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Theophylline 100 mg quick-release oral tablet formulation and its physicochemical properties

Number of pages: 162 File Format: word File Code: 32023
Year: 2016 University Degree: Master's degree Category: Medical Sciences
Tags/Keywords: Asthma disease - Cloud opener - Direct compression - EPO - HPMC6 - ODT - Rapid-release oral tablets - Respiratory tracts - Theophylline
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  • Summary of Theophylline 100 mg quick-release oral tablet formulation and its physicochemical properties

    Dissertation

    To receive the degree of Doctor of Pharmacy

    Persian summary

    Orally quick-release tablets are solid pharmaceutical forms that have received special attention in the last three decades and are proposed as an alternative to regular tablets and capsules.

    These tablets quickly disintegrate in contact with oral saliva in less than 1 minute without leaving any residue and turn into soluble fine granules, and as a result, they are easily swallowed and easily absorbed perigastrically. The purpose of this thesis is to prepare and evaluate the formulation of fast opening oral tablets, theophylline 100 mg. Theophylline belongs to the xanthine family, which is used in the treatment of asthma and obstructive diseases of the respiratory tract.

    The amount of theophylline in each tablet is 100 mg. We named the formula from a total of 29 formulas under series A, in which we investigated the opening effect of 3 super-opening agents: croscarmellose sodium, crospovidone, sodium starch glycolate (with percentages of 2%, 3% and 5%) and Fmelt-C. Then, physicochemical control tests including diameter, uniformity, weight, erosion, hardness, opening time, tests to determine the amount of effective substance and dissolution are performed, and finally A6 formulation was selected as the best formulation among the top 10 formulations. Then, in the next series of formulations under title B, we sought to add mannitol (DC grade) and reduce Avicel as a filler, in order to improve the taste and solubility. Finally, in order to achieve the desired taste, sweeteners and flavorings, as well as polymers covering the taste, were used in different percentages. Due to the high bitterness of the medicine and lack of covering with sweeteners and flavors, we had to use different polymers to mask the taste. In series C, we investigated the masking effect, opening time and solubility changes with different ratios (Edrajet EPO-drug). The highest amount of polymer with the opening time below 1 minute was observed in C3, but still the taste was not suitable. In the series of formulas under the D series, we were looking for cellulosic polymers with flavor coating properties. In general, this series had a good taste, but it was unfavorable in terms of opening time, and the best case was the HPMC6 polymer named D2, which is still considered unfavorable for a fast-opening tablet, about 3 minutes. In series E, we used the combination of C3 and D2 and reduced the amount of cellulose derivative to 1% of the drug. This formulation was suitable in terms of release profile, opening time and taste. Finally, in the F series, by adding various flavorings and sweeteners and checking the taste by 10 volunteers, the formulation with 2% peppermint essence was considered more ideal than the others and was selected as the superior formulation. Due to the lack of this pharmaceutical form in Iran, it is hoped that this product can be produced in domestic factories.

    Vocabulary: ODT, theophylline, direct condensation, cloud opener, Edragit EPO, HPMC6,

    The necessity and importance of the subject

    Theophylline is a derivative of xanthines. It is used in asthma and COPD. The way to take this medicine is oral. Its available pharmaceutical forms in the country include 200 mg tablets, 200 mg slow-release tablets and capsules. It is also available in the form of theophylline-G syrup (theophylline 50 mg + guaiafensine 30 mg) in 5 ml of syrup (1).

    The oral route is easy to use Among the oral pharmaceutical forms are tablets, which are prioritized over syrups and liquid pharmaceutical forms due to ease of manufacture, proper stability, and easier transportation. But these forms also have drawbacks. The first problem that comes to them is the problem of swallowing. Some people, including children and the elderly, do not have a high swallowing ability. Also, people suffering from nausea, people during shortness of breath and acute attacks caused by respiratory tract obstruction, schizophrenic patients are among the cases that somehow make swallowing pills difficult (2).The second disadvantage of tablets is that, after being swallowed, the tablets must go through the stage of opening and dissolution, and since the stage of opening and turning into a solution form is a time-consuming process, this causes a delay in the onset of the therapeutic effect (3).

