety of topical cancers, both of skin and oral cavity. Combination of NSAIDs is likely to provide much higher effectiveness at lower doses. Since the mechanism of action NSAIDs is highly diversified and there is sufficient evidence of individual responses to each NSAID, a topical combination product is likely to be more effective. A pharmaceutical composition for use in the treatment of pain and inflammation and the treatment of muscle spasms and associated pain, soreness and tightness of muscles in a mammalian organism and adapted for topical administration, said composition comprising: (i) an analgesic and anti-inflammatory effective amount of at least one drug chosen from each of the groups of NSAIDs consisting of propionic acid derivatives, acetic acid derivatives, fenamic acid derivatives, biphenyl carbolic acid derivatives, oxicam derivatives and (ii) an amount effective in the treatment of muscle spasms, and associated symptoms, of a muscle relaxant selected from the group consisting of cyclobenzaprine, chlorzoxanzone, methocarbamol, dantrolene and the pharmaceutically acceptable salts thereof.  PDF

US 09/681127 | Vaginal Administration of Apomorphine to treat sexual dysfunction in females.

Vaginal administration of a dopaminergic agent to treat sexual dysfunction in human females. Contrary to development of similar products developed for male erectile dysfunction, our approach is for a locally applied product in women instead of a systemically administered product to yield three major advantages: physical, psychological and pharmacological. Most women who would need this product would benefit from physical supplementation of lubrication, a psychological stimulation because of touch and finally and strong pharmacological response mediated through dopaminergic system. The most surprising aspect of our research was that the side effects associated with these compounds when given through oral routes were nonexistent in vaginal delivery systems. This is the first product for female frigidity that is based on a molecule that is safe and in use for decades. The projections for female dysfunction are much higher since the incidence of disorder is also much higher. It is projected that almost 80% of women experience periods of frigidity and lack of libido during their childbearing years. A method of ameliorating sexual dysfunction in a human female which comprises administering to said human female, apomorphine or a pharmaceutically acceptable acid addition salt thereof as a vaginal dosage form and in an amount sufficient to increase intra-clitoral blood flow and vaginal wall blood flow on stimulation of said human female but less than the amount that induces substantial nausea, the typical side effect of using apomorphine given systemically. PDF

US 09/681117 | Use of lizard oil in treating sexual impotency and frigidity.

A method of using animal fats containing high concentration of a specific natural long-chain acid, erucic acid, to treat male erectile dysfunction. Anecdotally, specialized animal fats have been used in the legends to treat a variety of medical disorders. We have studied a specific fat and discovered the mechanism responsible for its action. In Asia and the Middle East, the raw fat from a lizard had purported characteristics of treating male erectile dysfunction. We studied the composition of this fat and discovered that it is rich in erucic acid, vitamin E and A among many other components. Erucic acid in the animal fat was found to be a potent component enhancing and maintaining blood flow to local tissue. When applied to penile area, the raw fat induced erection, we proved in our findings showing the reasons for it. A method for treating frigidity and enhancing sexuality in females having a clitoris comprising the step of topically applying and rubbing to the surface of the clitoris and optionally to its surrounding areas the fat deposits derived from Uromastix hardwickii. PDF

US 09/681110 | Use of erucic acid in enhancing blood flow to tissues.

Compositions for the application of erucic acid as an adjuvant to enhance blood flow to tissue. This is a GRAS compound that was discovered by NPI to enhance blood flow to peripheral tissues upon local application; applications tested in treating male erectile dysfunction and female frigidity are discovered both alone and in combination with sildenafil and apomorphine. Significant role in arthritis, diabetes afflicted patient treatment and enhancing effects of other drugs applied locally. A method for enhancing blood flow to tissues by applying erucic acid. PDF.

US 09/671847 | Dopaminergic and Lipase Inhibitor Weight Loss Composition.

Combinations of existing, widely used, safe, dopaminergic drug combined with a newly identified lipase enzyme inhibitor (such as orlistat), which is also widely used in pharmaceutical formulations and considered to be totally safe for administration to humans. This combination product provides a significant advance in the field of weight management. The CNS compound curbs the carbohydrate satiety response incumbent in the use of lipase inhibitors (such as orlistat) and combined it with a safe lipase inhibitor. The patent application also covers combination with other currently approved lipase inhibitors. PDF.

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Reading comprehension

Books are historically printed with text aligned horizontally and whereas we get used to reading even when we tilt head to right or left when our eyes are misaligned, such is not the case with those suffering from dyslexia or ADHD; text printed at an angle resolves this problem.

US 15/188636 | Visual Axis Optimization for Enhanced Readability and Comprehension.

A method for improving readability and comprehension of text and images by those in need of improving readability and comprehension of text and images comprising printing the text and images at an angle to reduce misalignment of a horizontal axis of the eyes and a horizontal axis of a printed text and image. PDF

15/383,971 | Angled Printed Book.

A method for improving readability and comprehension of printed text or image by printing at an angle as a mirror image on the left and right page of a bound book is disclosed. A book comprising: a plurality of bound leaves having a left page and a right page; a text or an image printed at an angle as mirror images on the left and the right pages in angular orientation. PDF.

14/308462 | Visual Axis Optimization for Enhanced Readability and Comprehension.