    Quick-release tablets are tablets that dissolve after contact with saliva within less than 1 minute. They are opened in the mouth and become a suspension or solution, and as a result, there is no need to use water for swallowing. Therefore, these forms have easy swallowing and fast absorption, and in addition to the advantages of solid pharmaceutical forms, they do not have the mentioned negatives, they are also in regular tablets (3-4-5).

    Given this issue and the advantages of these tablets compared to regular tablets, the importance of this drug in respiratory diseases and the lack of research in the field of making and removing the bitterness of theophylline, we considered it necessary to conduct this research.

     

    1-2. Statement of the problem

    Quick-release oral tablets are one of the new drug delivery systems that have attracted considerable attention. This pill disintegrates and dissolves in the oral cavity in less than 60 seconds without the need to drink water, and this is a good thing for the elderly and children or patients who have difficulty swallowing regular pills (4).

    Theophylline is a derivative of xanthines that has been used in asthma and COPD with the following functions:

    1. Relaxing the smooth muscles of the respiratory tracts (bronchodailation) like other methylxanthines by inhibiting the phosphodiesterase enzyme and increasing intracellular cAMP directly causes the relaxation of the smooth muscles of the respiratory tracts and pulmonary vessels.

    2. Suppressing the response of the respiratory tract to stimulants (non-bronchodaliation) (6)

    Due to the use of theophylline in these diseases and the quick response and high bioavailability of ODT tablets, as well as the ease of use in these patients, especially during respiratory attacks, and also due to the lack of studies in this field and the novelty of the method, we decided to take measures in this field. Our goal in this research is to manufacture this drug inside the country, due to its absence in the pharmaceutical market of Iran and the better availability of the drug.

    1-3. Objective (main objectives)

    Formulation of theophylline 100 mg tablet in an oral opening form and subsequently, performing physicochemical tests on it, to reach the selected formulation with desirable characteristics.

    1-4. Objective (sub-objectives)

    Study and make an orally opening pharmaceutical product and conduct related control experiments

    Evaluate different formulations and use different polymers to achieve a form that opens faster.

  • Contents & References of Theophylline 100 mg quick-release oral tablet formulation and its physicochemical properties

    List: Persian summary. The necessity and importance of the subject.. 4

    1-2. Statement of the problem.. 5

    1-3. Goal (main goal).. 5

    1-4. Objectives (sub-objectives). An introduction to pharmaceutical forms. 9

    2-1-1-1. Oral route. 9

    2-1-1-2. Buccal Route. 10

    2-1-1-3. Rectal route. 10

    2-1-1-4. Inhalation Route. 10

    2-1-1-5. Local use (Transdermal Route). 10

    2-1-1-6. Parenteral route. 10

    2-1-2. Some considerations of oral drug delivery. 11

    2-1-2-1. Grouping of oral drug delivery systems. 12

    2-1-2-1-1. Grouping based on physiological considerations. 12

    2-1-2-1-2. Grouping based on the mobility of the pharmaceutical system. 13

    2-1-2-1-3. Grouping based on the structural characteristics of drug delivery. 13

    2-1-2-2. Types of oral drug delivery systems. 14

    2-1-2-2-1. Cheek tablets.. 14

    2-1-2-2-2. Sublingual tablets. 14

    2-1-2-2-3. Chewable tablets.. 14

    2-1-2-2-4. Lozenges.. 14

    2-1-2-2-5. Pastes.. 14

    2-1-2-2-6. Gels.. 15

    2-1-2-2-7. Oral aerosols.. 15

    2-1-2-2-8. Mouthwashes.. 15

    2-1-2-2-9. Dental systems. 15

    2-1-2-2-10. Toothache drops. 16

    2-1-2-2-11. Gums.. 16

    2-1-2-2-12. Mucus, adhesives.. 16

    Part II: quick-release oral tablets

    2-2-1. Tablets.. 18

    2-2-1-1. Benefits of pills.. 18

    2-2-1-2. Disadvantages of pills.. 20

    2-2-1-3. All kinds of pills.. 20

    2-2-1-3-1. Oral tablets.. 21

    2-2-1-3-2. Tablets used in the oral cavity. 26

    2-2-1-3-3. Pills that are taken by other means than mouth. 27

    2-2-1-3-4. Tablets used to prepare solutions. 28

    2-2-1-4. Quick release tablets. 29

    2-2-1-4-1. Benefits of immediate release tablets. 30

    2-2-1-4-2. Disadvantages of quick release tablets. 31

    2-2-1-4-3. Remarkable items in the preparation of quick release tablets. 32

    2-2-1-4-4. Rapid release tablet formulations. 33

    2-2-1-4-4-1. Effective ingredients in the formulation of quick-release tablets. 33

    2-2-1-4-4-2. Excipients in the formulation of quick-release tablets. 34

    2-2-1-4-4-2-1. Diluents. 35

    2-2-1-4-4-2-2. Adhesives.. 35

    2-2-1-4-4-2-3. Lubricants. 35

    2-2-1-4-4-2-4. Dyes. 36

    2-2-1-4-4-2-5. Sweeteners. 36

    2-2-1-4-4-2-6. flavorings 37

    2-2-1-4-4-2-7. Openers.. 37

    2-2-1-4-4-2-7-1. Types of openers. 38

    2-2-1-4-4-2-7-2. New openers. 38

    2-2-1-4-4-2-7-3. Effective factors in the opening of tablets. 39

    2-2-1-4-4-2-7-4. Mechanism of action of openers. 40

    2-2-1-4-5. Methods of producing quick release tablets. 49

    2-2-1-4-5-1. direct compression.. 49

    2-2-1-4-5-2. Dry granulation. 50

    2-2-1-4-5-3. Wet granulation. 50

    2-2-1-4-6. New technologies for making fast-release tablets. 51

    2-2-1-4-6-1. Zydis technology. 51

    2-2-1-4-6-2. Orasolv technology. 53

    2-2-1-4-6-3. Durasolv technology. 54

    2-2-1-4-6-4. Wowtab technology. 55

    2-2-1-4-6-5. Flashdose technology. 55

    2-2-1-4-6-6. Flashtab technology. 55

    2-2-1-4-6-7. Oraquick technology. 56

    2-2-1-4-7. Physicochemical control tests of quick release tablets. 57

    2-2-1-4-7-1. The appearance of the tablet. 55

    2-2-1-4-7-2. Pharmaceutical form uniformity test. 56

    2-2-1-4-7-2-1. Weight uniformity test. 57

    2-2-1-4-7-2-2. Content uniformity test. 58

    2-2-1-4-7-3. Difficulty.. 58

    2-2-1-4-7-4. Erodibility test. 59

    2-2-1-4-7-5. Open time test. 59

    2-2-1-1-4-6. Test to determine the amount of active pharmaceutical ingredient. 60