A method of improving readability and comprehension of text and images comprising printing or displaying the text and images at an angle to align with the horizontal axis of the eyes of the reader. PDF

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Drug Delivery

Drug entities become a useful product for clinical use only if they can be safely delivered to a known or purported site of action in the body. Many drugs are not administered orally because they are decomposed by the gastrointestinal fluids or during passage through liver. Drugs administered through buccal cavity avoid both impediments but the bitter taste of many drugs makes this a less desirable route of administration. In the invention described below, a chewing gum base is used wherein carbon dioxide is produced upon chewing that helps anesthetize taste buds to allow bitter drug taken through buccal cavity, such as various amines used for weight loss management. One of the most reliable route of administration is through suppositories; the invention below describes a suppository base using erucic acid that helps improve local circulation and therefore, the absorption of drug contained in the suppository. A blank suppository can be used to stimulate female sex organs as well.

US 6,462,083 | Suppository Base.

 A suppository base composition of erucic acid and beeswax with improved chemical stability, moldability, and shelf-life. The inventive suppository base also stimulates localized blood flow to the administration site. A suppository base composition comprising erucic acid present in an amount of about 90 to about 99 percent by weight and beeswax present in in an amount of about 1 to about 10 percent by weight. PDF

US 4,639,368 | Chewing gum containing a medicament and taste maskers.

 A chewing gum composition adapted to supply a medicament to the oral cavity for local application thereto or for buccal absorption of said medicament which comprises a chewing gum base, an orally administrable medicament, a taste masking generator of carbon dioxide and optionally a taste bud desensitizing composition. A chewing gum composition adapted to supply a medicament to the oral cavity comprising, a chewing gum base, an orally administrable medicament capable of being absorbed through the buccal cavity, said medicament consisting essentially of phenylpropanolamine, and a carbon dioxide generator. PDF

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Clinical Testing

Drug actions are often proportional to the quantity of drug at the site of action; what drives molecules within the body is its thermodynamic activity, not the observed concentration. Based on this observation, methods for testing drug activity are described that remove the need to expose humans to testing new drugs for their activity evaluation. Protein drugs can change their structure and their activity and toxicity because of changes in their structure; a thermodynamic stress applied to molecules causing a shift in structure is used to compare molecular structures.

US 14/160837 | Thermodynamic Equivalence Surrogate Test (TEST) For Bioequivalence.

 A method for establishing bioequivalence of drug products by comparing the thermodynamic potential of the release of a drug substance from drug products according to a set of statistically differentiated dissolution profiles of an active drug substance contained in the drug product. A method for measuring the thermodynamic potential of the release of an active drug substance contained in a drug product comprising comparing a test drug product with a reference drug product by a set of statistically differentiated dissolution profiles of the active drug substance contained in the drug products. 2. A method for determining drug bioequivalence comprising measuring the thermodynamic potential between a test drug substance and a reference drug substance under conditions that yield a difference in their dissolution profiles, wherein equivalence of thermodynamic potential demonstrates drug bioequivalence. 4. A method for determining drug bioequivalence comprising measuring the thermodynamic potential between a test drug substance and a reference drug substance under conditions wherein the inter-particulate binding and the intermolecular interactions are disrupted. 5. A method for determining drug bioequivalence comprising measuring the thermodynamic potential between a test drug substance and a reference drug substance under thermodynamic stress conditions that modify the release characteristics of the test and reference drug substances to yield a difference in their dissolution profiles, wherein the stress condition is chosen based on its ability to alter the dissolution profile allowing the determination of drug equivalence. PDF

US 13/961571 | Methods for Comparing a Structure of a First Biomolecule and a Second Biomolecule.

 Methods to assess structural similarity of a first biomolecule and a second biomolecule by detecting one or more responses of the first and second biomolecule to thermodynamic stress conditions induced by osmotic and dielectric changes including, detecting a shift in fluorescence emission and/or a change in the intensity of the emission. 1. A method of comparing structural similarity of a first biomolecule to a second biomolecule, the method comprising: altering a concentration of one or more components in a solution comprising a first biomolecule; measuring at least one of a fluorescence emission wavelength and/or an intensity of fluorescence emission of the first biomolecule in the solution; and comparing the fluorescence emission wavelength and/or the intensity of fluorescence of the first biomolecule in the solution to a fluorescence emission wavelength and/or an intensity of fluorescence emission in a second solution comprising a second biomolecule having the same concentration of the one or more components. A method of determining if a first biomolecule is structurally similar to a second biomolecule, the method comprising: altering the concentration of one or more components in a solution comprising a first biomolecule; measuring at least one of a fluorescence emission wavelength and/or intensity of fluorescence emission of the first biomolecule in the solution; altering the concentration of one or more components in a second solution comprising a second biomolecule; measuring the florescence emission wavelength and/or the intensity of fluorescence emission of the second biomolecule in the second solution; comparing the fluorescence emission wavelength and/or the intensity of fluorescence emission of the first biomolecules in the solution to a fluorescence emission wavelength and/or an intensity of fluorescence emission of the second biomolecule in a second solution having the same concentration of the one or more components and the same concentration of the second biomolecule as a concentration of the first biomolecule; and determining whether the first biomolecule is structurally similar to the second biomolecule, wherein the first biomolecule is determined to be structurally similar to the second biomolecule where the fluorescence emission wavelength and/or the intensity of fluorescence emission of the first biomolecule in the solution and the second biomolecule in the second solution are substantially similar. PDF