    2-2-1-1-4-7. Stability test.. 60

    2-2-1-4-8. Characteristics of some ingredients in the formulation.61

    2-2-1-4-8-1. Sodium croscarmellose. 61

    2-2-1-4-8-2. Cross povidone. 62

    2-2-1-4-8-3. Sodium starch glycolate. 63

    2-2-1-4-8-4. Mannitol. 64

    2-2-1-4-8-5. Microcrystalline cellulose. 65

    2-2-1-4-8-6. aspartame 66

    2-2-1-4-8-7. Odrajit-aye. 66

    2-2-1-4-8-8. Hydroxypropyl methyl cellulose. 67

    The third part: Asthma

    2-3. asthma 69

    2-3-1. Signs and symptoms of the disease. 69

    2-3-2. Causes and etiology. 69

    2-3-3. Pathophysiology. 70

    2-3-4. prevention 72

    2-3-5. diagnosis 73

    2-3-5-1. Pattern of symptoms. 73

    2-3-5-2. skin test 73

    2-3-5-3. Pulmonary function test. 73

    2-3-5-3-1. Arterial blood gases (ABG). 73

    2-3-5-3-2. Spirometry. 74

    2-3-6. treatment 75

    2-3-6-1. Medicines used. 77

    2-3-7. Differential diagnosis. 79

    Section four: chronic obstructive pulmonary disease

    2-4. Chronic obstructive pulmonary disease. 82

    2-4-1. definition 82

    2-4-2. Symptoms. 82

    2-4-3. Pathology. 82

    2-4-3-1. emphysema 83

    2-4-3-2. bronchitis 83

    2-4-4. Differences between asthma and COPD. 83

    2-4-5. Cause of disease. 84

    2-4-6. diagnosis 85

    2-4-7. treatment 85

    2-4-7-1. Vaccination. 85

    2-4-7-2. exercise 86

    2-4-7-3. Bronchodilators. 86

    2-4-7-4. Corticosteroids. 87

    2-4-7-5. Another treatment. 87

    2-4-7-6. surgery 87

    2-4-8. Therapeutic goals. 88

    Part Five: Theophylline

    2-5-1. Theophylline. 90

    2-5-2. Molecular weight of the anhydrous form. 90

    2-5-3. Chemical name. 90

    2-5-4. Formula. 90

    2-5-5. Brand name. 90

    2-5-6. Pharmaceutical forms now. 90

    2-5-7. Mechanism of action. 90

    2-5-8. Pharmacokinetics. 91

    2-5-9. Cases and dosage. 92

    2-5-10. Contraindications 92

    2-5-11. Precautions. 92

    2-5-12. side effects 92

    2-5-13. Drug interactions. 93

    2-5-14. Recommended tips. 93

    Chapter Three: Materials and Methods

    Introduction. 95

    3-1. Devices used. 95

    3-2. Materials used. 96

    3-3. Work done. 97

    3-3-1. Preformulation studies done on theophylline powder. 97

    3-3-1-1. Investigating the organoleptic properties of theophylline powder. 97

    3-3-1-2. Determining the shedding of theophylline powder (checking Karr's index and Hasner's coefficient). 97

    3-3-1-3. Investigating the compressibility of theophylline powder. 98

    3-3-1-4. Determination of UV spectrum of theophylline. 98

    3-3-1-5. Drawing the FTIR spectrum of theophylline. 99

    3-4. Preparation of fast-release theophylline tablet formulations. 99

    3-4-1. The method and preparation of theophylline quick-release oral tablet formulations by direct compression method. . 99

    3-4-1-1. Preparation of quick-release tablet formulations of theophylline series A. 100

    3-4-1-2. Preparation of formulations of theophylline series B quick-release tablets. 101

    3-4-1-3. Preparation of C-series theophylline quick-release tablet formulations. 102

    3-4-1-4. Preparation of D-series theophylline quick-release tablet formulations. 103

    3-4-1-5. Preparation of E-series theophylline quick-release tablet formulations. 103

    3-4-1-6. Preparation of F-series theophylline fast-release tablet formulations. 104

    3-5. Physicochemical control tests performed on fast-dissolving tablet formulations. 105

    3-5-1. Examining the appearance properties of tablets. 105

    3-5-2. Examining the hardness of tablets. 105

    3-5-3. Examining the erodibility of tablets. 105

    3-5-4. Determination of thickness and diameter of tablets. 106

    3-5-5. Checking the uniformity of the weight of tablets. 106

    3-5-6. Tablet opening time tests. 106

    3-5-7. Draw the standard graph of theophylline at ?max = 272 nm in water. 106

    3-5-8. Determination of theophylline amount and content uniformity. 106

    3-5-9. Dissolution test and drug release method. 107

    3-5-10. Taste test on superior formulation. 108

    Chapter Four: Results

    4-1. The results of pre-formulation studies conducted on theophylline powder. 110

    4-1-1.

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